Drug intelligence / Profile preview

MK-4541

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-4541 is a steroidal selective androgen receptor modulator (SARM) and 4‑azasteroid derivative developed by Merck. It acts as both a potent androgen receptor antagonist and a 5α-reductase inhibitor. In preclinical studies and animal models it has demonstrated mixed agonistic (androgenic/anabolic) effects in muscle and bone while exerting antagonistic (antiandrogenic) effects in the prostate and prostate cancer cells. MK‑4541 suppresses testosterone levels—likely via antigonadotropic activity—and inhibits proliferation/induces apoptosis in androgen-dependent prostate cancer cells. It also increases lean body mass and muscle function under androgen-deficient conditions. The compound was investigated for potential use in treating prostate cancer but has not advanced beyond preclinical development or been marketed[1][2][5].

Other names
2,2,2-trifluoroethyl N-[(1S,3aS,3bS,5aR,9aR,9bS,11aS)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinolin-1-yl]carbamate
02

Targets

SRD5A (Steroid 5-alpha-reductase)AR (Adrenergic receptors)

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