DT-9045 / Kainova Therapeutics - LARVOL DELTA

DT-9045, a novel PAR2 inhibitor with best-in-class properties that reduces resistance to both EGFR-targeting therapies and immunotherapy in oncology models (AACR 2024) - "This preclinical candidate has shown strong potency in alleviating the resistance to both EGFR-targeting therapies and immunotherapy in preclinical cancer models. IND-enabling studies are currently ongoing to bring this new hope for cancer patients to the clinic."

Oncology • CD4 • CD8

PAR2 inhibitors reduce resistance to immunotherapy against cancer (AACR 2025) - "Domain Therapeutics has identified a novel PAR2 biased NAM, DT-9045, orally available and with clear competitive advantages. IND-enabling studies are currently ongoing to bring this new hope for cancer patients to the clinic."

Oncology • IL10

Domain Therapeutics Presents Novel Data Addressing Key Challenges in Oncology at AACR 2025 (PRNewswire) - "...demonstrating the promising potential of its PAR2 biased NAM in overcoming resistance to immune checkpoint blockade (ICB) and addressing T cell dysfunction in cancer. The preclinical findings revealed that PAR2 biased NAM: Synergizes with anti-PD1 therapy, turning macrophage phenotype and cytokine profile toward a pro-inflammatory TME. Promotes antigen-presenting cells and T cells, facilitating robust antitumoral responses...This research provides critical insights into the mechanisms of PAR2 inhibition, positioning Domain's PAR2 biased NAM program as a transformative therapeutic approach to overcome tumor resistance to ICB and restore effective immune control."

Preclinical • Oncology

Domain Therapeutics to Present Latest Data on DT-9045, a First-in-class Negative Allosteric Modulator of PAR2 for Immuno-oncology, at AACR 2024 Annual Meeting, Highlighting Clear Competitive Advantages of This Candidate (Businesswire) - "Domain Therapeutics...announces 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) Annual Meeting 2024 in San Diego, California....IND-enabling studies are currently ongoing to advance the candidate toward the clinic."

Preclinical • Oncology • Solid Tumor

Domain Therapeutics announces nomination of first-in-class PAR2 NAM candidate, DT-9045, to unlock new cancer treatment possibilities (GlobeNewswire) - "Domain Therapeutics...announces the nomination of a drug candidate, a Negative Allosteric Modulator (NAM) of protease-activated receptor 2 (PAR2), DT-9045, with first-in-class potential for immuno-oncology, particularly for fibrotic tumors....Domain nominated DT-9045 as a first-in-class PAR2 NAM clinical candidate based on its added-value, unique properties and greater therapeutic potential in comparison to biologics targeting PAR2 currently in the clinic by several competitors....Domain has established a clear biomarker strategy guiding the clinical positioning for DT-9045 and with pre-IND studies in progress, the Company’s expectations are for Phase I ascending dose studies in recurrent or metastatic solid tumors to start by mid-2025."

New molecule • New P1 trial • Oncology • Solid Tumor