Darinaparsin

Organoarsenic Compound / Small Molecule Peptide Conjugate (organic Arsenical)Rx: PrescriptionCompound: Approved

Also known as: Darinastat, DMAG, S-dimethylarsino-glutathione, ZIO-101

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Darinaparsin (ZIO-101) is an organic arsenical compound approved in Japan for relapsed or refractory peripheral T-cell lymphoma (PTCL). It offers a potentially more favorable toxicity profile compared to inorganic arsenic trioxide while retaining anti-tumor activity through ROS-mediated apoptosis and cell cycle arrest.

Mechanism of Action

Darinaparsin is an organic arsenical that induces apoptosis in cancer cells via mitochondrial dysfunction, generation of reactive oxygen species (ROS), disruption of the mitogen-activated protein kinase (MAPK) pathway, and inhibition of angiogenesis. It is taken up more selectively by tumor cells compared to inorganic arsenic trioxide and interferes with glutathione metabolism.

Routes of Administration

Intravenous

Goals & Uses

  • Induction of tumor cell apoptosis via ROSMechanism/pharmacologyHigh
  • Treatment of relapsed/refractory peripheral T-cell lymphoma (PTCL)OncologyHigh
  • Treatment of acute myeloid leukemia (AML)Hematologic MalignancyModerate
  • Treatment of myelodysplastic syndrome (MDS)OncologyLow

Contraindications

  • QT prolongation / cardiac arrhythmiasCardiacHigh
  • Severe hepatic impairmentOrganHighLiver function concerns
  • Hypersensitivity to arsenic compoundsAllergyHigh
  • Severe renal impairmentOrganModerateKidney function concerns
  • PregnancyPopulationHighPotential fetal risk or insufficient safety data

Adverse Effects

  • Peripheral neuropathyNeurologicalUncommon
  • QT interval prolongationCardiacUncommon
  • Nausea/vomitingGastrointestinalCommon
  • Elevated liver enzymes (hepatotoxicity)HepaticUncommon
  • FatigueGeneralCommonLow energy or tiredness
  • MyelosuppressionHematologicUncommon

Drug Interactions

  • Arsenic trioxideHigh
  • QT-prolonging agents (e.g., fluoroquinolones, antiarrhythmics)High
  • Thiol-containing compounds (e.g., N-acetylcysteine, glutathione precursors)Moderate

Population Constraints

  • Patients with electrolyte abnormalitiesMetabolicRelative
  • Pediatric patientsAgeRelative
  • Patients with pre-existing peripheral neuropathyNeurologicalRelative
  • Pregnant womenReproductiveAbsolute

Regulatory Status

  • European UnionUnknownNo EMA marketing authorization identified; considered investigational in Europe.
  • United StatesInvestigationalNot FDA-approved; investigated in Phase I/II trials for hematologic malignancies. FDA orphan drug designation granted.
  • United KingdomUnknownNo MHRA approval identified as of available data.

Approved in Japan (2021) under the brand name Darinastat for relapsed/refractory peripheral T-cell lymphoma. Investigated in the US and internationally as an investigational agent; not FDA-approved. Orphan drug designation granted by FDA for hematologic malignancies.

Evidence & Sources

No sources recorded yet.

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