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How is platinum used in chemotherapy?

Platinum plays a very important role in chemotherapy through platinum-based drugs that are used to treat various cancers. Here’s a clear breakdown:


1. Platinum Compounds in Chemotherapy

  • The most common platinum-based drugs are:
    • Cisplatin
    • Carboplatin
    • Oxaliplatin
  • These drugs contain platinum ions coordinated with nitrogen-donor ligands, making them reactive toward DNA.

2. Mechanism of Action

  1. Activation Inside Cells
    • Platinum drugs are neutral or slightly charged outside the cell.
    • Inside the cell, they undergo aquation, replacing ligands with water molecules, forming reactive platinum species.
  2. Binding to DNA
    • Platinum ions form covalent bonds with DNA, usually at guanine bases.
    • This creates DNA cross-links, either:
      • Intrastrand (between bases on the same DNA strand)
      • Interstrand (between bases on opposite strands)
  3. Disruption of DNA Function
    • Cross-linked DNA cannot unwind properly.
    • This blocks DNA replication and transcription, preventing the cancer cell from dividing.
  4. Inducing Cell Death
    • DNA damage triggers apoptosis (programmed cell death) in cancer cells.

3. Clinical Applications

  • Cisplatin: Widely used for testicular, ovarian, bladder, and lung cancers.
  • Carboplatin: Similar to cisplatin but less toxic to kidneys; used for ovarian and lung cancers.
  • Oxaliplatin: Often used for colorectal cancer, especially in combination therapies.

4. Side Effects

  • Platinum drugs can affect normal cells too, causing:
    • Kidney toxicity (nephrotoxicity)
    • Nerve damage (neurotoxicity)
    • Nausea and vomiting (gastrointestinal toxicity)
    • Bone marrow suppression (myelosuppression)
  • Doctors often give hydration and protective agents to reduce side effects.

5. Advantages

  • Effective against rapidly dividing cancer cells.
  • Can be used alone or in combination with other chemotherapeutic agents.
  • Can overcome resistance in some cancers when combined with other drugs.

Summary:
Platinum-based chemotherapy drugs work by binding to DNA, forming cross-links, and preventing replication, which ultimately kills cancer cells. Their effectiveness, however, is balanced against side effects on normal tissues.


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