Drug intelligence / Profile preview

toremifene + anastrozole

Development stage
Preclinical
Lead developer
Orion Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Toremifene + anastrozole is a combination of two oral small molecule drugs used in the management of hormone receptor-positive breast cancer, particularly in postmenopausal women. Toremifene is a selective estrogen receptor modulator (SERM) that acts as an antagonist on breast tissue estrogen receptors, thereby inhibiting the proliferative action of estrogens on mammary epithelium. Anastrozole is a nonsteroidal aromatase inhibitor that blocks the conversion of androgens to estrogens by inhibiting the aromatase enzyme, leading to reduced circulating estrogen levels. The rationale for combining these agents is to achieve more complete estrogen blockade through dual mechanisms—receptor antagonism and suppression of endogenous estrogen synthesis. However, while combinations like SERM plus aromatase inhibitor have been studied with other agents (e.g., atamestane), there are no major clinical trials or regulatory approvals specifically for the combination of toremifene and anastrozole together[1][2][5]. Both drugs individually are approved for use in hormone receptor-positive breast cancer.

02

Targets

CYP19A1 (Aromatase)ESR2 (ERβ)ESR1 (ERα)

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