Drug intelligence / Profile preview

all-trans retinoic acid + tamoxifen

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of all-trans retinoic acid (ATRA) and tamoxifen. ATRA is a derivative of vitamin A that acts primarily as an agonist for retinoic acid receptors, promoting cell differentiation and apoptosis. Tamoxifen is a selective estrogen receptor modulator (SERM) that antagonizes estrogen receptor alpha (ERα), inhibiting estrogen-driven tumor growth. The combination has been studied for its additive or synergistic antitumor effects in several cancers, including ERα-positive ovarian cancer, advanced breast cancer, and acute promyelocytic leukemia (APL). Mechanistically, ATRA can inhibit genes related to the ERα signaling pathway and enhance sensitivity to tamoxifen in ERα-positive tumors[1][2][3]. In leukemia models, tamoxifen enhances the differentiation-inducing and growth-inhibitory effects of ATRA[4]. This combination aims to overcome resistance mechanisms seen with single-agent therapy.

Other names
ATRA + tamoxifenall-trans-retinoic acid and tamoxifen
02

Targets

RARA (Retinoic acid receptor alpha)ESR1 (ERα)PIN1 (Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1)

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