Brain tumors are not rare. In the United States, nearly 11,000 new patients were seen in 1976.1 This number can be expected to increase as systemic cancers are controlled more effectively and as longevity is prolonged. Most patients with primary or metastatic brain tumors are treated by surgery, glucocorticoid "decompression," radiotherapy, or chemotherapy—alone or in various combinations. The therapeutic yield from surgery alone has reached its zenith. While radiotherapy prolongs survival, and radiosensitizers such as metronidazole may add to its efficacy,2,3 it seems likely that further advances in the treatment of brain tumors will come from chemotherapy. To date, chemotherapy of brain tumors has been disappointing, to say the least.
Most oncologists assume that to be useful for brain tumor chemotherapy a drug must be lipid soluble, be unionized at physiologic pH, and be of relatively small molecular size in order to enter the brain from the
Vick NA, Khandekar JD, Bigner DD. Chemotherapy of Brain Tumors: The "Blood-Brain Barrier" Is Not a Factor. Arch Neurol. 1977;34(9):523–526. doi:10.1001/archneur.1977.00500210025002
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