🔴 Red Flag (Important) Information
QT prolongation: monitor ECGs - risk of serious arrhythmia
Hepatotoxicity: Monitor LFTs
Neutropenia: Frequent and potentially severe.
Interstitial Lung Disease (ILD) / Pneumonitis: Rare but potentially fatal. Monitor for new or worsening cough, dyspnoea, or hypoxia — stop immediately if suspected.
Contraindicated in pregnancy, breastfeeding, and in patients allergic to soya or peanuts (contains soya lecithin).
Generic name: Ribociclib
Brand name: Kryxana
Drug class: Cyclin-dependent kinase (CDK) 4/6 inhibitor
Formulation: Film-coated tablets, 200 mg
Mechanism of action:
Inhibits CDK4/6 → blocks phosphorylation of retinoblastoma (Rb) protein → arrests cell cycle in G1 → inhibits proliferation of HR⁺, HER2⁻ breast cancer cells.
HR-positive, HER2-negative locally advanced or metastatic breast cancer
In combination with an aromatase inhibitor or fulvestrant.
In premenopausal/perimenopausal women, combine with an LHRH agonist (e.g. leuprolide).
Standard dose: 600 mg (3 × 200 mg tablets) orally once daily for 21 days, followed by 7 days off (28-day cycle).
With or without food: Either.
Missed dose: Skip if >12 hours late; do not double up.
Adjustments:
Grade ≥3 toxicity → hold until ≤Grade 1, then resume at 400 mg or 200 mg as tolerated.
QTcF >500 ms → hold; resume only if <480 ms and at reduced dose.
Strong CYP3A4 inhibitor → reduce to 400 mg daily.
Hypersensitivity to ribociclib, soya, or peanut.
Concomitant QT-prolonging drugs or strong CYP3A4 modulators.
Pregnancy or breastfeeding.
Severe or unstable cardiac disease.
QT monitoring: ECGs at baseline, day 14, start of cycle 2, then as indicated.
Liver function: Check LFTs baseline, day 14, and periodically.
FBC: Monitor for neutropenia pattern.
Respiratory: Stop if ILD/pneumonitis suspected.
Diet: Avoid grapefruit juice (CYP3A4 inhibition).
Very common (>10%)
Neutropenia, nausea, fatigue, alopecia, increased LFTs, diarrhoea, vomiting.
Common (1–10%)
QT prolongation, infection, thrombocytopenia, anaemia, rash, decreased appetite.
Serious (uncommon)
Hepatotoxicity, ILD/pneumonitis, severe neutropenia with fever, Stevens–Johnson syndrome.
Elderly: No dose adjustment required.
Hepatic impairment: Mild–moderate: no change; severe: use with caution and frequent LFTs.
Renal impairment: Mild–moderate: no change; caution if severe.
Pregnancy: Contraindicated — teratogenic. Use effective non-hormonal contraception during and for 21 days after therapy.
Breastfeeding: Contraindicated.
Continue until disease progression or unacceptable toxicity.
Interrupt / reduce dose for:
Grade ≥3 neutropenia or elevated ALT/AST.
QTcF >480 ms.
Permanently discontinue for:
QTcF >500 ms or serious arrhythmia.
ALT/AST >5× ULN or concurrent bilirubin >2× ULN.
Confirmed ILD/pneumonitis or hypersensitivity.
Switch therapy when:
Disease progression occurs (consider alternate endocrine ± targeted therapy).
Persistent or recurrent Grade ≥3 toxicity despite dose reduction.
https://pi-pil-repository.sahpra.org.za/wp-content/uploads/2022/08/Kryxana-PI-21-July-2022.pdf
| Generic Name | Ribociclib |
|---|---|
| Drug Class | CDK 4/6 Inhibitors |
| Cost | |
| Company | |
|---|---|
| Drug Rep | Admin |
| Indications | Breast Cancer |
| Dosage |