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Rakovina Therapeutics has been recognized by Life Sciences Review Magazine as the exclusive recipient of “Top 10 Therapeutics Companies in Canada – 2023,” based on our proprietary methodology, reflecting its position in the industry. This profile has been developed by the Life Sciences Review research and editorial team based on insights from an interview with , .

Rakovina Therapeutics
Forerunners in Novel DNA-damage Response (DDR) Technologies

Rakovina Therapeutics

Jeffrey Bacha, Executive Chairman; Mads Daugaard, President, and Chief Scientific Officer; David Hyman, Chief Financial Officer, Rakovina TherapeuticsJeffrey Bacha, Executive Chairman; Mads Daugaard, President, and Chief Scientific Officer; David Hyman, Chief Financial Officer
The first approved DDR-based cancer treatments, poly-ADP-ribose-polymerase (PARP) inhibitors, specifically targeted the DNA damage response in BRCA1/2 mutant breast and ovarian malignancies. Since then, research into the processes that enhance tumors’ sensitivity to PARP inhibitors and their applications in treating various cancer types has grown exponentially. However, there are several drawbacks to the first generation of PARP inhibitors.

One, first-generation PARP inhibitors provide their best results with cancers that have pre-existing flaws in their DNA repair mechanisms. In contrast, tumors that can effectively repair DNA damage show limited or no response. At the same time, an inability to bridge the blood-brain barrier adversely affects their impact on cancer that metastasizes to the central nervous system (CNS). This exemplifies how new treatment approaches that target the DNA-damage repair (DDR) mechanisms and concentrate on PARP inhibitor combinations need more focus.

One company at the forefront of developing new cancer treatments based on novel DNA-damage response (DDR) technologies is Vancouver-based Rakovina Therapeutics Inc. It has a pipeline of novel drug candidates that it is seeking to advance into human clinical trials with the goal of obtaining market approval for new cancer therapeutics from Health Canada, the United States Food and Drug Administration, and other international regulatory agencies.

Rakovina Therapeutics offers three distinct drug series, each with unique properties. The first series, Rakovina Therapeutics’ kt-2000 series is a patented class of highly potent oral inhibitors of PARP that has been designed to have a better capacity to pass the blood-brain barrier.

The Company’s second class of DDR drug candidates, the kt-3000 series are “Dual Action” DDR inhibitors that have been designed to selectively inhibit both PARP and a secondary DDR pathway associated with treatment resistance to PARP inhibitors. Rakovina Therapeutics’ third series is kt- 4000 DNA Damaging DDR inhibitors, which release a potent DNA-damaging agent while inhibiting DDR to selectively kill cancer cells.

Today, Rakovina Therapeutics is seeking to optimize lead compounds from these series in collaboration with the University of British Columbia. The company is targeting cancers with a high risk of CNS metastasis and those which have become resistant to treatment with FDA-approved PARP inhibitors. Rakovina Therapeutics is seeking to optimize each drug series against subsets of major cancers such as ovarian, prostate, pancreatic, and rare cancers such as Ewing sarcoma to identify unique properties that may allow the management of treatment-resistant tumors.

“Rakovina Therapeutics focuses on designing new treatment options that will be pertinent and valuable for patients,” Jeffery Bacha, executive chairman of Rakovina Therapeutics.

Rakovina Therapeutics is currently in the final stages of lead optimization which is being conducted at the University of British Columbia. Rakovina’s robust and collaborative relationship with the University of British Columbia and the Vancouver Prostate Center provides access to stateof- the-art laboratory space and equipment. The collaboration also brings a range of infrastructure and expertise and empowers Rakovina Therapeutics to concentrate on core lead optimization activities.

We focus on the development of novel therapeutics pertinent and valuable for patients

“A major strength of this model is its in-house nature, which gives us direct oversight of all R&D processes and facilitates fine-tuning of potential drug candidates in a timely manner,” Mads Daugaard, president and chief scientific officer of Rakovina Therapeutics.

Utilizing the cutting-edge technology made available through its partnership with the University of British Columbia, Rakovina Therapeutics is positioned for success. Its role in developing impactful treatment options for Ewing sarcoma, a bone and soft tissue cancer with a very high risk of metastasizing, exemplifies its potential. FDA-approved PARP inhibitors only show a modest therapeutic effect on Ewing sarcoma, while their combination with histone deacetylase (HDAC) enzyme inhibitors is constrained by overlapping toxicities and varying pharmacokinetics. Rakovina Therapeutics’ kt-3000 series is part of a new class of bi-functional small-molecule therapeutic candidates that combine inhibition of PARP and HDAC in a single molecule as a practical method of offering patients a real clinical benefit. Advancing a kt-3000 lead candidate into the clinical study will represent a major milestone for the Company.

Rakovina Therapeutics continues to develop new precision medications that target crucial DDR pathway mutations, hallmarks of many cancers, by drawing on the extensive experience of its team in drug discovery research, preclinical and clinical development, and regulatory affairs.

Rakovina Therapeutics News

Rakovina Therapeutics Inc. Announces Plan to Apply to Extend Warrant Expiry Dates

Tuesday, March 14, 2023

VANCOUVER, British Columbia - Rakovina Therapeutics Inc. announces that it may apply to the TSX Venture Exchange (the “TSXV”) to extend the expiry date of 11,414,750 common share purchase warrants (the “Warrants”) issued by the Company. The original term of the Warrants was two years and they currently expire on March 25, 2023. The Company proposes to extend the expiry date by up to 12 months (the “Warrant Extension”). No other terms of the Warrants are to be amended and the exercise price of each Warrant will remain at $0.40. The proposed amendment of the Warrants is subject to TSXV approval. The extension of the Warrants, if any, would only be effective upon TSXV approval and receipt of the requisite confirmation from the holders of the Warrants.
Additional Information
The TSXV has neither approved nor disapproved the content of this press release. Neither the TSXV nor its Regulation Services Provider (as that term is defined in policies of the TSXV) accepts responsibility for the adequacy or accuracy of this release.
Notice regarding 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 medical device 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.

Rakovina Therapeutics and Variational AI Announce Drug Discovery Collaboration

Tuesday, October 01, 2024

Companies will jointly research DNA-damage response kinase targets to identify potential drug candidates for the treatment of cancer
VANCOUVER -
Rakovina Therapeutics Inc. (TSX-V: RKV) a biopharmaceutical company committed to advancing new cancer therapies based on novel DNA-damage response technologies and Variational AI, developer of the Enki™ generative artificial intelligence (AI) platform for drug discovery, announced today a research collaboration aimed at leveraging each company’s expertise to identify and develop novel small-molecule therapies against DNA-damage response (DDR) targets for the treatment of cancer.
Under the terms of the agreement Rakovina Therapeutics has been granted an exclusive right to compounds generated by the Enki™ platform against the selected target product profiles and an option to license validated drug candidates for further development. Variational AI will employ the EnkiTM platform to identify novel inhibitors of specific DDR kinase targets selected by Rakovina Therapeutics. Rakovina Therapeutics will synthesize and evaluate the viability of these drug candidates as potential cancer therapies in its laboratories at the University of British Columbia.
According to Rakovina Therapeutics Executive Chairman Jeffrey Bacha, “This collaboration is an ideal addition to our already established Deep Docking AI partnership as it expands Rakovina Therapeutics’ pipeline beyond our current focus of developing next-generation PARP inhibitors.”
“Leveraging Variational AI’s expertise in kinases where it overlaps with our DDR interest will significantly increase partnering opportunities as ‘big pharma’ maintains a close interest on novel therapies against these targets,” added Bacha.
Rakovina Therapeutics will pay a low upfront fee to initiate work against each selected target and a “TPP Fee” upon exercise of its option to acquire rights to drug candidates meeting a pre-specified target-product profile (TPP) and additional payments upon achievement of specified development milestones. Additional financial terms were not disclosed.
According to Variational AI CEO Handol Kim, “We are thrilled to be partnering with Rakovina Therapeutics in their quest for lifesaving, cancer drugs. Variational AI is at the forefront of Artificial Intelligence drug discovery and we look towards a successful and lasting partnership. Our unique Enki™ Platform is the first commercially accessible foundation model for small molecules and represents an ideal drug discovery solution for Rakovina Therapeutics for these initial targets and beyond.”

Top 10 Therapeutics Companies in Canada – 2023
Current Issue

Company : Rakovina Therapeutics

Management
Jeffrey Bacha, Executive Chairman; Mads Daugaard, President, and Chief Scientific Officer; David Hyman, Chief Financial Officer

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