Clinical trial

An Open-Label Study to Evaluate the Absolute Bioavailability of Genz-112638 and the Absorption, Metabolism, and Excretion of [14C]-Genz-112638 in Male Subjects

ID

Name

GZGD02107

Description

Objectives: To determine pharmacokinetic (PK) variables, including absolute bioavailability (F), of Genz-99067, the free base of the L-tartaric acid salt of Genz-112638 as it exists in plasma, after a single intravenous (IV) dose and after a single oral dose of Genz-112638 (unlabeled). To determine the PK, total recovery, routes and rates of excretion, and the metabolic profile of Genz-99067 after 5 days of BID oral dosing with unlabeled Genz-112638 followed by a single dose of \[14C\]-Genz-112638.

Trial arms

Trial start

2009-06-03

Estimated PCD

2009-07-05

Trial end

2009-07-05

Status

Completed

Phase

Early phase I

Treatment

Genz-112638

Pharmaceutical form:Solution-Route of administration:IV

Arms:

Treatment Period 1 -2, Treatment Period 1-4

Other names:

GZ385660/ eliglustat, Cerdelga

Genz-112638

Pharmaceutical form:Capsule-Route of administration:Oral

Arms:

Treatment Period 1 -2, Treatment Period 1-4

Other names:

GZ385660/ eliglustat

[14C]-Genz-112638

Pharmaceutical form:Solution-Route of administration:Oral

Arms:

Treatment Period 1-4

Other names:

GZ385660/ eliglustat

Size

10

Primary endpoint

Assessment of pharmacokinetic (PK) parameter: Cmax

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: Tmax

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: AUC0-∞

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: AUC0 -τ

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: AUC0-∞/D

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: AUC0-τ/D

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: F

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: CL/F

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: t½

Multiple timepoints up to Day 26

Pharmacokinetic (PK) parameter: Absolute bioavailability (F) of single-dose oral versus single-dose IV administration

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: Total radioactivity excreted in urine and feces

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: Total radioactivity in whole blood and plasma

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: % relative abundance of each component in samples of plasma or excreta

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: The percentage of the administered dose attributed to each component in samples of urine or feces

Multiple timepoints up to Day 26

Assessment of pharmacokinetic (PK) parameter: The radioactivity of [14C]-Genz-99067 and each major metabolite in plasma, as identified by radio-profiling

Multiple timepoints up to Day 26

Noncompartmental PK parameters: AUC0-t

Multiple timepoints up to Day 26

Noncompartmental PK parameters: AUC0-∞

Multiple timepoints up to Day 26

Noncompartmental PK parameters: Cmax

Multiple timepoints up to Day 26

Noncompartmental PK parameters: Tmax

Multiple timepoints up to Day 26

Noncompartmental PK parameters: t½

Multiple timepoints up to Day 26

Noncompartmental PK parameters: Vz/F

Multiple timepoints up to Day 26

Noncompartmental PK parameters: CL/F

Multiple timepoints up to Day 26

Noncompartmental PK parameters for urine and feces: Cum Ae

Multiple timepoints up to Day 26

Noncompartmental PK parameters for urine and feces: % dose

Multiple timepoints up to Day 26

Renal clearance (CLR) for total plasma radioactivity and Genz-99067

Multiple timepoints up to Day 26

PK parameters [AUC0-τ, AUC0-∞, Cmax, Tmax, t½] and metabolite ratio for metabolite(s) of Genz-99067

Multiple timepoints up to Day 26

Eligibility criteria

Inclusion Criteria: Having given written informed consent prior to undertaking any study-related procedure The subject has a body weight of 50 to 100 kg \[110 to 220 pounds (lb)\] with a body mass index (BMI) less than 30 kilograms per square meter (kg/m2) at Screening. The subject's physical examination results, vital signs, laboratory assessments, and cardiac assessments are within normal limits or, if abnormal, are not clinically significant at Screening and Day -1. Exclusion Criteria: Participants are excluded from the study if any of the following criteria apply: Prolonged QTc interval (eg, repeated demonstration of a QTc interval ≥450 msec), family history of long QT or Brugada Syndrome, and/or history of sudden death in a first-degree relative. The subject receives an immunization within 30 days of providing informed consent. The subject has a history of drug allergies (eg, significant rash, hives, etc in response to antibiotics). The above information is not intended to contain all considerations relevant to the potential participation in a clinical trial.

Protocol

{'studyType': 'INTERVENTIONAL', 'phases': ['PHASE1'], 'designInfo': {'allocation': 'NON_RANDOMIZED', 'interventionModel': 'SEQUENTIAL', 'primaryPurpose': 'BASIC_SCIENCE', 'maskingInfo': {'masking': 'NONE'}}, 'enrollmentInfo': {'count': 10, 'type': 'ACTUAL'}}

Updated at

2023-11-22

1 organization

2 products

1 indication

Organization

Product

Indication

Gaucher's Disease Type I

Product

[14C]-Genz-112638