Drug intelligence / Profile preview

fluoxymesterone

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

Overview

Fluoxymesterone is a synthetic androgen and anabolic steroid (AAS) used primarily to treat low testosterone levels in males (hypogonadism), delayed puberty in boys, and as palliative therapy for certain types of breast cancer in women. It acts as an agonist of the androgen receptor, mimicking the effects of endogenous testosterone. In men and boys, it replaces or supplements natural testosterone to promote normal development and function of male sexual organs and secondary sex characteristics. In women with hormone-responsive breast cancer, it suppresses estrogen production by antagonizing estrogen receptors or through negative feedback on the hypothalamic-pituitary-gonadal axis[1][2][3][5][6]. Fluoxymesterone is orally active due to its 17α-methyl group but carries a risk of hepatotoxicity[5]. It was first described in 1956 and introduced for medical use in 1957[5].

Brand names
HalotestinAndroxyUltandrenOra-Testryl
Other names
fluoxymesterone
02

Targets

HSD11B2 (11β-HSD2)AR (Adrenergic receptors)ER (Estrogen receptor)

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