How Rakovina Therapeutics is Integrating AI to Break Cancer’s Codes

• The addressable global market for new cancer therapies based on DNA-damage response inhibitors (DDRi) is projected to grow to US$18 billion by the year 2030
• Rakovina Therapeutics’ proprietary use of a leading AI technology can deliver up to a 100-fold acceleration of virtual screening and a 6,000-fold enrichment of favorable candidate drug molecules in the final dataset
• This approach could reduce compound screening and validation stages by years, save millions in development costs, and advance the most promising drug candidates into human clinical trials faster than ever before

Decoding an Enigma

‘Machine Intelligence’ was a phrase first coined by English mathematician Alan Turing in 1950, to describe his computer science theories of a thinking machine with the capacity to learn. This was the beginning of what we know as Artificial Intelligence, or AI, today.

During the war years, Turing applied his generational genius to refine the ‘Bombe’, an electro-mechanical machine that could scramble immense numbers of code keys at a staggering pace, far beyond any human capacity. This led to the decoding of Germany’s Enigma-enciphered messages, shortening WWII and helping assure an Allied victory.

Today, Canadian drug development company Rakovina Therapeutics Inc. (TSXV: RKV) is using advanced AI technology to help decode another menacing enigma—cancer. By harnessing powerful algorithms to screen billions of molecular structures at blinding speeds, and validating new DDRi drug candidates in its world-class wet labs at the University of British Columbia, the company is ushering in a new era of precision drug discovery and lead optimization.

AI is a tool that can level the playing field for us versus other competing companies, decrease the risk that we are not going to find the molecule we are looking for, and drive incredible cost reduction and speed.

—  Jeffrey Bacha, co-founder & Executive Chairman, Rakovina Therapeutics

Breaking with Tradition – The AI Advantage

Traditional drug development can take 12-14 years from investigative start to market launch. The average cost of developing a new cancer medicine is approximately USD $3 billion, with 90 percent of candidates failing to advance through human clinical trials. Yet, big pharma investments continue to be robust.

Rakovina Therapeutics is purposing AI to reduce the traditional preclinical drug development process by years, shrink its associated costs by millions, and better mitigate clinical trial risks through superior predictive modeling of new drug candidates.

The company’s Co-founder and Executive Chairman, Jeffrey Bacha, believes Rakovina Therapeutics is well-positioned to attract the interest of a big pharma partner, because he knows they are looking for exactly what Rakovina Therapeutics is in the process of realizing.

“We have seen multiple deals now where preclinical DDRi drug candidates that have been validated in a pre-clinical laboratory setting, but never tested on people, are being licensed for a billion plus dollars in value, with cash up front payments in excess of a 100 million dollars to secure access to the rights of those molecules,” says Bacha, who believes Rakovina Therapeutics’ innovations and advancements make the company an even more attractive partner.

Merck, Roche, and Novartis were the pharmaceutical giants involved in these licensing and collaboration agreements with three drug development companies in the DDRi therapeutics space, namely Hengrui, Repare Therapeutics, and Artios respectively. However, none had the odds-improving advantage of AI driven drug discovery and lead optimization, and would have spent years in the lab burning through millions of dollars to get to their lead molecules.

“AI is a tool that can level the playing field for us versus other competing companies, decrease the risk that we are not going to find the molecule we are looking for, and drive incredible cost reduction and speed,” Bacha stated.

The Deep DockingTM AI Platform that Rakovina Therapeutics has exclusive access to for its DDRi research applications, is a computational modeling technique created by Dr. Artem Cherkasov, PhD, a Professor at UBC and Senior Scientist at the Vancouver Prostate Centre. His platform was used to quickly identify potential COVID-19 therapeutics in early 2021 by screening 1.4 billion candidates in 3.5 weeks, which in-part led to emergency authorization that same year in December for the lifesaving anti-viral drug Paxlovid.

According to Bacha, who has 25 years in the health sector including with NASDAQ listed companies, Dr. Cherkasov’s deep learning platform is among the most advanced in the world, and has the additional advantage of being directed by a man who is both an expert in AI as well as a medicinal chemist.

“The odds of success are different, but in both cases, you are looking for a needle in the haystack, looking for that one molecule that hits the right target, looking for that metabolic profile that allows it to hang around the body long enough to deal with the tumor,” Bacha added.

But with Deep DockingTM, Bacha thinks the likelihood of success will be higher because the company is looking at the entire haystack instead of just a corner, or even half of it.

“We believe we will see the molecule, and that it is highly likely the algorithms will be smart enough to deduce it for the short list, to advance to validation in our wet labs, and subsequently into human clinical trials with pharmaceutical partners,” Bacha stated.

DDR Inhibitors – A US$18 Billion Projected Market

Rakovina Therapeutics is focusing on the discovery and validation of new drugs that precisely target the DNA-damage response network, or DDR, in cells. The DDR is responsible for maintaining our genome stability by detecting and repairing anomalies that may appear. In 75% of solid tumor cancers, however, the DDR network is defective, allowing cell mutations to escape detection and take root, leading to the potential growth, replication, and spread of cancerous tumors.

Rakovina Therapeutics’ approach, led by world-renowned DDR cancer researcher Dr. Mads Daugaard, PhD, who is the company’s President and Chief Scientific Officer, is to identify new DNA-damage response inhibitors, or DDRi, to stop the replication of damaged DNA and essentially kill the cancerous cells by turning off their ability to reproduce.

Four, first-generation approved DDRi therapeutics called PARPi (poly ADP-ribose polymerase enzyme inhibitors), have made important contributions as additive therapies to standard treatments for certain breast, ovarian and prostate cancers. In 2022, global sales of PARPi exceeded US$4.2 billion, projected to grow to US$18 billion by 2030.

Rakovina Therapeutics seeks to build on the success of PARPi with its own novel DDRi candidates, mitigating PARPi limitations and improving future cancer treatments as a result.

Rakovina Therapeutics is advancing through evaluation and validation of a pipeline of novel DDRi drug candidates. The market guidance has been that the company expects to have initial outputs from its AI collaboration in the form of recommended molecular structures in the fall of this year.

It will then move forward with synthesizing those candidates in its laboratories and would anticipate presenting initial pre-clinical data at a peer-reviewed scientific meeting in November 2024. Bacha believes the presentation of data and direction could be a game changing reveal, and the company has full rights to any lead molecules identified through the algorithms.

Technician culturing cancer cells in Rakovina Therapeutics’ laboratory at the University of British Columbia.

On co-founding the company, Bacha named it “Rakovina” Therapeutics drawing on his proud Slovak heritage, with the word meaning cancer. And when Rakovina Therapeutics was initially funded through a capital pool company transaction, it merged with another entity called Vincero Capital Corp., meaning “I will win” in Italian.

What emerged was the blended mantra of “I will beat cancer”. Combined now with Rakovina Therapeutics’ deep bench of seasoned professionals, advanced laboratory infrastructure, pioneering use of AI technology, and suite of novel drug candidates in the wings, the long war against cancer may about to be consequentially shortened.

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