Summary of clofazimine PK simulations
The elimination half-life of clofazimine is approximately 25 days, thus it is assumed that the exposure clofazimine reaches steady state in plasma by day 126 (approximately five half-lives).
| Study (Model) | Clofazimine Dosing Regimen | Simulated Population | Observed Population | PK Measurement of Substrate |
|---|---|---|---|---|
| Model development | ||||
| Clofazimine PK (Internal data) | 50 mg once daily for 43 days (fasting) | Age range: 35–64 years; proportion of females: 25% n = 120 (10 trials of 12 subjects) | Age range: 35–64 years; proportion of females: 25% n = 12 | Day 1: Tmax, Cmax, and AUC0–24 h |
| Clofazimine PK (Internal data) | 100 mg once daily for 43 days (fasting) | Age range: 45–70 years; proportion of females: 50% n = 120 (10 trials of 12 subjects) | Age range: 45–76 years; proportion of females: 50% n = 12 | Day 1: Tmax, Cmax, and AUC0–24 h |
| Model application | ||||
| Clofazimine PK | 100 mg once daily for 126 days (fasting) | Age range: 18–70 years; proportion of females: 50% n = 100 (10 trials of 10 subjects) | NA | Day 126: Cmax and AUC0–24 h |
AUC0–24 h, area under plasma-drug concentration curve between 0 and 24 hours; NA, not applicable; Tmax, time to reach maximum concentration.