Healthy
Conditions
Keywords
Danicopan, ACH-0144471, ALXN2040, Absorption, Distribution, Metabolism, Excretion, Total Radioactivity, ADME
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 \[14C\].
Interventions
DRUG[14C]-Danicopan
Liquid-filled capsules.
Sponsors
Achillion, a wholly owned subsidiary of Alexion
Alexion Pharmaceuticals, Inc.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
Key Inclusion Criteria: * 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. Key
Exclusion criteria
* 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.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| [14C]-Danicopan Metabolites In Plasma, Urine, And Feces | 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: Cmax | Up to 96 hours postdose |
| Plasma PK Of Danicopan After A Single Oral Dose Of [14C]-Danicopan: Tmax | Up to 96 hours postdose |
| 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 |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Incidence Of Treatment-emergent Adverse Events | Day 1 through Day 10 | — |
| 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 | \[14C\]-Danicopan metabolic profiling in plasma, urine, and feces was performed in samples containing sufficient amounts of radioactivity. The percent of dose represented by each of the metabolites was calculated using the radioactivity concentration equivalent data combined with the metabolic profiling data. The percentage of each identified metabolite to total radioactivity in plasma was estimated based on plasma metabolic profiling data. |
Countries
New Zealand
Outcome results
None listed