Drug intelligence / Profile preview

defactinib + paclitaxel

Development stage
Phase 1
Lead developer
Verastem Oncology
Modality
Small Molecules
Administration
Oral (defactinib), Intravenous (paclitaxel)
01

Overview

Defactinib + paclitaxel is a combination therapy of **defactinib**, an oral small molecule inhibitor of focal adhesion kinase (FAK), and **paclitaxel**, a microtubule-stabilizing chemotherapeutic agent. Defactinib inhibits FAK, a kinase that supports tumor cell survival, proliferation, invasion, and angiogenesis, and reduces cancer stem cell populations. Paclitaxel binds β-tubulin and stabilizes microtubule polymerization, impairing cell division and cytoskeleton organization. Preclinical studies and early-phase clinical trials have demonstrated that the combination acts synergistically, with defactinib increasing intracellular drug availability and enhancing paclitaxel’s cytotoxic effects through increased microtubule polymerization and reduced cell division. The combination has shown promising activity and tolerability in advanced solid tumors, particularly ovarian cancer and pancreatic ductal adenocarcinoma[1][3].

Other names
defactinibPTXdefactinib + PTX
02

Targets

FAK (Focal adhesion kinase)PTK2BTUBB (Tubulin (alpha and beta subunits))

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