BAY 2476568 / Bayer - LARVOL DELTA

Biochemical analysis of EGFR exon20 insertion variants insASV and insSVD and their inhibitor sensitivity. (PubMed, Proc Natl Acad Sci U S A) - "Biochemical, structural, and cellular studies of a diverse panel of EGFR inhibitors revealed that the more recently developed compounds BAY-568, TAS6417, and TAK-788 inhibit EGFR insASV and insSVD in a mutant-selective manner, with BAY-568 being the most potent and selective versus wild-type (WT) EGFR. Cocrystal structures with WT EGFR reveal the binding modes of each of these inhibitors and of poziotinib, a potent but not mutantselective inhibitor, and together they define interactions shared by the mutant-selective agents. Collectively, our results show that these exon20 insertion variants are not inherently inhibitor resistant, rather they differ in their drug sensitivity from WT EGFR. However, they are similar to each other, indicating that a single inhibitor should be effective for several of the diverse exon 20 insertion variants."

EGFR exon 20 • Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Bayer to Present New Clinical Data in Indolent non-Hodgkin’s Lymphoma and Additional Research on its Oncology Portfolio at AACR Annual Meeting 2021 (Businesswire) - “Bayer will also reveal the latest data from its differentiated early pipeline across other focus areas, including precision molecular oncology and immuno-oncology. For the first time, Bayer will be presenting preclinical data on investigational small molecule epidermal growth factor receptor (EGFR) exon 20 inhibitor BAY 2476568…In the area of immuno-oncology, Bayer will showcase preclinical findings on investigational oral small molecule inhibitor BAY-405, which is thought to target the intracellular immune checkpoint MAP4K1 (HPK1), jointly developed in the strategic research alliance with the German Cancer Research Center (DKFZ) in Heidelberg, Germany.”

EGFR exon 20 • Preclinical • Oncology