Drug intelligence / Profile preview

revamilast + methotrexate

Development stage
Phase 2
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

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

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