Carboplatin

Carboplatin is a platinum-based chemotherapy agent used for treating many types of human cancer, including small cell lung cancer, ovarian cancer, and esophageal carcinoma. Carboplatin exerts its biological effects by interacting with cellular targets such as genomic DNA, tubulin, and other proteins . Carboplatin is believed to work through DNA crosslinking mechanisms similar to other platinum agents. Carboplatin is supplied as a crystalline solid and is available as both an API for pharmaceutical manufacturing and as an analytical reference standard. The compound is freely soluble in water (17.6 mg/mL) .

Product Parameters

Pharmacokinetics

In patients with normal renal function, the plasma concentration declines approximately 30 minutes after intravenous administration, and the curve shows a biphasic distribution. The half-life is 1 to 2 hours, and the terminal half-life is 2.6 to 5.9 hours. The highest tissue concentrations are found in the liver, kidneys, skin and tumors, which indicates that the distribution of carboplatin is similar to that of cisplatin. Unlike cisplatin, only a very small amount of carboplatin is bound to plasma proteins. The drug is mainly excreted by the kidneys, but there is no tubular secretion as observed with cisplatin. This may explain the reduced incidence of nephrotoxicity associated with carboplatin. 65% of the dose is excreted in the first 12 hours, 6% in the next 12 hours, and only 3 to 5% is excreted within 96 hours. It is still unclear whether the remainder is excreted via the bile or through other routes. All platinum detected in 24-hour urine is unmodified carboplatin, which indicates that metabolism occurs very rarely, if at all. In patients with low creatinine clearance, the half-life is longer, so the dose should be adjusted accordingly.

Function and Application

The scope of action of carboplatin is generally similar to that of cisplatin. The main advantage of this new analog is its difference in toxicity. Currently, carboplatin is used as palliative treatment for recurrent ovarian cancer, including patients who have previously received cisplatin. Clinical studies have also indicated that carboplatin can produce objective responses in head and neck tumors, small cell lung cancer and testicular seminoma.

At present, carboplatin is mainly used clinically to treat small cell lung cancer, ovarian cancer, testicular cancer, germ cell tumors, thyroid cancer, nasopharyngeal carcinoma, and can also be used for malignant tumors such as cervical cancer, non-small cell lung cancer, esophageal cancer, seminoma, bladder cancer, mesothelioma, pediatric brain tumors and other head and neck cancers. Patients who cannot tolerate cisplatin due to renal function impairment, intractable vomiting, hearing loss or neurotoxicity can use this product. It has no cross-resistance with other chemotherapeutic drugs, and can be used alone or in combination with other chemical drugs, and can also be combined with surgery and radiotherapy to improve the therapeutic effect.

Application

Carboplatin is a platinum-based anticancer drug that damages DNA by forming intrastrand cross-links with adjacent guanine residues. The antitumor effect of these drugs is achieved through the activity of DNA mismatch repair deficiency (MMR vaccine) and the induction of programmed cell death.

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