I

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.

10 Ways To Fight Off Cancer

10 Ways To Fight Off Cancer

Learning About 10 Ways Fight Off Cancer Can Have Amazing Benefits For Your Life The Best Tips On How To Keep This Killer At Bay Discovering that you or a loved one has cancer can be utterly terrifying. All the same, once you comprehend the causes of cancer and learn how to reverse those causes, you or your loved one may have more than a fighting chance of beating out cancer.

Get My Free Ebook


Post a comment