Kintor Pharmaceutical Limited is pleased to announce that the investigational new drug application of GT20029 for androgenetic alopecia and acne vulgaris indications has been accepted by the National Medical Products Administration of China.
GT20029 is a topical androgen receptor (“AR”) degrader developed by using Kintor’s in-house Proteolysis Targeting Chimera (“PROTAC”) platform. PROTAC is a small molecule composed of (i) a recruiting element for a protein of interest (“POI”); (ii) an E3 ubiquitin ligase recruiting element; and (iii) a linker bounding (i) and (ii). After the ternary complex is formed, by bridging the gap between a POI and an E3 ubiquitin ligase and inducing their proximity, PROTAC can induce the ubiquitination of the POI and then degrade the POI.
As each PROTAC molecule can degrade multiple AR proteins, drugs based on PROTAC can achieve efficacy with a low dosage. In addition, as long as there are a small amount of PROTAC molecules in the cells, the efficacy of the drugs can be maintained, which can significantly reduce the dosing frequency as compared to other small molecule drugs.
Excessive activation of systemic and local AR pathways is an important link in the pathogenesis of androgenic alopecia and acne. The mechanism of action of GT20029 is to recruit the AR protein to the E3 ubiquitin ligase for degradation. GT20029 will not cause excessive drug accumulation and notable side effects. While achieving efficacy, GT20029 can effectively avoid systemic exposure to mitigate or avoid the side effects of oral androgen signaling pathway inhibitors.
Dr. Tong Youzhi, the founder, chairman and CEO of Kintor Pharmaceutical, commented, “The major obstacle of PROTAC drugs is oral absorption due to the large molecular weight. Therefore, we developed a topical AR degrader first based on PROTAC platform. At the same time, we are also developing an oral PROTAC drug targeting the AR.
Both indications of androgenetic alopecia and acne vulgaris have huge unmet clinical needs. According to animal experiments, the efficacy of GT20029 is superior to other small molecule AR inhibitors. As the sixth drug candidate of Kintor in the clinical stage, we hope to quickly explore its safety, recommended dosage and dosing frequency for clinical use, seeking innovative drug strategies of applying PROTAC molecule in local treatment.”
About Kintor Pharmaceutical Limited
Founded in 2009, Kintor Pharmaceuticals aims to become a leading enterprise in the R&D and commercialization of “best-in-class” and “first-in-class” innovative therapies. The Company initially focused on androgen receptor (AR) related diseases and researched and developed product portfolios in multiple channels covering cancers with a globally high incidence and illnesses yet to meet their clinical requirements, such as COVID-19, prostate cancer, breast cancer, liver cancer ,hair loss and acne.
Kintor Pharmaceuticals has prospectively developed a diversified product pipeline that includes small molecule innovative drugs, bio-innovative drugs and combination therapies, including 5 products that are undergoing clinically researched androgen receptor antagonists, ALK-1 monoclonal antibody, mTOR kinase inhibitors and Hedgehog inhibitors, as well as PD-L1/TGF-β dual-targeting antibody, AR-Degrader and c-Myc inhibitors that are undergoing preclinical research. Globally, the Company has more than 60 issued patents or under review, many of which are listed as the “Major New Drugs Discovery” in National 12th and 13th Five-Year Plans. On 22 May 2020, the Company was officially listed on the Hong Kong Stock Exchange with the stock ticker 9939.HK.
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