Hepatic ImpairmentPhase 1NCT06736340
Pharmacokinetics and Safety of Rupatadine in Participants With Hepatic Impairment Compared to Control Participants.
A Phase 1 study testing Rupatadine in people with Hepatic Impairment, run by Noucor Health S.A. at 7 sites in 2 countries.
Trial summary
The purpose of this study is to assess the PK and safety of rupatadine (10 mg) and its active metabolites in participants with mild, moderate, or severe hepatic impairment compared to matched control participants with normal hepatic function. Read more about this study
- Who is it for?
- Ages 18 years and olderHealthy volunteers can take part
- Conditions the study is for
- Hepatic Impairment
- What is being tested?
- Rupatadine
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 26 participants
- Where
- 7 sitesin 2 countries
- Study dates
- 17 Nov 2022to 9 Apr 2025
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 years and older
- All sexes
- Healthy volunteers accepted
- Adult, Older adult
Who may be able to join
- Participants with normal hepatic function and participants with mild, moderate, or severe hepatic impairment who meet the following criteria will be considered eligible to participate in the clinical study:
- Participant understands the study procedures and agrees to participate in the study by giving written informed consent prior to any study-mandated procedure.
- Able to communicate well with the Investigator, to understand and comply with the study requirements.
- Willing to comply with study restrictions stated in Section 5.3 (lifestyle considerations).
- Male or female Caucasian subject, between 18 and 75 years (inclusive) of age.
- Body mass index (BMI) is between 18 to 35 kg/m2 at Screening.
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- Women of childbearing potential (WoCBP) must have a negative serum pregnancy test at Screening, a negative urine pregnancy test on Day -1, and agree to consistently and correctly use (from 30 days prior to dosing, during the entire study, and for at least 30 days after dosing), a highly effective method of contraception (i.e., failure rate of < 1%) (Section 10.4 [Appendix 4]). Such methods include:
- Hormonal contraceptives: combined (estrogen- and progesterone-containing) contraception associated with inhibition of ovulation using oral, intravaginal, or transdermal route of administration.
- Note: If a hormonal contraceptive is used, it must be initiated at least 30 days before dosing.
- Intrauterine device.
- Intrauterine hormone-releasing system.
- Bilateral tubal occlusion.
- Vasectomized partner, provided that the partner is the sole sexual partner and that the vasectomized partner has received medical assessment of the surgical success.
- Sexual abstinence, defined as refraining from heterosexual intercourse from 30 days prior to dosing up to at least 30 days after dosing, if this is the preferred and usual lifestyle of the subject. WoCBP must also agree not to donate ova from the time of informed consent until 30 days after dosing
- Women of non-childbearing potential (WoNCBP), i.e., postmenopausal (defined as 12 consecutive months with no menses without an alternative medical cause, confirmed by a follicular stimulating hormone [FSH] test), with previous bilateral salpingectomy, bilateral salpingo-oophorectomy or hysterectomy, or with premature ovarian failure (confirmed by a specialist), XY genotype, Turner syndrome, uterine agenesis (Section 0 [Appendix 4]).
- Male participants are infertile, vasectomized (who has received medical assessment of the surgical success) or must agree to abstain from, or to use a condom, during heterosexual intercourse with a woman of childbearing potential (Section 0 [Appendix 4]).
- Male participants must agree not to donate sperm, from the time of informed consent until 30 days after dosing.
- Participant agrees to refrain from consuming grapefruit juice, grapefruits, and grapefruitcontaining products from at least 7 days before the dose administration, and until the EOS Visit.
- Able to tolerate venipuncture.
- No clinically relevant abnormalities on rest vital signs.
- No clinically relevant abnormalities on 12-lead ECG.
- For participants with normal hepatic function the following criteria must be met in addition:
- No clinically relevant diseases captured in medical history at Screening.
- No clinically relevant abnormalities on physical examination and Screening and Baseline.
- No clinically relevant abnormalities on clinical laboratory tests at Screening.
- Weight within ±15% to his/her matched participant(s) enrolled in the study.
- Biological sex matched to his/her matched participant(s) enrolled in the study.
- Age within ±10 years to his/her matched participant(s) enrolled in the study.
- Normal Blood Pressure (BP) measured on the same arm, after 5 min in the supine position at Screening and Baseline defined as:
- Systolic Blood Pressure (SBP) 90-140 mmHg, Diastolic Blood Pressure (DBP) 60-90 mmHg, and pulse rate 60-100 bpm (inclusive) for subjects < 65 years of age.
- SBP 95-160 mmHg, DBP 65-95 mmHg, and pulse rate 60-100 bpm (inclusive) for subjects ≥ 65 years of age.
- For participants with mild, moderate, or severe hepatic impairment the following criteria must be met in addition:
- No clinically relevant abnormalities on clinical laboratory tests at Screening, except for those related to liver cirrhosis.
- SBP 90-160 mmHg, DBP 60-95 mmHg, and pulse rate 60-100 bpm (inclusive), measured on the same arm, after 5 min in the supine position at Screening and Baseline.
- Participant has a diagnosis of chronic (> 6 months), stable (no acute episodes of illness within the previous 2 months due to deterioration in hepatic function) hepatic impairment, defined by Child Pugh Classification, with features of cirrhosis due to any etiology.
- Child-Pugh scale score (see Section 4.2 for Child-Pugh Classification) from 5 to 6 (mild hepatic impairment), 7 to 9 (moderate hepatic impairment) or 10 to 15 (severe hepatic impairment) at the Screening Visit.
- Stable concomitant medications for at least 21 days prior to dosing and up to the EOS visit.
Who cannot join
- Participants with normal hepatic function and participants with mild, moderate, or severe hepatic impairment who meet one or more of the following criteria will not be considered eligible to participate in the clinical study:
- Pregnant or lactating women.
- Participant is unlikely to comply with the protocol requirements, instructions and study related restrictions; e.g., uncooperative attitude, inability to return for the EOS Visit and improbability of completing the clinical study.
- Any psychological, emotional problems, any disorders or resultant therapy that is likely to invalidate informed consent, or limit the ability of the participant to comply with the protocol requirements.
- History of hypersensitivity to rupatadine, desloratadine or any of the excipients, or to medicinal products with similar chemical structures.
- History of clinically significant lactose, galactose, or fructose intolerance.
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- Any clinically relevant acute or chronic disease which could jeopardize the safety of the participant or impact the validity of the study results.
- History or presence of clinically significant angioedema.
- Use of caffeine-containing beverages exceeding 800 mg per day (Section 5.3.2) at Screening.
- Nicotine consumption (e.g., smoking, nicotine patch, nicotine chewing gum, or electronic cigarettes) from 48 h prior to Baseline (Day -1) until discharge from confinement (Day 2).
- Positive test result for urine alcohol and drugs of abuse (amphetamines, benzodiazepines, cannabinoids, cocaine and opiates) at Screening and Baseline.
- Note: Subjects receiving stable treatment of methadone and benzodiazepines will be allowed to be enrolled in the study even if the urine drug screen test is positive.
- Veins unsuitable for intravenous puncture on either arm (e.g., veins that are difficult to locate, access, or puncture, veins with a tendency to rupture during or after puncture).
- Participation in another clinical trial with an experimental drug within 2 months or 5 halflives (whichever is longer) before the Screening or in more than 2 clinical studies within 1 year prior to Screening.
- Positive results at Screening from either the hepatitis B or C serology based on hepatitis B surface antigen, hepatitis B surface antibody, hepatitis B core antibody (Ig M and total antihepatitis B core antibody), and hepatitis C virus antibody (HCV) markers, except for vaccinated subjects or subjects with past resolved hepatitis.
- Note: If HCV antibody is present, HCV RNA analysis should be performed, and the result must be "not detected".
- History of heart, liver or kidney transplantation.
- Active malignant neoplastic disease or carcinoma (including leukemia, lymphoma, malignant melanoma), or myeloproliferative disease, regardless of the time since treatment.
- Use of any of the following within 2 weeks prior to investigational medicinal product (IMP) administration or 5 half-lives, whichever is longer:
- Enzyme-modifying drugs known to induce/inhibit hepatic drug metabolism (e.g., azole antifungals [ketoconazole, itraconazole, fluconazole, posaconazole, voriconazole], macrolide antibiotics [erythromycin, clarithromycin], diltiazem, human immunodeficiency virus (HIV) protease inhibitors, nefazodone, rifampicin, phenytoin, dexamethasone, troglitazone, and barbiturates)
- CYP3A4 substrates with a narrow therapeutic index (e.g., ciclosporin, tacrolimus, sirolimus, everolimus, cisapride)
- Desloratadine
- Clinically significant abnormalities on ECG repolarization (QTcF > 450 ms in males and > 470 ms in females) at Screening.
- Loss of 250 mL or more blood within 3 months prior to screening.
- For participants with normal hepatic function, the additional criteria must not be met:
- History or clinical evidence of alcohol or drug abuse within the 3 years prior to Screening.
- Estimated glomerular filtration rate (eGFR) < 90 mL/min for subjects aged ≤ 45 years, and <70 mL/min for subjects aged > 45 years, as determined by the Cockcroft-Gault equation, at Screening.
- Intake of any prescribed medication (including vaccines) including over-the-counter (OTC) medication (including herbal and dietary supplements such as St John's Wort, homeopathic preparations, vitamins and minerals) that could affect the outcome of the study as judged by the Investigator, within 14 days before the administration of the IMP or less than 5 times the half-life of that medication, whichever is longer (excluding contraceptives and hormone replacement therapy).
- For participants with mild, moderate or severe renal impairment, the additional criteria must not be met:
- Severe portal hypertension or surgical porto-systemic shunts, including transjugular intrahepatic portosystemic shunt
- eGFR < 60 mL/min as determined by the Cockcroft-Gault equation, at Screening.
- History or clinical evidence of infection with hepatitis B and/or hepatitis C within the preceding 6 months.
Trial locations and contacts
7 sites in 2 countries.
7 sites in 2 countries
Spain4 sites
Municipal Institute Of Medical Investigation
Barcelona, 08003
Hospital Universitario De La Princesa
Madrid, 28006
Hospital Clinico San Carlos
Madrid, 28040
Hospital Universitario La Paz
Madrid, 28046
Portugal3 sites
Centro Hospitalar De Vila Nova De Gaia Espinho
Gaia, 4434-502
Hospital Pedro Hispano
Matosinhos Municipality, 4450-113
BlueClinical Phase I
Porto, Porto District, 4250-449
About this study
Official title: A Study to Investigate Pharmacokinetics and Safety of Rupatadine (10 mg) and Its Active Metabolites in Participants With Hepatic Impairment Compared to Matched Control Participants With Normal Hepatic Function.
The purpose of this study is to assess the PK and safety of rupatadine (10 mg) and its active metabolites in participants with mild, moderate, or severe hepatic impairment compared to matched control participants with normal hepatic function. The study duration will be up to 38 days, including Screening, Baseline, Study Period, and EOS Visit assessments. Rupatadine 10 mg tablet will be administered as single dose.
Read the detailed description
This is an open-label, non-randomized, parallel group study comparing the PK after administration of a single 10 mg dose of rupatadine to participants with hepatic impairment with matched control participants with normal hepatic function (matched in terms of age, gender, and body weight).
For each participant, the study visits will consist of a screening period (Day -28 to Day -2), a baseline evaluation (Day -1), a single dose treatment period (Day 1), and an End of Study (EOS) Visit (Day 10). Additionally, from Day 2 to EOS participants will go back to the clinic every day for blood drawing.
Participants who meet the eligibility criteria at Screening and Baseline will be enrolled into the study.
All Baseline safety evaluation results must be reviewed prior to dosing. Participants will be domiciled at the clinic from Day -1 until 24 hours after dosing on Day 1 (Day 2).
On Day 1, participants will receive a single dose of rupatadine 10 mg after an overnight fast of 10 hours and will continue to fast for 4 hours postdose.
Participants will undergo sequential PK sampling over the following 192 hours along with other safety assessments as described in schedule of activities (SoA).
The participant groups will be consecutively enrolled into the study. Enrollment of participants with mild, moderate, and severe hepatic impairment will be staggered, so that dosing of participants with mild hepatic impairment will be started first. Dosing of the next group will be started only after evaluation of blood PK, safety and tolerability data until 72-hour postdose of at least 6 participants with hepatic impairment from the previous group and after the assessment of safety and tolerability results are judged to be satisfactory by Safety Committee.
An EOS assessment for each participant will occur at Day 10 after the administration of rupatadine.
The total study duration for each participant, including Screening, Baseline, Study Period, and EOS assessments, is approximately 38 days.
- Conditions
- Hepatic Impairment
- Being tested
- Rupatadine
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
RupatadineDrug
Also called Pafinur
10mg tablets
| Study group | Role | What they receive |
|---|---|---|
| Hepatic imparement mild | Experimental | Not described Receives: Drug: Rupatadine |
| Hepatic imparement moderate | Experimental | Not described Receives: Drug: Rupatadine |
| Hepatic imparement severe | Experimental | Not described Receives: Drug: Rupatadine |
| Hepatic normal functions | Experimental | Not described Receives: Drug: Rupatadine |
What is being measured
The primary outcome is the main question the study is designed to answer.
Area under the plasma concentration-time curve from time zero to last time point (AUC0-t) of rupatadine
To assess the pharmacokinetics (PK), including the area under the plasma concentration-time curve from time zero to last time point (AUC0-t), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of rupatadine
To assess the pharmacokinetics (PK), including the Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Peak plasma concentration (Cmax) of rupatadine
To assess the pharmacokinetics (PK), including the Peak plasma concentration (Cmax), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Time of maximum plasma concentration (tmax) of rupatadine
To assess the pharmacokinetics (PK), including the Time of maximum plasma concentration (tmax), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Plasma fraction unbound (fu) of rupatadine
To assess the pharmacokinetics (PK), including the Plasma fraction unbound (fu), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Terminal elimination rate constant (kel) of rupatadine
To assess the pharmacokinetics (PK), including the Terminal elimination rate constant (kel), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Terminal half-life (t1/2) of rupatadine
To assess the pharmacokinetics (PK), including the Terminal half-life (t1/2), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Apparent total clearance (CL/F) of rupatadine
To assess the pharmacokinetics (PK), including the Apparent total clearance (CL/F), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Renal clearance (CLR) of rupatadine
To assess the pharmacokinetics (PK), including the Renal clearance (CLR), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Apparent non-renal clearance (CLNR/F) of rupatadine
To assess the pharmacokinetics (PK), including the Apparent non-renal clearance (CLNR/F), calculated as apparent total clearance - renal clearance, of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Apparent volume of distribution during terminal phase (V/F) of rupatadine
To assess the pharmacokinetics (PK), including the Apparent volume of distribution during terminal phase (V/F) of rupatadine, after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Peak plasma concentration (Cmax) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
To assess the pharmacokinetics (PK), including the peak plasma concentration (Cmax) of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Area under the plasma concentration-time curve from time zero to last time point (AUC0-t) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
To assess the pharmacokinetics (PK), including the area under the plasma concentration-time curve from time zero to last time point (AUC0-t), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
To assess the pharmacokinetics (PK), including the area under the plasma concentration-time curve from time zero to infinity (AUC0-inf), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Terminal elimination rate constant (kel) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
To assess the pharmacokinetics (PK), including the terminal elimination rate constant (kel), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Time of maximum plasma concentration (tmax) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
To assess the pharmacokinetics (PK), including the time of maximum plasma concentration (tmax), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Terminal half-life (t1/2) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
To assess the pharmacokinetics (PK), including the terminal half-life (t1/2), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Metabolic ratio (MR) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
To assess the pharmacokinetics (PK), including the Metabolic ratio of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Measured: 10 days
Secondary outcomes (23)
Area under the plasma concentration-time curve from time zero to last time point (AUC0-t) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the Area under the plasma concentration-time curve from time zero to last time point (AUC0-t)
Measured: 1 day
Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf)
Measured: 1 day
Peak plasma concentration (Cmax) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the Peak plasma concentration (Cmax)
Measured: 1 day
Time of maximum plasma concentration (tmax) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the time of maximum plasma concentration (tmax)
Measured: 1 day
Terminal elimination rate constant (kel) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the terminal elimination rate constant (kel)
Measured: 1 day
Terminal half-life (t1/2) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the terminal half-life (t1/2)
Measured: 1 day
Apparent total clearance (CL/F) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the apparent total clearance (CL/F)
Measured: 1 day
Renal clearance (CLR) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the renal clearance (CLR)
Measured: 1 day
Apparent non-renal clearance (CLNR/F) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the apparent non-renal clearance (CLNR/F)
Measured: 1 day
Apparent Volume of Distribution During Terminal Phase (V/F) of unbound (free) rupatadine
To assess the PK parameters of unbound (free) rupatadine, including the apparent Volume of Distribution During Terminal Phase (V/F)
Measured: 1 day
Incidence of treatment-emergent adverse events (TEAEs)
To determine the safety and tolerability, including the incidence of treatment-emergent adverse events (TEAEs), of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in heart rate (electrocardiogram (ECG) parameters)
To determine the safety and tolerability, including the change from Baseline in electrocardiogram (ECG) parameters, including the heart rate, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in PR interval (electrocardiogram (ECG) parameters)
To determine the safety and tolerability, including the change from Baseline in electrocardiogram (ECG) parameters, including the PR interval, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in QRS complex (electrocardiogram (ECG) parameters)
To determine the safety and tolerability, including the change from Baseline in electrocardiogram (ECG) parameters, including the QRS complex, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in QT interval (electrocardiogram (ECG) parameters)
To determine the safety and tolerability, including the change from Baseline in electrocardiogram (ECG) parameters, including the QT interval, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in body temperature (vital signs)
To determine the safety and tolerability, including the change from Baseline in vital signs, including the body temperature, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in pulse rate (vital signs)
To determine the safety and tolerability, including the change from Baseline in vital signs, including the pulse rate, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in blood pressure (vital signs)
To determine the safety and tolerability, including the change from Baseline in vital signs, including the blood pressure, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in selected safety laboratory tests, including hematology
To determine the safety and tolerability, including the change from Baseline in selected safety laboratory tests, including hematology, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in selected safety laboratory tests, including clinical chemistry
To determine the safety and tolerability, including the change from Baseline in selected safety laboratory tests, including clinical chemistry, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in selected safety laboratory tests, including coagulation
To determine the safety and tolerability, including the change from Baseline in selected safety laboratory tests, including coagulation, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in selected safety laboratory tests, including routine urinalysis
To determine the safety and tolerability, including the change from Baseline in selected safety laboratory tests, including routine urinalysis, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Change from Baseline in body weight
To determine the safety and tolerability, including the change from Baseline in body weight, of rupatadine after a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants
Measured: 10 days
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted16 Dec 2024
- Study start17 Nov 2022
- Primary completion9 Apr 2025
- Study completion9 Apr 2025
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (24)Papers the sponsor has linked to this study.
- Other trials for Hepatic ImpairmentStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Other
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Model description
- This is an open-label, non-randomized, parallel group study comparing the PK after administration of a single 10 mg dose of rupatadine to participants with hepatic impairment with matched control participants with normal hepatic function (matched in terms of age, gender, and body weight).
- Masking
- None (open label)
- Enrolment
- 26 participants (actual)
Sponsor and investigators
- Lead sponsor
- Noucor Health S.A.
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Serafim Guimarães, MD, Principal investigator, Blueclinical Investigacao E Desenvolvimento Em Saude Lda.Rosa Maria Príncipe, MD, Principal investigator, Hospital Pedro HispanoJoana Cochicho, MD, Principal investigator, Centro Hospitalar de Vila Nova de Gaia/EspinhoDolores Ochoa Mazarro, MD, Principal investigator, Fundación de Investigación Biomédica - Hospital Universitario de La PrincesaAna Maria Aldea Perona, MD, Principal investigator, Municipal Institute Of Medical InvestigationGermán Soriano Pastor, MD, Principal investigator, Fundació Institut de Recerca de l'Hospital de la Santa Creu i Sant PauAlberto Borobia Pérez, MD, Principal investigator, Hospital Universitario La PazAntonio Portolés Pérez, MD, Principal investigator, Hospital Clinico San Carlos
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT06736340
- Sponsor's protocol ID
- DC08RUP/1/21
- Status last verified
- Nov 2024
- First submitted
- 27 Apr 2022
- Last updated
- 28 May 2025
- Results posted
- No
- Data monitoring committee
- Yes
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
- Individual data sharing
- No
Publications
Billah MM, Chapman RW, Egan RW, Gilchrest H, Piwinski JJ, Sherwood J, Siegel MI, West RE Jr, Kreutner W. Sch 37370: a potent, orally active, dual antagonist of platelet-activating factor and histamine. J Pharmacol Exp Ther. 1990 Mar;252(3):1090-6.
PubMed 2319461Eiser NM, Mills J, Snashall PD, Guz A. The role of histamine receptors in asthma. Clin Sci (Lond). 1981 Apr;60(4):363-70. doi: 10.1042/cs0600363.
PubMed 7249528Cuss FM, Dixon CM, Barnes PJ. Effects of inhaled platelet activating factor on pulmonary function and bronchial responsiveness in man. Lancet. 1986 Jul 26;2(8500):189-92. doi: 10.1016/s0140-6736(86)92489-x.
PubMed 2873440Henocq E, Vargaftig BB. Accumulation of eosinophils in response to intracutaneous PAF-acether and allergens in man. Lancet. 1986 Jun 14;1(8494):1378-9. doi: 10.1016/s0140-6736(86)91683-1. No abstract available.
PubMed 2872485Piwinski JJ, Wong JK, Green MJ, Ganguly AK, Billah MM, West RE Jr, Kreutner W. Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines. J Med Chem. 1991 Jan;34(1):457-61. doi: 10.1021/jm00105a069. No abstract available.
PubMed 1671420Prescott SM, Zimmerman GA, McIntyre TM. The production of platelet-activating factor by cultured human endothelial cells: Regulation and function. In Platelet-activating factor and related lipid mediators. Snyder F, Ed. New York: Plenum Press, 1987: 323-340.
Katiyar S, Prakash S. Pharmacological profile, efficacy and safety of rupatadine in allergic rhinitis. Prim Care Respir J. 2009 Jun;18(2):57-68. doi: 10.3132/pcrj.2008.00043.
PubMed 18695846Mullol J, Bousquet J, Bachert C, Canonica WG, Gimenez-Arnau A, Kowalski ML, Marti-Guadano E, Maurer M, Picado C, Scadding G, Van Cauwenberge P. Rupatadine in allergic rhinitis and chronic urticaria. Allergy. 2008 Apr;63 Suppl 87:5-28. doi: 10.1111/j.1398-9995.2008.01640.x.
PubMed 18339040Queralt M, Brazis P, Merlos M, de Mora F, Puigdemont A. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. doi: 10.1007/PL00000216.
PubMed 10959557Merlos M, Ramis I, Balsa D, Queralt M, Brazís P, Puigdemont A. Inhibitory effect of rupatadine on TNF-a release from human monocytes and mast cell lineHMC-1. J.Allergy Clin. Immunol. 2000 105(Suppl.1): S62.
Bartra J, Valero AL, del Cuvillo A, Davila I, Jauregui I, Montoro J, Mullol J, Sastre J. Interactions of the H1 antihistamines. J Investig Allergol Clin Immunol. 2006;16 Suppl 1:29-36. No abstract available.
PubMed 17357375del Cuvillo A, Mullol J, Bartra J, Davila I, Jauregui I, Montoro J, Sastre J, Valero AL. Comparative pharmacology of the H1 antihistamines. J Investig Allergol Clin Immunol. 2006;16 Suppl 1:3-12. No abstract available.
PubMed 17357372Olkkola KT, Ahonen J. Midazolam and other benzodiazepines. Handb Exp Pharmacol. 2008;(182):335-60. doi: 10.1007/978-3-540-74806-9_16.
PubMed 18175099Picado C. Rupatadine: pharmacological profile and its use in the treatment of allergic disorders. Expert Opin Pharmacother. 2006 Oct;7(14):1989-2001. doi: 10.1517/14656566.7.14.1989.
PubMed 17020424Izquierdo I, Merlos M, Garcia-Rafanell J. Rupatadine: a new selective histamine H1 receptor and platelet-activating factor (PAF) antagonist. A review of pharmacological profile and clinical management of allergic rhinitis. Drugs Today (Barc). 2003 Jun;39(6):451-68. doi: 10.1358/dot.2003.39.6.799450.
PubMed 12944997
Study at a glance
From the registry record, last updated by the sponsor on 28 May 2025. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Study to Investigate Pharmacokinetics and Safety of Rupatadine (10 mg) and Its Active Metabolites in Participants With Hepatic Impairment Compared to Matched Control Participants With Normal Hepatic Function.
- ClinicalTrials.gov ID
- NCT06736340
- Acronym / sponsor ID
- DC08RUP/1/21
- Conditions
- Hepatic Impairment
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 26 participants (actual)
- Lead sponsor
- Noucor Health S.A.Industry (pharma, biotech, devices)
- Study start
- 17 Nov 2022 (actual)
- Primary completion
- 9 Apr 2025 (actual)
- Study completion
- 9 Apr 2025 (actual)
- First posted
- 16 Dec 2024 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The purpose of this study is to assess the PK and safety of rupatadine (10 mg) and its active metabolites in participants with mild, moderate, or severe hepatic impairment compared to matched control participants with normal hepatic function. The study duration will be up to 38 days, including Screening, Baseline, Study Period, and EOS Visit assessments. Rupatadine 10 mg tablet will be administered as single dose.
Detailed description
This is an open-label, non-randomized, parallel group study comparing the PK after administration of a single 10 mg dose of rupatadine to participants with hepatic impairment with matched control participants with normal hepatic function (matched in terms of age, gender, and body weight).
For each participant, the study visits will consist of a screening period (Day -28 to Day -2), a baseline evaluation (Day -1), a single dose treatment period (Day 1), and an End of Study (EOS) Visit (Day 10). Additionally, from Day 2 to EOS participants will go back to the clinic every day for blood drawing.
Participants who meet the eligibility criteria at Screening and Baseline will be enrolled into the study.
All Baseline safety evaluation results must be reviewed prior to dosing. Participants will be domiciled at the clinic from Day -1 until 24 hours after dosing on Day 1 (Day 2).
On Day 1, participants will receive a single dose of rupatadine 10 mg after an overnight fast of 10 hours and will continue to fast for 4 hours postdose.
Participants will undergo sequential PK sampling over the following 192 hours along with other safety assessments as described in schedule of activities (SoA).
The participant groups will be consecutively enrolled into the study. Enrollment of participants with mild, moderate, and severe hepatic impairment will be staggered, so that dosing of participants with mild hepatic impairment will be started first. Dosing of the next group will be started only after evaluation of blood PK, safety and tolerability data until 72-hour postdose of at least 6 participants with hepatic impairment from the previous group and after the assessment of safety and tolerability results are judged to be satisfactory by Safety Committee.
An EOS assessment for each participant will occur at Day 10 after the administration of rupatadine.
The total study duration for each participant, including Screening, Baseline, Study Period, and EOS assessments, is approximately 38 days.
Study design
- Primary purpose
- Other
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Number of arms
- 4
- Model description
- This is an open-label, non-randomized, parallel group study comparing the PK after administration of a single 10 mg dose of rupatadine to participants with hepatic impairment with matched control participants with normal hepatic function (matched in terms of age, gender, and body weight).
| Arm | Type | Receives |
|---|---|---|
| Hepatic imparement mild | Experimental | Drug: Rupatadine |
| Hepatic imparement moderate | Experimental | Drug: Rupatadine |
| Hepatic imparement severe | Experimental | Drug: Rupatadine |
| Hepatic normal functions | Experimental | Drug: Rupatadine |
Who may qualify
- Ages
- 18 years and older
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult, Older adult
Key inclusion criteria (37 listed)
- Participants with normal hepatic function and participants with mild, moderate, or severe hepatic impairment who meet the following criteria will be considered eligible to participate in the clinical study:
- Participant understands the study procedures and agrees to participate in the study by giving written informed consent prior to any study-mandated procedure.
- Able to communicate well with the Investigator, to understand and comply with the study requirements.
- Willing to comply with study restrictions stated in Section 5.3 (lifestyle considerations).
- Male or female Caucasian subject, between 18 and 75 years (inclusive) of age.
Key exclusion criteria (32 listed)
- Participants with normal hepatic function and participants with mild, moderate, or severe hepatic impairment who meet one or more of the following criteria will not be considered eligible to participate in the clinical study:
- Pregnant or lactating women.
- Participant is unlikely to comply with the protocol requirements, instructions and study related restrictions; e.g., uncooperative attitude, inability to return for the EOS Visit and improbability of completing the clinical study.
- Any psychological, emotional problems, any disorders or resultant therapy that is likely to invalidate informed consent, or limit the ability of the participant to comply with the protocol requirements.
- History of hypersensitivity to rupatadine, desloratadine or any of the excipients, or to medicinal products with similar chemical structures.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| RupatadineAlso: Pafinur10mg tablets | Drug | Hepatic imparement mild, Hepatic imparement moderate, Hepatic imparement severe, Hepatic normal functions |
Primary outcome
Area under the plasma concentration-time curve from time zero to last time point (AUC0-t) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the area under the plasma concentration-time curve from time zero to last time point (AUC0-t), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Peak plasma concentration (Cmax) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Peak plasma concentration (Cmax), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Time of maximum plasma concentration (tmax) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Time of maximum plasma concentration (tmax), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Plasma fraction unbound (fu) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Plasma fraction unbound (fu), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Terminal elimination rate constant (kel) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Terminal elimination rate constant (kel), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Terminal half-life (t1/2) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Terminal half-life (t1/2), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Apparent total clearance (CL/F) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Apparent total clearance (CL/F), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Renal clearance (CLR) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Renal clearance (CLR), of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Apparent non-renal clearance (CLNR/F) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Apparent non-renal clearance (CLNR/F), calculated as apparent total clearance - renal clearance, of rupatadine after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Apparent volume of distribution during terminal phase (V/F) of rupatadine
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Apparent volume of distribution during terminal phase (V/F) of rupatadine, after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Peak plasma concentration (Cmax) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
Time frame: 10 days
To assess the pharmacokinetics (PK), including the peak plasma concentration (Cmax) of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Area under the plasma concentration-time curve from time zero to last time point (AUC0-t) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
Time frame: 10 days
To assess the pharmacokinetics (PK), including the area under the plasma concentration-time curve from time zero to last time point (AUC0-t), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
Time frame: 10 days
To assess the pharmacokinetics (PK), including the area under the plasma concentration-time curve from time zero to infinity (AUC0-inf), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Terminal elimination rate constant (kel) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
Time frame: 10 days
To assess the pharmacokinetics (PK), including the terminal elimination rate constant (kel), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Time of maximum plasma concentration (tmax) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
Time frame: 10 days
To assess the pharmacokinetics (PK), including the time of maximum plasma concentration (tmax), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Terminal half-life (t1/2) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
Time frame: 10 days
To assess the pharmacokinetics (PK), including the terminal half-life (t1/2), of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
Metabolic ratio (MR) of metabolites UR-12338, desloratadine (UR-12790), 3-OH desloratadine (UR-12788), 5-OH desloratadine (UR-12767), and 6-OH desloratadine (UR-12766)
Time frame: 10 days
To assess the pharmacokinetics (PK), including the Metabolic ratio of rupatadine metabolites after administration of a single dose of 10 mg in participants with mild, moderate, and severe hepatic impairment in comparison to normal hepatic function (control) participants.
23 secondary outcomes
Area under the plasma concentration-time curve from time zero to last time point (AUC0-t) of unbound (free) rupatadine
Time frame: 1 day
Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of unbound (free) rupatadine
Time frame: 1 day
Peak plasma concentration (Cmax) of unbound (free) rupatadine
Time frame: 1 day
Time of maximum plasma concentration (tmax) of unbound (free) rupatadine
Time frame: 1 day
Terminal elimination rate constant (kel) of unbound (free) rupatadine
Time frame: 1 day
Terminal half-life (t1/2) of unbound (free) rupatadine
Time frame: 1 day
Apparent total clearance (CL/F) of unbound (free) rupatadine
Time frame: 1 day
Renal clearance (CLR) of unbound (free) rupatadine
Time frame: 1 day
Apparent non-renal clearance (CLNR/F) of unbound (free) rupatadine
Time frame: 1 day
Apparent Volume of Distribution During Terminal Phase (V/F) of unbound (free) rupatadine
Time frame: 1 day
Incidence of treatment-emergent adverse events (TEAEs)
Time frame: 10 days
Change from Baseline in heart rate (electrocardiogram (ECG) parameters)
Time frame: 10 days
Change from Baseline in PR interval (electrocardiogram (ECG) parameters)
Time frame: 10 days
Change from Baseline in QRS complex (electrocardiogram (ECG) parameters)
Time frame: 10 days
Change from Baseline in QT interval (electrocardiogram (ECG) parameters)
Time frame: 10 days
Change from Baseline in body temperature (vital signs)
Time frame: 10 days
Change from Baseline in pulse rate (vital signs)
Time frame: 10 days
Change from Baseline in blood pressure (vital signs)
Time frame: 10 days
Change from Baseline in selected safety laboratory tests, including hematology
Time frame: 10 days
Change from Baseline in selected safety laboratory tests, including clinical chemistry
Time frame: 10 days
Change from Baseline in selected safety laboratory tests, including coagulation
Time frame: 10 days
Change from Baseline in selected safety laboratory tests, including routine urinalysis
Time frame: 10 days
Change from Baseline in body weight
Time frame: 10 days
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 28 May 2025.
- Background: PubMed 2319461Billah MM, Chapman RW, Egan RW, Gilchrest H, Piwinski JJ, Sherwood J, Siegel MI, West RE Jr, Kreutner W. Sch 37370: a potent, orally active, dual antagonist of platelet-activating factor and histamine. J Pharmacol Exp Ther. 1990 Mar;252(3):1090-6.
- Background: PubMed 7249528Eiser NM, Mills J, Snashall PD, Guz A. The role of histamine receptors in asthma. Clin Sci (Lond). 1981 Apr;60(4):363-70. doi: 10.1042/cs0600363.
- Background: PubMed 2873440Cuss FM, Dixon CM, Barnes PJ. Effects of inhaled platelet activating factor on pulmonary function and bronchial responsiveness in man. Lancet. 1986 Jul 26;2(8500):189-92. doi: 10.1016/s0140-6736(86)92489-x.
- Background: PubMed 2872485Henocq E, Vargaftig BB. Accumulation of eosinophils in response to intracutaneous PAF-acether and allergens in man. Lancet. 1986 Jun 14;1(8494):1378-9. doi: 10.1016/s0140-6736(86)91683-1. No abstract available.
- Background: PubMed 1671420Piwinski JJ, Wong JK, Green MJ, Ganguly AK, Billah MM, West RE Jr, Kreutner W. Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines. J Med Chem. 1991 Jan;34(1):457-61. doi: 10.1021/jm00105a069. No abstract available.
- BackgroundPrescott SM, Zimmerman GA, McIntyre TM. The production of platelet-activating factor by cultured human endothelial cells: Regulation and function. In Platelet-activating factor and related lipid mediators. Snyder F, Ed. New York: Plenum Press, 1987: 323-340.
- Background: PubMed 18695846Katiyar S, Prakash S. Pharmacological profile, efficacy and safety of rupatadine in allergic rhinitis. Prim Care Respir J. 2009 Jun;18(2):57-68. doi: 10.3132/pcrj.2008.00043.
- Background: PubMed 18339040Mullol J, Bousquet J, Bachert C, Canonica WG, Gimenez-Arnau A, Kowalski ML, Marti-Guadano E, Maurer M, Picado C, Scadding G, Van Cauwenberge P. Rupatadine in allergic rhinitis and chronic urticaria. Allergy. 2008 Apr;63 Suppl 87:5-28. doi: 10.1111/j.1398-9995.2008.01640.x.
- Background: PubMed 10959557Queralt M, Brazis P, Merlos M, de Mora F, Puigdemont A. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. doi: 10.1007/PL00000216.
- BackgroundMerlos M, Ramis I, Balsa D, Queralt M, Brazís P, Puigdemont A. Inhibitory effect of rupatadine on TNF-a release from human monocytes and mast cell lineHMC-1. J.Allergy Clin. Immunol. 2000 105(Suppl.1): S62.
- Background: PubMed 17357375Bartra J, Valero AL, del Cuvillo A, Davila I, Jauregui I, Montoro J, Mullol J, Sastre J. Interactions of the H1 antihistamines. J Investig Allergol Clin Immunol. 2006;16 Suppl 1:29-36. No abstract available.
- Background: PubMed 17357372del Cuvillo A, Mullol J, Bartra J, Davila I, Jauregui I, Montoro J, Sastre J, Valero AL. Comparative pharmacology of the H1 antihistamines. J Investig Allergol Clin Immunol. 2006;16 Suppl 1:3-12. No abstract available.
- Summary of Product Characteristics (SmPC) for rupatadineLink provided by the sponsor.
- Individual participant dataSharing planned: No
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Serafim Guimarães, MD principal investigator
Blueclinical Investigacao E Desenvolvimento Em Saude Lda.
Rosa Maria Príncipe, MD principal investigator
Hospital Pedro Hispano
Joana Cochicho, MD principal investigator
Centro Hospitalar de Vila Nova de Gaia/Espinho
7 sites in 2 countries: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Rupatadine in people with Hepatic Impairment, run by Noucor Health S.A. at 7 sites in 2 countries.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 37 inclusion and 32 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 28 May 2025. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 7 sites in Spain, Portugal. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Area under the plasma concentration-time curve from time zero to last time point (AUC0-t) of rupatadine (time frame: 10 days). The study lists 18 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT06736340, which also lists 24 linked publications.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 28 May 2025.