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tretinoin + decitabine
- Development stage
- Unknown
- Lead developer
- The First Affiliated Hospital
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
The combination of tretinoin (all-trans retinoic acid, ATRA) and decitabine is an investigational therapeutic regimen being evaluated for the treatment of myeloid malignancies, specifically myelodysplastic syndrome with excess blasts (MDS-EB). This combination leverages the synergistic effects of a differentiating agent and a hypomethylating agent. Tretinoin is a retinoid that binds to retinoic acid receptors (RARs) to induce the terminal differentiation of myeloid progenitor cells. Decitabine is a nucleoside analog that inhibits DNA methyltransferases (DNMTs), leading to the hypomethylation of DNA and the reactivation of silenced tumor suppressor genes. Research conducted by The First Affiliated Hospital, College of Medicine, Zhejiang University suggests that decitabine may sensitize malignant cells to the differentiating effects of tretinoin, potentially overcoming the differentiation block characteristic of high-risk MDS and acute myeloid leukemia.
- Other names
- ATRA + decitabineall-trans retinoic acid + decitabinedecitabine + tretinoin
02
Targets
NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)RARB (Retinoic acid receptor beta)RARA (Retinoic acid receptor alpha)RARG (Retinoic acid receptor gamma)DNMT1 (DNA (cytosine-5)-methyltransferase 1)
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