The effects of androgens on drug metabolism and transport: clinical pharmacologic considerations for people assigned female at birth

INTRODUCTION: Endogenous and exogenous androgens influence health outcomes across the life course in people assigned female at birth. However, little is known about how exogenous testosterone and androgen-rich conditions affect drug metabolism and transport in this population. AREAS COVERED: To link in vitro mechanistic findings with clinically observed effects on drug metabolism and transport, we conducted a narrative synthesis of in vivo evidence on the effects of testosterone on drug metabolism and transport among people assigned female at birth. We searched PubMed, Google Scholar, and Embase from database inception through 2 March 2026, for studies evaluating the effects of exogenous testosterone and androgen-rich conditions, including polycystic ovary syndrome (PCOS), on drug metabolism and transport in cisgender women and transgender people. EXPERT OPINION: The effects of testosterone and other androgens on drug metabolism and transport remain understudied in people assigned female at birth. As research continues to examine the roles of endogenous and exogenous androgens in cardiovascular health, musculoskeletal health, and cognition in this population, investigators should assess clinical pharmacology considerations in parallel. This should include well-designed probe-substrate studies when feasible, as well as using prescribed medications as clinical probes of relevant drug-metabolizing enzymes and transporters.