Мы используем файлы cookie.
Продолжая использовать сайт, вы даете свое согласие на работу с этими файлами.
Dermatologic drugs
Pyrilutamide
Другие языки:

    Pyrilutamide

    Подписчиков: 0, рейтинг: 0
    Pyrilutamide
    Pyrilutamide high res.png
    Clinical data
    Other names KX-826
    Routes of
    administration    		 Topical
    Drug class Nonsteroidal antiandrogen
    ATC code
    • None
    Identifiers
    • 4-(3-(4-cyano-2-fluoro-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide
    Chemical and physical data
    Formula C21H15F5N4O2S
    Molar mass 482.43 g·mol−1
    3D model (JSmol)
    • CNC(=O)C1=C(F)C=C(C=C1)N1C(=S)N(C(=O)C1(C)C)C1=C(F)C(=C(C=C1)C#N)C(F)(F)F
    • InChI=1S/C21H15F5N4O2S/c1-20(2)18(32)29(14-7-4-10(9-27)15(16(14)23)21(24,25)26)19(33)30(20)11-5-6-12(13(22)8-11)17(31)28-3/h4-8H,1-3H3,(H,28,31)
    • Key:CGRMNGGGSWLDDC-UHFFFAOYSA-N

    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) and acne in China and the United States. As of October 2022, it is in phase 3 clinical trials for androgenic alopecia and phase 2 trials for acne.

    Development

    Pyrilutamide successfully completed phase II clinical trials in China and is currently in phase II clinical trials in the U.S for the potential treatment of androgenetic alopecia in males. It is currently in phase II clinical trials in China for the potential treatment of androgenetic alopecia in females. The drug was expected to enter phase III clinical trials in Q1 2022 in China and conducted over 24 weeks across more than 20 sites with a sample size of 416.

    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.

    Adverse effects

    Pyrilutamide is generally well-tolerated. The most common adverse event is contact dermatitis.

    Pharmacology

    Plasma concentration of pyrilutamide and metabolite KX-982 in different dose groups in phase Ib clinical trials in China

    Pharmacodynamics

    Pyrilutamide binds to the androgen receptor with a very high affinity with an IC50 of 0.28 nM. Reference drug bicalutamide had an IC50 of 3.1 nM.

    Pharmacokinetics

    In Phase I clinical trials, pyrilutamide and metabolite KX-982's systemic absorption was evaluated across different doses of 0.5, 2, 6, 12, and 24 mg/body/day.



    Новое сообщение