Safety and pharmacokinetics of CL-197, a potent compound with low cytotoxicity against HIV-1: a randomized, double-blind, placebo-controlled, first-in-human phase 1 clinical trial.
Yuming Guo, Yonggang Li, Pan Zhao et al.
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In 30 seconds
This single-centre, randomized, double-blind, placebo-controlled, dose-escalation phase 1 trial assessed safety, tolerability and pharmacokinetics of single-dose CL-197 in healthy adults aged 18–45 years. Five dose levels from 1 to 100 mg were studied; the 1 mg group was open-label. CL-197 was reported as well tolerated at all doses. Plasma exposure was approximately dose-proportional, although AUC measures were nonlinear across the dose range. The mean plasma half-life increased from 1.39 to 10.20 h, while the mean PBMC half-life was 61.29 h and 43.80 h in the 30 mg and 60 mg groups, respectively.
Key findings
- CL-197 was well tolerated at all five dose levels in this first-in-human study of healthy adults.
- Mean plasma half-life increased from 1.39 to 10.20 h across doses; AUC 0-t and AUC 0-∞ showed nonlinear characteristics from 1 to 100 mg.
- Mean PBMC half-life was 61.29 h in the 30 mg group and 43.80 h in the 60 mg group.
Why it matters
The trial provides initial human safety and pharmacokinetic data for an investigational HIV-1 compound. The prolonged intracellular half-life observed in PBMCs is relevant to evaluating whether extended dosing intervals may be feasible, while the small, early-phase study supports further investigation rather than conclusions about efficacy or routine use.
What to keep in mind
This was a single-centre phase 1 study in healthy adults, assessing single-dose safety and pharmacokinetics; it does not establish efficacy or safety with repeated dosing.