PX-866 + vemurafenib

PX-866 + vemurafenib is a combination therapy evaluated primarily in advanced solid tumors harboring BRAF V600 mutations, notably melanoma. PX-866 is an orally available, irreversible pan-isoform inhibitor of phosphatidylinositol 3-kinase (PI3K), while vemurafenib is a BRAF kinase inhibitor targeting the BRAF V600 mutation. The combination is designed to simultaneously inhibit both the PI3K/AKT/mTOR pathway, which is associated with tumor growth and resistance mechanisms, and the BRAF-driven MAPK signaling pathway. This dual inhibition strategy aims to prevent or overcome resistance seen with monotherapy. Clinical studies have shown the combination is tolerated at the maximum single-agent dose of PX-866 with a reduced dose of vemurafenib. The antitumor activity may be higher in patients with PTEN loss. The main developer for PX-866 is Oncothyreon. Vemurafenib (Zelboraf) was developed by Roche/Genentech. The combination has been tested in phase I clinical trials, with preliminary antitumor efficacy and biomarker exploration[1][3][4][5].

Other names

PX-866 + Zelboraf