Oxaliplatin

• Oxalatoplatin
• Trans-L -(-) -diaminocyclohexane oxalatoplatin
• Oxalato [( 1R, 2R)- cyclohexane ] platinum (II)
• Pt ( oxalato )-trans- l - diaminocyclohexane

L01XA03

Cytostatic

Attention

14.3 mg · kg -1 ( LD50, rat, ip)

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Oxaliplatin is an effective cytostatic drug from the group of platinum derivatives and is marketed by sanofi -aventis. It is approved in combination with 5- fluorouracil (5- FU) and folinic acid ( FS) for the treatment of colorectal cancer ( FOLFOX regimen ).

Chemistry

Oxaliplatin is an anticancer drug that belongs to a new class of platinum complexes in which the platinum with a 1.2 - Diaminocyclohexyl ligand ( short DACH ligand) and a complexed oxalate. Oxaliplatin is a pure enantiomer, cis- [ oxalato (trans -l-1 ,2- diaminocyclohexane ) platinum ].

Pharmacology

Effectiveness

The effectiveness of the combination therapy of oxaliplatin with 5-Fluoruracil/Folinsäure ( 5-FU/FA ) is demonstrated in numerous studies. Oxaliplatin is included in all guidelines for the treatment of colorectal cancer for the respective therapeutic areas with the highest level of recommendation. Recent studies suggest that an additional combination with the monoclonal antibody bevacizumab, survival rates can continue to improve significantly.

Application

Oxaliplatin is used in combination with 5- fluorouracil and folinic acid and is approved in adults

• For the adjuvant treatment of colon cancer stage III (Dukes' C) after complete resection of primary tumor,
• For the treatment of metastatic colorectal cancer.

A common combination is the FOLFOX4 regimen with oxaliplatin infusion on the first day, followed by a continuous infusion of 5 -fluorouracil over two days.

Mechanism of Action

Oxaliplatin causes resulting in the body metabolic products, similar to interact as with cis- or carboplatin with DNA and form cross-links within and between the DNA strands. 1,2- Diaminocyclohexyl ligand ( ligand - DACH ) influences the cell's ability to tolerate DNA -platinum adducts. This is the basis of the difference in the effect of oxaliplatin and Cis-/Carboplatin. The DACH - platinum adducts, which are formed from oxaliplatin, inhibit DNA synthesis stronger than the cis- diamino- platinum adducts, which are formed from cis- and carboplatin.

Side effects

The most common side effects of oxaliplatin in combination with 5 -fluorouracil and folinic acid are diarrhea, nausea, vomiting, and inflammation of the mucous membranes, changes in blood count and peripheral - sensory neuropathy ( n ) ( neurological discomfort ). The latter is often dose limiting.

Development

Trade names

Benda platinum ( D), Croloxat (D), Eloxatin (D, A, CH), Medoxa (D ), various generics (D, A)