Rakovina Therapeutics and Variational AI Expand Collaboration to Advance Next-Generation ATR Inhibitors

Rakovina Therapeutics Inc. (TSX-V: RKV) (FSE: 7JO0) ("Rakovina"), a biopharmaceutical company advancing innovative cancer therapies through AI-powered drug discovery and Variational AI, a leader in generative artificial intelligence for small-molecule design, today announced the expansion of their collaboration focused on the continued optimization of Rakovina's kt-5000 series of ATR inhibitors.

Building on their existing collaboration, the companies have signed a new agreement to focus on lead optimization of drug candidates identified by Variational AI's Enki™ generative AI platform and selected by Rakovina for further evaluation in the kt-5000 ATR inhibitor program. Under the expanded scope of work, Variational AI will apply its generative AI platform to iteratively optimize the initial leads with the goal of identifying a clinical candidate in months versus the industry standard of years.

Variational AI will generate and prioritize multiple optimized compound designs, while Rakovina will retain full control over which candidates to advance into laboratory testing and further development. The expanded collaboration is intended to accelerate the identification of high-quality development candidates while reducing the time and cost typically required in early-stage drug discovery.

Rakovina's kt-5000 program comprises a series of small-molecule inhibitors targeting ATR (ataxia telangiectasia and Rad3-related), a central regulator of the DNA damage response that enables cancer cells to survive replication stress and DNA damage. ATR inhibition has emerged among big pharma companies as a promising therapeutic strategy in solid tumors, including cancers with DNA repair deficiencies such as ovarian, breast, and prostate cancer.

Rakovina recently reported results from the kt-5000 series, including compounds with dual ATR/mTOR activity and designed to achieve central nervous system (CNS) penetration at the Society for NeuroOncology annual meeting. These preclinical findings highlight efforts to address known limitations of existing ATR inhibitors and support continued optimization of the compounds.

"ATR is a proven oncology target, but real differentiation comes from optimizing the drug itself," said Jeffrey Bacha, executive chairman of Rakovina Therapeutics. "This expanded collaboration with Variational AI enables a highly focused, AI-driven refinement of kt-5000 compounds identified for further evaluation, with particular attention to potency, selectivity, and CNS penetration. The result is a more efficient path to identifying high-quality candidates while maintaining strategic flexibility for development and partnering."

"Our Enki™ generative AI platform efficiently explores novel chemical space and has already generated promising leads for Rakovina," said Handol Kim, Co-Founder and CEO of Variational AI. "With this expanded collaboration, we are now applying Enki™ to exploit these novel leads through local chemical search to efficiently perform lead optimization and enable Rakovina to get to human trials faster."

About Variational AI
Variational AI is a generative AI drug discovery company redefining the unit economics of small-molecule drug discovery and development. Based in Vancouver, Canada, Variational AI has developed Enki™, a proprietary generative AI foundation model that designs novel, optimized small-molecule drug candidates with improved potency, selectivity, and synthesizability to help partners accelerate early discovery and lead optimization. The company's multidisciplinary team of machine learning and drug discovery experts aims to transform how transformative therapeutics are discovered by leveraging state-of-the-art generative AI. For more information, please visit www.variational.ai

About Rakovina Therapeutics Inc.
Rakovina Therapeutics is a biopharmaceutical research company focused on the development of innovative cancer treatments. Our work is based on unique technologies for targeting the DNA-damage response powered by Artificial Intelligence (AI) using the proprietary Deep-Docking™ and Enki™ platforms. By using AI, we can review and optimize drug candidates at a much greater pace than ever before.

The Company has established a pipeline of distinctive DNA-damage response inhibitors with the goal of advancing one or more drug candidates into human clinical trials in collaboration with pharmaceutical partners. Further information may be found at www.rakovinatherapeutics.com.

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