Ribociclib

What is Ribociclib?

• Ribociclib (Kisqali) is a kinase inhibitor used for the treatment of certain kinds of breast cancer.

What are the uses of this medicine?

This medicine used in combination with:

• an aromatase inhibitor to treat pre/perimenopausal or postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer that has spread to other parts of the body (metastatic), as the first endocrine-based therapy; or
• fulvestrant to treat postmenopausal women with HR-positive, HER2-negative metastatic breast cancer as the first endocrine-based therapy or with disease progression following endocrine therapy.

How does this medicine work?

• Ribociclib (rye" boe sye' klib) is an orally available, small molecule inhibitor of cyclin-dependent kinases 4 and 6 that is used in combination with aromatase inhibitors in the therapy of postmenopausal women with metastatic breast cancer that is positive for the estrogen hormone receptor (ER+), but negative for human epidermal growth factor receptor 2 (HER2-).
• The cyclin kinases 4 and 6 regulate the cellular transition from the G1 to the S phase of the cell cycle acting through the retinoblastoma protein (Rb) pathway.
• Inhibition of this transition blocks the progression of the cell cycle and results in growth arrest in rapidly dividing cells.
• Components of this pathway are often mutated or overexpressed in cancer cells.
• In several clinical trials, the addition of ribociclib to letrozole (aromatase inhibitor) therapy of advanced or metastatic breast cancer (ER+, HER2-) in postmenopausal women was associated with a prolongation of disease-free but not overall survival.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid concomitant use of strong CYP3A inhibitors (e.g., boceprevir, clarithromycin, conivaptan, grapefruit juice, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, and voriconazole). If coadministration of Kisqali with a strong CYP3A inhibitor cannot be avoided, reduce the dose of Kisqali to 400 mg once daily.
• Avoid concomitant use of strong CYP3A inducers (e.g., phenytoin, rifampin, carbamazepine, and St John’s wort (Hypericum perforatum)).
• The dose of sensitive CYP3A substrates with narrow therapeutic indices may need to be reduced when given concurrently with Kisqali.
• Avoid coadministration of Kisqali with medicinal products with a known potential to prolong QT, such as antiarrhythmic medicines (including, but not limited to amiodarone, disopyramide, procainamide, quinidine, and sotalol), and other drugs that are known to prolong the QT interval (including, but not limited to, chloroquine, halofantrine, clarithromycin, haloperidol, methadone, moxifloxacin, bepridil, pimozide, and ondansetron).

Is this medicine FDA approved?

• It was approved for use in the United States in 2017.

How should this medicine be used?

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

Recommended Dosage:

• 600 mg orally (three 200 mg tablets) taken once daily with or without food for 21 consecutive days followed by 7 days off treatment.
• Dose interruption, reduction, and/or discontinuation may be required based on individual safety and tolerability.

Administration

• Take Kisqali exactly as your healthcare provider tells you.
• Do not change your dose or stop taking Kisqali unless your healthcare provider tells you.
• Take Kisqali each day at about the same time, preferably in the morning.
• You may take Kisqali with or without food.
• Swallow Kisqali tablets whole. Do not chew, crush, or split Kisqali tablets before swallowing them.
• Do not take any Kisqali tablets that are broken, cracked, or that look damaged. If you miss a dose of Kisqali or vomit after taking a dose of Kisqali, do not take another dose on that day. Take your next dose at your regular time.
• If you take too much Kisqali, call your healthcare provider right away or go to the nearest hospital emergency room.
• Inform your healthcare provider if you are pre- or perimenopausal.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 200 mg

This medicine is available in fallowing brand namesː

• Kisqali

What side effects can this medication cause?

The most common side effects of this medicine include:

• neutropenia
• diarrhea
• headache
• nausea
• leukopenia
• constipation
• infections
• vomiting
• rash
• fatigue
• hair loss
• cough

Kisqali may cause serious side effects, including:

• Lung problems
• Severe skin reactions
• Heart rhythm problems (QT prolongation)
• Liver problems

What special precautions should I follow?

• Avoid eating grapefruit and drinking grapefruit juice during treatment with Kisqali since these may increase the amount of Kisqali in your blood.
• 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.
• 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.
• Monitor electrocardiograms (ECGs) and electrolytes prior to initiation of treatment with Kisqali. Repeat ECGs at approximately Day 14 of the first cycle and at the beginning of the second 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.
• Kisqali is not indicated for concomitant use with tamoxifen.
• Increases in serum transaminase 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.
• Kisqali may cause neutropenia. Perform complete blood count (CBC) before initiating therapy with Kisqali. Monitor CBC every 2 weeks for the first 2 cycles, at the beginning of each subsequent 4 cycles, and as clinically indicated.
• Kisqali Can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception during therapy.

What to do in case of emergency/overdose?

• There is limited experience with reported cases of overdose with Kisqali in humans.

management for overdosage:

• General symptomatic and supportive measures should be initiated in all cases of overdose where necessary.

Can this medicine be used in pregnancy?

• Based on findings from animal studies and the mechanism of action, Kisqali can cause fetal harm when administered to a pregnant woman.

Can this medicine be used in children?

• The safety and efficacy of Kisqali in pediatric patients has not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: ribociclib
• Inactive ingredients: colloidal silicon dioxide, crospovidone, hydroxypropylcellulose, magnesium stearate, and microcrystalline cellulose. The film-coating contains iron oxide black, iron oxide red, lecithin (soya), polyvinyl alcohol (partially hydrolyzed), talc, titanium dioxide, and xanthan gum.

Who manufactures and distributes this medicine?

• Distributed by:
• Novartis Pharmaceuticals Corporation
• East Hanover, New Jersey

What should I know about storage and disposal of this medication?

• Store Kisqali at 68°F to 77°F (20°C to 25°C).
• Keep Kisqali in the original container.
• Keep Kisqali and all medicines out of the reach of children.

• Dailymed label info on Ribociclib
• FDA Ribociclib

Ribociclib Resources
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