Ribociclib

Ribociclib is an inhibitor of cyclin-dependent kinase (CDK) 4 and 6. These kinases are activated upon binding to D-cyclins and are downstream of signaling pathways which lead to cell cycle progression and cellular proliferation.

• KISQALI is a kinase inhibitor indicated: in combination with an aromatase inhibitor for the adjuvant treatment of adults with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative stage II and III early breast cancer at high risk of recurrence. ( 1 ) for the treatment of adults with HR-positive, HER2-negative advanced or metastatic breast cancer in combination with: an aromatase inhibitor as initial endocrine-based therapy; or fulvestrant as initial endocrine-based therapy or following disease progression on endocrine therapy.ICD-10: C50.919

• None. None.contraindicated

KISQALI tablets are taken orally with or without food in combination with an aromatase inhibitor or fulvestrant. ( 2 ) Early Breast Cancer Recommended starting dose: 400 mg orally (two 200 mg tablets) taken once daily with or without food for 21 consecutive days followed by 7 days off treatment. ( 2.1 ) Advanced or Metastatic Breast Cancer Recommended starting dose: 600 mg orally (three 200 mg tablets) taken once daily with or without food for 21 consecutive days followed by 7 days off treatment. ( 2.1 ) Dose interruption, reduction, and/or discontinuation may be required based on individual safety and tolerability. ( 2.2 ) 2.1 Recommended Dosage Important Administration Instructions KISQALI can be taken with or without food [see Clinical Pharmacology (12.3)] . Pre/perimenopausal women, or men, treated with the combination KISQALI plus an aromatase inhibitor or fulvestrant, should be treated with a luteinizing hormone-releasing hormone (LHRH) agonist according to current clinical practice standards. Patients should take their dose of KISQALI at approximately the same time each day, preferably in the morning. If the patient vomits after taking the dose, or misses a dose, no additional dose should be taken that day. The next prescribed dose should be taken at the usual time. KISQALI tablets should be swallowed whole (tablets should not be chewed, crushed or split prior to swallowing). No tablet should be ingested if it is broken, cracked, or otherwise not intact.

Interstitial Lung Disease (ILD)/Pneumonitis: Patients treated with CDK 4/6 inhibitors should be monitored for pulmonary symptoms indicative of ILD/pneumonitis. Interrupt and evaluate patients with new or worsening respiratory symptoms suspected to be due to ILD/pneumonitis. Permanently discontinue KISQALI in patients with recurrent symptomatic or severe ILD/pneumonitis. ( 2.2 , 5.1 ) Severe Cutaneous Adverse Reactions (SCARs): Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and drug-reaction with eosinophilia and systemic symptoms (DRESS) can occur with KISQALI treatment. Permanently discontinue KISQALI in patients with SCARs or other life-threatening cutaneous reactions. ( 2.2 , 5.2 ) QT Interval Prolongation: Monitor electrocardiograms (ECGs) and electrolytes prior to initiation of treatment with KISQALI. Repeat ECGs at approximately Day 14 of the first cycle, and as clinically indicated. Monitor electrolytes at the beginning of each cycle for 6 cycles, and as clinically indicated. Avoid using KISQALI with drugs known to prolong QT interval and/or strong CYP3A inhibitors. ( 2.2 , 5.3 , 7.1 , 7.4 ) Increased QT Prolongation with Concomitant Use of Tamoxifen: KISQALI is not indicated for concomitant use with tamoxifen. ( 5.4 ) Hepatotoxicity: Increases in serum transaminase and bilirubin levels have been observed. Perform liver function tests (LFTs) before initiating treatment with KISQALI. Monitor LFTs every 2 weeks for the first 2 cycles, at the beginning of each subsequent 4 cycles, and as clinically indicated.

The following adverse reactions are discussed in greater detail in other sections of the labeling: Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.1)] Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.2)] QT Interval Prolongation [see Warnings and Precautions (5.3, 5.4)] Hepatotoxicity [see Warnings and Precautions (5.5)] Neutropenia [see Warnings and Precautions (5.6)] In patients with early breast cancer, the most common (incidence ≥ 20%) adverse reactions, including laboratory abnormalities, are lymphocytes decreased, leukocytes decreased, neutrophils decreased, hemoglobin decreased, alanine aminotransferase increased, aspartate aminotransferase increased, infections, creatinine increased, platelets decreased, headache, nausea, and fatigue. ( 6 ) In patients with advanced or metastatic breast cancer, the most common (incidence ≥ 20%) adverse reactions, including laboratory abnormalities, are leukocytes decreased, neutrophils decreased, hemoglobin decreased, lymphocytes decreased, aspartate aminotransferase increased, gamma glutamyl transferase increased, alanine aminotransferase increased, infections, nausea, creatinine increased, fatigue, platelets decreased, diarrhea, vomiting, headache, constipation, alopecia, cough, rash, back pain, and glucose serum decreased. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Novartis Pharmaceuticals Corporation at 1-888-669-6682 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and the mechanism of action, KISQALI can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1)] . There are no available human data informing the drug-associated risk. In animal reproduction studies, administration of ribociclib to pregnant animals during organogenesis resulted in increased incidences of post implantation loss and reduced fetal weights in rats and increased incidences of fetal abnormalities in rabbits at exposures 0.6 or 1.5 times the exposure in humans, respectively, at the highest recommended dose of 600 mg/day based on AUC (see Data) . Advise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk of major birth defects is 2%-4% and of miscarriage is 15%-20% of clinically recognized pregnancies in the U.S. general population. Data Animal Data In embryo-fetal development studies in rats and rabbits, pregnant animals received oral doses of ribociclib up to 1000 mg/kg/day and 60 mg/kg/day, respectively, during the period of organogenesis. In rats, 300 mg/kg/day resulted in reduced maternal body weight gain and reduced fetal weights accompanied by skeletal changes related to the lower fetal weights.

Metabolism

Ribociclib exhibited over-proportional increases in exposure (C max and AUC) across the dose range of 50 mg to 1200 mg (0.083 to 2 times of the approved recommended high dose) following both single dose and repeated doses of KISQALI. Following repeated 600 mg once daily administration, steady-state was generally achieved after 8 days and ribociclib accumulated with a mean accumulation ratio of 2.5 (range, 0.97 to 6.4), and mean (coefficient of variation (CV%)) steady-state ribociclib C max was 1820 (62%) ng/mL and AUC was 23800 (66%) ng*h/mL.

• Mar 13, 2017NDANDA209092Novartis
• May 4, 2017NDANDA209935Novartis

1. 1Neutropenia3,86913%
2. 2Nausea3,69512%
3. 3Fatigue3,66612%
4. 4Malignant Neoplasm Progression2,6458.7%
5. 5Death2,5138.2%
6. 6Vomiting2,0826.8%
7. 7Diarrhoea2,0156.6%
8. 8White Blood Cell Count Decreased1,8926.2%
9. 9Pain1,8045.9%
10. 10Metastases To Bone1,6945.5%
11. 11Dyspnoea1,5745.2%
12. 12Breast Cancer Metastatic1,5685.1%
13. 13Asthenia1,5585.1%
14. 14Malaise1,5585.1%
15. 15Anaemia1,4724.8%

The 10 most recently updated of 241 ClinicalTrials.gov registrations naming Ribociclib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 435 enrolled · Stemline Therapeutics, Inc.
  NCT05563220updated 2026-06-12
• Testing Whether Hormone Therapy With Ribociclib is as Effective as Chemotherapy Followed by Hormone Therapy With Ribociclib for the Treatment of High Anatomic Stage Breast Cancer With Low Recurrence Risk, The RxFINE-Low Trial
  Recruiting · Phase 3 · Interventional · 1,978 enrolled · National Cancer Institute (NCI)
  NCT07391774updated 2026-06-12
• Study of LEE011, BYL719 and Letrozole in Advanced ER+ Breast Cancer
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 255 enrolled · Novartis Pharmaceuticals
  NCT01872260updated 2026-06-11
• Roll-over Study to Allow Continued Access to Ribociclib
  Active not recruiting · Phase 4 · Interventional · 134 enrolled · Novartis Pharmaceuticals
  NCT05161195updated 2026-06-11
• A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer
  Recruiting · Phase 1 · Phase 2 · Interventional · 316 enrolled · Hoffmann-La Roche
  NCT04802759updated 2026-06-09
• Phase IIIb Study of Ribociclib + ET in Early Breast Cancer
  Recruiting · Phase 3 · Interventional · 1,400 enrolled · Novartis Pharmaceuticals
  NCT05827081updated 2026-06-09
• [177Lu]Lu-NeoB in Combination With Ribociclib and Fulvestrant in Participants With ER+, HER2- and GRPR+ Advanced Breast Cancer
  Recruiting · Phase 1 · Interventional · 48 enrolled · Novartis Pharmaceuticals
  NCT05870579updated 2026-06-08
• Adherence and Safety of Ribociclib Plus Aromatase Inhibitors in Patients With Early Stage, HR+ and HER2- Breast Cancer
  Not yet recruiting · Phase 4 · Interventional · 90 enrolled · Institute of Oncology Ljubljana
  NCT07630948updated 2026-06-05
• The CDK4/6 Inhibitor Dosing Knowledge (CDK) Study
  Recruiting · Phase 3 · Interventional · 500 enrolled · American Society of Clinical Oncology
  NCT06377852updated 2026-06-05
• A Study to Evaluate Efficacy and Safety of Giredestrant Compared With Fulvestrant (Plus a CDK4/6 Inhibitor), in Participants With ER-Positive, HER2-Negative Advanced Breast Cancer Resistant to Adjuvant Endocrine Therapy (pionERA Breast Cancer)
  Recruiting · Phase 3 · Interventional · 1,050 enrolled · Hoffmann-La Roche
  NCT06065748updated 2026-06-04

Frequently asked questions

How does Ribociclib work?

Ribociclib is an inhibitor of cyclin-dependent kinase (CDK) 4 and 6. These kinases are activated upon binding to D-cyclins and are downstream of signaling pathways which lead to cell cycle progression and cellular proliferation.

What is Ribociclib used for?

According to FDA labeling, Ribociclib carries indications including: KISQALI is a kinase inhibitor indicated: in combination with an aromatase inhibitor for the adjuvant treatment of adults with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative stage II and III early breast cancer at high risk of recurrence. ( 1 ) for the treatment of adults with HR-positive, HER2-negative advanced or metastatic breast cancer in combination with: an aromatase inhibitor as initial endocrine-based therapy; or fulvestrant as initial endocrine-based therapy or following disease progression on endocrine therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ribociclib?

Ribociclib is classified as Cyclin-dependent kinase (CDK) inhibitors, Kinase Inhibitor, Cytochrome P450 3A Inhibitors, Kinase Inhibitors, Cellular Growth Phase Arrest, Cellular Proliferation Alteration.

What are the brand names for Ribociclib?

Ribociclib is marketed under brand names including Kisqali.

What are the contraindications for Ribociclib?

Ribociclib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.