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hydroxyflutamide
- Development stage
- Phase 2
- Lead developer
- Merck
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral (as Metabolite Of Flutamide), Other (e.g., Local Injection In Research Settings)
01
Overview
Hydroxyflutamide is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of flutamide. It acts as a potent competitive antagonist of the androgen receptor (AR), with higher affinity for AR than flutamide itself. Hydroxyflutamide blocks the action of endogenous and exogenous androgens by preventing their binding to AR, thereby inhibiting androgen-driven cellular processes such as those involved in prostate cancer progression. Flutamide is considered a prodrug for hydroxyflutamide, which mediates its therapeutic effects. Hydroxyflutamide has been investigated primarily for prostate cancer treatment[1][2][3][4].
- Other names
- 2-hydroxyflutamideHFOHF
02
Targets
AR (Adrenergic receptors)
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