Drug intelligence / Profile preview

enzastaurin + carboplatin + paclitaxel

Development stage
Phase 2
Lead developer
Denovo Biopharma
Modality
Small Molecules
Administration
Oral (enzastaurin), Intravenous (carboplatin), Intravenous (paclitaxel)
01

Overview

This is a combination regimen consisting of **enzastaurin**, **carboplatin**, and **paclitaxel**. - **Enzastaurin** is an oral small molecule **serine/threonine kinase inhibitor** that primarily inhibits **protein kinase C beta (PKCβ)**, with antiangiogenic and pro-apoptotic effects[3][1]. - **Carboplatin** is a platinum-based cytotoxic **alkylating agent** that induces DNA crosslinking, resulting in apoptosis of cancer cells[1][3]. - **Paclitaxel** is a cytotoxic **antimicrotubule agent** that stabilizes microtubules, preventing cell division and causing cell death[1][3]. This combination has been studied as first-line therapy and maintenance regimen for **advanced ovarian cancer** and **primary peritoneal carcinoma**, aiming to improve progression-free survival compared to standard chemotherapy. The combination is given with paclitaxel and carboplatin administered intravenously, and enzastaurin given orally. Studies indicate that the safety profile is manageable and pharmacokinetics are not significantly altered by co-administration[3][1]. However, in randomized phase II trials, the addition of enzastaurin did not significantly improve progression-free survival compared to standard chemotherapy[3][5].

02

Targets

DNAPKC (Protein kinase C family)PRKCB (Protein kinase C beta)TUBB (Tubulin (alpha and beta subunits))

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