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6-Thioguanine: A Drug With Unrealized Potential for Cancer Therapy #MMPMID24928612
Munshi PN; Lubin M; Bertino JR
Oncologist 2014[Jul]; 19 (7): 760-5 PMID24928612show ga
This review suggests that the full potential of 6-thioguanine (6-TG) in cancer therapy may not have been reached. The authors contrast 6-TG and the more widely used 6-mercaptopurine; discuss 6-TG metabolism, pharmacokinetics, dosage and schedule; and summarize many of the early studies that have shown infrequent but nevertheless positive results with 6-TG treatment. The combination of 6-TG and a natural compound, methylthioadenosine (MTA), may provide selective treatment of cancers that have lost the gene methylthioadenosine phosphorylase (MTAP). Administration of MTA decreases 6-TG toxicity to normal host tissues, thus permitting use of increased therapeutic doses of 6-TG. Combinations of 6-TG with other agents, such as methotrexate or pralatrexate, may also enhance therapeutic effects in MTAP-deficient tumors.