On November 25, 2024 Rakovina Therapeutics Inc. (TSX-V: RKV) ("Rakovina" or the "Company"), a biopharmaceutical company committed to advancing new cancer therapies based on novel DNA-damage response targeting technologies, reported the presentation of a poster showcasing initial results of its Deep Docking Artificial Intelligence (AI) drug discovery screening at the 29th Annual Meeting and Education Day of the Society for Neuro-Oncology (SNO), which was held November 21-24 in Houston, TX (Press release, Rakovina Therapeutics, NOV 25, 2024, View Source;utm_medium=rss&utm_campaign=rakovina-therapeutics-presents-ai-driven-drug-discovery-research-at-society-for-neuro-oncology-annual-meeting [SID1234648617]).
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The poster, titled "Utilizing Artificial Intelligence for the Discovery of Novel PARP1-Selective Inhibitors for Use Against Brain Tumors," highlighted a rapid virtual multi-billion compound screen to identify selective inhibitors of PARP-1, a key enzyme involved in DNA repair that plays a critical role in brain cancer progression. Inhibition of PARP-1 has shown promise in sensitizing cancer cells to treatment.
The poster provided insight into the compounds’ chemical properties affecting absorption, stability, and the ability to cross the blood-brain barrier. The poster also profiled candidates that are predicted to have similar or improved PARP-1 selectivity and central nervous system (CNS) exposure compared with AZD9574, a novel development-stage blood-brain barrier penetrant and selective inhibitor of PARP-1.
"Our team reached a significant milestone this fall with the initial results of our Deep Docking AI screening efforts, successfully evaluating billions of molecular structures within the projected timeframe described at the outset of the collaboration," said Jeffrey Bacha, Executive Chairman of Rakovina Therapeutics. "We were thrilled to present these preliminary findings to leading brain cancer researchers, clinicians, and potential pharmaceutical partners at the prestigious SNO conference. Our poster highlighted the transformative power of AI in accelerating the discovery of potential best-in-class drug candidates."
"Our innovative approach is not only improving the efficiency of drug discovery, but it is also enhancing the specificity and efficacy of potential therapeutics. Our novel class of PARP-1 selective inhibitors can offer hope for more effective treatments in the fight against primary brain tumors and cancers that have metastasized to the brain," he added. "The next step is to select a lead candidate molecule based on wet lab validation for target selectivity, metabolic and pharmacokinetic parameters, CNS penetration, and activity against cancer."
First-generation poly (ADP-ribose) polymerase (PARP) inhibitors have dramatically improved patient outcomes in certain mutated cancers but are limited in their utility to treat brain malignancies as they cannot pass through the blood-brain barrier. They also have adverse side effects that are possibly driven by the collateral inhibition of PARP-2. The successful development of a PARP-1 selective CNS penetrant inhibitor could reduce toxicity while providing a new therapeutic option for brain tumors.
Upcoming Video Conference Call
Rakovina Therapeutics will host a video conference call on Wednesday, November 27, 2024, at 10 am PST to further discuss the data presented at the Society for Neuro-Oncology Annual Meeting and discuss next steps and upcoming milestones in the PARP inhibitor and other development programs.
Register for the webinar or access the live stream here:
About the Society for Neuro-Oncology (SNO) Annual Meeting
The SNO Annual Meeting is the premier global event in neuro-oncology, bringing together over 2,600 researchers, clinicians, and scientists from more than 40 countries to advance the field of neuro-oncology. This influential conference features leading experts in oncology, providing a platform for the latest research, treatments, and innovations. The 2024 meeting took place at the George R. Brown Convention Center in Houston, Texas, from November 21-24. For more information, visit: View Source