Interest in the development and therapeutic potential of nonsteroidal tissue-selective
androgen receptor modulators (SARMs) a has increased dramatically within the past
decade. Rapidly expanding knowledge of nuclear hormone receptor structure and function
and successful proof-of-principle clinical trials with SARMs have revived an almost dormant
search for improved androgens. This Award Address attempts to chronicle the landmark
discoveries (with emphasis on our work), organize the SARM landscape into clinically …

Androgens play an essential role in differentiation and growth of the male reproductive tract,
pubertal maturation and development of secondary male sex characteristics, initiation and
regulation of spermatogenesis, and male sexual behavior (1). Steroidal androgens increase
muscle mass, bone mass, and strength; stimulate male pattern baldness; and alter serum
lipid profiles and fat distribution (2). Testosterone (T), synthesized and secreted by the
testes, and its more potent 5α-reduced metabolite, dihydrotestosterone (DHT), are the …