Phase 1Phase 1NCT04327089
Study to Evaluate the Pharmacokinetics and Drug-Drug Interactions of Setanaxib in Healthy Adult Male and Female Subjects
A Phase 1 study testing Setanaxib in people with Phase 1, run by Calliditas Therapeutics AB at 1 site in France.
Trial summary
The study is a monocentric, open label, phase 1 study to evaluate the pharmacokinetics, and in particular the dose proportionality of setanaxib and its metabolites after a single oral dose (400 mg, 800 mg, 1200 mg, and 1600 mg) (Part 1) and after multiple oral doses (Part 2). Read more about this study
- Who is it for?
- Ages 18 to 49 yearsHealthy volunteers can take part
- Conditions the study is for
- Phase 1
- What is being tested?
- Setanaxib
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 64 participants
- Where
- 1 siteFrance
- Study dates
- 24 Jun 2020to 23 Mar 2021
- 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 49 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Healthy adult male or female aged 18 to 49 years
- Provision of written informed consent to participate as shown by a signature on the subject consent form
- Smoke no more than 5 cigarettes a day are permitted. Smocking (including the use of smocking substitute e.g. nicotine patch) is not permitted from screening to the end of study visit
- Body weight of at least 45kg and a BMI included between 18.0 and 35.0 kg/m2
- Female subjects of childbearing potential must use a highly effective method of contraception to prevent pregnancy for 4 weeks before inclusion and must agree to continue strict contraception for 30 days after last administration of IMP. Male participants with female partners of childbearing potential must be willing to use a condom and require their partner to use an additional form of adequate contraception as approved by the Investigator. This requirement begins at the time of informed consent and ends at least 3 months after the last administration of IMP. Male study participants must also not donate sperm from baseline until 3 months after the last administration of IMP.
- Considered as healthy after a comprehensive clinical assessment (detailed medical history and complete physical examination)
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- Normal Blood Pressure (BP) and Heart Rate (HR) at the screening visit after 10 minutes in supine position.
- Normal ECG recording on a 12-lead ECG at the screening visit:
- Laboratory parameters within the normal range of the laboratory (hematological, blood chemistry tests, urinalysis). Individual values out of the normal range can be accepted if judged non-clinically significant by the Investigator
- Has not consumed and agrees to abstain from taking any dietary supplements or non-prescription drugs over the 7 days prior to screening.
- Has not consumed and agrees to abstain from taking any prescription drugs except contraception.
- Has not consumed alcohol containing beverages over the 48 hours prior to hospitalization
- Has not consumed grapefruit or grapefruit juice over the 48 hours prior to hospitalization
- Has the ability to understand the requirements of the study and is willing to comply with all study procedures
- Registered with the French Social Security in agreement with the French law on biomedical experimentation and register to the "Fichier national des personnes qui se prêtent à des recherches biomédicales"
Who cannot join
- Have already received setanaxib
- Contraindication(s) for any of the substrates used in the study
- Any history or presence of cardiovascular, pulmonary, gastro-intestinal, hepatic, renal, metabolic, hematological, neurologic, psychiatric, systemic or infectious disease
- Any history of severe cardiovascular disease, and any personal or family history of long QT syndrome, or evidence of abnormalities in cardiac conduction
- Frequent headaches and / or migraine, recurrent nausea and / or vomiting
- Symptomatic hypotension whatever the decrease of blood pressure or asymptomatic postural hypotension defined by a decrease in SBP or DBP equal to or greater than 20 mmHg within two minutes when changing from the supine to the standing position
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- Blood donation (including in the frame of a clinical study) within 2 months before administration;
- General anesthesia within 3 months before administration
- Presence or history of drug hypersensitivity, or allergic disease diagnosed and treated by a physician
- Inability to abstain from intensive muscular effort
- No possibility of contact in case of emergency
- Any drug intake (except paracetamol or oral contraception) during the last month prior to the first administration
- History or presence of drug or alcohol abuse (alcohol consumption > 40 grams / day)
- Excessive consumption of beverages with xanthine bases (> 4 cups or glasses / day) during the last 30 days
- Positive Hepatitis B surface (HBs) antigen or anti Hepatitis C Virus (HCV) antibody, or positive results for Human Immunodeficiency Virus (HIV) 1 or 2 tests
- Positive results of screening for drugs of abuse
- Any contraindication to the administration of midazolam, adefovir, losartan, omeprazole, sitagliptin
- Subject who, in the judgment of the Investigator, is likely to be non-compliant or uncooperative during the study, or unable to cooperate because of a language problem, poor mental development
- Currently in exclusion period from a previous study
- Administrative or legal supervision
- Subject who would receive more than 4500 euros as indemnities for his participation in biomedical study within the 12 last months, including the indemnities for the present study.
- Minor, pregnant or breast-feeding women, persons deprived of liberty by judicial or administrative decision, persons receiving psychiatric care and persons admitted to a health or social institution, adult subject to legal protection or unable to express consent.
- Positive results for SARS-CoV-2 tests.
Trial locations and contacts
1 site in 1 country.
About this study
Official title: An Open-Label Phase 1 Study to Evaluate the Pharmacokinetics and Drug-Drug Interactions of Setanaxib in Healthy Adult Male and Female Subjects
The study is a monocentric, open label, phase 1 study to evaluate the pharmacokinetics, and in particular the dose proportionality of setanaxib and its metabolites after a single oral dose (400 mg, 800 mg, 1200 mg, and 1600 mg) (Part 1) and after multiple oral doses (Part 2).
Read the detailed description
The study is a monocentric, open label, phase 1 study to evaluate the pharmacokinetics, and in particular the dose proportionality of setanaxib and its metabolites after a single oral dose (400 mg, 800 mg, 1200 mg, and 1600 mg) (Part 1) and after multiple oral doses (Part 2). The study will include 2 parts conducted in separate cohorts of subjects.
- Part 1 of the study will be an open label, single dose study evaluating the pharmacokinetics, and in particular the dose proportionality of setanaxib formulated as tablets, in 4 separate cohorts of 6 to 8 healthy adult subjects
- Part 2 of the study will assess the pharmacokinetics of setanaxib tablets, expand the evaluation of potential drug-drug interactions, and assess the safety of setanaxib tablets at doses up to 1600mg/day for 14 days in separate 2 cohorts. The evaluation of drug-drug interactions will be carried out only at the top dose. Accordingly, a larger cohort (i.e. 16 subjects) will be included in Cohort 7.
- Conditions
- Phase 1
- Being tested
- Setanaxib
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
SetanaxibDrug
Also called GKT137831
Nox 1/4 inhibitor
| Study group | Role | What they receive |
|---|---|---|
| Part 1- Cohort 1 | Experimental | Single oral dose of 400 mg Setanaxib administered as 1x400 mg tablet in fasting conditions. Receives: Drug: Setanaxib |
| Part 1- Cohort 2 | Experimental | Single oral dose of 800 mg Setanaxib administered as 2x400 mg tablet in fasting conditions. Receives: Drug: Setanaxib |
| Part 1- Cohort 3 | Experimental | Single oral dose of 1200 mg Setanaxib administered as 3x400 mg tablet in fasting conditions. Receives: Drug: Setanaxib |
| Part 1- Cohort 4 | Experimental | Single oral dose of 1600 mg Setanaxib administered as 4x400 mg tablet in fasting conditions. Receives: Drug: Setanaxib |
| Part 2- Cohort 5 | Experimental | Repeated 10-Day dosing of 1200mg/day of Setanaxib administered as 2x400mg tablet in the morning and as 1x400mg tablet in the evening in fedding conditions. Receives: Drug: Setanaxib |
| Part 2- Cohort 6 | Experimental | Repeated 10-Day dosing of 1600mg/day of Setanaxib administered as 2x400mg tablet in the morning and as 2x400mg tablet in the evening in fedding conditions. Receives: Drug: Setanaxib |
| Cohort 7 | Experimental | Repeated 10-Day dosing of 1600mg/day of Setanaxib administered as 2x400mg tablet in the morning and as 2x400mg tablet in the evening in fedding conditions. Additionnaly, this cohort includes the evaluation of potential Drug-Drug interactions with CYPs and transporters. Receives: Drug: Setanaxib |
What is being measured
The primary outcome is the main question the study is designed to answer.
Dose proportionality of setanaxib tablets after single oral administration of different doses.
Measure the AUC and bioavailability (particularly the dose proportionality) of setanaxib tablets, after single oral administration of different doses (400, 800, 1200 and 1600mg) in healthy adult male and female subjects.
Measured: 144 hours
Drug-drug interactions of multiple oral administrations of setanaxib with 5 drugs that interact with CYP3A4, OAT1, OAT3, 2C9 and 2C19.
Measure the changes in AUC of 5 drugs that interact with CYP3A4, OAT1, OAT3, 2C9 and 2C19 in healthy adult male (8) and female (8) subjects after multiple administrations of Setanaxib at dose of 1600mg only (cohort 6) or 800mg (cohort 7).
Measured: 14 days
Assessment of safety after multiple oral administration of different doses of setanaxib.
To evaluate the biological, physiological and treatment-related adverse events of setanaxib after multiple oral administration doses up to 1600 mg/day in healthy male and female subjects.
Measured: 10 days
Secondary outcomes (2)
Assessment of safety after single oral administration of different doses of setanaxib.
To evaluate the biological, physiological and treatment-related adverse events of setanaxib tablets after single oral administration of 4 different doses in healthy male and female subjects.
Measured: 144 hours
Dose proportionality of setanaxib tablets after multiple oral administration of different doses.
Measure the AUC and bioavailability (particularly the dose proportionality) of setanaxib tablets after multiple oral administration at 2 different doses in healthy adult male and female subjects.
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 posted30 Mar 2020
- Study start24 Jun 2020
- Primary completion23 Mar 2021
- Study completion23 Mar 2021
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 Phase 1Studies 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
- Single group
- Model description
- Open-Label Phase 1 Study
- Masking
- None (open label)
- Enrolment
- 64 participants (actual)
Sponsor and investigators
- Lead sponsor
- Calliditas Therapeutics AB
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT04327089
- Sponsor's protocol ID
- GSN000310
- Status last verified
- May 2021
- First submitted
- 12 Mar 2020
- Last updated
- 30 Jun 2022
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
- Individual data sharing
- Undecided
Publications
Gage MC, Thippeswamy T. Inhibitors of Src Family Kinases, Inducible Nitric Oxide Synthase, and NADPH Oxidase as Potential CNS Drug Targets for Neurological Diseases. CNS Drugs. 2021 Jan;35(1):1-20. doi: 10.1007/s40263-020-00787-5. Epub 2021 Jan 30.
PubMed 33515429
Study at a glance
From the registry record, last updated by the sponsor on 30 Jun 2022. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- An Open-Label Phase 1 Study to Evaluate the Pharmacokinetics and Drug-Drug Interactions of Setanaxib in Healthy Adult Male and Female Subjects
- ClinicalTrials.gov ID
- NCT04327089
- Acronym / sponsor ID
- GSN000310
- Conditions
- Phase 1
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 64 participants (actual)
- Lead sponsor
- Calliditas Therapeutics ABIndustry (pharma, biotech, devices)
- Study start
- 24 Jun 2020 (actual)
- Primary completion
- 23 Mar 2021 (actual)
- Study completion
- 23 Mar 2021 (actual)
- First posted
- 30 Mar 2020 (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 study is a monocentric, open label, phase 1 study to evaluate the pharmacokinetics, and in particular the dose proportionality of setanaxib and its metabolites after a single oral dose (400 mg, 800 mg, 1200 mg, and 1600 mg) (Part 1) and after multiple oral doses (Part 2).
Detailed description
The study is a monocentric, open label, phase 1 study to evaluate the pharmacokinetics, and in particular the dose proportionality of setanaxib and its metabolites after a single oral dose (400 mg, 800 mg, 1200 mg, and 1600 mg) (Part 1) and after multiple oral doses (Part 2). The study will include 2 parts conducted in separate cohorts of subjects.
- Part 1 of the study will be an open label, single dose study evaluating the pharmacokinetics, and in particular the dose proportionality of setanaxib formulated as tablets, in 4 separate cohorts of 6 to 8 healthy adult subjects
- Part 2 of the study will assess the pharmacokinetics of setanaxib tablets, expand the evaluation of potential drug-drug interactions, and assess the safety of setanaxib tablets at doses up to 1600mg/day for 14 days in separate 2 cohorts. The evaluation of drug-drug interactions will be carried out only at the top dose. Accordingly, a larger cohort (i.e. 16 subjects) will be included in Cohort 7.
Study design
- Primary purpose
- Other
- Allocation
- Non-randomised
- Intervention model
- Single group
- Masking
- None (open label)
- Number of arms
- 7
- Model description
- Open-Label Phase 1 Study
| Arm | Type | Receives |
|---|---|---|
| Part 1- Cohort 1 | Experimental | Drug: SetanaxibSingle oral dose of 400 mg Setanaxib administered as 1x400 mg tablet in fasting conditions. |
| Part 1- Cohort 2 | Experimental | Drug: SetanaxibSingle oral dose of 800 mg Setanaxib administered as 2x400 mg tablet in fasting conditions. |
| Part 1- Cohort 3 | Experimental | Drug: SetanaxibSingle oral dose of 1200 mg Setanaxib administered as 3x400 mg tablet in fasting conditions. |
| Part 1- Cohort 4 | Experimental | Drug: SetanaxibSingle oral dose of 1600 mg Setanaxib administered as 4x400 mg tablet in fasting conditions. |
| Part 2- Cohort 5 | Experimental | Drug: SetanaxibRepeated 10-Day dosing of 1200mg/day of Setanaxib administered as 2x400mg tablet in the morning and as 1x400mg tablet in the evening in fedding conditions. |
| Part 2- Cohort 6 | Experimental | Drug: SetanaxibRepeated 10-Day dosing of 1600mg/day of Setanaxib administered as 2x400mg tablet in the morning and as 2x400mg tablet in the evening in fedding conditions. |
| Cohort 7 | Experimental | Drug: SetanaxibRepeated 10-Day dosing of 1600mg/day of Setanaxib administered as 2x400mg tablet in the morning and as 2x400mg tablet in the evening in fedding conditions. Additionnaly, this cohort includes the evaluation of potential Drug-Drug interactions with CYPs and transporters. |
Who may qualify
- Ages
- 18 to 49 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (15 listed)
- Healthy adult male or female aged 18 to 49 years
- Provision of written informed consent to participate as shown by a signature on the subject consent form
- Smoke no more than 5 cigarettes a day are permitted. Smocking (including the use of smocking substitute e.g. nicotine patch) is not permitted from screening to the end of study visit
- Body weight of at least 45kg and a BMI included between 18.0 and 35.0 kg/m2
- Female subjects of childbearing potential must use a highly effective method of contraception to prevent pregnancy for 4 weeks before inclusion and must agree to continue strict contraception for 30 days after last administration of IMP. Male participants with female partners of childbearing potential must be willing to use a condom and require their partner to use an additional form of adequate contraception as approved by the Investigator. This requirement begins at the time of informed consent and ends at least 3 months after the last administration of IMP. Male study participants must also not donate sperm from baseline until 3 months after the last administration of IMP.
Key exclusion criteria (23 listed)
- Have already received setanaxib
- Contraindication(s) for any of the substrates used in the study
- Any history or presence of cardiovascular, pulmonary, gastro-intestinal, hepatic, renal, metabolic, hematological, neurologic, psychiatric, systemic or infectious disease
- Any history of severe cardiovascular disease, and any personal or family history of long QT syndrome, or evidence of abnormalities in cardiac conduction
- Frequent headaches and / or migraine, recurrent nausea and / or vomiting
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 |
|---|---|---|
| SetanaxibAlso: GKT137831Nox 1/4 inhibitor | Drug | Cohort 7, Part 1- Cohort 1, Part 1- Cohort 2, Part 1- Cohort 3, Part 1- Cohort 4, Part 2- Cohort 5, Part 2- Cohort 6 |
Primary outcome
Dose proportionality of setanaxib tablets after single oral administration of different doses.
Time frame: 144 hours
Measure the AUC and bioavailability (particularly the dose proportionality) of setanaxib tablets, after single oral administration of different doses (400, 800, 1200 and 1600mg) in healthy adult male and female subjects.
Drug-drug interactions of multiple oral administrations of setanaxib with 5 drugs that interact with CYP3A4, OAT1, OAT3, 2C9 and 2C19.
Time frame: 14 days
Measure the changes in AUC of 5 drugs that interact with CYP3A4, OAT1, OAT3, 2C9 and 2C19 in healthy adult male (8) and female (8) subjects after multiple administrations of Setanaxib at dose of 1600mg only (cohort 6) or 800mg (cohort 7).
Assessment of safety after multiple oral administration of different doses of setanaxib.
Time frame: 10 days
To evaluate the biological, physiological and treatment-related adverse events of setanaxib after multiple oral administration doses up to 1600 mg/day in healthy male and female subjects.
2 secondary outcomes
Assessment of safety after single oral administration of different doses of setanaxib.
Time frame: 144 hours
Dose proportionality of setanaxib tablets after multiple oral administration of different doses.
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 30 Jun 2022.
- Derived from this study: PubMed 33515429Gage MC, Thippeswamy T. Inhibitors of Src Family Kinases, Inducible Nitric Oxide Synthase, and NADPH Oxidase as Potential CNS Drug Targets for Neurological Diseases. CNS Drugs. 2021 Jan;35(1):1-20. doi: 10.1007/s40263-020-00787-5. Epub 2021 Jan 30.
- Individual participant dataSharing planned: Undecided
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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.
The record lists no contact. Use the official record to reach the sponsor.
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 Setanaxib in people with Phase 1, run by Calliditas Therapeutics AB at 1 site in France.
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 15 inclusion and 23 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 30 Jun 2022. 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 France. 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?
Dose proportionality of setanaxib tablets after single oral administration of different doses. (time frame: 144 hours). The study lists 3 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 NCT04327089, 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 30 Jun 2022.