Drug intelligence / Profile preview

RO4929097 + carboplatin + paclitaxel

Development stage
Phase 1
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

RO4929097 + carboplatin + paclitaxel is an investigational combination regimen composed of three agents: - **RO4929097** is a potent and selective small-molecule inhibitor of gamma secretase, an enzyme complex that mediates activation of Notch receptors. By inhibiting gamma secretase, RO4929097 blocks Notch signaling—a pathway implicated in tumor cell proliferation and maintenance of cancer stem cells—leading to reduced tumor growth and increased differentiation[1][3][4][8]. - **Carboplatin** is a platinum-based chemotherapeutic agent that induces DNA crosslinking and damage, resulting in apoptosis of rapidly dividing cells[10]. - **Paclitaxel** (Taxol) is a microtubule-stabilizing agent that inhibits mitosis by preventing microtubule depolymerization during cell division[10]. This combination leverages the targeted inhibition of the Notch pathway with cytotoxic chemotherapy to enhance antitumor effects. The regimen has been explored in early-phase clinical trials for various solid tumors.

Other names
gamma-secretase inhibitor RO4929097carboplatinpaclitaxel
02

Targets

DNAGSEC (Gamma-Secretase Complex)NOTCH (Neurogenic locus notch homolog protein 3)TUBB (Tubulin (alpha and beta subunits))

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