Theralase Discovers New Mechanism of Action of Lead Drug
Theralase Technologies (TLTFF) has announced a significant breakthrough in cancer treatment research. Their lead drug Ruvidar has been proven preclinically to effectively inhibit DeUbiquitinating Enzymes (DUBs), which are linked to various cancers and neurodegenerative diseases.
The research demonstrates that Ruvidar works through a dual mechanism: it inhibits DUBs activity in a dose-dependent manner and induces oxidative stress through Reactive Oxygen Species (ROS) production. At 100 μM concentration, Ruvidar nearly eliminates DUBs activity completely.
This discovery is particularly significant as DUBs are associated with drug resistance in cancer treatments. By targeting DUBs, Ruvidar could potentially be used in combination with various chemotherapy drugs and radiotherapy to combat chemoradiotherapy-resistant cancers.
Theralase Technologies (TLTFF) ha annunciato una svolta significativa nella ricerca sul trattamento del cancro. Il loro farmaco principale, Ruvidar, ha dimostrato preclinicamente di inibire efficacemente gli enzimi DeUbiquitinanti (DUBs), collegati a diversi tipi di tumori e malattie neurodegenerative.
La ricerca mostra che Ruvidar agisce tramite un meccanismo doppio: inibisce l'attività dei DUBs in modo dose-dipendente e induce stress ossidativo attraverso la produzione di specie reattive dell'ossigeno (ROS). A una concentrazione di 100 μM, Ruvidar quasi elimina completamente l'attività dei DUBs.
Questa scoperta è particolarmente importante poiché i DUBs sono associati alla resistenza ai farmaci nei trattamenti oncologici. Mirando ai DUBs, Ruvidar potrebbe essere utilizzato in combinazione con diversi farmaci chemioterapici e la radioterapia per combattere i tumori resistenti alla chemioradioterapia.
Theralase Technologies (TLTFF) ha anunciado un avance significativo en la investigación del tratamiento del cáncer. Su medicamento principal, Ruvidar, ha demostrado preclínicamente inhibir eficazmente las enzimas DeUbiquitinantes (DUBs), que están relacionadas con varios tipos de cáncer y enfermedades neurodegenerativas.
La investigación demuestra que Ruvidar actúa mediante un mecanismo dual: inhibe la actividad de las DUBs de forma dependiente de la dosis e induce estrés oxidativo a través de la producción de especies reactivas de oxígeno (ROS). A una concentración de 100 μM, Ruvidar casi elimina por completo la actividad de las DUBs.
Este descubrimiento es especialmente relevante ya que las DUBs están asociadas con la resistencia a medicamentos en tratamientos contra el cáncer. Al dirigirse a las DUBs, Ruvidar podría usarse en combinación con varios fármacos de quimioterapia y radioterapia para combatir cánceres resistentes a la quimiorradioterapia.
Theralase Technologies (TLTFF)는 암 치료 연구에서 중요한 돌파구를 발표했습니다. 그들의 주요 약물인 Ruvidar는 여러 암과 신경퇴행성 질환과 관련된 탈유비퀴틴화 효소(DUBs)를 전임상 시험에서 효과적으로 억제하는 것으로 입증되었습니다.
연구에 따르면 Ruvidar는 이중 메커니즘으로 작용합니다: 용량 의존적으로 DUBs 활성을 억제하고 반응성 산소종(ROS) 생성을 통해 산화 스트레스를 유도합니다. 100 μM 농도에서 Ruvidar는 DUBs 활성을 거의 완전히 제거합니다.
이 발견은 DUBs가 암 치료에서 약물 내성과 관련이 있기 때문에 특히 중요합니다. DUBs를 표적으로 함으로써 Ruvidar는 다양한 화학요법 약물 및 방사선 요법과 병용하여 화학방사선 치료에 내성을 가진 암을 치료하는 데 사용할 수 있을 가능성이 있습니다.
Theralase Technologies (TLTFF) a annoncé une avancée majeure dans la recherche sur le traitement du cancer. Leur médicament principal, Ruvidar, a démontré en phase préclinique une inhibition efficace des enzymes de déubiquitination (DUBs), liées à divers cancers et maladies neurodégénératives.
La recherche montre que Ruvidar agit par un mécanisme double : il inhibe l'activité des DUBs de manière dose-dépendante et induit un stress oxydatif via la production d'espèces réactives de l'oxygène (ROS). À une concentration de 100 μM, Ruvidar élimine presque complètement l'activité des DUBs.
Cette découverte est particulièrement importante car les DUBs sont associées à la résistance aux médicaments dans les traitements du cancer. En ciblant les DUBs, Ruvidar pourrait potentiellement être utilisé en combinaison avec divers médicaments de chimiothérapie et la radiothérapie pour lutter contre les cancers résistants à la chimioradiothérapie.
Theralase Technologies (TLTFF) hat einen bedeutenden Durchbruch in der Krebsbehandlungsforschung bekannt gegeben. Ihr führendes Medikament Ruvidar hat präklinisch nachgewiesen, dass es DeUbiquitinierende Enzyme (DUBs) effektiv hemmt, die mit verschiedenen Krebsarten und neurodegenerativen Erkrankungen in Verbindung stehen.
Die Forschung zeigt, dass Ruvidar durch einen doppelten Mechanismus wirkt: Es hemmt die DUBs-Aktivität dosisabhängig und induziert oxidativen Stress durch die Produktion reaktiver Sauerstoffspezies (ROS). Bei einer Konzentration von 100 μM eliminiert Ruvidar nahezu vollständig die DUBs-Aktivität.
Diese Entdeckung ist besonders bedeutend, da DUBs mit Medikamentenresistenzen bei Krebsbehandlungen in Zusammenhang stehen. Durch die gezielte Hemmung der DUBs könnte Ruvidar potenziell in Kombination mit verschiedenen Chemotherapeutika und Strahlentherapie eingesetzt werden, um chemoradiotherapie-resistente Krebsarten zu bekämpfen.
- Preclinical proof of new dual mechanism of action for lead drug Ruvidar
- Near-complete DUBs inhibition achieved at 100 μM concentration
- Potential for combination therapy with existing cancer treatments
- Possible expansion into treatment of neurodegenerative diseases
- Still in preclinical stage for this mechanism of action
- Clinical safety and efficacy yet to be demonstrated
Theralase(R) Has Discovered a New Mechanism of Action in Its War on Cancer; Specifically, Ruvidar's(TM) Ability to Inhibit DeUbiquitinating Enzymes, an Important Class of Enzymes Which Have Been Linked to Numerous Cancers and Neurogenerative Diseases
Toronto, Ontario--(Newsfile Corp. - April 28, 2025) - Theralase® Technologies Inc. (TSXV: TLT) (OTCQB: TLTFF) ("Theralase®" or the "Company"), a clinical stage pharmaceutical company dedicated to the research and development of light, radiation, sound and/or drug-activated small molecules and their formulations, intended for the safe and effective destruction of various cancers, bacteria and viruses, is pleased to announce that RuvidarTM has recently been proven preclinically to be an effective inhibitor of DeUbiquitinating Enzymes ("DUBs"), an important class of enzymes which have been linked to numerous cancers and neurogenerative diseases.
DUBs cause cellular damage by removing ubiquitin or ubiquitin-like molecules from target proteins.
Ubiquitin is a small protein found in all eukaryotic cells (animals, plants and humans), which plays a crucial role in regulating various cellular processes, such as: gene expression, DNA repair, cytokine signaling, cell metabolism, cell cycle and cell death. It functions primarily through ubiquitination, a process where ubiquitin is conjugated to target proteins, marking them for degradation or altering their activity.
Altered DUBs activity is associated with multitudes of pathologies, including cancer; therefore, DUBs represent novel candidates for target-directed drug development.1
Drug resistance to chemotherapy and molecularly targeted therapies are an ongoing challenge in cancer treatments. The underlying mechanisms of resistance to cytotoxic chemotherapeutics and to drugs that target a specific molecule are not understood completely. In recent years, emerging evidence has frequently suggested that the dysregulation of DUBs plays important roles in the development of drug resistance; hence, DUBs enable cancer cells to escape cell death and survive when exposed to a variety of anti-cancer drugs. Therefore, there exists the potential application of utilizing DUBs inhibitors in combinational therapies to overcome drug resistance.2
Targeting DUBs with inhibitors like Ruvidar™ is a very promising strategy to overcome drug resistance.
In previous Theralase® research, it was demonstrated that Ruvidar™ induces oxidative stress in cells through the production of Reactive Oxygen Species ("ROS").
In the latest research, we have investigated the effects of Ruvidar™ on DUBs activity and have demonstrated that Ruvidar™ inhibits DUBs activity in a dose-dependent manner.
This direct inhibition of DUBs, coupled with the known production of ROS by Ruvidar™, are an exciting new combination of the mechanisms of action of the effects that Ruvidar™ has on cancer cells, leading to a significant reduction in cancer cell growth.
Image 1
To view an enhanced version of this graphic, please visit:
https://images.newsfilecorp.com/files/2786/249867_7992a5b9e462d901_001full.jpg
As shown in the figure above, increasing the amount of Ruvidar™ in cells directly correlates with a reduction in DUBs activity, with 100 µM of Ruvidar™ leading to almost no DUBs activity.
Dr. Mark Roufaiel, Research Scientist, Theralase® stated, "Our latest research provides compelling evidence that RuvidarTM not only induces oxidative stress through the production of ROS to destroy cancer cells, but also directly inhibits DUBs activity-a key host mechanism exploited by the cancer cell to evade immune defenses. This dual mechanism positions Ruvidar™ as a promising therapeutic candidate, particularly against cancers, where traditional chemotherapeutics demonstrate limited effectiveness."
Arkady Mandel, M.D., Ph.D., D.Sc., Chief Scientific Officer, Theralase® stated, "With the increasing prevalence of chemoradiotherapy resistant cancers, Ruvidar™, as an effective DUBs inhibitor, may be indispensable clinically to be used as a combinational therapy with various chemotherapy drugs and/or radiotherapy to provide a safe and effective treatment against various forms of chemoradiotherapy resistant cancers. The discovery of Ruvidar's™ effectiveness against DUBs is a notable milestone in the development of Theralase®'s small molecule program and can be used for treating cancer, but could be expanded far beyond this to the treatment of age associated medical conditions, various neurodegenerative diseases, such as Alzheimer's, Parkinson's and Multiple Sclerosis, as well as to effectively combat various infectious diseases".
Roger DuMoulin-White, B.Sc., P.Eng., Pro.Dir., President and Chief Executive Officer, Theralase® stated, "According to recent peer-reviewed research, reducing DUBs plays a very important role in the war against cancer and its innate ability to build up drug resistance. This latest research reinforces an additional mechanism of action beyond direct cancer destruction and indirect immune stimulation, stripping away one of cancer's final defence mechanisms. As Theralase® pursues clinical development of Ruvidar™ for numerous cancers, such as brain and lung cancer, I look forward to reporting out on the clinical safety and efficacy of these programs."
References:
1 Farshi P et al. Deubiquitinases (DUBs) and DUB inhibitors: a patent review. Expert Opin Ther Pat. 2015;25(10):1191-1208.
2 Fujing Ge et al. Deubiquitinating enzymes: Promising targets for drug resistance, Drug Discovery Today. Volume 27. Issue 9. 2022. Pages 2603-2613.
About Theralase® Technologies Inc.:
Theralase® is a clinical stage pharmaceutical company dedicated to the research and development of light, radiation, sound and/or drug-activated small molecule compounds, their associated drug formulations and the light systems that activate them, with a primary objective of efficacy and a secondary objective of safety in the destruction of various cancers, bacteria and viruses.
Additional information is available at theralase.com and www.sedarplus.ca
Neither TSX Venture Exchange nor its Regulation Services Provider (as that term is defined in the policies of the TSX Venture Exchange) accepts responsibility for the adequacy or accuracy of this release.
Forward Looking Statements:
This news release contains Forward-Looking Statements ("FLS") within the meaning of applicable Canadian securities laws. Such statements include; but, are not limited to statements regarding the Company's proposed development plans with respect to small molecules and their drug formulations. FLS may be identified by the use of the words "may, "should", "will", "anticipates", "believes", "plans", "expects", "estimate", "potential for" and similar expressions; including, statements related to the current expectations of the Company's management regarding future research, development and commercialization of the Company's small molecules; their drug formulations; preclinical research; clinical studies and regulatory approvals.
These statements involve significant risks, uncertainties and assumptions; including, the ability of the Company to fund and secure the regulatory approvals to successfully complete various clinical studies in a timely fashion and implement its development plans. Other risks include: the ability of the Company to successfully commercialize its small molecule and drug formulations; the risk that access to sufficient capital to fund the Company's operations may not be available on terms that are commercially favorable to the Company or at all; the risk that the Company's small molecule and drug formulations may not be effective against the diseases tested in its clinical studies; the risk that the Company fails to comply with the terms of license agreements with third parties and as a result loses the right to use key intellectual property in its business; the Company's ability to protect its intellectual property; the timing and success of submission, acceptance and approval of regulatory filings. Many of these factors that will determine actual results are beyond the Company's ability to control or predict.
Readers should not unduly rely on these FLS, which are not a guarantee of future performance. There can be no assurance that FLS will prove to be accurate as such FLS involve known and unknown risks, uncertainties and other factors which may cause actual results or future events to differ materially from the FLS.
Although the FLS contained in the press release are based upon what management currently believes to be reasonable assumptions, the Company cannot assure prospective investors that actual results, performance or achievements will be consistent with these FLS.
All FLS are made as of the date hereof and are subject to change. Except as required by law, the Company assumes no obligation to update such FLS.
For investor information on the Company, please feel to reach out Investor Inquiries - Theralase Technologies.
For More Information:
1.866.THE.LASE (843-5273)
416.699.LASE (5273)
theralase.com
Kristina Hachey, CPA
Chief Financial Officer X 224
khachey@theralase.com
To view the source version of this press release, please visit https://www.newsfilecorp.com/release/249867
FAQ
What is the new mechanism of action discovered for Theralase's (TLTFF) drug Ruvidar?
How effective is TLTFF's Ruvidar in inhibiting DUBs activity?
What potential applications does Theralase's (TLTFF) Ruvidar have beyond cancer treatment?
How might TLTFF's Ruvidar help overcome cancer drug resistance?
