What is oxaliplatin?
This medication is used to treat advanced cancer of the colon and rectum. Oxaliplatin Injection is a chemotherapy drug that contains platinum.It is used in combination with other medications to slow or stop cancer cell growth.
- Single-use vials of 50 mg or 100 mg oxaliplatin as a sterile, preservative-free lyophilized powder for reconstitution.
- Single-use vials of 50 mg, 100 mg or 200 mg oxaliplatin as a sterile, preservative-free, aqueous solution at a concentration of 5 mg/ml.
Dosage and administration
- In combination with 5-fluorouracil/leucovorin every 2 weeks. For advanced disease, treatment is recommended until disease progression or unacceptable toxicity. For adjuvant use, treatment is recommended for a total of 6 months (12 cycles):
Day 1: 85 mg/2ml intravenous infusion in 250-500 mL 5% Dextrose injection, USP and leucovorin 200 mg/2ml intravenous infusion in 5% Dextrose Injection, USP both given over 120 minutes at the same time in separate bags using a Y-line, followed by 5-fluorouracil 400 mg/m2 intravenous bolus given over 2-4 minutes, followed by 5-fluorouracil 600 mg/m2 intravenous infusion in 500 mL 5% Dextrose Injection, USP (recommended) as a 22-hour continuous infusion.
Day 2: Leucovorin 200 mg/m2 intravenous infusion over 120 minutes, followed by 5-fluorouracil 400 mg/m2 intravenous bolus given over 2-4 minutes, followed by 5-fluorouracil 600 mg/m2 intravenous infusion in 500 mL 5% Dextrose Injection, USP (recommended) as a 22-hour continuous infusion.
- Dose Modification Recommendations Prior to subsequent therapy cycles, patients should be evaluated for clinical toxicities and recommended laboratory tests.
Adjuvant Therapy in Patients with Stage III Colon Cancer Neuropathy and other toxicities were graded using the NCI CTC scale version 1 .For patients who experience persistent Grade 2 neurosensory events that do not resolve, a dose reduction to 75 mg/m2 should be considered.
For patients with persistent Grade 3 neurosensory events, discontinuing therapy should be considered. The in fusional 5-fluorouracil/leucovorin regimen need not be altered.
A dose reduction to 75 mg/m2 and infusional 5-fluorouracil to 300 mg/m2 bolus and 500 mg/m2 22 hour infusion is recommended for patients after recovery from grade 3/4 gastrointestinal (despite prophylactic treatment) or grade 4 neutropenia or grade 3/4 thrombocytopenia.
Indications and Usage
- Colon cancer, stage II, adjuvant treatment in combination with 5-fluorouracil/leucovorin.
- Gastric carcinoma, advanced or metastatic.
- Metastatic colorectal cancer (cancer of the colon or rectum that has spread to other areas of the body), first-line therapy, in combination with bevacizumab and capecitabine.
- Metastatic pancreatic adenocarcinoma (cancer of the pancreas that has spread to other areas of the body), first-line treatment, in combination with 5-fluorouracil, leucovorin, and irinotecan.
Mechanism of action
Oxaliplatin Injection undergoes nonenzymatic conversion in physiologic solutions to active derivatives via displacement of the labile oxalate ligand. Several transient reactive species are formed, including monoaquo and diaquo DACH platinum, which covalently bind with macromolecules. Both inter-and intrastrand Pt-DNA crosslinks are formed. Crosslinks are formed between the N7 positions of two adjacent guanines (GG), adjacent adenine-guanines (AG), and guanines separated by an intervening nucleotide (GNG). These crosslinks inhibit DNA replication and transcription. Cytotoxicity is cell-cycle nonspecific.