Drug intelligence / Profile preview

ormeloxifene

Development stage
Unknown
Lead developer
CSIR-Central Drug Research Institute
Modality
Small Molecules
Administration
Oral
01

Overview

Ormeloxifene is a third-generation selective estrogen receptor modulator (SERM) used primarily as a non-hormonal, non-steroidal oral contraceptive. It is marketed in India and has also been introduced for the treatment of dysfunctional uterine bleeding and menorrhagia. Ormeloxifene acts by selectively modulating estrogen receptors, exhibiting both estrogenic activity (in tissues such as bone, vagina, cardiovascular system, and CNS) and anti-estrogenic activity (notably in the uterus and breast). As a contraceptive, it inhibits endometrial receptivity to blastocyst signals without affecting ovulation or hormonal axes. The drug is administered orally once weekly after an initial loading period. It has also been investigated for use in conditions like mastalgia, fibroadenoma of the breast, endometriosis, fibroids, and potentially advanced breast cancer[1][2][3][5].

Brand names
SaheliCentron
Other names
levormeloxifenetrans-7-methoxy-2,2-dimethyl-3-phenyl-4-(4-(2-pyrrolidinoethoxy)phenyl)-chroman hydrochloride
02

Targets

CTNNB1 (Beta-catenin)ESR2 (ERβ)ESR1 (ERα)

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