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ribociclib (Kisqali)

Indication: - in combination with letrozole or fulvestrant, prolongs progression free survival in metastatic breast cancer * intended for postmenopausal women with estrogen receptor- positive, HER2-negative metastatic breast cancer Dosage: - 600 mg PO QD on days 1-21 each 28-day cycle - give with letrozole 2.5 mg/day PO on days 1-28 [3] Adverse effects: - neutropenia (59.5% vs 0.9% with letrozole alone) - leukopenia (21.0% vs 4.5%). - nausea (51.5% vs 28.5%) - diarrhea (35.0% vs 22.1%) - alopecia (33.2% vs 15.5%) - vomiting (29.3% vs 15.5%) Mechanism of action: - CDK4/CDK6 inhibitor (CDK4I) Clinical trials: - MONALEESA-2 trial supported by Novartis - lead author Hortobagyi disclosed relationships with Novartis, Eli Lilly, & Pfizer - several co-investigators disclosed relationships with multiple companies that produce & market products used to treat breast cancer

General

small inhibitory antineoplastic agent (ib drug) cyclin-dependent kinase inhibitor (CDKI, CDKN)

Database Correlations

PUBCHEM correlations

References

  1. Bankhead C Anti-CDK4/6 Boosts PFS in Metastatic Breast Cancer MedPage Today. Jan 3, 2017 http://www.medpagetoday.com/hematologyoncology/BreastCancer/62304 - MONALEESA-2 trial was supported by Novartis - Hortobagyi GN, et al. Ribociclib + letrozole significantly extends progression-free survival in the first-line treatment of HR+/HER2- advanced breast cancer bvs letrozole alone: First results from the phase III MONALEESA-2 study. ESMO 2016. Abstract LBA1. - Hortobagyi GN, Stemmer SM, Burris HA et al. Ribociclib as first-line therapy for HR-positive, advanced breast cancer. N Engl J Med. 2016 Nov 3;375(18):1738-1748. PMID: 27717303 Free Article
  2. O'Shaughnessy J, Petrakova K, Sonke GS et al Ribociclib plus letrozole versus letrozole alone in patients with de novo HR+, HER2- advanced breast cancer in the randomized MONALEESA-2 trial. Breast Cancer Res Treat. 2017 Nov 21. PMID: 29164421
  3. Windle ML. FDA New Drug and Biologic Approvals -- 2017 Year-in-Review Medscape - Jan 11, 2018. https://reference.medscape.com/viewarticle/890871 - U.S. Food and Drug Administration. Novel Drug Approvals for 2017. https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DrugInnovation/ucm537040.htm
  4. FDA News Release. July 18, 2018 FDA approves first cancer drug through new oncology review pilot that enables greater development efficiency. https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm613801.htm
  5. Slamon DJ, Neven P, Chia S et al Overall Survival with Ribociclib plus Fulvestrant in Advanced Breast Cancer. N Engl J Med 2020; 382:514-524. Feb 6. PMID: 31826360 https://www.nejm.org/doi/full/10.1056/NEJMoa1911149

Component-of

letrozole/ribociclib (Femara/Kisqali)