Drug intelligence / Profile preview

mycophenolate mofetil + bortezomib

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

Overview

This is a combination of two pharmaceutical agents, mycophenolate mofetil and bortezomib. Mycophenolate mofetil is an immunosuppressant that acts as a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), thereby suppressing lymphocyte proliferation and immune responses. It is primarily used to prevent organ transplant rejection and treat autoimmune diseases such as lupus nephritis, scleroderma, rheumatoid arthritis, and vasculitis[1][6]. Bortezomib is a small molecule proteasome inhibitor that blocks the 26S proteasome in cells, leading to cell cycle arrest and apoptosis—especially in malignant plasma cells. It is approved for the treatment of multiple myeloma and mantle cell lymphoma[8]. The combination has been investigated in clinical trials for conditions such as systemic sclerosis (scleroderma) and graft-versus-host disease after transplantation[2][4], with preclinical studies also exploring its efficacy in lupus nephritis models[3]. The rationale for combining these drugs lies in their complementary mechanisms—targeting both immune suppression (mycophenolate mofetil) and direct cytotoxicity or modulation of immune cell function (bortezomib).

02

Targets

PSMB6 (Proteasome 20S subunit beta 6)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)PSMB5 (Proteasome subunit beta Type-5)

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