Drug intelligence / Profile preview

tofacitinib + mycophenolate mofetil

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Tofacitinib + mycophenolate mofetil is a combination of two immunosuppressive small molecules: tofacitinib, a Janus kinase (JAK) inhibitor, and mycophenolate mofetil (MMF), an inosine monophosphate dehydrogenase inhibitor. Both agents are used alone or with other drugs to suppress pathological immune responses in diseases such as autoimmune disorders and transplant rejection. Their combination is rarely used but has been reported for severe, treatment-refractory inflammatory diseases, such as hidradenitis suppurativa, and is considered an aggressive immunosuppressive regimen. Tofacitinib blocks intracellular signaling required for lymphocyte activation by inhibiting JAK1 and JAK3; MMF inhibits de novo purine synthesis in lymphocytes, suppressing both T and B cell proliferation. Co-administration further increases immunosuppression, with major risks due to compounded immunodeficiency, though evidence for this specific combination is limited and based largely on case reports[5][3].

02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)JAK3 (Janus kinase 3)TYK2 (Tyrosine kinase 2)

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