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Primary Target

Protein kinase C theta

2

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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Investigational

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Highest Phase

Phase II

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Approval Year

Unknown

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Condition

Diffuse large B-cell lymphoma

2

Uveal melanoma

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Treatment Modality

Primary

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CNS Activity

CNS Non-penetrant

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Originator

Novartis|Ohio State University

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Chemical

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CAS

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ChEMBL

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DRUG BANK

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EVMPD

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FDA UNII

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SOTRASTAURIN

7I279E1NZ8

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Protein kinase C eta

Protein kinase C theta

Protein kinase C delta

Protein kinase C beta

Protein kinase C alpha

Conditions:

Diffuse large B-cell lymphoma

Sotrastaurin, an orally-active, first-in-class immunomodulator, is under development by Novartis for the treatment of uveal melanoma and diffuse-large B-cell lymphoma. Sotrastaurin is a low molecular mass synthetic compound that potently inhibits the...

PKC α, β and the θ isoforms resulting in selective NF-κB inactivation. Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay. Inhibition of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act synergistically with other chemotherapeutic agents. PKC, a family of serine/threonine protein kinases overexpressed in certain types of cancer cells, is involved in cell differentiation, mitogenesis, inflammation, and the activation and survival of lymphocytes. Sotrastaurin is currently in phase II trials by Novartis for the treatment of large B-cell lymphoma and uveal melanoma. Sotrastaurin was in Phase II of clinical development for the prevention of acute rejection after solid organ transplantation and psoriasis, but this reseach had being discontinued.

SOTRASTAURIN ACETATE

R1SIA15KZ1

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Search for Structure

Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Protein kinase C eta

Protein kinase C theta

Protein kinase C delta

Protein kinase C beta

Protein kinase C alpha

Conditions:

Diffuse large B-cell lymphoma

Sotrastaurin, an orally-active, first-in-class immunomodulator, is under development by Novartis for the treatment of uveal melanoma and diffuse-large B-cell lymphoma. Sotrastaurin is a low molecular mass synthetic compound that potently inhibits the...

PKC α, β and the θ isoforms resulting in selective NF-κB inactivation. Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay. Inhibition of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act synergistically with other chemotherapeutic agents. PKC, a family of serine/threonine protein kinases overexpressed in certain types of cancer cells, is involved in cell differentiation, mitogenesis, inflammation, and the activation and survival of lymphocytes. Sotrastaurin is currently in phase II trials by Novartis for the treatment of large B-cell lymphoma and uveal melanoma. Sotrastaurin was in Phase II of clinical development for the prevention of acute rejection after solid organ transplantation and psoriasis, but this reseach had being discontinued.

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