Small molecule
PubChem CID 5702198
Cisplatin
Platinol
- Mechanism of action
- Platinum-based DNA crosslinking agent
- In plain language
- Locks onto a cancer cell's DNA and crosslinks the strands together, jamming the machinery it needs to copy itself and triggering the cell to die.
- How it works
- Cisplatin is a platinum coordination complex that, once inside the cell, undergoes aquation (loss of chloride ligands) to form a reactive electrophilic species. This activated form binds covalently to the N7 position of purine bases in genomic DNA, forming predominantly intrastrand (and some interstrand) cross-links, most commonly 1,2-d(GpG) adducts. These adducts distort the DNA helix and block normal transcription and replication machinery. The resulting unrepaired DNA damage activates cell-cycle checkpoints and apoptotic signaling pathways, producing cytotoxicity that is not restricted to a specific phase of the cell cycle.
- Therapeutic applications
- FDA-approved for the treatment of advanced (metastatic) testicular cancer, typically as combination chemotherapy following appropriate surgical and/or radiotherapeutic intervention; advanced (metastatic) ovarian cancer, as combination therapy or as single-agent secondary therapy in patients refractory to prior chemotherapy; and advanced bladder cancer (transitional cell carcinoma) no longer amenable to local treatment such as surgery or radiotherapy, typically as a single agent.
- Class
- Small molecule
- Therapeutic area
- Oncology
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