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Drug intelligence / Profile preview
avutometinib + defactinib + gemcitabine + nab-paclitaxel
- Development stage
- Phase 2
- Lead developer
- Verastem Oncology
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a four-drug combination regimen under investigation for the treatment of metastatic pancreatic ductal adenocarcinoma (PDAC). Avutometinib (also known as VS-6766) is an oral RAF/MEK clamp inhibitor that targets the MAPK pathway. Defactinib is an oral selective focal adhesion kinase (FAK) inhibitor. Gemcitabine is a nucleoside analog used as chemotherapy, and nab-paclitaxel is a nanoparticle albumin-bound formulation of paclitaxel that disrupts microtubule function. The combination aims to exploit synergistic antitumor activity by targeting both tumor cell signaling pathways and cytotoxic mechanisms. This regimen has shown promising preliminary efficacy in first-line metastatic PDAC in early-phase clinical trials[1][4][5][7].
- Other names
- GnP (for gemcitabine and nab-paclitaxel)avutometinib (VS-6766)
02
Targets
DNAFAK (Focal adhesion kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)RNR (Ribonucleotide reductase)TUBB (Tubulin (alpha and beta subunits))DNA polymerase familyRAF1 (c-Raf-1 (Y340D/Y341D))
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