Ribociclib

Ribociclib 2D Structure
Brand name: Kisqali
IUPAC: 7-cyclopentyl-N,N-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide
FDA approval: Yes
Manufacturer Link
Usage:

Ribociclib is administered in oral tablet form and approved for use in metastatic breast cancer.  Also of note is that Ribociclib is the first hormonal based therapy for women who have gone through menopause and have metastatic breast cancer.1

 

 

  • 1Treatment Information. (n.d.). Retrieved July 11, 2017, from https://www.us.kisqali.com/metastatic-breast-cancer/information-for/treatment?site=43700019303308773&source=01030&irmasrc=kiswb25130&gclid=CPGM9-qxgtUCFTyVswodrBkBnA&gclsrc=ds
Mechanism:

Ribociclib is a CDK 4/6 inhibitor, which means it works by stopping kinases that work to cause abnormal cell proliferation.  In turn, this allows cells to avoid issues in their cell cycle that lead to the spread of cancer and growth of tumors. 1

 

  • 1Tripathy, D., Bardia, A., & Sellers, W. R. (2017, July 01). Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors. Retrieved July 11, 2017, from https://www.ncbi.nlm.nih.gov/pubmed/28351928
Side effects:

The most serious side effects associated with Ribociclib include: heart rhythm problems, liver problems and low white blood cell count.

Other side effects include: yellowing of the skin, dark urine, drowsiness, loss of appetite, abdominal pain and bruising.1  

 

  • 1Treatment Information. (n.d.). Retrieved July 11, 2017, from https://www.us.kisqali.com/metastatic-breast-cancer/information-for/treatment?site=43700019303308773&source=01030&irmasrc=kiswb25130&gclid=CPGM9-qxgtUCFTyVswodrBkBnA&gclsrc=ds
Contraindications:

Patients taking Ribociclib should avoid pomegranate and grapefruit juice, as it could cause a severe reaction where there is a larger amount of Ribociclib in the blood.  Males prescribed Ribociclib may develop a fertility problem and should be aware that this may alter their ability to father a child.1

  • 1Treatment Information. (n.d.). Retrieved July 11, 2017, from https://www.us.kisqali.com/metastatic-breast-cancer/information-for/treatment?site=43700019303308773&source=01030&irmasrc=kiswb25130&gclid=CPGM9-qxgtUCFTyVswodrBkBnA&gclsrc=ds