Drug intelligence / Profile preview

epristeride

Development stage
Unknown
Lead developer
Ono Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Epristeride is an orally administered **small molecule steroidal antiandrogen** developed for the treatment of benign prostatic hyperplasia (BPH), particularly marketed and used in China[1][2][5][13][14]. Its primary **mechanism of action** is **irreversible, non-competitive inhibition of 5α-reductase type II**, the enzyme that converts testosterone into dihydrotestosterone (DHT)[1][13][14][17]. By selectively inhibiting this isoenzyme, epristeride substantially lowers DHT levels in the prostate, although its effect on circulating DHT is more modest (25–54% reduction)[1][2][9][14]. Epristeride differs from other 5α-reductase inhibitors like finasteride and dutasteride by forming a stable ternary complex with the enzyme, substrate, and cofactor, effectively rendering the enzyme inactive[1]. The drug was first introduced in China around 2000, after earlier abandonment of development in the US and other countries[1][2]. Its primary and only approved indication is **benign prostatic hyperplasia**.

Brand names
AipulieteChuanliu
Other names
epristeride
02

Targets

SRD5A2 (Steroid 5-alpha-reductase type II)

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