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."

Also known as

  • Code names: LEE011, LEE-011
  • Brand name: Kisqali

References

  1. 1.0 1.1 Ribociclib (Kisqali) package insert
  2. Ribociclib (Kisqali) package insert (locally hosted backup)
  3. Kisqali manufacturer's website