Drug intelligence / Profile preview

4-hydroxytestosterone

Development stage
Phase 2
Lead developer
Curadis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Transdermal
01

Overview

**4-hydroxytestosterone** is a synthetic anabolic-androgenic steroid (AAS) and a derivative of testosterone with a hydroxy group at the fourth carbon position. It was first patented in 1955 by G.D. Searle & Company but has never been marketed for therapeutic use[1][2][4]. The compound exhibits moderate anabolic, mild androgenic, and anti-aromatase properties; it acts as an androgen receptor agonist and modulates estrogen receptors[7][8]. It is structurally related to clostebol (4-chlorotestosterone) and formestane—formestane acts as a prohormone for this compound[1][2]. While it has been investigated for potential use in breast cancer due to its anti-estrogenic effects, there are currently no approved indications. The drug is prohibited in sports by the World Anti-Doping Agency due to its performance-enhancing potential[1][2].

Other names
4,17beta-dihydroxy-4-androstene-3-oneAndrost-4-ene-4,17beta-diol-3-oneDesmethylenestebol2141-17-5
02

Targets

AR (Adrenergic receptors)ESR2 (ERβ)ESR1 (ERα)

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