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Rakovina Therapeutics Inc. ("Rakovina" or the "Company") (TSX-V: RKV)(FSE: 7JO0) is pleased to announce the successful presentation of new data at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, held October 23–27 in Boston, Massachusetts. The Company's poster, titled "Novel ATR inhibitors with CNS penetrance developed by artificial intelligence," highlights promising results from its AI-driven kt-5000AI drug discovery program for Ataxia telangiectasia and Rad3-related protein serinethreonine kinase (ATR) inhibitors for cancer therapy.
Through its collaboration with Variational AI, Rakovina Therapeutics utilized the Enki™ generative AI platform to identify novel small-molecule candidates predicted to meet a defined target product profile for CNS-penetrant ATR inhibition. Data presented at the conference confirm that multiple lead compounds achieved this profile, demonstrating potent ATR inhibition together with clear evidence of central nervous system exposure.
While multiple ATR inhibitors are in development globally, none have yet demonstrated meaningful central nervous system penetration. Rakovina's kt-5000AI program is advancing next-generation, AI-designed ATR inhibitors with confirmed CNS exposure, potentially extending the benefits of ATR-targeted therapy to patients with primary brain tumors and brain metastases, where effective treatments remain limited.
In cell-based assays, multiple compounds demonstrated:
- >50% inhibition of ATR activity below 200 nM;
- potency exceeding reference compounds such as ceralasertib, tuvusertib, and elimusertib;
- equal selectivity across the PIKK kinase family compared to reference compounds; and
- metabolic stability following incubation with human liver microsomes
In in vivo pharmacokinetic studies, lead compounds demonstrated:
- measurable drug concentrations in both plasma and brain tissue following intraperitoneal dosing at 5 mg/kg, indicating CNS penetration; and
- good tolerability after single-dose administration, supporting continued optimization and preclinical development
"Presenting at AACR-NCI-EORTC is an opportunity to highlight Rakovina's progress in translating AI-discovered compounds into preclinical validation to the scientific community," said Prof. Mads Daugaard, President and Chief Scientific Officer of Rakovina Therapeutics. "ATR is a central regulator of DNA damage repair and a validated target across multiple tumor types. Developing ATR inhibitors capable of penetrating the blood–brain-barrier could expand treatment options for patients with primary brain tumors and brain metastases, areas where few effective therapies exist."
About the AACR-NCI-EORTC 1
Hosted by the American Association for Cancer Research, the National Cancer Institute, and the European Organisation for Research and Treatment of Cancer, the 2025 Molecular Targets and Cancer Therapeutics conference attracts academics, scientists, regulatory agency staff, investors, and biotech and pharmaceutical industry representatives from across the globe to discuss innovations in drug development, target selection, the impact of new discoveries in cellular and molecular biology, and early clinical trials. For more information, please visit: https://www.aacr.org/meeting/aacr-nci-eortc-international-conference-on-molecular-targets-and-cancer-therapeutics-2025/
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 .
Neither TSX Venture Exchange nor its Regulation Services Provider (as that term is defined in the policies of the TSXV) accepts responsibility for the adequacy or accuracy of this release.
Notice Regarding Rakovina Therapeutics Forward-Looking Statements:
This release includes forward-looking statements regarding the company and its respective business, which may include, but is not limited to, statements with respect to the proposed business plan of the company and other statements. Often, but not always, forward-looking statements can be identified by the use of words such as "plans," "is expected," "expects," "scheduled," "intends," "contemplates," "anticipates," "believes," "proposes" or variations (including negative variations) of such words and phrases, or state that certain actions, events, or results "may," "could," "would," "might," or "will" be taken, occur, or be achieved. Such statements are based on the current expectations of the management of the company. The forward-looking events and circumstances discussed in this release may not occur by certain specified dates or at all and could differ materially as a result of known and unknown risk factors and uncertainties affecting the company, including risks regarding the biopharmaceutical industry, economic factors, regulatory factors, the equity markets generally, and risks associated with growth and competition.
Although the company has attempted to identify important factors that could cause actual actions, events, or results to differ materially from those described in forward-looking statements, there may be other factors that cause actions, events, or results to differ from those anticipated, estimated, or intended. No forward-looking statement can be guaranteed. Except as required by applicable securities laws, forward-looking statements speak only as of the date on which they are made, and the company undertakes no obligation to publicly update or revise any forward-looking statement, whether as a result of new information, future events, or otherwise. The reader is referred to the company's most recent filings on SEDAR+ for a more complete discussion of all applicable risk factors and their potential effects, copies of which may be accessed through the company's profile page at www.sedar.com.
For Further Information Contact:
Michelle Seltenrich, BSc MBA
Director, Corporate Development
IR@rakovinatherapeutics.com
778-773-5432
1 AACR (American Association for Cancer Research) https://www.aacr.org/meeting/aacr-nci-eortc-international-conference-on-molecular-targets-and-cancer-therapeutics-2025/, accessed October 13, 2025
