Thyroid receptor agonists for the treatment of androgenetic alopecia

被引：17
|
作者：
Li, Jie Jack [1 ]
Mitchell, Lorna H. [1 ]
Dow, Robert L. [2 ]
机构：
[1] Pfizer Global Res & Dev, Dept Chem, Michigan Labs, Ann Arbor, MI 48105 USA
[2] Pfizer Global Res & Dev, Cardiovasc & Metab Dis Chem, Groton, CT 06340 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 01期
关键词：
Thyromimetics; Androgenetic alopecia; Topical drug; Skin penetration; Photo-irritation; PROLIFERATION;
D O I：
10.1016/j.bmcl.2009.10.109
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A thyroid hormone receptor beta subtype-selective thyromimetic 5 was found to be efficacious in both mouse and monkey hair growth models after topical applications. It penetrates the skin according to the test in human cadaver skin mounted onto Franz diffusion chambers. The serum drug level of 5 is below the limit of quantification during tests in the bald stump-tailed macaques (Macaca arctoides). It is tested negative in the 3T3 neutral red uptake (NRU) phototoxicity test, indicating a low risk for causing photo-irritation. It is also rapidly metabolized according to the PK data, thus the systemic exposure is limited. (c) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：306 / 308
页数：3
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