Study of Radiolabeled Danicopan in Healthy Male Participants

NCT04889391 | Completed Phase 1 FDA Drug

• 1 other identifier: ACH471-005
• Study Type: interventional
• Target: 8
• Locations: 1 country
• Sites: 1

Brief Summary

This was an open-label study to evaluate the absorption, distribution, metabolism, and excretion of radioactivity in healthy male participants following a single 150-milligram (mg) oral dose of carbon-14 (\[14C\])-ACH-014447 (\[14C\])-danicopan) containing approximately 100 microcuries (µCi) of \[14C\].

Conditions

Healthy

Keywords

Danicopan; ACH-0144471; ALXN2040; Absorption; Distribution; Metabolism; Excretion; Total Radioactivity; ADME

Outcome Measures

Primary Outcomes (10)

• Mean Cumulative Percentages Of Total Radioactivity Recovered In Urine And Feces Following A Single Oral Dose Of [14C]-Danicopan

  Up to 96 hours postdose or maximum of 216 hours postdose for extended collection period

• Whole Blood And Plasma Pharmacokinetics (PK) Of Total Radioactivity After A Single Oral Dose Of [14C]-Danicopan: Area Under The Concentration-time Curve From Time 0 To The Time Of Last Quantifiable Concentration (AUC0-t)

  Up to 96 hours postdose or maximum of 216 hours postdose for extended collection period

• Whole Blood And Plasma PK Of Total Radioactivity After A Single Oral Dose Of [14C]-Danicopan: Area Under The Concentration-time Curve Extrapolated to Infinity (AUC0-inf)

  Up to 96 hours postdose or maximum of 216 hours postdose for extended collection period

• Whole Blood And Plasma PK Of Total Radioactivity After A Single Oral Dose Of [14C]-Danicopan: Maximum Observed Concentration (Cmax)

  Up to 96 hours postdose or maximum of 216 hours postdose for extended collection period

• Whole Blood And Plasma PK Of Total Radioactivity After A Single Oral Dose Of [14C]-Danicopan: Time To Maximum Observed Concentration (Tmax)

  Up to 96 hours postdose or maximum of 216 hours postdose for extended collection period

• Plasma PK Of Danicopan After A Single Oral Dose Of [14C]-Danicopan: AUC0-t

  Up to 96 hours postdose

• Plasma PK Of Danicopan After A Single Oral Dose Of [14C]-Danicopan: AUC0-inf

  Up to 96 hours postdose

• Plasma PK Of Danicopan After A Single Oral Dose Of [14C]-Danicopan: Cmax

  Up to 96 hours postdose

• Plasma PK Of Danicopan After A Single Oral Dose Of [14C]-Danicopan: Tmax

  Up to 96 hours postdose

• [14C]-Danicopan Metabolites In Plasma, Urine, And Feces

  Up to 96 hours postdose or maximum of 216 hours postdose for extended collection period

Secondary Outcomes (2)

• Percentage Of Total Radioactivity Detected For Each [14C]-Danicopan Metabolite in Plasma, Urine, And Feces

  Up to 96 hours postdose or maximum of 216 hours postdose for extended collection period

• Incidence Of Treatment-emergent Adverse Events

  Day 1 through Day 10

Study Arms (1)

[14C]-Danicopan

EXPERIMENTAL

Participants were administered a single oral dose of danicopan between 151 and 154 mg (nominal dose of 150 mg), providing approximately 100 μCi of \[14C\] radiolabel in the form of \[14C\]-danicopan.

Drug: [14C]-Danicopan

Interventions

[14C]-Danicopan DRUG

Liquid-filled capsules.

Also known as: ALXN2040, ACH-014447, ACH-4471, ACH4471, 4471

[14C]-Danicopan

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy was defined as having no clinical relevant abnormalities identified by a detailed medical history, physical exam, blood pressure and pulse rate measurements, 12-lead electrocardiogram, and clinical laboratory tests.
• Body mass index of ≥ 18 and ≤ 30 kilograms (kg)/meter squared and weight of ≥ 50 kg and ≤ 100 kg.
• Regular daily bowel movements (that is, production of at least 1 stool per day).
• Non-smoker or ex-smoker who had not used tobacco or nicotine products for ≥ 3 months prior to screening.

You may not qualify if:

• History or clinically relevant evidence of significant cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, neurological, or psychiatric disease.
• History of conditions or procedures possibly affecting drug absorption or excretion. A history of appendectomy, cholecystectomy, and hernia repair was allowed if they were not associated with complications.
• Active bacterial infection or clinically significant active viral infection, a body temperature \> 38°Celcius, or other evidence of infection on Day 1, or with a history of febrile illness within 7 days prior to Day 1.
• Healthy participants who had been exposed to significant radiation levels of \> 5 millisieverts in the last year prior to screening.
• Clinically significant laboratory abnormalities at screening or Day -1, as well as absolute neutrophil counts, platelets, and hemoglobin outside of reference ranges.

Sponsors & Collaborators

• Alexion Pharmaceuticals, Inc.: lead
• Achillion, a wholly owned subsidiary of Alexion: collaborator

Study Sites (1)

Clinical Trial Site

Auckland, New Zealand

Location

MeSH Terms

Interventions

danicopan

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 12, 2021
• First Posted: May 17, 2021
• Study Start: September 14, 2017
• Primary Completion: October 15, 2017
• Study Completion: October 15, 2017
• Last Updated: May 17, 2021

Record last verified: 2021-05

Locations

NZ (1)