Class: Cytoprotective agent (prodrug → active free thiol metabolite WR-1065).
Mechanism:
- Selectively scavenges free radicals and provides protection to normal tissues from chemotherapy and radiation damage.
- Normal tissues take up the drug more than tumor tissues due to higher alkaline phosphatase activity and better vascularization.
Indications (Oncology Practice)
- Prevention of nephrotoxicity from cisplatin.
- Reduction of xerostomia in head and neck cancer patients receiving radiation.
- Investigated/used off-label for protection against hematologic and neurotoxicities of chemotherapy.
Dosing (Common Regimens)
-
Cisplatin nephroprotection:
- 910 mg/m² IV over 15 minutes, 30 minutes before cisplatin.
- Radiation-induced xerostomia:
- 200 mg/m² IV daily, 15–30 minutes before radiation therapy.
- Administer with patient supine to minimize hypotension risk.
Key Toxicities / Side Effects
- Hypotension (most significant; monitor BP closely).
- Nausea/vomiting (premedicate with antiemetics).
- Hypocalcemia (monitor electrolytes).
- Flushing, sneezing, somnolence.
- Rare: allergic reactions, seizures.
Monitoring
- Blood pressure before and during infusion.
- Serum electrolytes (especially calcium).
- Observe for nausea/vomiting and manage aggressively.
Pharmacist Pearls
- Give with IV fluids and antiemetic prophylaxis.
- Stop infusion if significant hypotension occurs.
- Not widely used in practice today (supportive care alternatives often preferred), but important for exams and niche clinical settings.