Study to Assess the Absorption, Distribution, Metabolism and Excretion (ADME) of [14C]-Pitolisant in Healthy Male Volunteers

An Open Label, Single-Period Repeated Dose Study Designed to Assess the Mass Balance Recovery, Metabolite Profile and Metabolite Identification of [14C]-Pitolisant, at Steady-State Conditions, in Healthy CYP2D6 Genotyped Male Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT02929342

Enrollment

Registered

2016-10-11

Start date

2016-07-31

Completion date

2016-08-31

Last updated

2016-10-11

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Volunteers

Brief summary

The purpose of this study is to better define the absorption and elimination pathways, and circulating metabolites of Pitolisant at steady state using Pitolisant radiolabelled, in healthy CYP2D6 genotyped male subject.

Interventions

DRUGPitolisant

RADIATION[14C]-Pitolisant

Study design

Allocation

NON_RANDOMIZED

Intervention model

PARALLEL

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

30 Years to 65 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy males aged 30 to 65 years. * Body mass index 18.0 to 35.0 kg/m2. * Genotyped with regard to their CYP2D6 status.

Exclusion criteria

* Participation in a clinical research study within the previous 3 months * Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 1999, shall participate in the study. * Regular alcohol consumption in males \>21 units per week. * Current smokers and those who have smoked within the last 12 months. * Evidence of renal impairment at screening, as indicated by an estimated creatinine clearance (CLcr) of \<90 mL/min using the Cockcroft-Gault equation. * Use of CYP2D6 inhibitors or inducers in the 28 days prior to IMP administration

Design outcomes

Primary

Measure	Time frame
Mass balance recovery of total radioactivity (Ae) in urine, faeces and expired air.	from Day 8 (pre-dose) to 120 h post 14C-radioactivity dose
Peak Plasma Concentration (Cmax), pitolisant and major metabolites.	From Day 1 (pre-dose) until 168hours post last dose
Area under the plasma concentration versus time curve [AUC(0-tau), AUC(0-inf), %AUCextrap], pitolisant and major metabolites.	From Day 1 (pre-dose) until 168hours post last dose
Volume of distribution (Vz/F), pitolisant and major metabolites.	From Day 1 (pre-dose) until 168hours post last dose
Apparent clearance (Clss/F), pitolisant and major metabolites.	From Day 1 (pre-dose) until 168hours post last dose
The slope of the apparent elimination phase (lambda-z), pitolisant and major metabolites.	From Day 1 (pre-dose) until 168hours post last dose
The apparent elimination half-life (T½), pitolisant and major metabolites.	From Day 1 (pre-dose) until 168hours post last dose
Time to reach Cmax (Tmax), pitolisant and major metabolites.	From Day 1 (pre-dose) until 168hours post last dose

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026