Drug intelligence / Profile preview

sotrastaurin + everolimus

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

Overview

AEB071 (sotrastaurin) is an oral small molecule inhibitor of protein kinase C (PKC), developed primarily as an immunosuppressant and for potential use in oncology. Everolimus is an oral mTOR inhibitor used to treat various cancers and to prevent organ transplant rejection. The combination of AEB071 (sotrastaurin) and everolimus has been investigated in preclinical models and early-phase clinical trials for synergistic immunosuppression and anti-tumor activity. Sotrastaurin blocks T-cell activation by inhibiting PKC signaling pathways[2][5][6], while everolimus inhibits the mechanistic target of rapamycin (mTOR), thereby interfering with cell proliferation, angiogenesis, metabolism, and immune responses[4][8]. This combination has shown promise in prolonging allograft survival in transplantation models[2][5] and is being studied for certain lymphomas such as CD79-mutant or ABC diffuse large B-cell lymphoma[3].

Brand names
AfinitorAfinitor DisperzZortress
Other names
sotrastaurin + everolimusAEB071 + everolimus
02

Targets

PRKCB (Protein kinase C beta)PRKCA (Protein kinase C alpha)FKBP1APRKCQ (Protein kinase C theta)PRKCD (Protein kinase C delta)Mechanistic target of rapamycin complex 1

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