Candidate Nomination in Record Time

CHALLENGES:

  • Fast follow on: competitors in phase I/II
  • Therapeutic indication: Identify new indication(s)  other than competitors and/or differentiation over current indication in clinic
  • Identify novel hit for analoging in absence of HTS screen
  • Deliver CCN in two years

EUROFINS ADVINUS APPROACH:

  • Novel and diverse six chemotypes designed to carry out parallel SAR to identify HITS in first three months
  • Identified four HITS and prioritized two series to provide two LEADS within 6 months
  • Developed novel in-vivo PD Assay
  • Nominated Optimized Lead for Candidate Selection within 10 months,
    • Progress was halted due to phototoxicity and human hepatocyte instability
    • Second lead series showed CYP TDI liability
  • SAR knowledge from earlier two series helped to design a new chemotype (Third) to overcome above hurdles in time
  • Identified new indication by exploring efficacy in various disease models and data mining with clients help
  • Identified clinical candidate with excellent efficacy and good therapeutic window and potential back-up compound is being profiled

ACHIEVEMENTS:

  • Filed three chemical composition of matter patents
  • This programs achieved clinical candidate nomination milestone from collaborator

CURRENT STATUS:

  • Nominated clinical candidate is being profiled for new indication and IND enabling studies ongoing.