Molecularly Targeted Agents

Due to breakthroughs in gene sequencing and methods of tumor characterization, cancer is rapidly being redefined from a paradigm of classification based on tissue of origin to one of specific molecular characteristics, such as abnormalities in HER2, BRCA, BRAF, ALK and EGFR genes and proteins. The ability to identify specific disease subpopulations through mutations such as HER2, BRCA, and EGFR in certain genes and proteins has proven critical in cancer drug discovery, making new treatments more effective than ever before. This type of “rational” drug design, in which targets are selected based on their observed role in cancer cell growth and survival, has been the cornerstone of BeiGene’s development efforts from the beginning, and we have three molecularly targeted product candidates now in clinical studies:

  • Zanubrutinib (BGB-3111) — an investigational small molecule inhibitor of Bruton’s tyrosine kinase (BTK)
  • Pamiparib (BGB-290) — an investigational small molecule inhibitor of PARP1 and PARP2;
  • Lifirafenib (BGB-283) — a small molecule inhibitor with RAF monomer and dimer inhibition activities.