Program description
Biased antagonist of PAR2
- Discovery
- Candidate
- Preclinical
- Phase I
DT-9046: a first-in-class biased antagonist of PAR2 addressing unmet medical needs in multiple inflammatory diseases
DT-9046, a highly differentiated first-in-class biased negative allosteric modulator (NAM) of Proteinase-Activated Receptors 2 (PAR2), represents a transformative approach to treating multiple inflammatory diseases, including atopic dermatitis (AD), inflammatory bowel disease (IBD), arthritis and pain. This potent, orally available small molecule is uniquely designed to selectively modulate the T helper type 2 (Th2) immune response, presenting a promising solution for patients facing limited treatment options.
Progressing through pre-IND studies with an outstanding data package with an outstanding data package, DT-9046 stands out with its unique mechanism of action. Unlike biologics and full antagonists in development, DT-9046 offers a more refined therapeutic solution to benefit patients. Domain’s NAM approach ensures key competitive advantages such as unsurmountability, preserving the drug’s blocking activity even in the presence of elevated endogenous ligand levels and under acidic conditions. Moreover, its biased ligand approach enables a highly selective modulation of PAR2 signalling, minimizing the risk of resistance while maintaining efficacy.
Backed by solid multi-patent protection, DT-9046 exemplifies Domain’s leadership in unlocking complex GPCR biology and delivering transformative therapies that meet critical patient needs.
Advancing GPCR-targeting therapeutics: Redefining PAR2 antagonism
Current treatments for the inflammatory diseases often fall short due to immune or treatment resistance. There is a pressing need for more effective treatments that target the underlying mechanisms in inflammatory diseases.
PAR2, widely regarded as one of the most challenging GPCR targets, has long eluded effective therapeutic solutions within the pharmaceutical industry. Leveraging Domain’s deep expertise in targeting complex GPCRs, DT-9046 provides a differentiated and competitive multimodal approach, addressing unmet medical needs of patients with inflammatory diseases.