Pantolactams as Androgen Receptor Antagonists for the Topical Suppression of Sebum Production

September 2011 in “ Bioorganic & Medicinal Chemistry Letters ”

Karen Elaine Sexton, Stephen Barrett, Katy L. Bridgwood, Matthew Carroll, Danielle Dettling, Daniel K. Du, Stephen A. Fakhoury, Victor Fedij, Lain-Yen Hu, Catherine R. Kostlan, David Pocalyko, N. Raheja, Yvonne E. Smith, Veerabahu Shanmugasundaram, Kimberly Jane Wade

pantolactams androgen receptor antagonists sebum production topical application wax esters Hamster Ear Model (+)-isomer AR antagonists

TLDR Pfizer found that pantolactam-based compounds can reduce sebum (skin oil) production when applied topically.

In 2011, Pfizer Global Research & Development conducted a study to identify potent androgen receptor (AR) antagonists that could suppress sebum production when applied topically. They discovered that pantolactam-based compounds were effective AR antagonists. When tested in the Hamster Ear Model, these compounds reduced wax esters, a major component of sebum, leading to further preclinical work. The study also revealed that all AR antagonist activity was found in the (+)-isomer for the pantolactams. Two compounds, 48 and 50, were chosen for additional preclinical studies due to their effectiveness in reducing sebum production.

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