Ribociclib (Kisqali)
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General information
Class/mechanism: Cyclin-dependent kinase (CDK) 4 and 6 inhibitor. Ribociclib inhibits DNA synthesis and cancer cell growth by blocking activity of the cyclin D-CDK4/6 complex which regulates cell cycle progression and cellular proliferation by phosphorylating the retinoblastoma protein (pRb). Inhibiting pRb phosphorylation has been observed to lead to cell cycle arrest in the G1 phase.[1][2][3]
Route: PO
Extravasation: n/a
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 3/13/2017: Initial FDA approval in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. (Based on MONALEESA-2 and MONALEESA-3)
- 7/18/2018: FDA approval expanded in combination with an aromatase inhibitor for pre/perimenopausal women with HR-positive, HER2-negative advanced or metastatic breast cancer, as initial endocrine-based therapy. (No longer limited to postmenopausal women; based on MONALEESA-7)
History of changes in FDA indication
- 8/22/2017: Initial authorization
Also known as
- Code names: LEE011, LEE-011
- Brand names: Kisqali, Kryxana