Drug intelligence / Profile preview

cyclosporin A + mycophenolate mofetil + methotrexate

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

Overview

This is a combination immunosuppressive regimen consisting of three agents: cyclosporin A (a calcineurin inhibitor), mycophenolate mofetil (an antimetabolite prodrug of mycophenolic acid), and methotrexate (an antimetabolite and antifolate agent). This triple-drug regimen is primarily used as prophylaxis against graft-versus-host disease (GVHD) in patients undergoing allogeneic hematopoietic stem cell transplantation, especially in the context of unrelated donor or haploidentical transplants. Each drug acts via a distinct mechanism to suppress immune responses: - Cyclosporin A inhibits calcineurin, thereby blocking T-cell activation by preventing transcription of interleukin-2 and other cytokines. - Mycophenolate mofetil inhibits inosine monophosphate dehydrogenase, suppressing de novo purine synthesis required for lymphocyte proliferation. - Methotrexate inhibits dihydrofolate reductase, interfering with DNA synthesis and cell replication. The combination aims to reduce the incidence and severity of acute and chronic GVHD while balancing risks such as infection or drug toxicity. This regimen is sometimes referred to as the "Beijing protocol" in certain transplant centers[4][2][3].

Other names
CSA + MMF + MTXcyclosporine A + mycophenolate mofetil + methotrexateciclosporin A + mycophenolate mofetil + methotrexate
02

Targets

DHFR (Dihydrofolate reductase)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)CN (Calcineurin)

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