Drug intelligence / Profile preview

tofacitinib + cyclosporine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Tofacitinib + cyclosporine is a combination of two immunosuppressive small molecule drugs. Tofacitinib is a Janus kinase (JAK) inhibitor that suppresses immune cell function by inhibiting intracellular signaling pathways involved in hematopoiesis and immune responses. It is primarily indicated for moderate-to-severe rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and polyarticular juvenile idiopathic arthritis in patients who have failed or are intolerant to TNF blockers[1][3][4][8]. Cyclosporine is a calcineurin inhibitor that prevents T cell activation by inhibiting the dephosphorylation and activation of nuclear factor of activated T cells (NF-AT), thereby reducing cytokine production such as IL-2[5]. Cyclosporine is used as an immunosuppressant in organ transplantation and various autoimmune diseases including ulcerative colitis[5]. The combination has been reported in case studies for steroid-refractory acute severe ulcerative colitis after failure with other therapies[2], but concurrent use increases the risk of serious immunosuppression and adverse effects; it is generally not recommended except under specific clinical circumstances.

Other names
Xeljanz XRciclosporin (alternative spelling for cyclosporine)
02

Targets

TYK2 (Tyrosine kinase 2)JAK2 (Janus kinase 2)PPIA (Peptidyl-prolyl cis-trans isomerase A)JAK1 (Janus kinase 1)JAK3 (Janus kinase 3)CN (Calcineurin)

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