Rakovina Therapeutics Showcases Potent AI-Developed ATR Inhibitors with CNS Penetrance at AACR-NCI-EORTC International Conference

Core Insights - Rakovina Therapeutics presented new data on its AI-driven kt-5000AI drug discovery program for ATR inhibitors at the AACR-NCI-EORTC conference, highlighting promising results for cancer therapy targeting CNS penetration [1][2][3] Company Developments - The collaboration with Variational AI utilized the Enki™ generative AI platform to identify novel small-molecule candidates for CNS-penetrant ATR inhibition, with multiple lead compounds achieving the desired profile [2][3] - Rakovina's kt-5000AI program is advancing next-generation ATR inhibitors that have confirmed CNS exposure, potentially benefiting patients with primary brain tumors and brain metastases [3][5] - The company aims to advance one or more drug candidates into human clinical trials in collaboration with pharmaceutical partners [6] Scientific Findings - In cell-based assays, lead compounds demonstrated over 50% inhibition of ATR activity below 200 nM, with potency exceeding reference compounds such as ceralasertib, tuvusertib, and elimusertib [7] - In vivo pharmacokinetic studies showed measurable drug concentrations in plasma and brain tissue after intraperitoneal dosing at 5 mg/kg, indicating CNS penetration and good tolerability after single-dose administration [7]