Ribociclib

Pronunciation: RYE-boe-SYE-klib
Brand name: Kisqali
Dosage form: tablets (200 mg)
Drug class: CDK 4/6 inhibitors

Medically reviewed by Melisa Puckey, BPharm. Last updated on Jul 9, 2024.

What is ribociclib?

Ribociclib is a targeted treatment used to treat breast cancer that is hormone receptor-positive, HER2-negative breast and has spread (metastasized) or cannot be removed by surgery.  Ribociclib is given in combination with other cancer medicines such as letrozole (Femara) or fulvestrant (Faslodex).

Ribociclib may help slow cancer growth and increase patients' overall survival, which means it may add more days to a person's life.

Ribociclib works by blocking proteins called CDK 4 and CDK 6, which have a role in cancer cells growing and dividing, by blocking the proteins helps to slow or stop cancer growth.

Ribociclib's brand name is Kisqali by Novartis, and is available as tablets that are taken once a day.

Who can take ribociclib?

Ribociclib is FDA approved for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer in combination with:

• an aromatase inhibitor as initial endocrine-based therapy; or
• fulvestrant as initial endocrine-based therapy or following disease progression on endocrine therapy in postmenopausal women or in men.

Ribociclib side effects

Common ribociclib side effects 

Common ribociclib side effects are low white blood cells, infections, cough, nausea, vomiting, diarrhea, constipation, feeling tired, rash, headache; or hair loss.

Serious ribociclib side effects 

Get emergency medical help if you have signs of an allergic reaction (hives, difficult breathing, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning eyes, skin pain, red or purple skin rash with blistering and peeling).

Seek medical treatment if you have a serious drug reaction that can affect many parts of your body. Symptoms may include: skin rash, fever, swollen glands, muscle aches, severe weakness, unusual bruising, or yellowing of your skin or eyes.

Ribociclib may cause serious side effects. Call your doctor at once if you have:

• fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness (like you might pass out);
• low white blood cell counts--fever, mouth sores, skin sores, sore throat, cough, trouble breathing;
• signs of inflammation in the lungs--new or worsening cough, painful or difficult breathing, wheezing, feeling short of breath even while resting; or
• liver problems--loss of appetite, upper stomach pain, tiredness, easy bruising or bleeding, dark urine, jaundice (yellowing of the skin or eyes).

Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Related/similar drugs

Enhertu, Ibrance, Trodelvy, Arimidex, Femara, Verzenio, Xeloda

Warnings

Ribociclib can cause serious side effects on your heart, liver, or lungs. Call your doctor at once if you have chest pain, fast or pounding heartbeats, trouble breathing, cough (with or without mucus), sudden dizziness, right-sided upper stomach pain, loss of appetite, unusual bleeding or bruising, dark urine, or yellowing of your skin or eyes.

Increased QT Prolongation can occur with concurrent use of tamoxifen.

Severe cutaneous adverse reactions (SCARs) can occur with this medicine.

Neutropenia (low neutrophils, a type of white blood cell) can occur with this medicine. You will have complete blood count (CBC) before starting treatment with this medicine, and  will have your CBC monitored every 2 weeks for the first 2 cycles, at the beginning of each subsequent 4 cycles, and as clinically indicated.

You will need frequent medical tests while taking ribociclib. Your cancer treatments may be delayed based on the results of these tests. Tell your doctor if you have signs of infection, such as fever or chills.

Kisqali can cause fetal harm when administered to a pregnant woman.

Before taking this medicine

You should not use ribociclib if you are allergic to it or any of the inactive ingredients in this medicine.

You should not use ribociclib if you also take tamoxifen.

Your doctor will perform blood tests to make sure you do not have conditions that would prevent you from safely using ribociclib.

Tell your doctor if you have ever had:

• slow heartbeats;
• heart disease or prior heart attack;
• long QT syndrome;
• an electrolyte imbalance (such as low levels of calcium, magnesium, phosphorus, or potassium in your blood);
• liver disease;
• kidney disease; or
• signs of infection (fever, chills).

If you are a women, tell your doctor whether or not you have gone through menopause.

Pregnancy

You may need to have a negative pregnancy test before starting this treatment.

Do not use ribociclib if you are pregnant. It could harm the unborn baby. Use effective birth control to prevent pregnancy while you are using ribociclib and for at least 3 weeks after your last dose.

This medicine may affect fertility (ability to have children) in men. Talk with your doctor if you have concerns about this risk.

Breastfeeding

You should not breastfeed while using this medicine and for at least 3 weeks after your last dose.

How should I take ribociclib?

Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.

Ribociclib is given in a 28-day treatment cycle. You will take the medicine for the first 21 days of each cycle, followed by 7 days off. Your doctor will determine how long to treat you with ribociclib.

Swallow the tablet whole and do not crush, chew, or break it.

Take the medicine at the same time each morning, with or without food.

If you vomit after taking the medicine, wait until the next day to take your next dose.

Do not use a broken or damaged pill.

You may need frequent medical tests to be sure ribociclib is not causing harmful effects. Your cancer treatments may be delayed based on the results.

Store ribociclib in the original container at room temperature, away from moisture and heat.

Ribociclib dosing information

Usual Adult Dose for Breast Cancer

Dose: 600 mg (three 200 mg tablets) orally once a day for 21 consecutive days followed by 7 days off for a complete cycle of 28 days. Patients should take their tablets at approximately the same time each day, preferably in the morning.  

When given with Kisqali is given with an aromatase inhibitor, refer to the Full Prescribing Information for the recommended dose of the aromatase inhibitor being used.

When given with Kisqali is given with fulvestrant, the recommended dose of fulvestrant is 500 mg administered on Days 1, 15, 29, and once monthly thereafter. Please refer to the Full Prescribing Information of fulvestrant. 

Pre/perimenopausal women, or men, treated with the combination Kisqali plus an aromatase inhibitor should be treated with a luteinizing hormone-releasing hormone (LHRH) agonist according to current clinical practice standards. 

Men treated with the combination of Kisqali plus fulvestrant should be treated with a luteinizing hormone-releasing hormone (LHRH) agonist according to current clinical practice standards. 

If the patient vomits after taking the dose, or misses a dose, no additional dose should be taken that day. The next prescribed dose should be taken at the usual time. Tablets should be swallowed whole (tablets should not be chewed, crushed or split prior to swallowing). No tablet should be ingested if it is broken, cracked, or otherwise not intact. 

Duration of treatment: Continue until disease progression or unacceptable toxicity

Dose modifications: Dose should be modified for drug interactions, adverse reactions and hepatic imairment.

Click on the link below for more detailed dosing information.

What happens if I miss a dose?

Skip the missed dose. Take your next dose at the regular time and stay on your once-daily schedule. Do not use 2 doses in one day.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking ribociclib?

Grapefruit may interact with ribociclib and lead to unwanted side effects. Avoid the use of grapefruit products.

Avoid taking an herbal supplement containing St. John's wort at the same time you are taking ribociclib.

What other drugs will affect ribociclib?

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.

Ribociclib can cause a serious heart problem. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.

Many drugs can affect ribociclib. This includes prescription and over-the-counter medicines, vitamins, and herbal products. 

CYP3A4 Inhibitors: Avoid concomitant use of ribociclib with strong CYP3A inhibitors. If strong inhibitors cannot be avoided, reduce ribociclib dose. 

CYP3A4 Inducers: Avoid concomitant use of ribociclib with strong CYP3A inducers. 

CYP3A Substrates: The dose of sensitive CYP3A substrates with narrow therapeutic indices may need to be reduced when given concurrently with ribociclib. 

Drugs Known to Prolong QT Interval: Avoid concomitant use of drugs known to prolong QT interval, such as anti-arrhythmic medicines

Not all possible interactions are listed here. Tell your doctor about all your current medicines and any medicine you start or stop using.

Kisqali (Ribociclib) Package Insert 

Review the Kisqali (Ribociclib) Package Insert for more detailed information about this medicine. Discuss any medical questions you have with your doctor or other health care provider. This is not all the information you need to know about this medicine for safe and effective use, and it does not take the place of talking to your doctor about your treatment.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer