Compounds developed through collaboration with Variational AI show targeted activity
Rakovina Therapeutics Inc. (“Rakovina” or the “Company”) (TSX-V: RKV) (FSE: 7JO0), a biopharmaceutical company advancing next-generation cancer therapies through artificial intelligence (AI)-powered drug discovery, today 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.
“The progress we’re seeing in the KT-5000AI program highlights the advantage of combining artificial intelligence with modern drug design,” said Dr. Mads Daugaard, Rakovina’s President and Chief Scientific Officer. “We’re particularly encouraged by the number of active compounds emerging from the first wave of screening and look forward to advancing the most promising candidates through further evaluation and development.”
ATR inhibitors represent a fast-growing class of oncology therapeutics, with the global ATR inhibitor market valued at approximately US $1.24 billion in 2024, expanding at a compound annual growth rate (CAGR) of nearly 17.8% through 2033, with forecasts projecting a market size of over US $5.1 billion by 2033 (source: Growth Markets Reports). This growth is fueled by increasing validation of ATR as an oncology target, rising need for therapies addressing replication stress and DNA repair–deficient tumors, and a shift toward personalized, AI-enabled drug development. Rakovina’s KT-5000AI series is well-positioned to capture value in this expanding landscape by delivering next-generation compounds with improved selectivity, potency, and therapeutic index.