alisertib

Alisertib is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase (AURKA). It acts as a reversible, ATP-competitive inhibitor with an IC50 in the low nanomolar range. By inhibiting Aurora A kinase, alisertib disrupts mitotic spindle apparatus assembly and chromosome segregation during cell division, leading to cell-cycle arrest, apoptosis, and autophagy in cancer cells. This mechanism underlies its potential antineoplastic activity. Alisertib was originally developed by Millennium Pharmaceuticals and later licensed to Puma Biotechnology for further development. It has been investigated primarily for various cancers including breast cancer (especially HER2-negative), small cell lung cancer, peripheral T-cell lymphoma, and other hematologic malignancies.

Other names

alisertibAlisertib sodiumAlsertib