Folic acid antagonists

Folic acid antagonists are substances that as analogs of folic acid in the DNA - and RNA engage-nucleotide synthesis and enzyme inhibition especially in the enzyme dihydrofolate reductase (DHFR), as well as others, exert their effect. Folic acid antagonists in the narrower sense are a small group of cytostatics ( antimetabolites ).

Drugs of the group

Cytostatics (affecting the human organism)

• Methotrexate (MTX) as the lead substance
• Pemetrexed
• Aminopterin

Anti-infectives (acting on pathogens)

• Pyrimethamine
• Trimethoprim

Other drug groups (folic acid inhibition as a side effect)

• Lamotrigine (minor)

History

Before pemetrexed was approved, the term folic acid antagonist was used as a synonym for methotrexate and is still very common today.

The chemist Yellapragada Subbarow developed the first folic acid antagonist in the form of aminopterin in 1947 in collaboration with the doctor Sidney Farber . It has been used very successfully in the treatment of leukemia in children, and they both also developed methotrexate .

See also

• Aminopterin syndrome

Individual evidence

1. ↑ ^{a b} Ruß, Endres, Arzneimittelpocket Plus 2008, 4th edition October 2007, ISBN 978-3-89862-287-5 .