Products
Ribociclib was approved in the United States, the EU, and many countries in 2017 in film-coated tablet form (Kisqali).
Structure and properties
Ribociclib (C23H30N8O, Mr = 434.5 g/mol) is present in the drug as ribociclibsuccinate, a pale yellow to yellow-brown crystalline powder.
Effects
Ribociclib (ATC L01XE42) has antitumor and antiproliferative properties. The effects are due to selective inhibition of cyclin-dependent kinases (CDK) 4 and 6, enzymes involved in the cell cycle, cell proliferation, DNA replication, and cell growth. Ribociclib inhibits the transition from G1 to S phase of the cell cycle.
Indications
In combination with an aromatase inhibitor for the treatment of postmenopausal women with HR-positive, HER2-negative, advanced, or metastatic breast cancer.
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals. For a therapeutic cycle of 21 days, followed by a 7-day break.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Ribociclib is a substrate of CYP3A4.
Adverse effects
The most common possible adverse effects include neutropenia, nausea, fatigue, diarrhea, hair loss, vomiting, constipation, headache, and back pain. Ribociclib prolongs the QT interval.
