Drug intelligence / Profile preview

isotretinoin + tamoxifen

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two small molecule drugs, isotretinoin and tamoxifen. Isotretinoin (13-cis-retinoic acid) is a retinoid primarily used for severe acne but also investigated for its anti-proliferative effects in cancer. Tamoxifen is a selective estrogen receptor modulator (SERM) widely used in the treatment and prevention of estrogen receptor-positive breast cancer. The combination has been studied preclinically and in early clinical trials as a potential anticancer strategy, leveraging the pro-apoptotic and differentiation-inducing effects of retinoids with the antiestrogenic activity of tamoxifen. Mechanistically, isotretinoin acts mainly through nuclear retinoic acid receptors to regulate gene expression involved in cell growth and differentiation, while tamoxifen antagonizes estrogen receptor signaling to inhibit proliferation of hormone-responsive tumor cells. Preclinical studies suggest that combining these agents may enhance antitumor efficacy or reduce toxicity associated with isotretinoin by modulating mitochondrial function[1][2][3].

02

Targets

RARA (Retinoic acid receptor alpha)ESR1 (ERα)ANT1/2/3 (Mitochondrial ADP/ATP translocase)ESR2 (ERβ)RARG (Retinoic acid receptor gamma)RARB (Retinoic acid receptor beta)

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