Gain Therapeutics Presents Data at 36ᵗʰ EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics Demonstrating Identification of Allosteric Inhibitors Targeting DDR2
Gain Therapeutics (NASDAQ: GANX) presented data at the 36th EORTC-NCI-AACR Symposium showcasing their allosteric inhibitor GT-03842, identified through their Magellan Drug Discovery Platform. The compound effectively targets and inhibits DDR2 phosphorylation, a protein associated with various cancer types and tumor progression. GT-03842 demonstrated dose-dependent inhibition in both HEK293 cells and a metastatic breast cancer model. The compound's unique mechanism, targeting outside the kinase domain, suggests potential advantages over traditional kinase inhibitors, including enhanced selectivity and reduced resistance.
Gain Therapeutics (NASDAQ: GANX) ha presentato dati al 36° Simposio EORTC-NCI-AACR, mostrando il loro inibitore allosterico GT-03842, identificato attraverso la loro piattaforma di scoperta di farmaci Magellan. Il composto agisce in modo efficace mirandosi e inibendo la fosforilazione di DDR2, una proteina associata a vari tipi di cancro e alla progressione dei tumori. GT-03842 ha dimostrato un'inibizione dipendente dalla dose sia nelle cellule HEK293 che in un modello di cancro al seno metastatico. Il meccanismo unico del composto, che agisce al di fuori del dominio della chinasi, suggerisce vantaggi potenziali rispetto agli inibitori tradizionali delle chinasi, inclusa una maggiore selettività e una riduzione della resistenza.
Gain Therapeutics (NASDAQ: GANX) presentó datos en el 36° Simposio EORTC-NCI-AACR, mostrando su inhibidor alostérico GT-03842, identificado a través de su Plataforma de Descubrimiento de Fármacos Magellan. El compuesto actúa de manera efectiva al dirigirse e inhibir la fosforilación de DDR2, una proteína asociada con varios tipos de cáncer y la progresión del tumor. GT-03842 demostró una inhibición dependiente de la dosis tanto en células HEK293 como en un modelo de cáncer de mama metastásico. El mecanismo único del compuesto, que actúa fuera del dominio de la quinasa, sugiere ventajas potenciales sobre los inhibidores tradicionales de quinasas, incluyendo una mayor selectividad y una reducción de la resistencia.
Gain Therapeutics (NASDAQ: GANX)는 36번째 EORTC-NCI-AACR 심포지엄에서 그들의 알로스테릭 억제제 GT-03842에 대한 데이터를 발표했습니다. 이 화합물은 Magellan 약물 발견 플랫폼을 통해 확인되었으며, 여러 암 유형과 종양 진행과 관련된 단백질인 DDR2의 인산화를 효과적으로 표적하고 억제합니다. GT-03842는 HEK293 세포와 전이성 유방암 모델 모두에서 용량 의존적으로 억제 효과를 보였습니다. 이 화합물은 키나제 도메인 외부를 표적하는 독특한 메커니즘을 가지고 있어 전통적인 키나제 억제제에 비해 향상된 선택성과 저항성 감소와 같은 잠재적 이점을 제시합니다.
Gain Therapeutics (NASDAQ: GANX) a présenté des données lors du 36e Symposium EORTC-NCI-AACR mettant en avant leur inhibiteur allostérique GT-03842, identifié grâce à leur plateforme de découverte de médicaments Magellan. Ce composé cible efficacement et inhibe la phosphorylation de la DDR2, une protéine associée à divers types de cancer et à la progression tumorale. GT-03842 a montré une inhibition dépendante de la dose tant dans des cellules HEK293 que dans un modèle de cancer du sein métastatique. Le mécanisme unique du composé, qui cible en dehors du domaine kinase, suggère des avantages potentiels par rapport aux inhibiteurs de kinase traditionnels, notamment une sélectivité accrue et une résistance réduite.
Gain Therapeutics (NASDAQ: GANX) hat Daten auf dem 36. EORTC-NCI-AACR-Symposium präsentiert, die ihren allosterischen Inhibitor GT-03842 zeigen, der über ihre Magellan-Arzneimittelentdeckungsplattform identifiziert wurde. Die Verbindung zielt effektiv auf die Inhibition der DDR2-Phosphorylierung ab, eines Proteins, das mit verschiedenen Krebsarten und dem Tumorwachstum in Verbindung steht. GT-03842 zeigte eine dosisabhängige Hemmung sowohl in HEK293-Zellen als auch in einem metastatischen Brustkrebsmodell. Der einzigartige Mechanismus des Verbindungen, der außerhalb des Kinase-Domains wirkt, deutet auf potenzielle Vorteile gegenüber traditionellen Kinase-Inhibitoren hin, einschließlich einer verbesserten Selektivität und reduzierter Resistenz.
- GT-03842 successfully demonstrated inhibition of DDR2 phosphorylation in both laboratory and cancer models
- The compound's novel mechanism may offer better selectivity and reduced resistance compared to traditional treatments
- Successful validation of the company's Magellan drug discovery platform
- Early-stage research with no clinical validation yet
- No efficacy or safety data in human subjects presented
Insights
The discovery of GT-03842 as an allosteric inhibitor of DDR2 represents a significant advancement in oncology drug development. This compound's ability to inhibit DDR2 phosphorylation through allosteric binding rather than targeting the kinase domain is particularly noteworthy, as it could potentially overcome the resistance issues commonly seen with traditional kinase inhibitors.
The data demonstrating efficacy in a metastatic breast cancer model is promising, especially considering DDR2's role in tumor progression and metastasis. The dose-dependent inhibition in HEK293 cells provides solid preclinical validation. However, it's important to note this is still early-stage research - while the mechanism is innovative, significant clinical development work remains before potential commercialization.
The novel allosteric approach could offer better selectivity and safety profiles compared to existing treatments, potentially leading to reduced side effects and improved patient outcomes. This could translate to meaningful market differentiation if clinical trials prove successful.
GT-03842, Identified by the Company’s Magellan Drug Discovery Platform, Effectively Hinders Phosphorylation and Activation of DDR2
GT-03842 May Offer Potential Favourable Therapeutic Attributes for Oncology Compared to Traditional Kinase Inhibitors
BETHESDA, Md., Oct. 23, 2024 (GLOBE NEWSWIRE) -- Gain Therapeutics, Inc. (Nasdaq: GANX) (“Gain”, or the “Company”), a clinical-stage biotechnology company leading the discovery and development of the next generation of allosteric small molecule therapies, today announced the presentation of a poster at the 36th EORTC-NCI-AACR (ENA) Symposium on molecular targets and cancer therapeutics that details the use of the Company’s Magellan drug discovery platform to identify allosteric inhibitors targeting discoidin domain receptor 2 (DDR2). ENA 2024 is being held October 23-25 in Barcelona, Spain.
“We believe the identification of allosteric small molecule inhibitors targeting DDR2 validates the Company’s Magellan platform. Our belief is strengthened that this innovative approach can one day result in much-needed novel therapeutics for people with DDR2-driven malignancies,” commented Joanne Taylor, Ph.D., Senior Vice President of Research at Gain.
The poster, “Identification of allosteric inhibitors targeting Discoidin Domain Receptor 2 (DDR2),” which was presented on-site on October 23 by Sara Cano-Crespo, Ph.D., Senior Scientist of Biology at Gain, detailed how the 3D structure of DDR2 guided a high-throughput virtual screening and subsequent experimental validation that resulted in GT-03842 and additional analogue compounds. Upon binding to collagen, DDR2 undergoes autophosphorylation, triggering its activation and initiating downstream signaling cascades. After conducting a phosphorylation assay based on AlphaLISA with HEK293 cells overexpressing DDR2, GT-03842 and its analogues were found to inhibit DDR2 phosphorylation in a dose-dependent manner.
Aberrant DDR2 phosphorylation is associated with various cancer types and is involved in critical processes in tumor progression, including proliferation, migration, invasion, metastasis, epithelial-mesenchymal transition, and immunotherapy resistance. In a metastatic breast cancer model, GT-03842 also reduced DDR2 phosphorylation. Additionally, GT-03842 inhibits DDR2 activity without targeting the kinase domain, showing the potential to overcome resistance and offer enhanced selectivity and safety compared to traditional kinase inhibitors.
A PDF of the poster presented at the 36th ENA Symposium on molecular targets and cancer therapeutics is available on the Science and Technology section of the Company’s website at https://gaintherapeutics.com/science-and-technology/posters.
About Gain Therapeutics, Inc.
Gain Therapeutics, Inc. is a clinical-stage biotechnology company leading the discovery and development of next generation allosteric therapies. Gain’s lead drug candidate, GT-02287 is currently being evaluated for the treatment of Parkinson’s disease with or without a GBA1 mutation. Results from a Phase 1 study of GT-02287 in healthy volunteers demonstrated favorable safety and tolerability, plasma exposure in the projected therapeutic range, CNS exposure, and target engagement and modulation of GCase enzyme.
Gain’s unique approach enables the discovery of novel, allosteric small molecule modulators that can restore or disrupt protein function. Deploying its highly advanced Magellan™ platform, Gain is accelerating drug discovery and unlocking novel disease-modifying treatments for untreatable or difficult-to-treat disorders including neurodegenerative diseases, rare genetic disorders and oncology.
Forward-Looking Statements
This release contains “forward-looking statements” made pursuant to the safe harbor provisions of the Private Securities Litigation Reform Act of 1995. These statements are typically preceded by words such as “believes,” “expects,” “anticipates,” “intends,” “will,” “may,” “should,” or similar expressions. These forward-looking statements reflect management’s current knowledge, assumptions, judgment and expectations regarding future performance or events. Although management believes that the expectations reflected in such statements are reasonable, they give no assurance that such expectations will prove to be correct or that those goals will be achieved, and you should be aware that actual results could differ materially from those contained in the forward-looking statements. Forward-looking statements are subject to a number of risks and uncertainties, including, but not limited to, risks associated with market conditions and the satisfaction of customary closing conditions related to the offering and uncertainties related to the offerings and the use of proceeds from the offerings. For a further description of the risks and uncertainties that could cause actual results to differ from those expressed in these forward-looking statements, as well as risks relating to the Company’s business in general, please refer to the Company’s prospectus supplement to be filed with the SEC, and the documents incorporated by reference therein, including the Company’s Form 10-K for the year ended December 31, 2023 and Form 10-Q for the quarter ended June 30, 2024.
All forward-looking statements are expressly qualified in their entirety by this cautionary notice. You are cautioned not to place undue reliance on any forward-looking statements, which speak only as of the date of this release. We have no obligation, and expressly disclaim any obligation, to update, revise or correct any of the forward-looking statements, whether as a result of new information, future events or otherwise.
Investor Contacts:
Apaar Jammu and Chuck Padala
ajammu@gaintherapeutics.com
chuck@lifesciadvisors.com
Media Contacts:
Russo Partners
Nic Johnson and Elio Ambrosio
nic.johnson@russopartnersllc.com
elio.ambrosio@russopartnersllc.com
(760) 846-9256
FAQ
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