Healthy SubjectsPhase 1NCT01877629
Clinical Study to Assess the Pharmacokinetics, Safety, and Tolerability of ACT-129968 in Healthy Subjects
A Phase 1 study testing ACT-129968 500 mg tablet and ACT-129968 250 mg capsule in people with Healthy Subjects, run by Idorsia Pharmaceuticals Ltd. at 1 site in Germany.
Trial summary
To explore the pharmacokinetics (PK) of a single dose of two different formulations of ACT-129968, i.e., tablet versus capsule and to evaluate the safety and tolerability of a single dose of two different formulations of ACT-129968, i.e., tablet versus capsule. Read more about this study
- Who is it for?
- Ages 18 to 45 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy Subjects
- What is being tested?
- ACT-129968 500 mg tablet and ACT-129968 250 mg capsule
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 20 participants
- Where
- 1 siteGermany
- Study dates
- 1 Jul 2011to 1 Jul 2011
- 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 to 45 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Signed informed consent in the local language prior to any study-mandated procedure.
- Women must have
- a negative serum pregnancy test at screening and
- a negative urine pregnancy test pre-dose on Day-1 of each treatment period.
- Women of childbearing potential must consistently and correctly use (from screening, during the entire study, and for at least 28 days after last study drug intake) a reliable method of contraception with a failure rate of < 1% per year, be sexually inactive, or have a vasectomized partner.
- Women not of childbearing potential are defined as post-menopausal (i.e., spontaneous amenorrhea for at least 1 year without an alternative medical cause) or surgically or naturally sterile.
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- No clinically significant findings on the physical examination at screening.
- Body mass index (BMI) of 18.0 to 28.0 kg/m^2 (inclusive) at screening.
- Systolic blood pressure (SBP) 100-145 mmHg, diastolic blood pressure (DBP) 50-90 mmHg, and pulse rate (PR) 45-90 bpm (inclusive), measured on the dominant arm (dominant arm = writing arm) after 5 minutes in the supine position at screening.
- 12-lead electrocardiogram (ECG) without clinically relevant abnormalities, measured after 5 minutes in the supine position at screening.
- Hematology, clinical chemistry, and urinalysis test results not deviating from the normal range to a clinically relevant extent at screening.
- Negative results from urine drug screen and breath alcohol test at screening and on admission to the unit (Day-1) in Period 1 and Period 2.
- Ability to communicate well with the investigator, in the local language, and to understand and comply with the requirements of the study.
Who cannot join
- Pregnant or lactating women.
- Known allergic reactions or hypersensitivity to any excipient of the drug formulation(s).
- History or clinical evidence of any disease and/or existence of any surgical or medical condition which might interfere with the absorption, distribution, metabolism, or excretion of the study drug (appendectomy and herniotomy allowed, cholecystectomy not allowed).
- Previous history of fainting, collapse, syncope, orthostatic hypotension, or vasovagal reactions.
- History or clinical evidence of allergic rhinitis or asthma.
- 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).
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- Previous exposure to the study medication.
- Treatment with another investigational drug within 3 months prior to screening or participation in more than four investigational drug studies within 1 year prior to screening.
- History or clinical evidence of alcoholism or drug abuse within the 3-year period prior to screening.
- Excessive caffeine consumption, defined as 800 mg per day at screening.
- Alcohol consumption of > 21 units/week or > 3 units/day.
- Smoking within 3 months prior to screening.
- Previous treatment with any prescribed or over-the-counter medications (including herbal medicines such as St John's Wort) within 2 weeks prior to first study drug administration.
- Loss of 250 mL or more of blood within 3 months prior to screening.
- Positive results from the hepatitis serology (Hepatitis B surface antigen and anti-hepatitis C virus), except for vaccinated subjects or subjects with past but resolved hepatitis (defined as positive finding for antibodies but negative findings for antigens), at screening.
- Positive results from the human immunodeficiency virus serology at screening.
- Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.
- Legal incapacity or limited legal capacity at screening.
Trial locations and contacts
1 site in 1 country.
About this study
Official title: A Single-center, Open-label, Two-period, Two-treatment, Crossover, Single-dose Study in Healthy Female and Male Subjects to Assess the Pharmacokinetics, Safety, and Tolerability of Two Different Formulations of ACT-129968
To explore the pharmacokinetics (PK) of a single dose of two different formulations of ACT-129968, i.e., tablet versus capsule and to evaluate the safety and tolerability of a single dose of two different formulations of ACT-129968, i.e., tablet versus capsule.
Read the detailed description
A total of 10 female and 10 male healthy subjects will be enrolled and will attend two treatment periods, separated by a 7-9 day washout. Over these two periods, two formulations of ACT-129968 (Treatment A: two capsules, 250 mg each; Treatment B: one tablet, 500 mg) will be administered in the sequence A/B or B/A to 10 subjects (5 females and 5 males) per sequence as determined by randomization.
- Conditions
- Healthy Subjects
- Being tested
- ACT-129968 500 mg tablet, ACT-129968 250 mg capsule
- Keywords
- Pharmacokinetics, Tolerability, Safety, ACT-129968
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
ACT-129968 500 mg tabletDrug
ACT-129968, a tetrahydropyridoindole derivative, is a chemoattractant receptor homologous molecule expressed on T helper 2 cells (CRTH2) antagonist
ACT-129968 250 mg capsuleDrug
ACT-129968, a tetrahydropyridoindole derivative, is a chemoattractant receptor homologous molecule expressed on T helper 2 cells (CRTH2) antagonist
| Study group | Role | What they receive |
|---|---|---|
| ACT-129968 tablet/capsules | Experimental | Subjects attend two treatment periods. In the first treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as a tablet (1 tablet, 500 mg) in the fasted state. In the second treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as capsules (2 capsules, 250 mg each) in the fasted state. There is a 7-9 day washout period between the first treatment period and the second treatment period. Receives: Drug: ACT-129968 500 mg tablet; Drug: ACT-129968 250 mg capsule |
| ACT-129968 capsules/tablet | Experimental | Subjects attend two treatment periods. In the first treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as capsules (2 capsules, 250 mg each) in the fasted state. In the second treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as a tablet (1 tablet, 500 mg each) in the fasted state. There is a 7-9 day washout period between the first treatment period and the second treatment period. Receives: Drug: ACT-129968 500 mg tablet; Drug: ACT-129968 250 mg capsule |
What is being measured
The primary outcome is the main question the study is designed to answer.
The area under the plasma concentration-time curve from time zero to time t of the last measured concentration above the limit of quantification (AUC0-t).
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
Measured: Up to 48 h in each treatment period (1 and 2)
The area under the plasma concentration-time curve from zero to infinity (AUC0-infinity).
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
Measured: Up to 48 h in each treatment period (1 and 2)
The maximum plasma concentration (Cmax)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
Measured: Up to 48 h in each treatment period (1 and 2)
The time to reach maximum plasma concentration (tmax)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
Measured: Up to 48 h in each treatment period (1 and 2)
The terminal elimination half-life (t½)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
Measured: Up to 48 h in each treatment period (1 and 2)
Secondary outcomes (12)
Change from baseline to each time point of measurement during each treatment period and to EOS in supine blood pressure
mmHg
Measured: Up to 13 days
Change from baseline to each time point of measurement during each treatment period and to EOS in pulse rate
bpm
Measured: Up to 13 days
Body weight at baseline and end of study visit
Measured: Up to 13 days
Change from baseline to EOS for hematology
Measured: Up to 13 days
Change from baseline to EOS for clinical chemistry
Measured: Up to 13 days
Change from baseline to EOS for pregnancy serum test
Measured: Up to 13 days
Change from baseline to EOS for virus serology
Measured: Up to 13 days
Change from baseline to each time point of measurement during each treatment period and to EOS in ECG variables
ECG variables are to be recorded at rest using a standard 12-lead ECG
Measured: Up to 13 days
Number of patients with treatment-emergent ECG abnormalities for each treatment period
Measured: from study drug administration on Day 1 up to 48 hours post-dose
Number of patients with treatment-emergent physical examination abnormalities at EOS
Measured: Up to 13 days
Number of patients with treatment-emergent AEs and SAEs for each treatment period
Measured: from study drug administration on Day 1 up to 48 hours post-dose
Number of patients with AEs leading to premature discontinuation of study drug
Measured: Entire duration of study
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted14 Jun 2013 (estimated)
- Study start1 Jul 2011
- Primary completion1 Jul 2011
- Study completion1 Jul 2011
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (1)Papers the sponsor has linked to this study.
- Other trials for Healthy SubjectsStudies 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
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 20 participants (actual)
Sponsor and investigators
- Lead sponsor
- Idorsia Pharmaceuticals Ltd.
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Daniela Baldoni, PharmD, PhD, Study director, Actelion
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT01877629
- Sponsor's protocol ID
- AC-060-104
- Status last verified
- Jul 2018
- First submitted
- 12 Jun 2013
- Last updated
- 10 Jul 2018
- Results posted
- No
- Data monitoring committee
- No
Publications
Baldoni D, Mackie A, Gutierrez M, Theodor R, Dingemanse J. Setipiprant, a selective oral antagonist of human CRTH2: relative bioavailability of a capsule and a tablet formulation in healthy female and male subjects. Clin Ther. 2013 Nov;35(11):1842-8. doi: 10.1016/j.clinthera.2013.09.003. Epub 2013 Oct 4.
PubMed 24095247
Study at a glance
From the registry record, last updated by the sponsor on 10 Jul 2018. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Single-center, Open-label, Two-period, Two-treatment, Crossover, Single-dose Study in Healthy Female and Male Subjects to Assess the Pharmacokinetics, Safety, and Tolerability of Two Different Formulations of ACT-129968
- ClinicalTrials.gov ID
- NCT01877629
- Acronym / sponsor ID
- AC-060-104
- Conditions
- Healthy Subjects
- Keywords
- Pharmacokinetics, Tolerability, Safety, ACT-129968
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 20 participants (actual)
- Lead sponsor
- Idorsia Pharmaceuticals Ltd.Industry (pharma, biotech, devices)
- Study start
- 1 Jul 2011
- Primary completion
- 1 Jul 2011 (actual)
- Study completion
- 1 Jul 2011 (actual)
- First posted
- 14 Jun 2013 (estimated)
- 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.
To explore the pharmacokinetics (PK) of a single dose of two different formulations of ACT-129968, i.e., tablet versus capsule and to evaluate the safety and tolerability of a single dose of two different formulations of ACT-129968, i.e., tablet versus capsule.
Detailed description
A total of 10 female and 10 male healthy subjects will be enrolled and will attend two treatment periods, separated by a 7-9 day washout. Over these two periods, two formulations of ACT-129968 (Treatment A: two capsules, 250 mg each; Treatment B: one tablet, 500 mg) will be administered in the sequence A/B or B/A to 10 subjects (5 females and 5 males) per sequence as determined by randomization.
Study design
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| ACT-129968 tablet/capsules | Experimental | Drug: ACT-129968 500 mg tablet, Drug: ACT-129968 250 mg capsuleSubjects attend two treatment periods. In the first treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as a tablet (1 tablet, 500 mg) in the fasted state. In the second treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as capsules (2 capsules, 250 mg each) in the fasted state. There is a 7-9 day washout period between the first treatment period and the second treatment period. |
| ACT-129968 capsules/tablet | Experimental | Drug: ACT-129968 500 mg tablet, Drug: ACT-129968 250 mg capsuleSubjects attend two treatment periods. In the first treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as capsules (2 capsules, 250 mg each) in the fasted state. In the second treatment period subjects receive a single, oral dose of ACT-129968 500 mg administered as a tablet (1 tablet, 500 mg each) in the fasted state. There is a 7-9 day washout period between the first treatment period and the second treatment period. |
Who may qualify
- Ages
- 18 to 45 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (13 listed)
- Signed informed consent in the local language prior to any study-mandated procedure.
- Women must have
- Women of childbearing potential must consistently and correctly use (from screening, during the entire study, and for at least 28 days after last study drug intake) a reliable method of contraception with a failure rate of < 1% per year, be sexually inactive, or have a vasectomized partner.
- Women not of childbearing potential are defined as post-menopausal (i.e., spontaneous amenorrhea for at least 1 year without an alternative medical cause) or surgically or naturally sterile.
- No clinically significant findings on the physical examination at screening.
Key exclusion criteria (18 listed)
- Pregnant or lactating women.
- Known allergic reactions or hypersensitivity to any excipient of the drug formulation(s).
- History or clinical evidence of any disease and/or existence of any surgical or medical condition which might interfere with the absorption, distribution, metabolism, or excretion of the study drug (appendectomy and herniotomy allowed, cholecystectomy not allowed).
- Previous history of fainting, collapse, syncope, orthostatic hypotension, or vasovagal reactions.
- History or clinical evidence of allergic rhinitis or asthma.
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 |
|---|---|---|
| ACT-129968 500 mg tabletACT-129968, a tetrahydropyridoindole derivative, is a chemoattractant receptor homologous molecule expressed on T helper 2 cells (CRTH2) antagonist | Drug | ACT-129968 capsules/tablet, ACT-129968 tablet/capsules |
| ACT-129968 250 mg capsuleACT-129968, a tetrahydropyridoindole derivative, is a chemoattractant receptor homologous molecule expressed on T helper 2 cells (CRTH2) antagonist | Drug | ACT-129968 capsules/tablet, ACT-129968 tablet/capsules |
Primary outcome
The area under the plasma concentration-time curve from time zero to time t of the last measured concentration above the limit of quantification (AUC0-t).
Time frame: Up to 48 h in each treatment period (1 and 2)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
The area under the plasma concentration-time curve from zero to infinity (AUC0-infinity).
Time frame: Up to 48 h in each treatment period (1 and 2)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
The maximum plasma concentration (Cmax)
Time frame: Up to 48 h in each treatment period (1 and 2)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
The time to reach maximum plasma concentration (tmax)
Time frame: Up to 48 h in each treatment period (1 and 2)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
The terminal elimination half-life (t½)
Time frame: Up to 48 h in each treatment period (1 and 2)
The plasma PK parameters for ACT-129968 will be derived by non-compartmental analysis of the plasma concentrationtime profiles.
12 secondary outcomes
Change from baseline to each time point of measurement during each treatment period and to EOS in supine blood pressure
Time frame: Up to 13 days
Change from baseline to each time point of measurement during each treatment period and to EOS in pulse rate
Time frame: Up to 13 days
Body weight at baseline and end of study visit
Time frame: Up to 13 days
Change from baseline to EOS for hematology
Time frame: Up to 13 days
Change from baseline to EOS for clinical chemistry
Time frame: Up to 13 days
Change from baseline to EOS for pregnancy serum test
Time frame: Up to 13 days
Change from baseline to EOS for virus serology
Time frame: Up to 13 days
Change from baseline to each time point of measurement during each treatment period and to EOS in ECG variables
Time frame: Up to 13 days
Number of patients with treatment-emergent ECG abnormalities for each treatment period
Time frame: from study drug administration on Day 1 up to 48 hours post-dose
Number of patients with treatment-emergent physical examination abnormalities at EOS
Time frame: Up to 13 days
Number of patients with treatment-emergent AEs and SAEs for each treatment period
Time frame: from study drug administration on Day 1 up to 48 hours post-dose
Number of patients with AEs leading to premature discontinuation of study drug
Time frame: Entire duration of study
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 10 Jul 2018.
- Derived from this study: PubMed 24095247Baldoni D, Mackie A, Gutierrez M, Theodor R, Dingemanse J. Setipiprant, a selective oral antagonist of human CRTH2: relative bioavailability of a capsule and a tablet formulation in healthy female and male subjects. Clin Ther. 2013 Nov;35(11):1842-8. doi: 10.1016/j.clinthera.2013.09.003. Epub 2013 Oct 4.
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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.
Daniela Baldoni, PharmD, PhD study director
Actelion
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing ACT-129968 500 mg tablet and ACT-129968 250 mg capsule in people with Healthy Subjects, run by Idorsia Pharmaceuticals Ltd. at 1 site in Germany.
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 13 inclusion and 18 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 10 Jul 2018. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in Germany. 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?
The area under the plasma concentration-time curve from time zero to time t of the last measured concentration above the limit of quantification (AUC0-t). (time frame: Up to 48 h in each treatment period (1 and 2)). The study lists 5 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 NCT01877629, which also lists 1 linked publication.
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 10 Jul 2018.