Darinaparsin
Also known as: Arsenic‑glutathione conjugate, DAR, Darinastat, DMAG, S-dimethylarsino-glutathione, S-dimethylarsino‑glutathione, ZIO-101
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Summary
Darinaparsin (S-dimethylarsino‑glutathione) is an organo‑arsenic derivative of the tripeptide glutathione under clinical investigation for peripheral T‑cell lymphoma, acute myeloid leukemia and other hematologic malignancies. It is administered intravenously and exerts cytotoxicity via oxidative stress and mitochondrial disruption.
Mechanism of Action
Arsenic moiety generates reactive oxygen species and disrupts mitochondrial function, leading to apoptosis and inhibition of cellular proliferation in malignant lymphoid and myeloid cells.
Routes of Administration
Goals & Uses
- Induction of tumor cell apoptosis via ROSMechanism/pharmacologyHigh
- Treatment of relapsed/refractory peripheral T-cell lymphoma (PTCL)OncologyHigh
- Myelodysplastic syndromesOncologyLow
- Treatment of acute myeloid leukemia (AML)Hematologic MalignancyModerate
- Peripheral T‑cell lymphomaOncologyModerate
- Acute myeloid leukemiaOncologyModerate
- Treatment of myelodysplastic syndrome (MDS)OncologyLow
Contraindications
- Known hypersensitivity to darinaparsin or arsenic‑containing compoundsAllergyHigh
- QT prolongation / cardiac arrhythmiasCardiacHigh
- Severe hepatic impairment (Child‑Pugh C)Liver DiseaseModerate
- 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
- Elevated transaminasesHepaticUncommon
- Nausea/vomitingGastrointestinalCommon
- Elevated liver enzymes (hepatotoxicity)HepaticUncommon
- FatigueGeneralCommonLow energy or tiredness
- Cytopenias (neutropenia, thrombocytopenia)HematologicCommon
- MyelosuppressionHematologicUncommon
Drug Interactions
- Arsenic trioxideHigh
- QT-prolonging agents (e.g., fluoroquinolones, antiarrhythmics)High
- Thiol-containing compounds (e.g., N-acetylcysteine, glutathione precursors)Moderate
- Strong CYP3A4 inhibitors (e.g., ketoconazole)Moderate
- Concurrent myelosuppressive chemotherapyHigh
Population Constraints
- Patients with electrolyte abnormalitiesMetabolicRelative
- Pediatric patientsAgeRelative
- Pediatric patients (<12 y)AgeRelative
- Patients with pre-existing peripheral neuropathyNeurologicalRelative
- Pregnant womenReproductiveAbsolute
Regulatory Status
- European UnionInvestigationalClinical trial authorization granted in several member states.
- United StatesInvestigationalIND holder; Phase II/III trials ongoing.
- United KingdomInvestigationalMHRA clinical trial approval; not marketed.
Not approved in any major jurisdiction; currently in Phase II/III clinical trials.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Darinaparsin?
Darinaparsin (S-dimethylarsino‑glutathione) is an organo‑arsenic derivative of the tripeptide glutathione under clinical investigation for peripheral T‑cell lymphoma, acute myeloid leukemia and other hematologic malignancies. It is administered intravenously and exerts cytotoxicity via oxidative stress and mitochondrial disruption.
What is Darinaparsin used for?
Darinaparsin is educationally associated with: Induction of tumor cell apoptosis via ROS, Treatment of relapsed/refractory peripheral T-cell lymphoma (PTCL), Myelodysplastic syndromes, Treatment of acute myeloid leukemia (AML), Peripheral T‑cell lymphoma, Acute myeloid leukemia, Treatment of myelodysplastic syndrome (MDS). Educational only — not medical advice.
How is Darinaparsin administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Darinaparsin?
Reported adverse effects include: Peripheral neuropathy, QT interval prolongation, Elevated transaminases, Nausea/vomiting, Elevated liver enzymes (hepatotoxicity), Fatigue, Cytopenias (neutropenia, thrombocytopenia), Myelosuppression. This list is not exhaustive — consult a qualified clinician.
Who should avoid Darinaparsin?
Recorded contraindications: Known hypersensitivity to darinaparsin or arsenic‑containing compounds, QT prolongation / cardiac arrhythmias, Severe hepatic impairment (Child‑Pugh C), Severe hepatic impairment, Hypersensitivity to arsenic compounds, Severe renal impairment, Pregnancy. Consult a qualified clinician before use.