Safety, tolerability, and pharmacokinetics of HL-300, a novel topical pan-JAK inhibitor, in healthy Chinese adults: a first-in-human, randomized, double-blind, placebo-controlled phase I trial

2026-06-09

PRE

Hui Qiu

Xingfei Zhang

Jie Huang

Lin Ye

Chan Zou

Jinlian Xie

Kunhong Deng

Qian Wu

Xiulin He

Congxin Liang

Yong Liu

Guang Yang

Guoping Yang

Chengxian Guo *

DOI：10.1080/13543784.2026.2687028

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HL-300 is a novel topical pan-JAK inhibitor targeting JAK1, JAK2, JAK3, and TYK2 for atopic dermatitis (AD). This first-in-human study evaluated its safety, tolerability, and pharmacokinetics (PK) in healthy Chinese adults. In a randomized, double-blind, placebo-controlled phase I trial, 36 subjects received single or multiple topical doses of HL-300 (0.25%, 0.5%, or 1.0%) or placebo. Safety and PK parameters were assessed. Following single dosing, HL-300 showed slow absorption, with mean Cmax ranging from 82.77 to 537.60 pg/mL and median Tmax of 24–36 h. After multiple dosing, steady state was reached by Day 6, with a Cmax,ss of 3059 pg/mL. Accumulation ratios for AUC and Cmax were 40.93 and 18.9, respectively. Most treatment-emergent adverse events were mild (Grade 1), and no serious adverse events were reported. HL-300 was generally safe and well tolerated after single and multiple topical administrations, showing low systemic exposure after single dosing and predictable PK with steady-state attainment after repeated dosing. These findings support further clinical development and dose optimization in patients with AD.

Keywords:

HL-300

JAK inhibitor

atopic dermatitis

pharmacokinetics

safety

phase I trial

Safety, tolerability, and pharmacokinetics of HL-300, a novel topical pan-JAK inhibitor, in healthy Chinese adults: a first-in-human, randomized, double-blind, placebo-controlled phase I trial

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