Drug intelligence / Profile preview

enzastaurin + bevacizumab + paclitaxel

Development stage
Preclinical
Lead developer
Denovo Biopharma
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a **combination regimen** of three agents used in oncology clinical trials: - **Enzastaurin** is an orally available serine/threonine protein kinase inhibitor targeting primarily **protein kinase C beta** and the **PI3K/AKT pathway**; it is known to suppress tumor cell proliferation, induce apoptosis, and inhibit tumor angiogenesis[1][2][5]. - **Bevacizumab** is a humanized monoclonal antibody against **vascular endothelial growth factor A (VEGF-A)**, preventing angiogenesis necessary for tumor growth[2][4]. - **Paclitaxel** is a microtubule stabilizing agent (a taxane) that inhibits mitosis. This triple combination is **investigational**. Enzastaurin has been studied with bevacizumab (without paclitaxel) in advanced and recurrent glioma and ovarian cancer, where the combination was found to be well tolerated but did not demonstrate additional benefit over bevacizumab alone[2][4]. The three-drug combination with paclitaxel has been considered or evaluated in various advanced solid tumors, but robust published data on this precise triplet are limited.

02

Targets

PRKCB (Protein kinase C beta)VEGFA (Vascular endothelial growth factor A)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)TUBB (Tubulin (alpha and beta subunits))

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