Drug intelligence / Profile preview

methotrexate + 6-thioguanine

Development stage
Unknown
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination chemotherapy regimen consisting of the antimetabolites methotrexate and 6-thioguanine, investigated by Memorial Sloan Kettering Cancer Center for the treatment of Langerhans cell histiocytosis (LCH). Methotrexate is a folate antimetabolite that inhibits dihydrofolate reductase, while 6-thioguanine is a purine analogue that incorporates into DNA and RNA and inhibits purine synthesis. In this specific protocol, methotrexate is administered followed by 6-thioguanine, with leucovorin calcium used as a rescue agent to mitigate methotrexate toxicity. The regimen is primarily targeted at patients with multifocal or multisystem LCH to induce and maintain remission.

Brand names
TrexallRheumatrexTabloid
Other names
MTX + 6-TGSequential 6-Thioguanine After MethotrexateSequential6-Thioguanine After MethotrexateSequential-6-Thioguanine After Methotrexatemethotrexate and 6-thioguanine
02

Targets

DHFR (Dihydrofolate reductase)DNAHPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)

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