InhiBET™ BET Inhibitor Platform

VYNE is developing novel therapies for immuno-inflammatory (I&I) diseases that target bromo-domain and extra-terminal domain proteins (BET).

InhiBET™ BET Inhibitor Platform:

BETs are a family of proteins characterized by two bromo-domain subunits (BD1 and BD2) plus an extra-terminal domain (EXT). BET proteins are believed to play a key role in the regulation of inflammatory and oncogenic genes involved in several diseases.

VYNE’s BET inhibitors (BETi’s) are based on its proprietary InhiBETTM platform and small molecule library.

VYNE reviewed the InhiBET™ Program in a Key Opinion Leader call on May 17, 2022.

InhiBET™ BET Inhibitor Programs:

The BRD4 BET Protein: BD1 and BD2 are bromodomains and EXT is an extra-terminal domain

VYN201: Locally administered Pan-BD BET inhibitor

Target Markets:

Designed to address diseases involving multiple, diverse inflammatory cell signaling pathways with low systemic exposure

  • Lead indication – Vitiligo
  • Other indications benefiting from local application and “soft drug” approach
Broad activity:
  • Binds to BD1 and BD2 domains
Competition:
  • Almost all BET inhibitors in development bind to BD1 and BD2 but are orally delivered with significant dose limiting toxicities
Targeted Near Term Milestones:
  • Q3 2023: VYN201 Phase 1b 16-week top line results in vitiligo

BRD4 BET Protein

VYN202: Oral BD2-selective BET inhibitor

VYN202 is an oral small molecule BET inhibitor in preclinical development for the treatment of immuno-inflammatory indications. VYN202 is being designed to achieve class-leading selectivity (BD2 vs. BD1), maximum potency versus BD2 and optimal oral bioavailability. By maximizing BD2 selectivity, VYNE believes VYN202 has the potential to be a more conveniently-administered non-biologic treatment option for both acute control and chronic management of immuno-inflammatory indications, where the damaging effects of unrestricted inflammatory signaling activity is common.

Target Markets1:
  • Immuno-inflammatory indications such as rheumatoid arthritis, systemic lupus erythematosus, ulcerative colitis/Crohn’s and multiple sclerosis; additional potential in myeloproliferative neoplastic disorders2
Focused activity:
  • Highly selective inhibition of BD2 domain of the BRD4 protein (Selectivity vs. BD1)
  • Targeting improved safety profile compared to oral pan-BD BET inhibitors
Targeted Near Term Milestones:
  • 2023: exercise of option, selection of indication & submission of IND

1 Initial indication to be communicated following candidate selection, exercise of option, IND-enabling studies and completion of requisite preclinical evaluations
2 List included is not exhaustive of potential indications