LY3295668

LY3295668 (also known as AK-01 or Erbumine) is an orally bioavailable small molecule inhibitor that selectively targets Aurora kinase A. Aurora kinase A is a serine/threonine protein kinase involved in the regulation of mitosis and cell division. Overexpression of this enzyme has been implicated in tumorigenesis and cancer progression. By inhibiting Aurora kinase A activity, LY3295668 disrupts mitotic spindle assembly and chromosome segregation, leading to inhibition of cell division and induction of apoptosis in cancer cells overexpressing this target[2][3][6]. The drug is being investigated primarily for various solid tumors including small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), metastatic breast cancer, neuroblastoma (especially MYC/MYCN-driven tumors), head and neck cancers, and triple-negative breast cancer[1][3][5]. It is currently under clinical evaluation with demonstrated disease control rates in early-phase studies[6].

Brand names

Erbumine

Other names

Aurora A kinase inhibitor LY3295668UNII-1WX8O5XV4RUNII1WX8O5XV4RUNII 1WX8O5XV4R1919888-06-4