Drug reference

Ribociclib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplasticATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AbirateroneSevereDatabaseDDInter
AcalabrutinibSevereDatabaseDDInter
AdalimumabSevereDatabaseDDInter
AdenosineSevereDatabaseDDInter

Mechanism

Ribociclib is an inhibitor of cyclin-dependent kinases 4 and 6, which are involved in cancer cell proliferation. Inhibition of these kinases results in the prevention of cancer cell growth.

Indications

Locally advanced or metastatic breast cancerHormone receptor (HR)-positive, HER2-negative advanced breast cancerbreast cancerER-positive and HER2-negative advanced or metastatic breast cancer (in combination with an aromatase inhibitor for pre-, peri-, or postmenopausal patients as initial endocrine-based therapy)ER-positive and HER2-negative advanced or metastatic breast cancer (in combination with fulvestrant for postmenopausal patients as initial endocrine-based therapy or following disease progression on endocrine therapy)In combination with endocrine therapy for high-risk, early-stage, ER-positive breast cancerFor 3 years in women with node-positive or high-risk node-negative, ER- and/or PR-positive, HER2-negative breast cancer who have completed adjuvant chemotherapyFor ER-positive metastatic breast cancer in combination with endocrine therapy

Dosing

Adult: 600 mg once daily for 21 consecutive days of repeated 28 day cycles, to be taken at approximately the same time each day, preferably in the morning. If concurrent use of potent inhibitors of CYP3A4 is unavoidable, reduce dose to 400 mg once daily; in those already taking 400 mg once daily, reduce dose to 200 mg once daily.
Max dose: 600 mg

Pharmacokinetics

Half-life

29.7 to 54.7 h (elimination)

Bioavailability

—

Protein binding

70%

Metabolism

CYP3A

Excretion

12%

Contraindications

Pre-existing QTc prolongation
Risk factors for QTc prolongation (including concomitant use of drugs known to prolong QTc interval)

Side effects

Common

AlopeciaAnaemiaAppetite decreasedAstheniaBack painConstipationCoughDecreased leucocytesDiarrhoeaDizzinessDry eyeDry mouthDyspnoeaElectrolyte imbalanceExcessive tearingFeverGastrointestinal discomfortHeadacheHepatic disordersIncreased risk of infectionNauseaNeutropeniaOropharyngeal painPeripheral oedemaQT interval prolongationnausea (>20%)fatigue (>20%)diarrhea (>20%)leukopenia (>20%)vomiting (>20%)alopecia (>20%)headache (>20%)rash (>20%)cough (>20%)

Serious

QT interval prolongation
Hepatic disorders
Increased risk of infection
Neutropenia
Anaemia
interstitial lung disease/pneumonitis
concentration-dependent increases in the QTc interval
severe cutaneous adverse reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)