kt-5000AI / Rakovina Therap - LARVOL DELTA

Rakovina Therapeutics Showcases Potent AI-Developed ATR Inhibitors with CNS Penetrance at AACR-NCI-EORTC International Conference (GlobeNewswire) - "The Company’s poster...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....In cell-based assays, multiple compounds demonstrated: >50% inhibition of ATR activity below 200 nM....In 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..."

Preclinical • Brain Cancer • CNS Tumor

Rakovina Therapeutics to Present New Data Highlighting Novel ATR Inhibitor with CNS Penetration at the AACR-NCI-EORTC International Conference (GlobeNewswire) - "Rakovina’s presentation will highlight the Company’s ATR inhibitor program developed in collaboration with Variational AI and their Enki generative AI platform....Data on the potency, selectivity, CNS penetrance and metabolic stability of select inhibitors will be presented and members of the team will be available for discussion with potential collaborators."

Preclinical • Brain Cancer • CNS Tumor

Rakovina Therapeutics KT-5000AI Program Yields Potent ATR Inhibitor Hits in Early Screening (GlobeNewswire) - "Rakovina Therapeutics...announced meaningful progress in its AI-driven KT-5000AI program, advancing the development of precision ATR (Ataxia Telangiectasia and Rad3-related) inhibitors designed to disrupt the DNA Damage Response pathway in cancer cells. Through its collaboration with Variational AI, Rakovina Therapeutics evaluated a vast chemical space of potential molecular structures using artificial intelligence to identify novel compounds designed to selectively inhibit ATR. A subset of these AI-generated candidates has been synthesized and has advanced through initial biological screening, with multiple compounds demonstrating potent ATR inhibition in nanomolar concentration range. The most promising candidates are being prioritized for further characterization and potential development."

Pipeline update • Solid Tumor