Drug intelligence / Profile preview

tacrolimus + mycophenolate mofetil + basiliximab + corticosteroids

Development stage
Phase 4
Lead developer
Astellas Pharma
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules, Recombinant Proteins and Enzymes
Administration
Oral, Intravenous
01

Overview

This is a **combination immunosuppressive regimen** used primarily in solid organ transplantation, particularly for the prevention of rejection in kidney and liver transplant recipients. It consists of four agents: - **Tacrolimus**: a calcineurin inhibitor, inhibits T-lymphocyte activation by blocking calcineurin, reducing interleukin-2 transcription. - **Mycophenolate mofetil**: an antimetabolite, suppresses lymphocyte proliferation by inhibiting inosine monophosphate dehydrogenase, blocking de novo purine synthesis in T- and B-lymphocytes. - **Basiliximab**: a chimeric monoclonal antibody targeting the interleukin-2 receptor alpha chain (CD25) on activated T cells, preventing their proliferation. - **Corticosteroids**: synthetic adrenocortical steroids (e.g., prednisone, methylprednisolone, prednisolone) with broad immunosuppressive and anti-inflammatory activity, suppress multiple immune pathways by modulating gene transcription. This regimen is often referred to as a **quadruple immunosuppressive regimen** and is used for both induction and initial maintenance in organ transplantation, especially in patients at moderate or high risk for acute rejection. The inclusion of basiliximab provides targeted IL-2 receptor blockade during the critical early post-transplant period, while the other agents provide ongoing immunosuppressive effect. This approach aims for strong early immunosuppression, with possible minimization or withdrawal of corticosteroids in the maintenance phase.

02

Targets

CN (Calcineurin)GR (Glucocorticoid receptor)IL2RA (Interleukin-2 receptor alpha subunit)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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