Drug intelligence / Profile preview

tofacitinib + tacrolimus

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Topical
01

Overview

Tofacitinib + tacrolimus 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, primarily used for autoimmune diseases such as rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and juvenile idiopathic arthritis[1][2][4][5]. Tacrolimus is a calcineurin inhibitor that prevents organ transplant rejection and treats certain inflammatory skin conditions by binding to FKBP12 and inhibiting calcineurin-dependent T-cell activation[8]. The combination of these agents can result in profound immunosuppression with an increased risk of serious infections and malignancies[3].

Other names
FK506 (for tacrolimus)Fujimycin (for tacrolimus)
02

Targets

JAK1 (Janus kinase 1)JAK3 (Janus kinase 3)PPP3CA (Protein phosphatase 3 catalytic subunit alpha)

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