Table 1. Chemotherapeutic regimens for brain metastasis of small cell lung cancer.
| Drug (trade name) | Treatment setting | Status (year approved) | Brain response rate (%)a | Side effects | Mechanisms of action |
|---|---|---|---|---|---|
| Cyclophosphamide | Front Line | Medical use (1959) | 53%/82%b | Acute myeloid leukemia | Crosslinks DNA at the guanine N-7 position |
| Etoposide (Etopophos) | Front Line | Medical use (1983) | 53%/82%b | Infusion site reactions, hair loss, constipation or diarrhea, metallic food taste, and bone marrow suppression | Forms complex with DNA and topoisomerase II to prevent re-ligation of the DNA strands, causes DNA strand breaks |
| Teniposide (Vumon) | Front Line | Phase III | 22%/57%b | Bone marrow suppression, gastrointestinal toxicity, hypersensitivity reactions, and reversible alopecia | Inhibitor of topoisomerase II, causes DNA double-strand breaks and DNA-protein crosslinks |
| Doxorubicin (Adriamycin) | Front Line | Medical use (1974) | 82%b | Cardiomyopathy, dyspigmentation, and skin eruptions | Causes double-stranded DNA breaks, blocks replication and reforming of the double helix |
| Vincristine (Oncovin) | Front Line | Medical use (1961) | 53%/82%b | Peripheral neuropathy, hyponatremia, constipation, and hair loss | Binds tubulin to stop the cell from separating its chromosomes during metaphase |
| Cisplatin | Front Line | Medical use (1979) | 85%c | Bone marrow suppression, hair loss, kidney toxicity, and vomiting | Interferes with DNA replication |
| Carboplatin (Paraplatin) | Front Line | Medical use (1986) | 40% | Low blood cell levels, nausea, and electrolyte problems | Causes intra-and inter-strand DNA crosslinking |
| Irinotecan (Camptosar) | Front Line | Medical use (1996) | 65% | Diarrhea, vomiting, bone marrow suppression, hair loss, shortness of breath, fever, and immunosuppression | Activates to SN-38, an inhibitor of topoisomerase I, inhibits DNA replication and transcription |
| Topotecan (Hycamtin) | Second line | FDA approved (2007) | 33% | Myelosuppression, anemia, thrombocytopenia, diarrhea, nausea, vomiting, stomatitis, constipation, asthenia | Causes single-stranded DNA breaks, topoisomerase I inhibitor |
a Highest rate of brain response to drugs in the chemotherapy-only arm. b Brain response rate in patients administered chemotherapy plus whole-brain radiation therapy. c Brain response rate in Cisplatin followed by multidrug regimen.