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.

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

InhiBET™ BET Inhibitor Programs:

Repibresib (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
Status:
  • Seeking development partner for program

BET Protein

VYN202: Oral BD2-selective BET inhibitor

VYN202 has been designed to achieve class-leading selectivity (BD2 vs. BD1), maximum potency versus BD2 and optimal oral bioavailability. Maximizing on-target potency vs. BD2 and minimizing affinity to BD1 may be the key to optimizing the benefit/risk profile of BET inhibitors for autoimmune diseases.

Target Markets:
  • Serious, immune-mediated diseases with limited effective treatment options
Focused activity:
  • VYN202 is believed to be the most potent and BD2-selective BET Inhibitor in clinical development1 which is designed to improve efficacy and tolerability
Status:
  • Q4 2024: Phase 1a SAD/MAD Complete
  • July 2025: Promising preliminary Phase 1b moderate-to-severe PSO data; no further enrollment of study
  • Repeat 12-week non-clinical toxicology study ongoing2

1 Based on readily available public information such as clintrials.gov, academic publications and corporate websites/presentations.
2 The repeat non-clinical toxicology study in dogs is intended to remedy the partial clinical hold in male clinical subjects.