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tretinoin + arsenic trioxide

Development stage
Unknown
Lead developer
Teva Pharmaceutical Industries
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Tretinoin + arsenic trioxide is a fixed combination regimen of two small molecule drugs—tretinoin (all-trans retinoic acid, ATRA) and arsenic trioxide—used primarily for the treatment of acute promyelocytic leukemia (APL). Tretinoin is a vitamin A derivative that induces differentiation of leukemic promyelocytes by targeting and degrading the PML/RARα fusion protein resulting from the t(15;17) translocation. Arsenic trioxide also targets PML/RARα but through different molecular mechanisms, including induction of apoptosis and partial differentiation. The combination has demonstrated synergistic effects in eliminating leukemic cells and is now considered standard first-line therapy for newly diagnosed low-risk APL (WBC ≤10,000/mcL), as well as an option for high-risk patients intolerant to anthracyclines or those who relapse after prior therapy. This regimen reduces reliance on traditional chemotherapy agents such as anthracyclines, thereby minimizing long-term toxicities[1][4][6][9].

Brand names
Trisenox
Other names
ATRA + arsenic trioxideall-trans retinoic acid + arsenic trioxideAsO/ATRA
02

Targets

RARA (Retinoic acid receptor alpha)PML-RARA (PML-retinoic acid receptor alpha fusion protein)

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