Clinical trial NCT02929342: Study to Assess the Absorption, Distribution, Metabolism and Excretion (ADME) of [14C]-Pitolisant in Healthy Male Volunteers
Official title: 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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Volunteers
Lead sponsor: Bioprojet
Sponsor class: OTHER
First posted: 2016-10-11
Enrollment: 8
Sex: MALE
Minimum age (years): 30
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: PARALLEL
Primary purpose: BASIC_SCIENCE

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.


Eligibility criteria: 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

Primary outcomes:
measure: Mass balance recovery of total radioactivity (Ae) in urine, faeces and expired air.
timeFrame: from Day 8 (pre-dose) to 120 h post 14C-radioactivity dose
measure: Peak Plasma Concentration (Cmax), pitolisant and major metabolites.
timeFrame: From Day 1 (pre-dose) until 168hours post last dose
measure: Area under the plasma concentration versus time curve [AUC(0-tau), AUC(0-inf), %AUCextrap], pitolisant and major metabolites.
timeFrame: From Day 1 (pre-dose) until 168hours post last dose
measure: Volume of distribution (Vz/F), pitolisant and major metabolites.
timeFrame: From Day 1 (pre-dose) until 168hours post last dose
measure: Apparent clearance (Clss/F), pitolisant and major metabolites.
timeFrame: From Day 1 (pre-dose) until 168hours post last dose
measure: The slope of the apparent elimination phase (lambda-z), pitolisant and major metabolites.
timeFrame: From Day 1 (pre-dose) until 168hours post last dose
measure: The apparent elimination half-life (T½), pitolisant and major metabolites.
timeFrame: From Day 1 (pre-dose) until 168hours post last dose
measure: Time to reach Cmax (Tmax), pitolisant and major metabolites.
timeFrame: From Day 1 (pre-dose) until 168hours post last dose
Secondary outcomes:
Other outcomes:
Locations:
Study officials:
affiliation: Quotient Clinical
name: Litza McKenzie, MD
role: PRINCIPAL_INVESTIGATOR
affiliation: Bioprojet Pharma
name: Thierry Duvauchelle, MD
role: STUDY_DIRECTOR
References: