Drug intelligence / Profile preview

5-azacitidine + tretinoin

Development stage
Unknown
Lead developer
Icahn School of Medicine
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

5-azacitidine + tretinoin is a combination therapy being investigated by the Icahn School of Medicine at Mount Sinai for the treatment of biochemically recurrent prostate cancer. The regimen consists of 5-azacitidine (5-AZA), a DNA methyltransferase inhibitor, and all-trans retinoic acid (ATRA, also known as tretinoin), a retinoic acid receptor (RAR) agonist. This combination is designed as a 'reprogramming therapy' to induce tumor cell dormancy in disseminated cancer cells. By inhibiting DNA methylation and activating retinoic acid signaling, the treatment aims to restore the TGF-β-SMAD4 signaling pathway and induce dormancy-regulating genes, such as NR2F1. The clinical goal is to delay disease progression and prolong PSA doubling time in patients with rising PSA levels after definitive local treatment, potentially avoiding or delaying the need for androgen deprivation therapy.

Other names
5-azacitidine + all-trans retinoic acidall-trans retinoic acid + 5-azacitidineATRA + 5-AZA
02

Targets

DNMT1 (DNA (cytosine-5)-methyltransferase 1)RARA (Retinoic acid receptor alpha)RARG (Retinoic acid receptor gamma)RARB (Retinoic acid receptor beta)

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