Drug intelligence / Profile preview

tamoxifen + letrozole

Development stage
Phase 3
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

A combination of two hormone therapy drugs used in the treatment of hormone receptor-positive breast cancer. Tamoxifen is a selective estrogen receptor modulator (SERM) that works by blocking estrogen receptors, preventing estrogen from stimulating cancer cell growth. Letrozole is an aromatase inhibitor that reduces the amount of estrogen produced in the body by blocking the enzyme aromatase. The BIG 1-98 trial was a significant study that compared these drugs as monotherapy and in sequential treatment approaches. Research has shown that letrozole monotherapy generally provides better outcomes than tamoxifen alone or the combination of both drugs administered simultaneously.

02

Targets

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

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