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:
  • Phase 1 Initiation in Vitiligo: 2H 2022

BRD4 BET Protein

VYN202: Oral BD2-selective BET inhibitor

Designed to selectively bind to BD2 and is being developed for major immuno-inflammatory diseases

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:
  • Candidate Selection – 2022

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