NCT02068235

Single-center, Open-label, Randomized, Two-way Crossover Study to Investigate the Absolute Bioavailability of a Single Oral Dose of Ponesimod in Healthy Male Subjects

Completed Phase 1 Last updated 20 May 2015

What this trial tests

Phase 1 trial testing Ponesimod 5mg i.v. in Healthy in 17 participants. Completed in 1 November 2014.

Timeline

1 August 2014

Primary endpoint
1 November 2014

1 November 2014

Quick facts

Lead sponsor	Actelion
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	crossover
Masking	none
Enrollment	17
Start date	1 August 2014
Primary completion	1 November 2014
Estimated completion	1 November 2014
Sites	1 location across United Kingdom

Drugs / interventions tested

• Ponesimod 5mg i.v. — full drug profile →
• Ponesimod i.v. — full drug profile →
• Ponesimod 10 mg tablet

Conditions studied

• Healthy — all drugs for Healthy →

Sponsor

Actelion — full company profile →

Who can join

Adults 18 to 45, male only, with Healthy. Healthy volunteers can join.

What's being measured

Primary outcomes are the specific endpoints the trial is designed to prove or disprove.

• Area under the plasma concentration-time curve (AUC(0-144h)) of ponesimod
  Time frame: 7 Days
  Blood samples for pharmacokinetic analysis will be taken immediately prior to dosing with ponesimod, and at various time points up to 7 days after dosing. AUC(0-144) will be calculated according to the linear trapezoidal rule using the measured concentration-time values above the limit of quantification.
• Area under the plasma concentration-time curve (AUC(0-infinity)) of ponesimod
  Time frame: 7 Days
  Blood samples for pharmacokinetic analysis will be taken immediately prior to dosing with ponesimod, and at various time points up to 7 days after dosing. AUC(0-infinity) will be calculated by combining AUC(0-144) and AUC(extra). AUC(extra) represents an extrapolated value obtained by Ct/λz, where Ct is the last plasma concentration measured above the limit of quantification and λz represents the
• Maximum plasma concentration (Cmax) of ponesimod
  Time frame: 7 Days
  Blood samples for pharmacokinetic analysis will be taken immediately prior to dosing with ponesimod, and at various time points up to 7 days after dosing. Cmax will be calculated on the basis of the blood sampling time points.
• Plasma half life (t1/2) of ponesimod
  Time frame: 7 Days
  Blood samples for pharmacokinetic analysis will be taken immediately prior to dosing with ponesimod, and at various time points up to 7 days after dosing. t1/2 will be calculated on the basis of the blood sampling time points.
• Time to maximum plasma concentration (tmax) after oral administration of ponesimod
  Time frame: 7 Days
  Blood samples for pharmacokinetic analysis will be taken immediately prior to dosing with ponesimod, and at various time points up to 7 days after dosing. tmax will be calculated on the basis of the blood sampling time points.
• Total body clearance (CL) after intravenous administration of ponesimod
  Time frame: 7 Days
  Blood samples for pharmacokinetic analysis will be taken immediately prior to dosing with ponesimod, and at various time points up to 7 days after dosing. CL Total body clearance will be calculated as follows: CL = Dose / AUC(0-infinity).

Sponsor's own description

This study consists of a single-dose pilot phase and a randomized, two-way crossover, single-dose main phase.The aim of this study is to evaluate the absolute bioavailability of the oral formulation (tablet) of ponesimod compared to an intravenous (i.v.) ponesimod formulation. Three subjects will be included in the pilot phase and 12 subjects in the main crossover phase.

Publications & conference data

1 peer-reviewed publication reference this trial (live from Europe PMC):

1. The S1P-S1PR Axis in Neurological Disorders-Insights into Current and Future Therapeutic Perspectives.
   Lucaciu A, Brunkhorst R, Pfeilschifter JM, Pfeilschifter W, et al · · 2020 · cited 53× · PMID 32580348 · DOI 10.3390/cells9061515