Oxaliplatin is a platinum-based chemotherapy drug in the same family as cisplatin and carboplatin. Compared to cisplatin the two amine groups are replaced by diamino cyclohexane (DACH) group to provide a greater antitumor effect. However, this leads to poorer water solubility, which was compensated by the addition of the chloride moieties. Due to this chemical moiety, oxaliplatin readily undergoes non-enzymatic biotransformation, thus complicating oxaliplatin's pharmacokinetics. Like most platinum-based compounds, oxaliplatin's mechanism of action is primarily through DNA damage through DNA crosslinking, particularly intrastrand and interstrand crosslinking. However, due to the structure of oxaliplatin, its adducts make the binding of mismatch repair protein to DNA harder compared to cisplatin or carboplatin's adducts, resulting in greater cytotoxic effects. The DACH moiety also prevents cross-resistance with cisplatin and carboplatin.
Although oxaliplatin has been investigated as a monotherapy, it is typically administered in combination with fluorouracil and leucovorin, known as the FOLFOX regimen, for the treatment of colorectal cancer. This is an effective combination treatment both as a first-line treatment and in patients refractory to an initial fluorouracil and leucovorin combination. Ongoing trials have also shown promising results for oxaliplatin use in nonHodgkin’s lymphoma, breast cancer, mesothelioma, and non-small cell lung cancer.
Oxaliplatin was approved by the FDA on January 9, 2004 and is currently marketed by Sanofi-Aventis under the trademark Eloxatin®.
Oxaliplatin, in combination with infusional fluorouracil and leucovorin, is indicated for the treatment of advanced colorectal cancer and adjuvant treatment of stage III colon cancer in patients who have undergone complete resection of the primary tumor.
The Sixth Hospital,Sun Yat-sen University, Guanzhou, Guangdong, China
O Neal Comprehensive Cancer Center at UAB, Birmingham, Alabama, United States
University of Southern California, Los Angeles, California, United States
University of California, Los Angeles UCLA, Los Angeles, California, United States
Site KR82003, Seocho-gu, Seoul, Korea, Republic of
Site KR82005, Seodaemun-gu, Seoul, Korea, Republic of
Site KR82001, Guro-gu, Seoul, Korea, Republic of
Fudan University Shanghai Cancer Center, Shanghai, China
ZhongShan hospital FuDan university, Shanghai, Shanghai, China
Asan Medical Center Hospital, Seoul, Korea, Republic of
Mayo Clinic - Arizona, Phoenix, Arizona, United States
USC/Norris Comprehensive Cancer Center, Los Angeles, California, United States
Fujian cancer hospital, Fuzhou, Fujian, China
Universitätsklinikum Augsburg, III. medizinische Klinik, Augsburg, Germany
DIK Deggendorf, Onkologische Ambulanz, Deggendorf, Germany
Universitätsklinikum Frankfurt, Klinik für Allgemein-, Viszeral- und Transplantationschirurgie,, Frankfurt, Germany
Second Affiliated Hospital of Zhejiang University School of Medicine, Hangzhou, Zhejiang, China
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