Ribociclib: First Global Approval.

Ribociclib is an oral, small-molecule inhibitor of cyclin-dependent kinase (CDK) 4 and 6 that is under development by Novartis for the treatment of cancer. CDKs play an important role in cell cycle progression and cellular proliferation, and inhibition of these kinases with ribociclib results in G1 phase cell-cycle arrest. Ribociclib, in combination with an aromatase inhibitor, was recently approved in the USA for the first-line treatment of advanced breast cancer and has been submitted for approval in the EU for this indication. Ribociclib is undergoing further phase III investigations in breast cancer and is being evaluated in phase I or II trials for various solid tumour types and haematological malignancies. This article summarizes the milestones in the development of ribociclib leading to this first global approval for use as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced or metastatic breast cancer.