Drug class

Folate Antagonists

Folate antagonists, also known as antifolates, are an antimetabolite drug class that structurally mimics folic acid and interferes with folate-dependent cellular metabolism. Read more about Folate Antagonists

66 drugs in this class 51 manufacturers

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Drugs in Folate Antagonists

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About Folate Antagonists.

Folate antagonists, also known as antifolates, are an antimetabolite drug class that structurally mimics folic acid and interferes with folate-dependent cellular metabolism.

They act primarily by competitively inhibiting key enzymes such as dihydrofolate reductase (DHFR) and thymidylate synthase, thereby blocking the synthesis of tetrahydrofolate cofactors necessary for de novo purine and pyrimidine nucleotide production and cellular replication.

Because rapidly dividing cells are uniquely susceptible to this disruption in DNA and RNA synthesis, folate antagonists are widely utilized in oncology for hematologic malignancies and solid tumors, in rheumatology for inflammatory conditions such as rheumatoid arthritis, and in infectious diseases to treat or prevent parasitic and bacterial infections.