A Trial to Study the Absorption, Metabolism, and Excretion of [14C]-Olinciguat in Healthy Male Volunteers

Cyclerion Therapeutics8 enrolled

Overview

The primary objective is to characterize the pharmacokinetics (PK) of olinciguat and total radioactivity and to assess the elimination of total radioactivity from a single oral dose of \[14C\]-olinciguat.

OLI-103 is a Phase 1 open-label, nonrandomized, single-dose study in up to 8 subjects that will be conducted at a single center in the US. Safety assessments will be performed throughout the clinic period and multiple PK samples will be collected. Subjects will be confined to the clinical research center for at least 8 days. The purpose of the study is to determine the absorption, metabolism, and excretion of \[14C\]-olinciguat and to characterize and determine, where possible, the metabolites present in plasma, urine, and feces after a single oral dose. The study will help identify and characterize olinciguat metabolites, evaluate the likelihood of effects of liver or kidney impairment on the disposition of olinciguat, and assess the likelihood of drug-drug interactions with olinciguat.

Study Type

INTERVENTIONAL

Allocation

Purpose

OTHER

Masking

NONE

Enrollment

Conditions

Healthy Volunteers

Interventions

[14C]-olinciguatDRUG

oral capsule

Eligibility

Sex: MALEMin age: 18 YearsMax age: 55 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Males of any race, between 18 and 55 years of age, inclusive * Body mass index between 18 and 32 kg/m2, inclusive * Subject is in good health and has no clinically significant findings on physical examination * Men must agree to use protocol-specified contraception and also to not donate sperm throughout the study and for at least 90 days after the final dose of study drug Exclusion Criteria: * Any active or unstable clinically significant medical condition * Use of any prescribed or non-prescribed medication Additional inclusion/exclusion criteria may apply per protocol

Locations (1)

Covance Clinical Research Unit Inc.

Madison, Wisconsin, United States

Outcomes

Primary Outcomes

Amount of total radioactivity excreted in urine (Aeu) and feces (Aef)

Time frame: up to Day 15

Cumulative Aeu and cumulative Aef

Time frame: up to Day 15

Percentage of total radioactivity excreted in urine (feu) and feces (fef)

Time frame: up to Day 15

Cumulative feu and cumulative fef

Time frame: up to Day 15

Percentage of total radioactivity in total excreta (feces + urine)

Time frame: up to Day 15

Area under the concentration-time curve (AUC) from time zero to infinity (AUC0-inf) of olinciguat in plasma

Time frame: up to Day 15

AUC0-inf of total radioactivity in plasma and whole blood

Time frame: up to Day 15

AUC from time zero to the last quantifiable concentration (AUC0-last) of olinciguat in plasma

Time frame: up to Day 15

AUC0-last of total radioactivity in plasma and whole blood

Time frame: up to Day 15

Maximum observed concentration (Cmax) of olinciguat in plasma

Time frame: up to Day 15

Cmax of total radioactivity in plasma and whole blood

Time frame: up to Day 15

Time of Cmax (Tmax) of olinciguat in plasma

Data from ClinicalTrials.gov

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Secondary Outcomes

Levels of metabolite radioactivity excreted in urine and feces

Time frame: up to Day 15

AUC0-inf of metabolite radioactivity levels in plasma

Time frame: up to Day 15

AUC0-inf of plasma metabolite radioactivity levels relative to AUC0-inf of plasma total radioactivity (Plasma AUC0-inf Ratio of Metabolite Radioactivity/Total Radioactivity)

Time frame: up to Day 15

Chromatographic retention time of metabolites

Time frame: up to Day 15

Molecular ion mass of metabolites

Time frame: up to Day 15

Characteristic mass spectrometry fragmentation ions of metabolites

Time frame: up to Day 15

Chemical structures (graphical representations showing atom connectivity) proposed for plasma, urine, and feces metabolites

Time frame: up to Day 15

Number(s) of participants with ≥1 treatment-emergent serious adverse event (SAE)

Time frame: up to Day 15

Number(s) of participants with ≥1 adverse event (AE) leading to study drug discontinuation

Time frame: up to Day 15

Number(s) of participants with ≥1 Grade ≥3 AE (per CTCAE v. 5.0)

Time frame: up to Day 15

Number(s) of participants with ≥1 clinically significant abnormal physical examination finding

Time frame: up to Day 15