NRX-4972 / Nurix Therap - LARVOL DELTA

Nurix Therapeutics Presents Positive Preclinical Data at the AACR 2025 Annual Meeting from Multiple Orally Available, Brain Penetrant Degraders Against Three High Value Oncology Targets (GlobeNewswire) - "In an oral presentation titled 'Identification of selective, orally bioavailable Aurora A degraders for treatment of pediatric and adult cancers,' Nurix will highlight preclinical data from studies of NRX-4972, an orally bioavailable and highly selective brain penetrant AURKA degrader. The data demonstrate that daily oral administration of NRX-4972 resulted in downregulation of MYCN as well as induction of DNA damage, apoptosis, and G2/M arrest, the latter set of effects being more pronounced in the context of degradation rather than AURKA inhibitor, which translated into significant efficacy in a model of neuroblastoma."

Preclinical • Neuroblastoma

Identification of selective, orally bioavailable aurora A degraders for treatment of pediatric and adult cancers (AACR 2025) - "Compounds with oral bioavailability and CNS exposure in mice were prioritized for further development.Our lead AURKA degrader, NRX-4972, has 58% oral bioavailability in C57BL/6 mice and moderate clearance (17.5 mL/min/kg)...Analysis of tumors isolated from treated mice revealed that AURKA degraders, but not inhibitors, rapidly induced DNA damage and apoptosis.The differentiated activity of AURKA degraders compared to enzymatic inhibitors in these preclinical studies suggests the potential for improved safety and efficacy in cancer patients. The ability of AURKA degraders to penetrate the CNS not only broadens their therapeutic potential to include pediatric brain cancers such as medulloblastoma but also offers a promising avenue for treating adult cancers with brain metastases, addressing an urgent unmet medical need."

Clinical • Brain Cancer • Breast Cancer • CNS Tumor • Hematological Malignancies • Medulloblastoma • Neuroblastoma • Neuroendocrine Tumor • Oncology • Solid Tumor • AURKB • CDK4 • CRBN • MYCN • RB1