Synthesis and Biological Evaluation of Amino-Pyridines as Androgen Receptor Antagonists for Stimulating Hair Growth and Reducing Sebum Production

    August 2007 in “ Bioorganic & Medicinal Chemistry Letters ”
    Lain-Yen Hu, Huangshu John Lei, Daniel K. Du, Theodore M. Johnson, Victor Fedij, Catherine R. Kostlan, Wen Yue, Mark Lovdahl, Jie Li, Matthew Carroll, Danielle Dettling, Jeffrey Asbill, Conglin Fan, Kimberly Jane Wade, David Pocalyko, Kimberly Lapham, Radhika Yalamanchili, Brian Samas, Derek Vrieze, Susan Ciotti, Teresa Krieger-Burke, Drago Robert Sliskovic, Howard G. Welgus
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    Studysummary This study found that a specific amino-pyridine compound showed potent androgen receptor antagonist activity, stimulating hair growth in mice and reducing sebum production in a hamster model. Our plain-language summary of this paper — not a Tressless recommendation.
    In 2007, Pfizer Global Research and Development synthesized and evaluated a series of amino-pyridines for their androgen antagonist activities. The most potent compound, (R)-(+)-6-[methyl-(1-phenyl-ethyl)-amino]-4-trifluoromethyl-nicotinonitrile, showed significant potential for stimulating hair growth and reducing sebum production. This was tested on two animal models: 10 male C3H/HeN mice and 5 male Syrian hamsters. The mice were treated twice daily for 4 weeks, and the hamsters were treated twice daily for 2 weeks. The compound was also found to be rapidly metabolized in rat, dog, and human hepatocytes, indicating favorable pharmacokinetic characteristics for a topical agent. The study concluded that this compound had remarkable in vivo activity for both stimulating hair growth and reducing sebum production, making it a promising candidate for topical applications.
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