Drug intelligence / Profile preview

VS-7375 + gemcitabine + nab-paclitaxel

Development stage
Phase 2
Lead developer
GenFleet Therapeutics
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous, Oral
01

Overview

VS-7375 + gemcitabine + nab-paclitaxel is an investigational combination regimen consisting of the oral KRAS G12D inhibitor VS-7375 (GFH375) and the standard-of-care chemotherapy backbone gemcitabine and nab-paclitaxel (GnP). VS-7375 is a potent, selective, non-covalent small-molecule inhibitor that targets both the active (ON) and inactive (OFF) states of the KRAS G12D mutant protein. Gemcitabine is a nucleoside analog that inhibits DNA synthesis, while nab-paclitaxel is an albumin-bound formulation of paclitaxel that stabilizes microtubules to arrest cell division. The combination is being developed by Verastem Oncology (outside of China) and GenFleet Therapeutics (in China) for the treatment of KRAS G12D-mutated solid tumors, primarily pancreatic ductal adenocarcinoma (PDAC). It is being evaluated in the Phase 1/2 TARGET-D 101 trial and the Phase 3 TARGET-D 301 trial as a first-line treatment for metastatic PDAC.

Other names
GFH375 + gemcitabine + nab-paclitaxelGFH375 + gemcitabine/nab-paclitaxelGFH375 + GnPGFH375 plus gemcitabine and nab-paclitaxelGFH-375 plus gemcitabine and nab-paclitaxelGFH 375 plus gemcitabine and nab-paclitaxelVS-7375 + gemcitabine/nab-paclitaxelVS-7375 + GnPVS-7375 plus gemcitabine and nab-paclitaxelVS7375 plus gemcitabine and nab-paclitaxelVS 7375 plus gemcitabine and nab-paclitaxel
02

Targets

DNAKRAS (Kirsten rat sarcoma viral oncogene homolog)RNR (Ribonucleotide reductase)TUBB (Tubulin (alpha and beta subunits))

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