Suzhou, November 24, 2022 – Kintor Pharmaceutical Limited (“Kintor Pharma”, HKEX: 9939), a clinical-stage biotechnology company developing innovative small molecules and biological therapeutics, today announced the top-line results for its phase I clinical trial of GT20029 for the treatment of androgenetic alopecia (AGA) and acne in China, which demonstrated the good safety, tolerability and pharmacokinetics of GT20029 in healthy subjects. Developed by Kintor Pharma’s proprietary Proteolysis Targeting Chimera (PROTAC) platform, GT20029 is the first topical PROTAC compound globally which has completed phase I clinical trial.
In preclinical studies, by degrading androgen receptor (AR) protein, GT20029 could block the shrinkage or miniaturization of hair follicles which was caused by the AR signaling pathway. As a result, it prevented the hair from thinning, softening or falling out, and GT20029 could also effectively inhibit sebaceous gland development and sebum secretion. GT20029 has a topical curative effect and can avoid systemic exposure by limiting skin penetration, achieving a good safety profile. The repeated pharmacodynamics studies in dihydrotestosterone (DHT)-induced AGA mouse model showed that GT20029 significantly reduced hair loss, with statistical difference. The study of testosterone propionate (TP)-induced skin hamster flank organ ance model showed that GT20029 significantly inhibited enlargement of flank organ, with statistical difference.
The phase I clinical trial in China is a randomized, double-blind, placebo-controlled study to evaluate the safety and pharmacokinetics of GT20029 (gel/tincture) in healthy subjects. This study is composed of single and multiple ascending dose administration (topical) of GT20029.
The phase I study showed that a total of 92 subjects received at least one treatment dose, including that 68 subjects received gel and 24 subjects received tincture. The 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 (below lower limit of quantification (LLOQ), 0.001ng/mL) 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 events (TRAE) were grade 1, and no TRAE above grade 1 was reported.
Dr. Youzhi Tong, Founder, Chairman and Chief Executive Officer of Kintor Pharma, commented, “As the first topical PROTAC compound in the world completed phase I clinical trial, GT20029 has shown a good safety and tolerability profile in nearly 100 healthy subjects. The phase I study has proved: 1) The pharmacokinetic results showed that the topical use of PROTAC compound could penetrate into the body, but the exposure was much lower than KX-826 (small molecule antagonist), indicating that the safety was controllable; 2) Skin surface Damage was not observed in repeated administration of topical PROTAC compound at a high dose (2%), demonstrating the safety of specific degradation of AR-targeted proteins in local use, and paving the way for the observation of drug efficacy in following phase II clinical trial.The company will choose the optimal dosage for Phase II clinical trial and strive to maintain its leading position in developing novel drugs through the in-house PROTAC platform worldwide.”
GT20029 is a topical androgen receptor (AR) degrader using Kintor Pharma’s PROTAC platform. The China National Medical Products Administration (NMPA) and the US Food and Drug Administration (FDA) cleared GT20029’s clinical trial application for treating AGA and acne in April 2021 and July 2021, respectively. In August 2022, Kintor Pharma has completed the enrollment and dosing of subjects for its China phase I clinical trial of GT20029. In October 2022, Kintor Pharma has completed the enrollment and dosage of subjects in its US phase I clinical trial of GT20029.