Cofactor for thymidylate synthase

FIGURE 2.30 Bypass of DHFR inhibition by leucovorin.

are 10-ethyl-10-deazaaminopterin (edatrexate) and 10-propargyl-10-deazaaminop-terin (PDX), which are under clinical investigation.40,41

o co2h

Edatrexate PDX

5.2. Nonclassical (lipophilic) DHFR inhibitors

Suppression of the glutamic chain leads to compounds that are not substrates for the folate active transport systems, and enter the cells by passive diffusion. They have the advantage of being active in cancer cells resistant to MTX because of transport defects. On the contrary, the lack of the glutamic acid side chain prevents polyglutamation and therefore these compounds are not retained within the cells and require more prolonged treatments. Among these compounds, trimetrexate is mainly used to treat pneumonias by Pneumocystis carinii and Toxoplasma gondii, although it is also used in the treatment of certain cancers, including colon cancer.42 Piritrexim is being assayed for similar applications, including the treatment of psoriasis, pneumonia, and several cancers.

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