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BAL3833

 
 
 

BAL3833 (also known as CCT3833) is a phase 1 orally available small-molecule drug candidate. It is a panRAF/SRC kinase inhibitor as it blocks BRAF and CRAF and also inhibits the SRC kinase family. The compound originates from The Institute of Cancer Research in London where it was developed by scientists funded by Cancer Research UK and the Wellcome Trust. It is currently being explored as a daily oral administration in a clinical phase 1 dose-escalation study in adult patients with advanced solid tumors, including metastatic melanoma.

RAF and SRC kinases play an important role in the transmission of cell growth and proliferation signals. If deregulated, they are associated with tumor growth and the development of resistance to current therapies. In particular, melanoma is often linked to a mutated BRAF kinase. BAL3833 demonstrated activity in preclinical studies in a range of patient-derived melanoma models with intrinsic or acquired resistance to selective BRAF inhibitors,1 as well as tumor models derived from colorectal, pancreatic and lung cancers associated with genetic changes resulting in activation of the RAF pathway.2

References
 

  1. M. R. Girotti et al. Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer Cell 2015 (27), 85-96
  2. G. Saturno et al. Therapeutic efficacy of the paradox-breaking panRAF and SRC drug CCT3833/BAL3833 in KRAS-driven cancer models. American Association for Cancer Research (AACR) annual meeting 2016, abstract LB-212

 

 

 
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