Drug updated on 6/24/2024

Dosage FormTablet (oral; 200 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies


  • Indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer in combination with an aromatase inhibitor as initial endocrine-based therapy.
  • Indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer in combination with fulvestrant as initial endocrine-based therapy or following disease progression on endocrine therapy in postmenopausal women or in men.

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  • Ribociclib (Kisqali) is recommended for the management of adult patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced or metastatic breast cancer. It is effective when used with an aromatase inhibitor as initial endocrine-based therapy or in combination with fulvestrant after disease progression on endocrine therapy.
  • Ten systematic reviews/meta-analyses provided insights into the drug's safety and effectiveness in comparison to others such as abemaciclib and palbociclib.
  • The comparative efficacy among ribociclib, abemaciclib, and palbociclib did not show statistical significance across the studies reviewed. Nonetheless, evidence supports the addition of CDK4/6 inhibitors like ribociclib to endocrine therapy to significantly enhance therapeutic efficacy.
  • Regarding adverse events, ribociclib and abemaciclib exhibited greater gastrointestinal toxicity than palbociclib. Palbociclib more frequently resulted in neutropenia but demonstrated a lower risk of severe infections. Ribociclib was associated with less severe transaminitis and neutropenia than abemaciclib.
  • Subgroup analysis indicated that the concurrent use of proton pump inhibitors might lead to worse outcomes for patients using palbociclib, but this was not significantly the case for ribociclib. This implies possible considerations for its use in specific patient subgroups. Furthermore, it showed a favorable profile in comparisons of overall survival rates, suggesting that individual patient factors could play a role in the decision-making process regarding its use.
  • In the context of neoadjuvant therapies involving CDK4/6 inhibitors combined with endocrine therapies as opposed to monotherapies or standard chemotherapy treatments; the combination therapies exhibited increased efficacy, albeit at higher toxicity levels. However, they still maintained better safety profiles than neoadjuvant chemotherapy alone.

Product Monograph / Prescribing Information

Document TitleYearSource
Kisqali (Ribociclib) Prescribing Information.2023Novartis Pharmaceuticals Corporation., East Hanover, NJ

Systematic Reviews / Meta-Analyses

Document TitleYearSource
Comparative overall survival of CDK4/6 inhibitors in combination with endocrine therapy in advanced breast cancer.2024Scientific Reports
A network meta-analysis of efficacy and safety for first-line and second/further-line therapies in postmenopausal women with hormone receptor-positive, HER2-negative, advanced breast cancer.2024BMC Medicine
An overview of the safety profile and clinical impact of CDK4/6 inhibitors in breast cancer-a systematic review of randomized phase II and III clinical trials.2023Biomolecules
Comparative efficacy and safety of different combinations of three CDK4/6 inhibitors with endocrine therapies in HR+/HER-2 - metastatic or advanced breast cancer patients: a network meta-analysis.2023BMC Cancer
The association between proton pump inhibitors and the effectiveness of CDK inhibitors in HR+/HER- advanced breast cancer patients: a systematic review and meta-analysis.2023Cancers
The likelihood of being helped or harmed as a patient-centred tool to assess cyclin dependent kinase 4/6 inhibitors clinical impact and safety in metastatic breast cancer: a systematic review and sensitivity-analysis.2023EClinicalMedicine
Neoadjuvant therapy of cyclin-dependent kinase 4/6 inhibitors combined with endocrine therapy in HR+/HER2− breast cancer: a systematic review and meta-analysis.2021Oncology Research and Treatment
CDK4/6 inhibitors in breast cancer: differences in toxicity profiles and impact on agent choice. A systematic review and meta-analysis.2021Expert Review of Anticancer Therapy
Efficacy and safety of CDK4/6 and PI3K/AKT/mTOR inhibitors as second-line treatment in postmenopausal patients with hormone receptor-positive, HER-2-negative metastatic breast cancer: a network meta-analysis.2021Expert Opinion on Drug Safety
Cyclin‑dependent kinase 4/6 inhibitors in combination with fulvestrant for previously treated metastatic hormone receptor‑positive breast cancer patients: a systematic review and meta‑analysis of randomized clinical trials.2020Cancer Treatment and Research Communications

Clinical Practice Guidelines

Document TitleYearSource
Early breast cancer: ESMO Clinical Practice Guideline for diagnosis, treatment and follow-up.2024Annals of Oncology
Breast Cancer. Version 3. 2020.2020Journal of the National Comprehensive Cancer Network