Novartis Kisqali (ribociclib) Monograph

Kisqali (ribociclib) is a kinase inhibitor indicated for the treatment of HR-positive, HER2-negative stage II and III early breast cancer at high risk of recurrence and HR-positive, HER2-negative advanced or metastatic breast cancer. Kisqali was originally approved by the U.S. Food and Drug Administration (FDA) in March of 2017 for for the treatment of postmenopausal women with HR-positive, HER2-negative advanced or metastatic breast cancer in combination with an aromatase inhibitor as initial endocrine-based therapy.

Read on to learn more about Kisqali, including its warnings and precautions, dosage and administration information, and more.

Medication Overview:

• Brand Name: Kisqali
• Generic Name: Ribociclib
• Treatment for: Breast cancer
• Manufacturer(s): Novartis
• Initial FDA Approval: March 2017

Warnings and Precautions:

• 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.
• 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.
• 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 six cycles, and as clinically indicated. Avoid using Kisqali with drugs known to prolong QT interval and/or strong CYP3A inhibitors.
• Increased QT Prolongation with Concomitant Use of Tamoxifen: Kisqali is not indicated for concomitant use with tamoxifen.
• Hepatotoxicity: Increases in serum transaminase and bilirubin levels have been observed. Perform liver function tests (LFTs) before initiating treatment with Kisqali. Monitor LFTs every two weeks for the first two cycles, at the beginning of each subsequent four cycles, and as clinically indicated.
• Neutropenia: Perform complete blood count (CBC) before initiating therapy with Kisqali. Monitor CBC every two weeks for the first two cycles, at the beginning of each subsequent four cycles, and as clinically indicated.
• Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of potential risk to a fetus and to use effective contraception during therapy.

Dosage and Administration:

Kisqali tablets are taken orally with or without food in combination with an aromatase inhibitor or fulvestrant.

• 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 seven days off treatment.
• 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 seven days off treatment.

Dose interruption, reduction, and/or discontinuation may be required based on individual safety and tolerability. 

Contraindications:

No contraindications listed.

Drug Interactions:

• CYP3A Inhibitors: Avoid concomitant use of Kisqali with strong CYP3A inhibitors. If strong inhibitors cannot be avoided, reduce Kisqali dose.
• CYP3A4 Inducers: Avoid concomitant use of Kisqali with strong CYP3A inducers.
• CYP3A Substrates: The dose of CYP3A substrates may need to be reduced when given concurrently with Kisqali.
• Drugs Known to Prolong QT Interval: Avoid concomitant use of drugs known to prolong QT interval, such as anti-arrhythmic medicines.

Adverse Reactions:

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.

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.

Example of Ribociclib in Guidelines

• Selection of Optimal Adjuvant Chemotherapy and Targeted Therapy for Early Breast Cancer
  • American Society of Clinical Oncology (ASCO), May 2024
  • "The Panel recommends, based on the phase III NATALEE trial, that adjuvant ribociclib (400 mg once daily, 3 weeks on followed by 1 week off) for 3 years plus ET may be offered to patients with anatomic stage II or III breast cancer who would have met criteria for study entry and have a high risk of recurrence."

Please note: This article is current as of April 10, 2026. Consult our clinical guidelines library or drug information tool to ensure you always have the most up-to-date information.

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