Platinum anticancer drugs carboplatin

Two of the most important platinum anticancer drugs are cisplatin (2.13) and carboplatin (2.14). Cisplatin is effective against testicular tumours, ovarian carcinoma and some other types of cancer, but relatively inactive against breast and lung cancers it is also a very toxic compound. Side effects include loss of high-frequency hearing, neuropathy and nausea. Kidney damage may also result, but is minimised... 

O Dwyer, P. J. Stevenson, J. P. Johnson, S. W. Clinical Status of Cisplatin, Carboplatin, and Other Platinum-based Antitumor Drugs. In Cisplatin Chemistry and Biochemistry of a Leading Anticancer Drug Lippert, B., Ed. Wiley-VCH New York 1999, pp 31-72. 

In 1965 Rosenberg et al. (8, 9) accidentally discovered the antiproliferative effect of cis-diammine platinum complexes, which led to the first clinical trials of cis-[PtCl2(NH3)2] 1 in 1971 and resulted in the clinical use of cisplatin worldwide. Cisplatin and carboplatin 2 are the most widely used anticancer drugs, and two other analogs, nedaplatin 3 and oxaliplatin 4 (chiral centers indicated), have recently been approved for clinical use in Japan and France, respectively. 

Cisplatin [SIS pla tin] is a member of the platinum coordination complex class of anticancer drugs. Because of cisplatin s severe toxicity, carboplatin [KAR bow pla tin] was developed. The therapeutic effectiveness of the two drugs is similar but their pharmacokinetics, patterns of distribution and dose-limiting toxicities differ. Cisplatin has synergistic cytotoxicity with radiation and other chemotherapeutic agents. 

Chemotherapy refers to drug administration with highly serious side effects, such as nausea, hand and foot rashes, mouth sores, and increased risk of infection, easy bruising, and so on. Therefore, liposomal carriers have been used in order to improve the drug s biodistribution and protect the patient from those side effects. The main anticancer drugs used to treat ovarian cancer are carboplatin and cisplatin, paclitaxel, topotecan, and lurtotecan. PEGylated liposomal doxorubicin has been approved as a regimen for patients with metastatic ovarian cancer refractory to both paclitaxel and platinum based-therapy [449],... 

Platinum-containing alkylating anticancer drug. Used for solid tumors (eg, testes, lung). Tox Neurotoxic and nephrotoxic. Carboplatin is similar. 

Fig.1 Selected platinum-based anticancer compoimds a cisplatin second generation anticancer drugs b carboplatin, c nedaplatin and d oxaliplatin and novel complexes with interesting dinical properties such as the orally administered e satraplatin and complexes designed to overcome cisplatin resistance f trans-dipyridine dichloroplatinum and g a platinum amino phosphine complex...

A number of platinum(II) complexes such as cisplatin and carboplatin Fig. 4.14 are important anticancer drugs. For example, cisplatin (4.12) is effective in the treatment of ovarian and testicular cancers. 

ANTICANCER AND IMMUNOMODULATING DRUGS CYTOTOXICS Platinum compounds-carboplatin, cisplatin, oxaliplatin... 

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