Ribociclib
KISQALI
Pronunciation: rye-boe-SYE-klib (kis-KAH-lee)
“Kiss koala, rib-o side-clip”
What it isCDK4/6 inhibitor; hormone receptor-positive HER2-negative breast cancer.
Why this oneIt is the CDK4/6 inhibitor with the clearest overall survival benefit in first-line advanced disease.
What limits itQT prolongation requiring ECG monitoring, and neutropenia. CYP3A4-dependent.
FDA-approved for
- HR-positive/HER2-negative breast cancer (2017)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HR+/HER2- early breast cancer, adjuvant (w/ aromatase inhibitor) | adult | 400 mg QD, 21 days on / 7 off | 400 mg QD, 21 days on / 7 off | 400 mg QD |
| HR+/HER2- advanced or metastatic breast cancer (w/ aromatase inhibitor or fulvestrant) | adult | 600 mg QD, 21 days on / 7 off | 600 mg QD, 21 days on / 7 off | 600 mg QD |
Renal Mild-moderate: no adjustment; severe: reduce starting dose to 200 mg
Hepatic Mild (Child-Pugh A): no adjustment; moderate-severe (B/C) in advanced disease: start 400 mg (no adjustment for early breast cancer)
Given in 28-day cycles: 21 days on, 7 days off
Instructions
- Swallow whole; do not chew, crush, or split; do not take broken/cracked tablets
- With or without food, same time each day (preferably morning)
- Pre/perimenopausal women and men: add an LHRH agonist
- Missed or vomited dose: skip, take next dose at usual time
- Strong CYP3A inhibitor: avoid; if unavoidable reduce to 200 mg (early) or 400 mg (advanced)
Available strengths
- tab 200 mg
Cautions
- Interstitial lung disease/pneumonitis (can be fatal); interrupt and evaluate new respiratory symptoms
- Severe cutaneous adverse reactions (SJS, TEN, DRESS); discontinue if confirmed
- QT interval prolongation (concentration-dependent); monitor ECG and electrolytes; avoid QT-prolonging drugs and strong CYP3A inhibitors
- Not for concomitant use with tamoxifen (increased QT prolongation)
- Hepatotoxicity; monitor LFTs
- Neutropenia; monitor CBC
- Embryo-fetal toxicity
Adverse reactions
- Neutropenia/leukopenia
- Anemia
- Lymphopenia
- Increased AST/ALT/GGT
- Increased creatinine
- Infections
- Nausea/vomiting
- Diarrhea
- Fatigue
- Thrombocytopenia
- Headache
- Alopecia
- Rash
Pregnancy Can cause fetal harm (animal embryo-fetal toxicity); no human data; effective contraception during and ≥3 weeks after last dose
Lactation Do not breastfeed during and for at least 3 weeks after the last dose
Cost
| Strength | #/mo | generic $/mo | brand $/mo | CostPlus | |
|---|---|---|---|---|---|
| 200 mg | tab | 30 qd | — | $9,549.95 | not offered |
Generic entry2036 est.
NO BOXED WARNINGS
Principal riskQT prolongation needing ECG monitoring
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
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