On January 8, 2026 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, reported the expansion of their collaboration focused on the continued optimization of Rakovina’s kt-5000 series of ATR inhibitors.

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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."

(Press release, Rakovina Therapeutics, JAN 8, 2026, View Source [SID1234661858])