Source: Health Sciences Authority (SG) Revision Year: 2021
Carboplatin is a second-generation platinum compound; non-classical alkylating agent and is cell-cycle-phase non-specific. It is a cytotoxic platinum complex that reacts with nucleophilic sites of DNA. This causes interstrand and intrastrand DNA cross links, which inhibit DNA, RNA and protein synthesis.
After a 1 hour infusion (20-520mg/m²) plasma levels of total platinum and free (ultrafilterable) platinum decay biphasically following first order kinetics. For free platinum the initial phase (t alpha) half-life is approximately 90 minutes, and the later phase (t beta) half-life approximately 6 hours. All free platinum is in the form of Carboplatin in the first 4 hours after administration.
Carboplatin is excreted primarily by glomerular filtration in urine, with recovery of 65% of a dose within 24 hours. Most of the drug is excreted within the first 6 hours. Approximately 32% of a given dose of carboplatin is excreted unchanged.
Protein binding of carboplatin reaches 85-89% within 24 hours of administration although during the first 4 hours only up to 29% of the dose is protein bound. Patients with poor renal function may require dosage adjustments due to altered pharmacokinetics of carboplatin.
The carcinogenic potential of carboplatin has not been studied, but compounds with similar mechanisms of action and mutagenicity profiles have been reported to be carcinogenic. Carboplatin has been shown to be mutagenic both in vitro and in vivo. It has also been shown to be embryotoxic and teratogenic in rats receiving the drug during organogenesis. Secondary malignancies have been reported in association with multi-drug therapy.
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