Antifolates in clinical development.

Abstract:

:Many novel antifolate compounds with unique pharmacologic properties are currently in clinical development. These newer antifolates differ from methotrexate, the most widely used and studied drug in this class, in terms of their lipid solubility and cellular transport affinity, their level of polyglutamation, and their specificity for inhibiting folate-dependent enzymes, such as dihydrofolate reductase, thymidylate synthase, or glycinamide ribonucleotide formyltransferase. The current status (ie, mechanism of action, clinical response rates, and toxicity) of some of the newer antifolate compounds presently in clinical testing, including edatrexate, piritrexim, raltritrexed, LY 231514, AG337, AG331, 1843U89, ZD 9331, and lometrexol, is reviewed.

journal_name

Semin Oncol

journal_title

Seminars in oncology

authors

Takimoto CH

subject

Has Abstract

pub_date

1997-10-01 00:00:00

pages

S18-40-S18-51

issue

5 Suppl 18

eissn

0093-7754

issn

1532-8708

journal_volume

24

pub_type

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