Generic
Oxaliplatin
12 brands available in the market
At a glance
Oxaliplatin is a platinum-based anticancer drug used for colon and rectal cancer. It binds to cancer cell DNA to inhibit cell growth and division.
Description
Oxaliplatin is a platinum-containing complex similar to cisplatin. After intracellular hydrolysis, the platinum compound binds to DNA forming cross-links which inhibit DNA replication and transcription, resulting in cell death. Cytotoxicity is cell-cycle nonspecific.
Indications
- Adjuvant treatment of stage III colon cancer (after complete resection of primary tumor)
- Treatment of advanced colorectal cancer
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
Platinum-based Alkylating Agent
Pharmacology
Oxaliplatin undergoes nonenzymatic conversion to active derivatives via displacement of oxalate ligand. Active derivatives form inter- and intrastrand Pt-DNA crosslinks (GG, AG, GNG) which inhibit DNA replication and transcription, causing cell death.
Mechanism of action
Prevents cancer cell growth by inhibiting DNA replication and transcription.
Dosage
Adult Dose (IV):
- Day 1: Oxaliplatin 85 mg/m² + Leucovorin 200 mg/m² (2 hr IV), then 5-FU 400 mg/m² IV bolus (2-4 min), then 5-FU 600 mg/m² IV infusion (22 hr)
- Day 2: Same regimen WITHOUT oxaliplatin
- Repeat every 2 weeks; Adjuvant: 12 cycles (6 months)
Dose Modification: Grade 2 neuropathy: 75 mg/m²; Grade 3 neuropathy: Discontinue; Grade 3/4 GI or hematological: 75 mg/m² + 5-FU 20% reduction
Administration
- IV infusion only; administered by doctor or nurse
- Dilute in 250-500 mL 5% Dextrose
- Administer with leucovorin using Y-line
Missed dose
Not generally applicable (scheduled administration); consult doctor if needed.
Side effects
Common Side Effects (≥40%):
- Peripheral sensory neuropathy
- Neutropenia
- Thrombocytopenia
- Anemia
- Nausea
- Increased transaminases and alkaline phosphatase
- Diarrhea
- Vomiting
- Fatigue
- Stomatitis
Serious: Anaphylactic reactions (2-3%), pulmonary fibrosis, QT prolongation
Precautions & warnings
- Allergic reactions (anaphylaxis) may occur; manage with epinephrine, corticosteroids, antihistamines
- Neurological toxicity: Avoid cold exposure, cold food/drinks
- Discontinue if pulmonary fibrosis symptoms occur
- Risk of QT prolongation; monitor ECG
- Caution while driving (may cause dizziness)
Contraindications
- Hypersensitivity
- Pregnancy
- Peripheral neuropathy with functional impairment
- Severe renal impairment
Drug interactions
- May decrease plasma levels of digoxin
- Increased risk of toxicity with nephrotoxic drugs
- Taxane derivatives should be administered before oxaliplatin (to limit myelosuppression)
Food interactions
Safety with alcohol not known; consult doctor.
Use in pregnancy
Use in Pregnancy: Oxaliplatin is highly unsafe during pregnancy (Category D); definite evidence of severe fetal harm.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Oxaliplatin is unsafe during breastfeeding; may cause toxicity to the baby.
Pediatric use
Safety and efficacy not established in children.
Geriatric use
Elderly (≥65 years) may require dose adjustment.
Renal / hepatic impairment
Renal Impairment: Mild-moderate (CrCl 30-80): No dose adjustment; Severe (CrCl <30): Reduce starting dose.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed.
Overdose effects
Overdose: Grade 4 thrombocytopenia, anemia, sensory neuropathy, laryngospasm, GI disorders, dyspnea, severe bradycardia; supportive treatment.
Storage conditions
Store in a cool and dry place, protected from light and moisture; keep out of reach of children.
Chemical structure
Oxaliplatin