On January 13, 2025 Rakovina Therapeutics Inc. (TSX-V: RKV), a biopharmaceutical company dedicated to advancing new cancer therapies based on novel DNA-damage response technologies, reported the successful achievement of a shortlist of AI-generated molecules targeting ATR (Ataxia Telangiectasia and Rad3-related protein) with specific designs for central nervous system (CNS) penetration (Press release, Rakovina Therapeutics, JAN 13, 2025, View Source;utm_medium=rss&utm_campaign=rakovina-therapeutics-announces-key-milestone-in-cancer-drug-innovation-in-collaboration-with-variational-ai [SID1234649672]).
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This milestone represents the first significant deliverable in Rakovina’s partnership with Variational AI, which leverages their state-of-the-art Enki platform to fast-track the discovery of innovative inhibitors for specific DNA damage response (DDR) kinase targets. ATR is an important drug target due its critical involvement in the DNA damage response (DDR). Its inhibition can lead to selective cancer cell death and improved therapeutic outcomes when combined with other treatments.
These new ATR-targeted inhibitors will now advance to chemical synthesis followed by preclinical validation, a critical step in Rakovina’s mission to address unmet medical needs in oncology.
Innovative Approach to Drug Discovery
The shortlisted molecules were developed using Variational AI’s proprietary Enki foundation model platform to generate novel chemical compounds from the estimated 1060 molecules in chemical space, far greater than any screening library. The platform identifies promising drug candidates while reducing timelines from years to just months. With CNS penetration capabilities, these molecules are poised to address cancers that metastasize to the brain or originate within the CNS, areas with historically limited treatment options.
This achievement is just the beginning of a dynamic journey. Rakovina is broadening its research scope with Variational AI to target additional DDR kinase pathways, with the vision of building a comprehensive pipeline of next-generation small-molecule therapies. By leveraging generative AI, the Company can eliminate traditional barriers, promising a new era of faster, more precise cancer treatment development.
"We are pleased to announce the achievement of this first milestone in our collaboration with Variational AI," said Jeffrey Bacha, Executive Chairman of Rakovina Therapeutics. "The identification of ATR-targeted drug candidates with CNS penetration exemplifies the transformative potential of AI in cancer therapy. This progress represents a meaningful step forward in our research and demonstrates the growing impact of AI in accelerating drug development and innovation in oncology."