The board of Kintor Pharmaceutical Limited announced the top-line results of its phase I clinical trial of GT20029, a topical androgen receptor proteolysis targeting chimera compound developed by the Group, for the treatment of androgenetic alopecia and acne in China, which demonstrated good safety, tolerability and pharmacokinetics in healthy subjects. Developed by the Company's proprietary PROTAC platform, GT20029 is the first topical PROTAC compound which has completed phase I clinical trial globally. The Phase I Clinical Trial is a randomized, double-blind, placebo-controlled study to evaluate the safety and pharmacokinetics of GT20029. The study is composed of single and multiple ascending dose administration of GT20029 on healthy subjects. The 92 subjects received at least one treatment dose, among which 68 subjects received gel and 24 subjects received tincture. The results showed that topical administration of GT20029 was safe and well-tolerated in healthy subjects with limited system exposure. Following a single dose administration, all subjects had no detectable drug concentrations at all time points. Following multiple-dose topical administration of GT20029, the mean maximum drug concentrations of all cohorts were lower than 0.05ng/mL. All treatment related adverse event were grade 1, and no TRAE above grade 1 was reported. By degrading AR protein, GT20029 could block the shrinkage and miniaturization of hair follicles which was caused by the AR signaling pathway. As the result, it prevented the hair from thinning, softening or falling out, and GT20029 could also effectively inhibit sebaceous gland developmentand sebum secretion. GT20029 has a topical curative effect and can avoid systemic exposure by limiting skin penetration, achieving good safety profile. The repeated pharmacodynamics studies in
dihydrotestosterone -induced mouse model showed that GT20029 significantly reduced hair loss, with statistical difference. The study of testosterone propionate -induced skin hamster flank organ acne model showed that GT20029 significantly inhibited enlargement of flank organ, with statistical difference.