VRN16 / Voronoi - LARVOL DELTA

VRN16: A novel PKMYT1 kinase selective inhibitor with wide therapeutic window (AACR 2025) - "In contrast, lunresertib inhibits BRAF kinase, confirmed to cause paradoxical activation of phospho-MEK and phospho-ERK signaling in the cells, similar to the effects observed with vemurafenib, a BRAF inhibitor...Although CDK2 inhibitors are also undergoing clinical trials with CCNE1+ as a major biomarker, VRN16 demonstrated superior efficacy in combination with gemcitabine in the OVCAR3 CDX, compared to the combination of BLU-222, a CDK2 inhibitor, with paclitaxel or carboplatin.In a 2-week repeated-dose oral toxicity study, VRN16 achieved a wide preclinical safety margin, more than 8-fold, compared to lunresertib with a limited safety margin. This wide therapeutic window highlights VRN16 as a novel therapeutic option for patients with CCNE1+ solid tumors or DNA damage sensitive tumors."

Late-breaking abstract • Breast Cancer • Carcinosarcoma • Gastric Cancer • Oncology • Ovarian Cancer • Sarcoma • Solid Tumor • Uterine Cancer • CCNE1 • CDK1 • PKMYT1 • TP53