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arsenic tetrasulfide
- Development stage
- Unknown
- Lead developer
- Harbin Yida Pharmaceutical
- Modality
- DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Arsenic tetrasulfide (As4S4), also known as tetraarsenic tetrasulfide or Realgar, is an inorganic arsenic compound with notable antitumor activity, particularly in acute promyelocytic leukemia (APL). It has been used in traditional Chinese medicine and is the active component of some oral formulations for APL. Mechanistically, it induces degradation and ubiquitination of the PML-RARα oncoprotein, leading to differentiation and apoptosis of leukemic cells. Arsenic tetrasulfide has demonstrated efficacy comparable to intravenous arsenic trioxide when combined with all-trans retinoic acid (ATRA) for APL treatment. It is approved by the China Food and Drug Administration as a second-line chemotherapeutic agent for APL and is available as an oral formulation in China[3][5][7]. Adverse effects include hepatotoxicity, diarrhea, and rarely QTc prolongation[5].
- Brand names
- Realgar
- Other names
- arsenicum sulphuratum rubrumruby sulfurruby of arsenic
02
Targets
TAFI (Carboxypeptidase B2)PP2A (Protein phosphatase 2A)PML-RARA (PML-retinoic acid receptor alpha fusion protein)
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