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Ribociclib information


Ribociclib
Clinical data
Trade namesKisqali
Other namesLEE 011
AHFS/Drugs.comMonograph
MedlinePlusa617008
License data
  • US DailyMed: Ribociclib
Routes of
administration
By mouth
ATC code
  • L01EF02 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[1][2]
  • CA: ℞-only[3]
  • US: ℞-only[4]
  • EU: Rx-only[5]
Pharmacokinetic data
BioavailabilityUnknown
Protein binding~70%
MetabolismLiver (CYP3A4)
Elimination half-life32.0 (29.7–54.7) hrs
Excretion69% feces, 23% urine
Identifiers
IUPAC name
  • 7-Cyclopentyl-N,N-dimethyl-2-{[5-(1-piperazinyl)-2-pyridinyl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide
CAS Number
  • 1211441-98-3
PubChem CID
  • 44631912
DrugBank
  • DB11730
ChemSpider
  • 30798107
UNII
  • TK8ERE8P56
KEGG
  • D10883
  • as salt: D10979
ChEMBL
  • ChEMBL3545110
ECHA InfoCard100.234.566 Edit this at Wikidata
Chemical and physical data
FormulaC23H30N8O
Molar mass434.548 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CN(C)C(=O)c1cc2cnc(nc2n1C3CCCC3)Nc4ccc(cn4)N5CCNCC5
InChI
  • InChI=1S/C23H30N8O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28)
  • Key:RHXHGRAEPCAFML-UHFFFAOYSA-N

Ribociclib, sold under the brand name Kisqali, is a medication used for the treatment of certain kinds of breast cancer.[6] Ribociclib is a kinase inhibitor.[7][8] It was developed by Novartis and Astex Pharmaceuticals.[9]

The most common side effects include infections, low levels of white blood cells, headache, cough, nausea (feeling sick), vomiting, diarrhea, constipation, tiredness, hair loss and rash.[5]

Ribociclib was approved by the US Food and Drug Administration (FDA) in March 2017,[10][11] by the European Medicines Agency (EMA) in August 2017,[5][12] and for use in the National Health Service (NHS) by National Institute for Health and Care Excellence (NICE) in February 2021.[7][13]

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
  2. ^ "Prescription medicines and biologicals: TGA annual summary 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 31 March 2024.
  3. ^ "Search Page - Drug and Health Product Register". 23 October 2014.
  4. ^ "Kisqali- ribociclib tablet, film coated". DailyMed. 4 May 2023. Retrieved 9 July 2023.
  5. ^ a b c "Kisqali EPAR". European Medicines Agency (EMA). 31 March 2023. Retrieved 9 July 2023. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  6. ^ FDA Professional Drug Information on Kisqali. Accessed 8 September 2017.
  7. ^ a b "Thousands of breast cancer patients to have routine access to NICE-approved drug combination". NICE (Press release). Retrieved 8 March 2021.
  8. ^ "Kisqali (ribociclib) Treatment: HR+/HER2- mBC". Novartis. Retrieved 24 August 2021.
  9. ^ "Novartis LEE011 (ribociclib) granted FDA Priority Review for first-line treatment of HR+/HER2- advanced breast cancer" (Press release). Novartis. 1 November 2016.
  10. ^ "Kisqali (ribociclib) Tablets". U.S. Food and Drug Administration (FDA). 28 March 2017. Retrieved 9 July 2023.
  11. ^ "FDA Clears Novartis Kisqali for Combination Breast Cancer Therapy". Genetic Engineering and Biotechnology News. 14 March 2017. Retrieved 9 July 2023.
  12. ^ "Kisqali: EPAR – Product Information" (PDF). European Medicines Agency. 31 August 2017.
  13. ^ "Life-extending drug for incurable breast cancer approved for NHS use". The Guardian. 26 February 2021. Retrieved 8 March 2021.

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