Drug intelligence / Profile preview

sotrastaurin + tacrolimus

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

Overview

Sotrastaurin + tacrolimus is a combination of two immunosuppressive drugs used primarily in the context of organ transplantation to prevent acute rejection. Sotrastaurin is a novel small molecule inhibitor of protein kinase C, which blocks early T cell activation and reduces cytokine production such as interleukin-2 and tumor necrosis factor. Tacrolimus is a calcineurin inhibitor that suppresses immune responses by inhibiting T-cell activation through blocking interleukin-2 transcription. The combination has been studied in clinical trials for kidney and liver transplantation, showing potentially enhanced immunosuppressive activity but also pharmacokinetic interactions—sotrastaurin increases tacrolimus exposure, requiring dose adjustments. Both agents are administered under close medical supervision due to risks including infection and malignancy[1][4][5][6].

Brand names
Prograf (tacrolimus)
Other names
sotrastaurin + tacrolimus
02

Targets

FKBP1APRKCA (Protein kinase C alpha)PRKCB (Protein kinase C beta)PRKCQ (Protein kinase C theta)CN (Calcineurin)

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