On January 6, 2025 Rakovina Therapeutics Inc. (TSX-V: RKV), a biopharmaceutical company focused on the development of new cancer therapies based on novel DNA-damage response technologies, reported the successful synthesis of novel small-molecule drug candidates designed under the Company’s artificial intelligence (AI) platform collaboration (Press release, Rakovina Therapeutics, JAN 6, 2025, View Source;utm_medium=rss&utm_campaign=rakovina-therapeutics-announces-receipt-of-ai-derived-drug-candidates-and-advancement-to-preclinical-validation [SID1234649438]).
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The initial batch of compounds have arrived at Rakovina’s state-of-the-art wet-lab facility at the University of British Columbia, where they will undergo rigorous testing for safety and efficacy. Designed to function as PARP1-selective inhibitors capable of crossing the blood-brain barrier (BBB); these candidates may address a critical gap in treating cancers involving the brain, such as BRCA-mutated breast cancer and glioblastoma.
This achievement highlights Rakovina’s commitment to leveraging AI for rapid and efficient identification of novel drug candidates, accelerating the development of promising cancer therapies. Using the Deep Docking AI platform, the Company screened billions of compounds in silico to pinpoint small molecules tailored to meet specific target product profiles. The compounds were designed to demonstrate favorable drug-like properties, including high potential for efficacy, safety, and optimal pharmacokinetic profiles, positioning them as strong contenders for further development.
Revolutionizing Cancer Care Through Innovation
First-generation poly (ADP-ribose) polymerase (PARP) inhibitors have dramatically improved patient outcomes in certain mutated cancers but are limited by side effects and in their utility to treat central nervous system (CNS) malignancies as they cannot readily pass through the blood-brain barrier. The successful development of a PARP-1 selective CNS-penetrant inhibitor could reduce toxicity while providing a new therapeutic option for brain tumors.
"This is a transformative moment for Rakovina Therapeutics," said Prof. Mads Daugaard, Chief Scientific Officer of Rakovina Therapeutics. "The delivery of these AI-designed compounds underscores the extraordinary potential of Artificial Intelligence to reshape drug discovery. By navigating chemical space with unparalleled precision, we can address critical unmet needs in oncology while significantly reducing the risks and timelines of traditional drug development. We are energized by this progress and remain steadfast in our mission to deliver innovative therapies to patients around the globe."
"Indeed, Rakovina’s ability to marry cutting-edge AI with its world-class scientific expertise positions the Company as a leader in the rapidly evolving biopharmaceutical landscape," added Jeff Bacha, Executive Chairman. "By leveraging validated AI to streamline the drug discovery process, Rakovina is not just accelerating timelines but redefining what’s possible in cancer research. The potential market for CNS-penetrant PARP inhibitors is vast, with significant demand for therapies that can address both brain cancers and BRCA-mutated malignancies."
"This achievement builds on the legacy of the Deep Docking AI platform, which has seen incredible success in the drug development space, including a landmark licensing deal with Roche that the platform facilitated in 2015," he added.
The 2015 licensing agreement between Roche and the University of British Columbia (UBC) for a potential treatment for advanced prostate cancer served as a strong validation of Dr. Artem Cherkasov’s AI-driven drug discovery platform. The deal, valued at up to $141.7 million USD with upfront payments, milestone payments, and royalties, underscored the platform’s ability to design clinically relevant drug candidates that address significant unmet medical needs.
Dr. Artem Cherkasov remarked, "With these newly synthesized drug candidates identified and now advancing into testing, Rakovina Therapeutics is delivering on its promise of innovation. This achievement positions the company to lead in addressing some of the most challenging cancers."