Drug intelligence / Profile preview

cyclosporin + sulfasalazine

Development stage
Unknown
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
01

Overview

Cyclosporin + sulfasalazine is a combination of two disease-modifying antirheumatic drugs (DMARDs) used primarily in the treatment of early, active rheumatoid arthritis. Cyclosporin (also known as cyclosporine or CyA) is an immunosuppressant that inhibits T cell activation by binding to cyclophilin and inhibiting calcineurin, thereby blocking the transcription of cytokines such as IL-2 involved in inflammatory responses. Sulfasalazine (SASP) is an anti-inflammatory agent metabolized into mesalazine and sulfapyridine; it modulates inflammatory processes through inhibition of prostaglandin synthesis and other mechanisms. The combination has been shown to reduce disease activity and prevent disability in patients with early rheumatoid arthritis who have not responded adequately to monotherapy. Clinical studies indicate improved efficacy compared to single-agent therapy, though gastrointestinal side effects may occur[1][2]. Both agents require careful monitoring for adverse effects.

Other names
cyclosporine + sulfasalazineCyA + SASP
02

Targets

PPIA (Peptidyl-prolyl cis-trans isomerase A)CN (Calcineurin)

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