Folate Antagonist: (Methotrexate)

Structure of Methotrexate:


MOA: 

  • Inhibition of Dihydrofolate Reductase (DHFR): The majority of antifolates work by inhibiting DHFR, an enzyme that reduces dihydrofolate to tetrahydrofolate. Tetrahydrofolate is a necessary component in the synthesis of nucleotide precursors, so when DHFR is inhibited, it leads to a deficiency in the nucleotide precursors, thus inhibiting DNA synthesis.

USES of ANTIMETABOLITES 

  1. Leukemia: Antimetabolites are commonly used to treat different types of leukemia
  2. Breast Cancer: These drugs are used in the treatment of breast cancer
  3. Ovarian Cancer: Antimetabolites are used to treat ovarian cancer
  4. Intestinal Cancer: These drugs are also used in the treatment of cancers of the intestinal tract
  5. Lung Cancer: Antimetabolites are used to treat lung cancers
ADVERSE EFFECT:
1. leukopenia 
2. nausea, vomiting 
3. Abdominal pain 
4. Ulcer 
5. dizziness 
6. Fever and chills etc. 

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