AR-PROTAC
| File:PROTAC AR Degrader-4 500.png | |
| Clinical data | |
|---|---|
| Routes of administration | Topical |
| Drug class | Nonsteroidal antiandrogen |
| Identifiers | |
| PubChem CID | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}} |
| Chemical and physical data | |
| Formula | C43H67N3O9 |
| Molar mass | 770.021 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
AR-Protac (developmental code name: GT-20029) is an AR degrader[1] produced by Kintor Pharmaceutical Limited that uses the PROTAC compound to degrade androgen receptors in the scalp, preventing dihydrotestosterone (DHT) from attaching to the scalp, which otherwise leads to hair loss. As of March 2023, it has completed Phase 1 clinical trials in both America and in China[2]. It is a topical solution, intended for use in treating androgenic alopecia. It can also be used for issues relating to acne.
Development
GT20029 is an androgen receptor (AR) degrader that utilizes Kintor Pharma's PROTAC platform. It received clearance from both the China National Medical Products Administration (NMPA) and the U.S. Food and Drug Administration (FDA) in April and July 2021, respectively, for its clinical trial application aimed at treating acne and androgenetic alopecia (AGA).[3]
In August 2022, Kintor Pharma successfully completed enrollment and dosing of participants in its China-based Phase I clinical trial for GT20029. In October 2022, it also finished enrolling and dosing participants for its Phase I clinical trial of GT20029 in the United States.[4]
On February 10, 2023, Dr. Youzhi Tong, the CEO of Kintor Pharma, announced plans to accelerate the initiation of Phase II clinical trials.[5]
Adverse effects
According to the trials held in the USA and China, there were no side effects detected. This is because there is no systemic absorption detected and therefore it has a better safety profile.[6]
Pharmacology
Pharmacodynamics
Repeat pharmacodynamics studies using a dihydrotestosterone (DHT)-induced mouse model showed that GT20029 significantly promoted hair growth, with statistical significance.[7]
References
- ↑ "Kintor Announces New Advanced Androgen Receptor Drug GT20029 – Follicle Thought". Retrieved 2023-03-09.
- ↑ "Kintor Pharma's GT20029 Performs Well in Phase 1 Trial of Acne and Androgenetic Alopecia". Practical Dermatology. Retrieved 2023-03-10.
- ↑ "Kintor Pharma Announces Positive Top-line U.S. Phase I Trial Results of GT20029, the World's First Topical Use PROTAC Compound_Kintor Pharmaceutical Limited". en.kintor.com.cn. Retrieved 2023-03-10.
- ↑ "Kintor Pharma's GT20029 Performs Well in Phase 1 Trial of Acne and Androgenetic Alopecia". Practical Dermatology. Retrieved 2023-03-10.
- ↑ "Kintor Pharma Announces Positive Top-line U.S. Phase I Trial Results of GT20029, the World's First Topical Use PROTAC Compound_Kintor Pharmaceutical Limited". en.kintor.com.cn. Retrieved 2023-03-10.
- ↑ Pharma, Kintor. "Kintor Pharma Announces Dosing of First Subject in US Phase I Clinical Trial of GT20029 for Androgenic Alopecia and Acne". www.prnewswire.com. Retrieved 2023-03-10.
- ↑ "Kintor's GT20029 IND for PROTAC AR Degrader Was Accepted by NMPA_Kintor Pharmaceutical Limited". en.kintor.com.cn. Retrieved 2023-03-09.
This article "AR-PROTAC" is from Wikipedia. The list of its authors can be seen in its historical and/or the page Edithistory:AR-PROTAC. Articles copied from Draft Namespace on Wikipedia could be seen on the Draft Namespace of Wikipedia and not main one.
