VRTX153 / Vrise Therap - LARVOL DELTA

VRTX153, Novel Small Molecule Inhibitor of KRASG12D. (AACR-NCI-EORTC 2023) - No abstract available

Oncology • KRAS

Targeting EGFR and PI3K pathways with KRASG12D inhibitor overcomes oncogenic dependence in pancreatic cancer (AACR 2023) - "FOLFIRINOX or gemcitabine plus nab-paclitaxel have been the standard of care for pancreatic cancer, but late stage prognosis often leads to disease progression of disease, with an overall 5 year survival of 11.5%, in the US, and 9% in Japan...Role of EGFR on the other hand in KRAS-dependent pancreatic cancer progression is not well understood, and cetuximab as single agent has not provided benefit in PDAC patients...Here we report a data for 40-point combination dose response matrix combining VRTX153, a novel and highly selective inhibitor of KRASG12D with Alpelisib (a p110α inhibitor) and an EGFR inhibitor using MTT assay. Effect on downstream markers such as pERK, pEGFR and pAKT is being investigated. In vivo pharmacological effect of these agents will be investigated in the due course of development."

Colorectal Cancer • Gastrointestinal Cancer • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor • KRAS • PIK3CA

Vrtx153, novel small molecule inhibitor of krasg12d (AACR 2023) - "VRTX153 inhibited ERK1/2 phosphorylation (pERK) and cell viability in KRASG12D-mutant cell lines in both 2D and 3D, as evaluated by CellTiter-Glo®. In-vivo translation of activity in a mouse xenograft model representing PDAC is being investigated."

Gastrointestinal Cancer • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor • HRAS • KRAS • NRAS