Antifolates in clinical development

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 polygl...

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Bibliographic Details
Published inSeminars in oncology Vol. 24; no. 5 Suppl 18; p. S18
Main Author Takimoto, C H
Format Journal Article
LanguageEnglish
Published United States 01.10.1997
Subjects
Aminopterin - analogs & derivatives
Aminopterin - pharmacology
Aminopterin - therapeutic use
Animals
Antimetabolites, Antineoplastic - pharmacology
Antimetabolites, Antineoplastic - therapeutic use
Clinical Trials as Topic
Drug Design
Enzyme Inhibitors - pharmacology
Enzyme Inhibitors - therapeutic use
Folic Acid Antagonists - pharmacology
Folic Acid Antagonists - therapeutic use
Glutamates - pharmacology
Glutamates - therapeutic use
Guanine - analogs & derivatives
Guanine - pharmacology
Guanine - therapeutic use
Humans
Indoles - pharmacology
Indoles - therapeutic use
Isoindoles
Pemetrexed
Pyrimidines - pharmacology
Pyrimidines - therapeutic use
Quinazolines - pharmacology
Quinazolines - therapeutic use
Tetrahydrofolates - pharmacology
Tetrahydrofolates - therapeutic use
Thiophenes - pharmacology
Thiophenes - therapeutic use
Thymidylate Synthase - antagonists & inhibitors
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Summary: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.
ISSN:0093-7754