A Study to Evaluate Cenerimod in Healthy Male Subjects
Study Details
Study Description
Brief Summary
The main objective of the study is to investigate the rate and routes of elimination of cenerimod and the mass balance in urine, feces, and expired air
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
| Phase 1 |
Study Design
Arms and Interventions
| Arm | Intervention/Treatment |
|---|---|
| Experimental: Treatment and observation period On Day 1, subjects will receive a single oral dose of 2 mg 14C-radiolabeled cenerimod. Subjects will be followed for 21 days during which blood, urine, feces, and expired air samples will be collected |
Drug: Cenerimod
Oral formulation of cenerimod (2mg) containing 100 μCi (3.7 MBq) of 14C-radiolabeled cenerimod
|
| Experimental: Extended observation period In case, radioactivity recovery does not meet the stopping criteria described in the protocol, the subjects will have to come for a maximum of 7 24-h in-clinic visits during which blood, urine, feces, and expired air samples will be collected |
Drug: Cenerimod
Oral formulation of cenerimod (2mg) containing 100 μCi (3.7 MBq) of 14C-radiolabeled cenerimod
|
Outcome Measures
Primary Outcome Measures
- Cumulative excretion calculated by summing up the daily radioactivity excretion measured by means of liquid scintillation counting in urine, feces, and expired air (if applicable) [From baseline up to a maximum of 99 days]
Secondary Outcome Measures
- Cmax (maximum plasma concentration) of 14C-radioactivity in whole blood and plasma [From baseline up to a maximum of 99 days]
Cmax is derived from the observed plasma concentration-time curves
- tmax (time to reach Cmax) of 14C-radioactivity in whole blood and plasma [From baseline up to a maximum of 99 days]
Tmax is derived from the observed plasma concentration-time curves
- t1/2 (terminal half-life) [From baseline up to a maximum of 99 days]
- Area under the plasma concentration-time curve (AUC) of 14C-radioactivity in whole blood and plasma [From baseline up to a maximum of 99 days]
AUC is defined for the time intervals from zero to time t of the last measured concentration above the limit of quantification and from zero to infinity
- Incidence of safety events of interest [From baseline up to a maximum of 99 days]
Events of interest are any abnormalities in ECG, vital signs or laboratory test results
- Number of participants with adverse events (AEs) [From baseline up to a maximum of 99 days]
Treatment-emergent AEs and treatment emergent serious AEs
- Cenerimod metabolites profiling in plasma [From baseline up to a maximum of 99 days]
Relative abundance expressed as percent of cenerimod
- Cenerimod metabolites profiling in urine [From baseline up to a maximum of 99 days]
Relative abundance expressed as percent of cenerimod
- Cenerimod metabolites profiling in feces [From baseline up to a maximum of 99 days]
Relative abundance expressed as percent of cenerimod
Eligibility Criteria
Criteria
Inclusion Criteria:
-
Signed informed consent in a language understandable to the subject prior to any study-mandated procedure
-
Healthy male subjects aged between 45 and 65 years (inclusive) at screening
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No clinically significant findings on the physical examination at screening
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Body mass index (BMI) of 18.0 to 30.0 kg/m2 (inclusive) at screening
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Systolic blood pressure (SBP) 100-145 mmHg and diastolic blood pressure (DBP) 50-90 mmHg, measured on either arm, after 5 min in the supine position at screening and at Day 1 pre-dose
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Heart rate (HR) 55-90 bpm (inclusive) measured with 12-lead ECG after 5 min in the supine position at screening and at Day 1 pre-dose
Exclusion Criteria:
-
Known hypersensitivity to cenerimod or to S1P receptor modulators, or to any excipients of the cenerimod drug formulation
-
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 treatment (appendectomy and herniotomy allowed, cholecystectomy not allowed)
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History or clinical evidence suggestive of active or latent tuberculosis including a positive QuantiFERON®-TB test at screening
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Any cardiac condition or illness (including 12-lead ECG abnormalities) with a potential to increase the cardiac risk of the subject based on the standard 12-lead ECG at screening and at Day 1 pre-dose
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Participation in another study with a radiation burden of > 0.1 mSv and ≤ 1 mSv in the period of 1 year prior to screening; a radiation burden of ≥ 1.1 mSv and ≤ 2 mSv in the period of 2 years prior to screening, etc. (add 1 year per 1 mSv)
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Any circumstances or conditions, which, in the opinion of the investigator, may affect the subject's full participation in the study or compliance with the protocol
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Any immunosuppressive treatment within 6 weeks or within 5 elimination half-lives of the immunosuppressive treatment, whichever is longer, before study treatment administration
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | PRA Health Science | Groningen | Netherlands | 9728 NZ |
Sponsors and Collaborators
- Idorsia Pharmaceuticals Ltd.
Investigators
- Study Director: Marie-Laure Boof, PhD, Actelion
Study Documents (Full-Text)
None provided.More Information
Publications
None provided.- AC-064-103