Chemistry:Pyrilutamide
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| Clinical data | |
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| Other names | KX-826 |
| Routes of administration | Topical |
| Drug class | Nonsteroidal antiandrogen |
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| Identifiers | |
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| Chemical and physical data | |
| Formula | C21H15F5N4O2S |
| Molar mass | 482.43 g·mol−1 |
| 3D model (JSmol) | |
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Pyrilutamide (developmental code name KX-826) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) – which is under development by Suzhou Kintor Pharmaceuticals, inc., a subsidiary of Kintor Pharmaceutical Limited, for the potential treatment of androgenic alopecia (androgen-dependent scalp hair loss)[1][2][3] As of October 2022, it is in phase 3 clinical trials for androgenic alopecia and phase 2 trials for acne.[2]
Development
The primary endpoint is the change from baseline in non-vellus target area hair count (TAHC) at the end of week 24. The drug will be dosed at 10 mg (0.5% BID) per patient per day in the trial.[4]
Adverse effects
Pyrilutamide is generally well-tolerated. The most common adverse event is contact dermatitis.[5]
Pharmacology
Pharmacodynamics
Pyrilutamide binds to the androgen receptor with a very high affinity with an IC50 of 0.28 nM. [3] Reference drug bicalutamide had an IC50 of 3.1 nM. [3]
References
- ↑ "What's New in Therapy for Male Androgenetic Alopecia?". American Journal of Clinical Dermatology 24 (1): 15–24. January 2023. doi:10.1007/s40257-022-00730-y. PMID 36169916.
- ↑ 2.0 2.1 "Pyrilutamide - Suzhou Kintor Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800053879.
- ↑ 3.0 3.1 3.2 Tong Y, "Substituted Thioimidazolidinone Androgen Receptor Antagonists and Uses Thereof", CA patent 2829322, published 2012-03-08, issued 2017-01-10, assigned to Suzhou Kintor Pharmaceuticals, Inc
- ↑ "Kintor Pharma Announces the Primary Endpoint of Phase II Clinical Study for KX-826's Treatment of Androgenetic Alopecia Was Met". https://en.kintor.com.cn/news/190.html.
- ↑ "Kintor Pharmaceutical (9939 HK) Specializing in AR-related innovative therapies". http://pdf.dfcfw.com/pdf/H3_AP202007241393752560_1.pdf.
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