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Eloxatin (Oxaliplatin)
Oxaliplatin forms platinum-DNA crosslinks that inhibit replication and transcription.
Oxaliplatin is a platinum-based chemotherapy agent indicated for adjuvant treatment of stage III colon cancer and advanced colorectal cancer in combination with fluorouracil and leucovorin. It forms DNA crosslinks that inhibit replication and transcription with cell-cycle nonspecific cytotoxicity. Primary risks include hypersensitivity reactions, QT prolongation, nephrotoxicity interactions, and altered clearance in renal impairment. The drug undergoes rapid nonenzymatic metabolism with renal excretion as the major elimination route and a long terminal half-life of 391 hours.
At a glance
| Generic name | Oxaliplatin |
|---|---|
| Sponsor | Yakult Honsha |
| Drug class | Platinum-based chemotherapy agent |
| Target | DNA |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2002 |
Mechanism of action
Oxaliplatin undergoes nonenzymatic conversion in physiologic solutions to active derivatives through 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 between the N7 positions of guanines at various configurations (GG, AG, GNG), which inhibit DNA replication and transcription. Cytotoxicity is cell-cycle nonspecific. In combination with fluorouracil, oxaliplatin exhibits greater antiproliferative activity than either compound alone in several tumor models including colon, mammary, and leukemia.
Approved indications
- Lymph Node Positive Colorectal Carcinoma
- Malignant tumor of stomach
- Metastasis from malignant tumor of colon
- Small intestine cancer
Boxed warnings
- WARNING: HYPERSENSITIVITY REACTIONS, INCLUDING ANAPHYLAXIS Serious and fatal hypersensitivity adverse reactions, including anaphylaxis, can occur with oxaliplatin within minutes of administration and during any cycle. Oxaliplatin is contraindicated in patients with hypersensitivity reactions to oxaliplatin and other platinum-based drugs [see Contraindications ( 4 )] . Immediately and permanently discontinue oxaliplatin for hypersensitivity reactions and administer appropriate treatment for management of the hypersensitivity reaction [see Warnings and Precautions ( 5.1 )]. WARNING: HYPERSENSITIVITY REACTIONS, INCLUDING ANAPHYLAXIS See full prescribing information for complete boxed warning. Serious and fatal hypersensitivity adverse reactions, including anaphylaxis, can occur with oxaliplatin within minutes of administration and during any cycle. Oxaliplatin is contraindicated in patients with hypersensitivity reactions to oxaliplatin and other platinum-based drugs. Immediately and permanently discontinue oxaliplatin for hypersensitivity reactions and administer appropriate treatment. ( 4 , 5.1 )
Common side effects
- Nausea
- Diarrhoea
- Fatigue
- Neutropenia
- Vomiting
- Peripheral sensory neuropathy
- Anaemia
- Neutrophil count decreased
- Constipation
- Neuropathy peripheral
- Thrombocytopenia
- Decreased appetite
Drug interactions
- Drugs that prolong QT interval
- Nephrotoxic products
- Oral anticoagulants (with fluorouracil/leucovorin)
Key clinical trials
- MOSAIC - Multicenter International Study of Oxaliplatin/ 5FU-LV in the Adjuvant Treatment of Colon Cancer (PHASE3)
- Comparison of Three Chemotherapy Regimens in Treating Patients With Metastatic Colorectal Cancer (PHASE3)
- Combination Chemotherapy in Treating Patients With Advanced Colorectal Cancer (PHASE3)
- A Study of Zilovertamab Vedotin (MK-2140) in Combination With Standard of Care in Participants With Relapsed or Refractory Diffuse Large B-Cell Lymphoma (rrDLBCL) (MK-2140-003) (PHASE2,PHASE3)
- A Study to Evaluate the Safety and Efficacy of Two Dose Levels of ONO-4578 With Opdivo®, in Combination With mFOLFOX6 and Bevacizumab Versus Standard of Care in Participants With Non-MSI-H/dMMR, PD-L1 Positive Advanced Colorectal Cancer (PHASE2)
- Neoadjuvant mFolfirinox With or Without Preoperative Concomitant Chemoradiotherapy in Patients With Borderline Resectable Pancreatic Carcinoma (PANDAS-PRODIGE 44) (PHASE2)
- Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial (PHASE2)
- Individual Response to Hyperthermic Intraperitoneal Chemotherapy (HIPEC) Treatment of Peritoneal Carcinomatosis From Peritoneal Mesothelioma or Atypical Mesothelial Proliferation or From Ovarian, Colorectal, or Appendiceal Histologies (PHASE1)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |