Drug intelligence / Profile preview

revamilast + methotrexate

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

**Revamilast + methotrexate** is a combination therapy for inflammatory autoimmune disorders, primarily rheumatoid arthritis and possibly psoriasis. Revamilast is a selective phosphodiesterase 4 (PDE4) inhibitor, acting as a novel oral anti-inflammatory agent. Methotrexate is a conventional disease-modifying antirheumatic drug (DMARD) that inhibits dihydrofolate reductase, impacting purine/pyrimidine synthesis and immune function. Combination therapy that includes a PDE4 inhibitor (such as apremilast, which has a mechanism analogous to revamilast) and methotrexate has been shown to have no significant pharmacokinetic drug-drug interaction. This type of combination is being developed to improve clinical outcomes in patients who do not achieve sufficient disease control with methotrexate monotherapy.

02

Targets

ADORA2A (Adenosine A₂A Receptor)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)TS (Thymidylate synthase)ADORA1 (Adenosine receptor A1 subtype)DHFR (Dihydrofolate reductase)PPAT (Amidophosphoribosyltransferase)PDE4 (Phosphodiesterase 4A1)

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