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

VANCOUVER, British Columbia, Oct. 27, 2025 (GLOBE NEWSWIRE) -- Rakovina Therapeutics Inc. ("Rakovina" or the "Company") (TSXV:RKV)(FSE: 7JO0) is pleased to announce the successful presentation of new data at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, held October 23–27 in Boston, Massachusetts. The Company's poster, titled "Novel ATR inhibitors with CNS penetrance developed by artificial intelligence," highlights promising results from its AI-driven kt-5000AI drug discovery program for Ataxia telangiectasia and Rad3-related protein serine/threonine kinase (ATR) inhibitors for cancer therapy.Through its collaboration with Variational AI, Rakovina Therapeutics utilized the EnkiTM generative AI platform to identify novel small-molecule candidates predicted to meet a defined target product profile for CNS-penetrant ATR inhibition. Data presented at the conference confirm that multiple lead compounds achieved this profile, demonstrating potent ATR inhibition together with clear evidence of central nervous system exposure.While multiple ATR inhibitors are in development globally, none have yet demonstrated meaningful central nervous system penetration. Rakovina's kt-5000AI program is advancing next-generation, AI-designed ATR inhibitors with confirmed CNS exposure, potentially extending the benefits of ATR-targeted therapy to patients with primary brain tumors and brain metastases, where effective treatments remain limited.In cell-based assays, multiple compounds demonstrated:>50% inhibition of ATR activity below 200 nM;potency exceeding reference compounds such as ceralasertib, tuvusertib, and elimusertib;equal selectivity across the PIKK kinase family compared to reference compounds; andmetabolic stability following incubation with human liver microsomesIn in vivo pharmacokinetic studies, lead compounds demonstrated:measurable drug concentrations in both plasma and brain tissue following intraperitoneal dosing at 5 mg/kg, indicating CNS penetration; andgood tolerability after single-dose administration, supporting continued optimization and preclinical development"Presenting at ...Full story available on Benzinga.com