Oxaliplatin

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Axiolatin, Eloxatin, Goxyral, Oxali, Oxaliplatin; Belgium: Eloxatin, Oxaliplatin, Oxaliplatine; Bulgaria: Eloxatin, Oxaliplatin; Czech Republic: Ebeoxal, Eloxatin, Livellin, Oxaliplatin, Oxaliplatina, Platox, Rezidol; Denmark: Eloxatin, Oxaliplatin; Estonia: Eloxatin, Livellin, Oksaliplatiin, Oloxayne, Oxaliplatin; Finland: Eloxatin, Oxaliplatin; France: Dacplat, Ebeoxal, Eloxatine, Oxaliplatine, Oxamed; Germany: Bendaplatin, Croloxat, Ebeoxal, Eloxatin, Euroxaliplatin, Medoxa, Oxaliplan, Oxaliplat, Oxaliplatin, Riboxatin; Greece: Eloxatin, Oxaliplatin, Oxaliplatine, Oxaliprol, Oxaltina, Plaxitin, Veraxatin; Hungary: Eloxatin, Livellin, Oxaliplatin, Oxaliplatine, Sinoxal; Ireland: Eloxatin, Oxaliplatin, Oxamed; Italy: Eloxatin, Oxaliplatino; Lithuania: Oxaliplatin; Netherlands: Eloxatin, Foxantal, Oxaliplatin, Oxaliplatine; Poland: Eloxatin, Oksaliplatyna, Oxalidix, Oxaliplatin, Oxaplatinum, Platox, Sinoxal; Portugal: Eloxatin, Oxaliplatina, Oxamed; Romania: Eloxatin, Oxaliplatin, Oxaliplatina, Rezidol; Slovakia: Ebeoxal, Eloxatin, Oxaliplatin, Oxaliplatina, Rezidol; Slovenia: Eloxatin, Oksaliplatin, Sinoxal; Spain: Eloxatin, Foxantal, Oxaliplatino, Oxitropic; Sweden: Eloxatin, Oxaliplatin, Oxamed, Oxitropic; UK: Eloxatin, Oxaliplatin.

North America

Canada: Eloxatin; USA: Eloxatin, Oxaliplatin.

Latin America

Argentina: Crisapla, Dabenzol, Dacplat, Goxyral, Kebir, Metaplatin, Mitog, O-Plat, Oxaliplatino, Oxaltie, Platinostyl, Plusplatin, Uxalun, Xaliplat; Brazil: Eloxatin, Ezulen, O-Plat, Oxaliplatina, Uxalun; Mexico: Eloxatin, Olipcis, Oxitan, Riptam.

Asia

Japan: Eloxatin.

Drug combinations

Oxaliplatin, Bevacizumab, Fluorouracil, and Leucovorin

Chemistry

Oxaliplatin: C~8~H~14~N~2~O~4~Pt. Mw: 397.29. (1) [SP-4-2-(1R-trans)]-(1,2-cyclohexanediamine-N,N’)[ethanedioato(2-)-O,O’]platinum; (2) cis-[(1R,2R)-1,2-Cyclohexanediamine-N,N’][oxalato(2-)-O,O’]platinum. CAS-61825-94-3 (1998).

Pharmacologic Category

Other Antineoplastic Agents; Platinum Compounds. (ATC-Code: L01XA03).

Mechanism of action

Consists of platinum atom complexed with 1,2-diaminocyclohexane and a labile oxalate ligand. Must undergo nonenzymatic activation before antineoplastic activity occurs. In physiologic solutions, labile oxalate ligand presumably displaced, forming several transient reactive complexes. Following intracellular hydrolysis, these complexes covalently bind to specific DNA base sequences, producing intrastrand and interstrand DNA cross-links, and so inhibiting DNA replication and transcription, resulting in cell death. Exhibits antitumor activity against colon carcinoma in vivo. Exhibits synergistic antiproliferative activity with fluorouracil.

Therapeutic use

Stage III colon cancer and advanced colorectal cancer.

Pregnancy and lactiation implications

Animal studies demonstrate fetal harm. There are no adequate studies in pregnant women. May cause permanent infertility in males. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

Esophageal cancer, gastric cancer, head and neck cancer, non-Hodgkin lymphoma, ovarian cancer, pancreatic cancer, non-small cell lung cancer.

Contraindications

Hypersensitivity to oxaliplatin, other platinum-containing compounds, or any component of the formulation. Pregnancy, breast-feeding, and severe renal impairment (CrCl <30 mL/minute).

Warnings and precautions

Anaphylactic/anaphylactoid reactions may occur within minutes of oxaliplatin administration. Allergic reactions may occur with any cycle and may include bronchospasm (rare), erythema, hypotension (rare), pruritus, rash, and/or urticaria. Two different types of peripheral sensory neuropathy may occur (one acute (within first 2 days), reversible, with primarily peripheral symptoms often exacerbated by cold, and a more persistent (>14 days) presentation which often interferes with daily activities (e.g. writing, buttoning, swallowing)). Hepatotoxicity (including hepatic failure and hepatitis) reported. May cause pulmonary fibrosis. Use with caution in renal impairment (risk of toxicity). Risk of adverse hematologic effects or adverse gastrointestinal effects associated with severe diarrhea/emesis may be increased with concomitant use of fluorouracil. When administered as sequential infusions, taxane derivatives (docetaxel, paclitaxel) should be administered before platinum derivatives (carboplatin, cisplatin, oxaliplatin) to limit myelosuppression and enhance efficacy. Elderly patients more sensitive to adverse events, particularly diarrhea, dehydration, hypokalemia, leukopenia, fatigue, and syncope.

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