Darinaparsin (Darvias)
Mechanism of action
From the NCI Drug Dictionary: A small-molecule organic arsenical with potential antineoplastic activity. Although the exact mechanism of action is unclear, darinaparsin, a highly toxic metabolic intermediate of inorganic arsenicals (iAs) that occurs in vivo, appears to generate volatile cytotoxic arsenic compounds when glutathione (GSH) concentrations are low. The arsenic compounds generated from darinaparsin disrupt mitochondrial bioenergetics, producing reactive oxygen species (ROS) and inducing ROS-mediated tumor cell apoptosis; in addition, this agent or its byproducts may initiate cell death by interrupting the G2/M phase of the cell cycle and may exhibit antiangiogenic effects. Compared to inorganic arsenic compounds such as arsenic trioxide (As2O3), darinaparsin appears to exhibit a wide therapeutic window.
Diseases for which it is used
History of changes in PMDA indication
- 2022-06-20: A drug with a new active ingredient indicated for the treatment of relapsed or refractory peripheral T-cell lymphoma. (Based on SP-02)
Also known as
- Code names: SP-02L, ZIO-101
- Brand name: Darvias