A Study to Evaluate Cenerimod in Healthy Male Subjects

Single-center, Open-label Study With 14C-radiolabeled Cenerimod to Investigate the Mass Balance, Pharmacokinetics, and Metabolism Following Single Oral Administration to Healthy Male Subjects

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

Study Overview

• Status: Completed
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: Cenerimod

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• Netherlands
  • Groningen, Netherlands, 9728 NZ
    • PRA Health Science

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 45 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes

Description

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
• No clinically significant findings on the physical examination at screening
• Body mass index (BMI) of 18.0 to 30.0 kg/m2 (inclusive) at screening
• 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
• 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)
• History or clinical evidence suggestive of active or latent tuberculosis including a positive QuantiFERON®-TB test at screening
• 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
• 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)
• 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
• Any immunosuppressive treatment within 6 weeks or within 5 elimination half-lives of the immunosuppressive treatment, whichever is longer, before study treatment administration

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: Non-Randomized
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / 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

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
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

Outcome Measure	Measure Description	Time Frame
Cmax (maximum plasma concentration) of 14C-radioactivity in whole blood and plasma	Cmax is derived from the observed plasma concentration-time curves	From baseline up to a maximum of 99 days
tmax (time to reach Cmax) of 14C-radioactivity in whole blood and plasma	Tmax is derived from the observed plasma concentration-time curves	From baseline up to a maximum of 99 days
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	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	From baseline up to a maximum of 99 days
Incidence of safety events of interest	Events of interest are any abnormalities in ECG, vital signs or laboratory test results	From baseline up to a maximum of 99 days
Number of participants with adverse events (AEs)	Treatment-emergent AEs and treatment emergent serious AEs	From baseline up to a maximum of 99 days
Cenerimod metabolites profiling in plasma	Relative abundance expressed as percent of cenerimod	From baseline up to a maximum of 99 days
Cenerimod metabolites profiling in urine	Relative abundance expressed as percent of cenerimod	From baseline up to a maximum of 99 days
Cenerimod metabolites profiling in feces	Relative abundance expressed as percent of cenerimod	From baseline up to a maximum of 99 days

Collaborators and Investigators

• Sponsor: Viatris Innovation GmbH
• Investigators: Study Director: Clinical Trials, Viatris Innovation GmbH

Study record dates

Study Major Dates

• Study Start: September 1, 2016
• Primary Completion (Actual): December 1, 2016
• Study Completion (Actual): December 1, 2016

Study Registration Dates

• First Submitted: September 13, 2016
• First Submitted That Met QC Criteria: September 22, 2016
• First Posted (Estimated): September 26, 2016

Study Record Updates

• Last Update Posted (Estimated): September 22, 2025
• Last Update Submitted That Met QC Criteria: September 16, 2025
• Last Verified: July 1, 2018

More Information

Terms related to this study

• Additional Relevant MeSH Terms: cenerimod
• Other Study ID Numbers: AC-064-103

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No