Drug intelligence / Profile preview

azathioprine + mycophenolate mofetil + methotrexate

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Recombinant Proteins and Enzymes, Antibody-Based Therapeutics, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous, Subcutaneous, Intramuscular, Intrathecal
01

Overview

This is a combination of three immunosuppressive drugs—azathioprine (a purine analog), mycophenolate mofetil (a prodrug of mycophenolic acid and an inosine monophosphate dehydrogenase inhibitor), and methotrexate (an antifolate antimetabolite). All three agents are used to suppress the immune system in various autoimmune diseases and to prevent organ transplant rejection. Azathioprine inhibits purine metabolism and nucleic acid synthesis to reduce lymphocyte proliferation[7][3]. Mycophenolate mofetil inhibits inosine monophosphate dehydrogenase 1 and 2, blocking guanosine nucleotide synthesis required for DNA/RNA production in lymphocytes[4]. Methotrexate inhibits dihydrofolate reductase and other enzymes involved in nucleotide synthesis, preventing cell division especially in rapidly dividing immune cells[6]. This combination may be considered for difficult-to-treat autoimmune or inflammatory conditions when single-agent therapy is insufficient[1][5].

Other names
AZAMMFMTX
02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)

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