Drug intelligence / Profile preview

azathioprine + mesalazine

Development stage
Unknown
Lead developer
Burroughs Wellcome (now GSK) and Tillotts Pharma AG
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Rectal, Intravenous
01

Overview

Azathioprine + mesalazine is a combination therapy used primarily in the management of inflammatory bowel diseases such as ulcerative colitis and Crohn's disease. Azathioprine is an immunosuppressive antimetabolite that inhibits purine synthesis, thereby suppressing T-lymphocyte proliferation. Mesalazine (also known as 5-aminosalicylic acid or 5-ASA) is an anti-inflammatory agent that acts locally in the colon to inhibit prostaglandin production via cyclooxygenase inhibition and modulate other inflammatory pathways. The combination can be effective for inducing or maintaining remission in patients with moderate to severe disease activity who are refractory to monotherapy. However, co-administration increases the risk of myelotoxicity due to pharmacokinetic interactions—mesalazine can inhibit thiopurine methyltransferase (TPMT), leading to higher levels of active thioguanines from azathioprine metabolism[1][2][3]. This necessitates careful monitoring for bone marrow suppression.

Other names
azathioprine and mesalazineazathioprine plus mesalazineazathioprine + mesalamineazathioprine and mesalamine
02

Targets

RAC1 (Rac family small GTPase 1)TPMT (Thiopurine S-methyltransferase)PPAT (Amidophosphoribosyltransferase)PGHS-1 (Prostaglandin G/H Synthase 1)

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