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Kintor’s GT20029 IND for PROTAC AR Degrader Was Accepted by NMPA

Kintor’s GT20029 IND for PROTAC AR Degrader Was Accepted by NMPA

(Summary description)Suzhou, Feb.2, 2021--Kintor Pharmaceutical Limited is pleased to announce that the investigational new drug ("IND") application of GT20029 for androgenetic alopecia and acne vulgaris indications has been accepted by the National Medical Products Administration (the "NMPA") of China.

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  • Time of issue:2021-02-02 10:31
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Suzhou, Feb.2, 2021--Kintor Pharmaceutical Limited (HKEX:9939) is pleased to announce that the investigational new drug ("IND") application of GT20029 for androgenetic alopecia and acne vulgaris indications has been accepted by the National Medical Products Administration (the "NMPA") 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 ofthe 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."

 

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