On March 26, 2024 Domain Therapeutics ("Domain" or "the Company"), a global clinical-stage biopharmaceutical company developing innovative drug candidates in immuno-oncology targeting G Protein-Coupled Receptors (GPCRs), reported that latest preclinical data on DT-9045, a novel protease-activated receptor 2 (PAR2) Negative Allosteric Modulator candidate, will be presented at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2024 in San Diego, California (Press release, Domain Therapeutics, MAR 26, 2024, View Source [SID1234641444]).
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Date/Time: 7 April 2024 1:30 PM – 5:00 PM PST – Section 27
Abstract number: 684 / 30
Poster session: PO.ET09.05 – Novel Antitumor Agents 2
Title: DT-9045, a novel PAR2 inhibitor with best-in-class properties that reduces resistance to both EGFR-targeting therapies and immunotherapy in oncology models
The abstract will be made available in the online Proceedings of the AACR (Free AACR Whitepaper).
PAR2 is one of the genes most significantly linked to resistance against immune checkpoint blockage (ICB) and T cells dysfunction in cancer patients. Its upregulation across a variety of cancer types and expression on diverse cells within the tumor microenvironment underscore PAR2’s critical role in cancer development.
Leveraging its integrated precision research approach, backed by over 20 years of solid GPCR expertise, Domain has developed a novel highly potent and selective PAR2 inhibitor, DT-9045. This first-in-class Negative Allosteric Modulator has shown unparalleled potential in oncology and immuno-oncology. Remarkably, when compared to its most advanced competitors positioned in other therapeutic areas, this candidate has demonstrated clear differentiated features. Moreover, several proof-of-concept studies have shown strong potency in models resistant to EGFR-targeting therapies and immunotherapy opening solid perspectives of strategic clinical positioning and revenues generation in tumor types that constitute a high medical unmet need.
DT-9045 is a small molecule, orally available, insurmountable, biased, and active in tumor-like conditions (high concentration of activating proteases and acidic pH). IND-enabling studies are currently ongoing to advance the candidate toward the clinic.
Stephan Schann, Chief Scientific Officer of Domain Therapeutics, commented: "We are excited to present our newest findings on DT-9045 at AACR (Free AACR Whitepaper). The results not only confirm the immense potential of our PAR2 inhibitor to change the way we treat cancer, but also emphasize its high potency and efficacy against several drug resistance, offering cancer patients clear therapeutic perspectives in immuno-oncology. More broadly, they reflect our deep commitment to precision research, pioneering innovative new GPCR targets in immunosuppression, designing clear competitive properties to deliver game-changing candidates. We eagerly anticipate advancing this groundbreaking research, with a focus on addressing a substantial unmet medical need for cancer patients."
This progress, follows the announcement in June 2023 when DT-9045 was nominated as a first-in-class clinical PAR2 antagonist. It has shown great therapeutic potential in enhancing the efficacy to immunotherapy aiming to substantially improve treatment outcomes for non-responding cancer patients.