Active Pharmaceutical Ingredients

Molecular Formula: PtCl2(NH3)2

Molecular Weight: 300.0

CAS No.: 15663-27-1

It is one of the most commonly used drugs in combined chemotherapy because of its wide anticancer spectrum, strong effect, synergistic effect with a variety of anticancer drugs, and no cross resistance.

Description

It is a yellow to orange crystalline powder. It is a heavy metal complex containing a central atom of platinum surrounded by two chloride atoms and two ammonia molecules in the cis position. It is soluble in water or saline at 1 mg/mL and in dimethylformamide at 24 mg/mL. It melts at 207°C.

Application

One of the applied platinum anticancer drugs. Its cure rate for testicular cancer is almost 100%, and it also has a good effect on ovarian cancer, lung cancer, head and neck cancer, bone cancer and other malignant tumors. Therefore, it is also known as “penicillin in anticancer drugs”.

Packing

Preserve in airtight containers.

Storage

Protect from light.

Minimum Order

One package

Aspect	Details
Mechanism of Action	Cisplatin is a platinum-based alkylating agent that exerts its cytotoxic effects by binding to DNA, forming intra-strand and inter-strand cross-links, which inhibit DNA synthesis and cell division. This leads to apoptosis through the activation of p53, caspases, and other pro-apoptotic pathways.
Pharmacokinetics	Cisplatin is primarily excreted through the kidneys, with approximately 10% excreted in bile. Its initial half-life is about 20 to 30 minutes, while its terminal half-life is around 24 hours. The drug is highly protein-bound, and its clearance is significantly affected by renal function.
Administration	Administered intravenously, often in combination with other chemotherapeutic agents. Patients require adequate hydration before, during, and after administration to minimize nephrotoxicity. Antiemetics are typically administered prophylactically to prevent nausea and vomiting.
Adverse Effects	Common side effects include nephrotoxicity, neurotoxicity, ototoxicity, and gastrointestinal disturbances such as nausea and vomiting. Other potential adverse effects include hepatotoxicity, cardiotoxicity, and electrolyte imbalances.
Storage Conditions	Cisplatin should be stored at room temperature (15° to 30°C) and protected from light. The drug is stable in its solid form but should be prepared and used according to specific guidelines to avoid degradation.
Special Considerations	Dose adjustments are necessary for patients with impaired renal function. Cisplatin is often used off-label for various malignancies, including breast cancer, lung cancer, and gastrointestinal cancers, due to its broad-spectrum activity.
Resistance and Combination Therapy	Resistance to cisplatin can occur through mechanisms such as increased DNA repair, altered drug uptake, and overexpression of anti-apoptotic proteins. Combination therapies with other agents, such as gemcitabine or paclitaxel, are often used to enhance efficacy and overcome resistance

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