Ribociclib (Kisqali)

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

Breast cancer

Patient drug information

Ribociclib (Kisqali) package insert^[1]

History of changes in FDA indication

2017-03-13: 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)
2018-07-18: 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 EMA indication

2017-08-22: Initial authorization

History of changes in Health Canada indication

2018-06-18: Initial notice of compliance in combination with letrozole for treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer as an initial endocrine-based therapy.
2020-02-07: Expanded indication (details unavailable)
2023-02-10: Expanded indication (details unavailable)

Also known as

Code names: LEE-011
Brand names: Kisqali, Kryxana

References

[insert-1] 1.0 ^1.1 Ribociclib (Kisqali) package insert

[2] Ribociclib (Kisqali) package insert (locally hosted backup)

[3] Kisqali manufacturer's website

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[2]

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