• Technical Name
  • BPR1R系列:新穎集落刺激因子1受體抑制劑作為癌症免疫調節劑
  • Operator
  • National Health Research Institutes (NHRI)
  • Booth
  • 精準健康(生技&新藥) Precision Health(Biotech & New Drug Development)
  • Contact
  • 李昆鴻
  • Email
  • quin22805@nhri.edu.tw
Technical Description We have identified a series of BPR1R compounds as highly selective CSF1R inhibitors with excellent oral bioavailability. In vivo, oral administration of BPR1R compounds delayed murine colon tumor growthreversed the immunosuppressive TME with increased M1/M2 ratio. The US & PCT patent application including more than 160 novel compounds was filed in April 20, 2020. Several potential compounds are undergoing candidate assessment for further preclinical studies.
Scientific Breakthrough \" Tumor growth inhibition (TGI) = 69 without body weight loss[TGI of pexidartinib = 57 at the same dose] Brain penetration: Brain-to-Plasma (B/P) ratio = 31. Concise synthesis within 5 to 7 steps [10 g scale]. Oral bioavailability (F) up to 38. High kinase selectivity: S(35) = 0.035 @ 1 µM against 403 kinases. High M2 TAM specificity: IC50 ratio against M1/M2 TAM 200 fold.\"
Industrial Applicability \"Immune therapy possesses a huge opportunity – combination with PD-1 mABcytotoxic agents show synergistic effects, which offer benefits than single-agent use. Our BPR1R inhibitors with high selectivity displayed low toxicity, which reduce the risk of combination use. Potential Treatment for Alzheimer's Disease (AD)Parkinson's Disease (PD) – CSF1R is a promising target associated with ADPD. Our compounds possessing excellent brain-penetrating ability provide the great opportunity as first-in-class agents for the treatment of ADPD.\"