ribociclib

Trade Name:

Kisqali™

Other Names:

Kisqali™

Appearance:

Tablet

Monograph Name:

ribociclib

Monograph Body:

Drug Monograph

A - Drug Name

ribociclib

COMMON TRADE NAME(S): Kisqali™

B - Mechanism of Action and Pharmacokinetics

Ribociclib is an inhibitor of cyclin-dependent kinase (CDK) 4 and 6. The cyclin D-CDK4/6 complex regulates cell cycle progression through phosphorylation of the retinoblastoma protein (pRb). Inhibition of pRb phosphorylation arrests the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth.

Absorption

Effects with food

No clinically significant effect on Cmax and AUC when administered with a high-fat, high-calorie meal

Peak plasma levels

1 to 4 hours

Time to reach steady state

8 days

Bioavailability

66% (after a single dose)

Distribution

PPB

70%

Distribution Sites

Equally distributed between red blood cells and plasma

Cross blood brain barrier?

Relatively low brain penetration observed in animals with intact blood brain barriers.

Metabolism

Ribociclib undergoes extensive hepatic metabolism mainly via CYP3A4.
No major metabolite was considered to have clinically relevant contribution to efficacy and safety.

Active metabolites

Inactive metabolites

Yes

Elimination

Ribociclib is eliminated mainly via the feces, with a small contribution from the renal route.

Half-life

32 hours

Feces

69% (total dose); 17% unchanged

Urine

23% (total dose); 12% unchanged

C - Indications and Status

Health Canada Approvals:

Breast cancer

Refer to the product monograph for a full list and details of approved indications.

D - Adverse Effects

Emetogenic Potential:

Minimal – No routine prophylaxis; PRN recommended

The adverse effects reported below were based on a phase III study of postmenopausal women with breast cancer, receiving ribociclib plus letrozole or placebo plus letrozole, where the incidence was > 2% more than placebo. Severe or life-threatening adverse effects from other sources and post-marketing are also included.

ORGAN SITE	SIDE EFFECT* (%)	ONSET**
Cardiovascular	QT interval prolonged (5%) (1% severe)	E
	Venous thromboembolism (4%) (may be severe)	E
Dermatological	Alopecia (35%)	E
	Rash, pruritus (24%) (may be severe)	I E
	Toxic epidermal necrolysis (rare)	E
Gastrointestinal	Abdominal pain (21%)	E
	Anorexia, weight loss (22%)	E
	Constipation (30%)	E
	Diarrhea (41%) (2% severe)	E
	Dry mouth (14%)	E
	Dyspepsia (11%)	I E
	Mucositis (16%)	E
	Nausea, vomiting (55%) (3% severe)	I
General	Edema - limbs (19%)	E
	Fatigue (43%)	E
Hematological	Myelosuppression ± infection, bleeding (77%) (64% severe)	E
Hepatobiliary	↑ LFTs (23%) (12% severe; <1% hepatotoxicity)	D
Metabolic / Endocrine	Abnormal electrolyte(s) (5%) (↓ Ca, ↓ K, ↓ PO4; 4% severe)	E
Musculoskeletal	Musculoskeletal pain (27%)	E
Nervous System	Dysgeusia (10%)	E
	Headache (29%)	E
	Insomnia (17%)	E
	Syncope (2%)	E
Ophthalmic	Dry eye (6%)	E
	Watering eyes (12%)	E
Renal	Creatinine increased (11%) (< 1% severe)	E
Respiratory	Dyspnea (16%)	E
	Pneumonitis (rare) (may be severe)	E D

* "Incidence" may refer to an absolute value or the higher value from a reported range.
"Rare" may refer to events with < 1% incidence, reported in post-marketing, phase 1 studies,
isolated data or anecdotal reports.

** I = immediate (onset in hours to days) E = early (days to weeks)
D = delayed (weeks to months) L = late (months to years)

The most common side effects for ribociclib include myelosuppression ± infection, bleeding, nausea, vomiting, fatigue, diarrhea, alopecia, constipation, headache, musculoskeletal pain, rash, pruritus, and ↑ LFTs.

Neutropenia was the most frequently reported side effect in patients treated with ribociclib plus any combination. The median time to onset for Grade > 2 neutropenia was 17 days, while the median time to resolution to Grade < 3 was 12 days.

Drug induced liver injury [ALT or AST > 3 x upper limit of normal (ULN) and total bilirubin > 2 x ULN, without cholestasis] or Hy’s Law has been reported with ribociclib combination therapy. In patients treated with ribociclib plus letrozole or fulvestrant, recovery to normal levels occurred within 154 days or within 121 to 532 days, respectively, after ribociclib discontinuation.

Median time to onset of QTcF > 480 msec was 15 days regardless of combination and these changes were reversible upon withholding the dose or modification. QTc prolongation is expected to be maximal between days 8 to 21 of the 28-day cycle during steady state treatment.

E - Dosing

Refer to protocol by which the patient is being treated.

Screen for hepatitis B virus in all cancer patients starting systemic treatment. Refer to the hepatitis B virus screening and management guideline.

Hypokalemia, hypomagnesemia and hypocalcemia should be corrected prior to starting or continuing ribociclib.

Ribociclib should be started only in patients with QTcF < 450 msec.

Pre/perimenopausal women, and men, treated with ribociclib and an aromatase inhibitor or fulvestrant should also be treated with luteinizing hormone-releasing hormone (LHRH) agonists according to local clinical practice.

Adults:

Advanced or Metastatic Breast Cancer:

Oral: 600 mg/day on Days 1 to 21, followed by 7 days off treatment, in 28-day cycles

In combination with an aromatase inhibitor (e.g., letrozole) or fulvestrant. Refer to regimen monographs for dosing details.

Early Breast Cancer:

Refer to the product monograph for details.

Dosage with Toxicity:

Advanced or Metastatic Breast Cancer:

Dose Level	Ribociclib Dose (mg/day) (21 days on, 7 days off)
0	600
-1	400
-2	200
-3	Discontinue

Toxicity	Severity		Ribociclib Dose
Neutropenia	Grade 3 (ANC 0.5 to <1 x 10⁹/L)		Hold dose until ANC > 1 x 10⁹/L, then restart at the same dose level. If recurs, hold dose until ANC > 1 x 10⁹/L, then restart with 1 dose level ↓.
	Grade 4 (ANC <0.5 x 10⁹/L) or febrile neutropenia		Hold dose until ANC > 1 x 10⁹/L, then restart with 1 dose level ↓.
QTcF	> 480 msec		Hold dose until QTcF resolves to < 480 msec, then restart with 1 dose level ↓. If recurs, hold dose until QTcF resolves to < 480 msec, then restart with 1 dose level ↓.
	> 500 msec		Hold dose until QTcF resolves to < 480 msec, then restart with 1 dose level ↓.
Torsade de Pointes, or polymorphic ventricular tachycardia, unexplained syncope or Signs/symptoms of serious arrhythmia	Any		Discontinue.
Bilirubin ≤ 2 x ULN	and	AST and/or ALT >3 to 5 x ULN (Grade 2)	If Baseline Grade 2: continue at current dose. If Baseline Grade 0-1: hold dose until ≤ baseline, then restart at the same dose. If recurs, hold dose until ≤ baseline, then restart with 1 dose level ↓.
	and	AST and/or ALT >5 to 20 x ULN (Grade 3)	Hold dose until ≤ baseline, then restart with 1 dose level ↓. If recurs, discontinue.
	and	AST and/or ALT >20 x ULN (Grade 4)	Discontinue.
Bilirubin > 2 x ULN, in the absence of cholestasis	and	AST and/or ALT >3 x ULN (Grade > 2) irrespective of baseline	Discontinue.
Interstitial lung disease (ILD)/pneumonitis	Grade 2 (symptomatic)		Hold dose until recovery to Grade < 1, then restart with 1 dose level ↓.
	Grade 3 or 4		Discontinue.
Severe cutaneous reactions (e.g. progressive widespread skin rash often with blisters or mucosal lesions)	Any		Discontinue.
Other related toxicity	Grade 3		Hold dose until Grade ≤ 1, then restart at same dose. If recurs, hold dose until Grade ≤ 1, then restart with 1 dose level ↓.
	Grade 4		Discontinue.

Dosage with Hepatic Impairment:

Ribociclib has not been studied in patients with moderate or severe hepatic impairment (ALT or AST > 5 x ULN or total serum bilirubin > ULN [except documented Gilbert’s syndrome]).

Advanced or Metastatic Breast Cancer:

Hepatic Impairment	Ribociclib Starting Dose
Mild (Child-Pugh class A)	No dose adjustment recommended
Moderate (Child-Pugh class B)	400 mg once daily; initiate treatment only if benefit outweighs risk
Severe (Child-Pugh class C)	400 mg once daily; initiate treatment only if benefit outweighs risk

Dosage with Renal Impairment:

Advanced or Metastatic Breast Cancer:

Creatinine Clearance^†	Ribociclib Starting Dose
≥ 30	No dose adjustment recommended.
15 to < 30	200 mg daily*; initiate treatment only if benefit outweighs risk.
< 15	No data available.

^†Reported as eGFR (mL/min/1.73m²)

*No data in breast cancer patients; data from healthy or non-cancer patients with severe renal impairment.

Dosage in the elderly:

No adjustment of the starting dose is required. No overall difference in safety was observed between patients over 65 years of age and younger patients.

Dosage based on gender:

No clinically relevant effects of gender on ribociclib pharmacokinetics parameters.

Dosage based on ethnicity:

No clinically relevant effects of race on ribociclib pharmacokinetics parameters.

Children:

The safety and efficacy of ribociclib in pediatric patients have not been established.

F - Administration Guidelines

Administer ribociclib with or without food, approximately at the same time each day, preferably in the morning.
Tablets should be swallowed whole and not chewed, crushed or split prior to swallowing. Tablets that are broken, cracked, or otherwise not intact should not be ingested.
If the patient vomits after taking ribociclib, do not give an extra dose; give the next dose at the usual time.
If a dose is missed, it should be skipped and the next dose given at the usual time, the next day. Patients should not take extra doses to make up for a missed dose.
Grapefruit, starfruit, Seville oranges, their juices or products should be avoided during ribociclib treatment.
Confirm the storage information that is listed on the product packaging. There is a new ribociclib supply that requires storage in a refrigerator between 2-8°C. Once dispensed, patients should store ribociclib between 20-25°C for up to 2 months. Keep in the original package to protect from moisture.

G - Special Precautions

Contraindications:

Patients with hypersensitivity to this drug or to any ingredient in the formulation.
Patients with untreated congenital long QT syndrome, a QTcF interval of ≥ 450 msec at baseline, and those who are at significant risk of developing QTc prolongation (for example, uncontrolled or significant cardiac disease including recent myocardial infarction, congestive heart failure, unstable angina and bradyarrhythmia).

Other Warnings/Precautions:

Ribociclib is associated with concentration-dependent QTc prolongation, with expected maximal QTc prolongation during steady state treatment between days 8 and 21 of the 28-day cycle.
Exercise caution in patients who are suspected to be at an increased risk of Torsades de Pointes during treatment with a QT-prolonging drug.
Avoid use in patients with uncorrected hypokalemia, hypomagnesemia, or hypocalcemia and other risk factors.
Use in caution in patients at risk of thromboembolic events.
Patients should exercise caution when driving or operating machinery due to syncope.

Other Drug Properties:

Carcinogenicity: Unknown
Phototoxicity: Unlikely

Pregnancy and Lactation:

Genotoxicity: No
Embryotoxicity: Documented in animals
Fetotoxicity: Documented in animals
Teratogenicity: Documented in animals
Pregnancy:
Ribociclib is not recommended for use in pregnancy. Adequate contraception should be used by patients and their partners during treatment, and for at least 21 days after the last dose.
Excretion into breast milk: Documented in animals
Breastfeeding:
Breastfeeding is not recommended during treatment and for at least 21 days after the last dose.
Fertility effects: Probable

Documented in animal studies in male animals

H - Interactions

Ribociclib is primarily metabolized by CYP3A is a time-dependent inhibitor of CYP3A. Therefore, medicinal products which can influence CYP3A enzyme activity may alter the pharmacokinetics of ribociclib and ribociclib can affect the pharmacokinetics of co-administered CYP3A substrates. Ribociclib has weak inhibitory effects on CYP1A2 substrates though no induction of CYP1A2, CYP2B6, CYP2C9 or CYP3A4 was observed in vitro.
Ribociclib may inhibit BCRP, OCT2, Multidrug and Toxic Compound Extrusion Protein-1 (MATE1) and human Bile Salt Export Pump (BSEP). Monitor patients closely when co-administering ribociclib and substrates of these transporters.
There is no clinically relevant interaction with letrozole, exemestane, anastrozole or fulvestrant.
There is no expected interaction with goserelin.

AGENT	EFFECT	MECHANISM	MANAGEMENT
CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, ritonavir, fruit or juice from grapefruit, Seville oranges or starfruit)	↑ ribociclib exposure (e.g. ritonavir ↑ ribociclib exposure by 3.2-fold)	↓ metabolism of ribociclib	Avoid strong CYP3A4 inhibitors. If unavoidable, ↓ ribociclib dose by 200mg (i.e. from 600mg to 400mg). After discontinuation of strong CYP3A4 inhibitor, resume ribociclib dose used prior to initiating the CYP3A4 inhibitor (after a washout period of at least 5 half-lives). Monitor closely.
CYP3A4 inducers (e.g. phenytoin, rifampin, dexamethasone, carbamazepine, phenobarbital, St. John’s Wort, etc)	↓ ribociclib exposure (e.g. rifampin ↓ ribociclib exposure by 89%)	↑ metabolism of ribociclib	Avoid strong CYP3A4 inducers.
CYP3A4 substrates with narrow therapeutic index (e.g. alfentanil, cyclosporine, dihydroergotamine, ergotamine, everolimus, fentanyl, midazolam, pimozide, quinidine, sirolimus and tacrolimus)	↑ CYP3A4 Substrate exposure (e.g. ribociclib ↑ midazolam exposure by 280%)	↓ metabolism of CYP3A4 Substrate	Avoid CYP3A4 substrates with a narrow therapeutic index. If unavoidable, consider reducing dose of substrate.
Drugs that may prolong QT (e.g. amiodarone, procainamide, sotalol, venlafaxine, amitriptyline, sunitinib, methadone, chloroquine, clarithromycin, haloperidol, fluconazole, moxifloxacin, domperidone, ondansetron, etc)	↑ risk of QT prolongation	Additive	Avoid concomitant use. If must co-administer, monitor as clinically indicated.
Drugs that disrupt electrolyte levels (e.g. loop/thiazide diuretics, laxatives, amphotericin B, high dose corticosteroids)	serum electrolyte imbalance	↓ electrolyte levels	Avoid to the extent possible.
Drugs that reduce heart rate (e.g. beta blockers, calcium channel blockers, digoxin)	↑ risk of arrhythmia		Avoid to the extent possible.
Tamoxifen	↑ risk of QT prolongation	↑ tamoxifen exposure by 2-fold with co-administration	Combined use is not recommended.
Statins	↑ risk of rhabdomyolysis	CDK inhibitors may ↑ statin exposure (Health Canada, 2025)	Consider close monitoring

I - Recommended Clinical Monitoring

Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.

Refer to the hepatitis B virus screening and management guideline for monitoring during and after treatment.

Recommended Clinical Monitoring

Monitor Type	Monitor Frequency
CBC	Baseline, every 2 weeks for the first 2 cycles, at the beginning of each subsequent 4 cycles and as clinically indicated
Liver function tests	Baseline, every 2 weeks for the first 2 cycles, at the beginning of each subsequent 4 cycles and as clinically indicated (more frequent monitoring required in patients with ≥ Grade 2 LFTs)
Electrolytes, including potassium, magnesium, calcium, and phosphorous	Baseline, at regular intervals during steady-state treatment in later cycles and as clinically indicated (for example, patients with QTc prolongation)
ECG	Baseline, repeat on day 14 of cycle 1, and then as clinically indicated (more frequent monitoring in patients at risk)
Renal function tests	Baseline and as clinically indicated
Clinical toxicity assessment of infection, bleeding, thromboembolism (close monitoring in patients at risk), pneumonitis, gastrointestinal and skin effects, and fatigue	At each visit

Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version

J - Supplementary Public Funding

Exceptional Access Program (EAP Website )

ribociclib - For the treatment of patients with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER 2)-negative, unresectable locally advanced or metastatic breast cancer in combination with an aromatase inhibitor or fulvestrant according to clinical criteria

K - References

Hortobagyi, G. N. et al. Ribociclib as first-line therapy for HR-positive, advanced breast cancer. New Engl. J. Med. 375, 1738–1748 (2016).

Product monograph: Kasqali (ribociclib). Novartis Pharmaceuticals. June 12, 2025.

Summary Safety Review - Cyclin-dependent Kinase Inhibitors (abemaciclib, palbociclib and ribociclib) and HMG-CoA Reductase Inhibitors (atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastatin and simvastatin) (Statins) - Assessing the Potential Risk of Rhabdomyolysis Due to Drug Interaction. Health Canada. Accessed April 25, 2025.

September 2025 Updated Pharmacokinetics, Adverse Effects, Dosing, Administration Guidelines, Pregnancy/Lactation, Interactions, and Monitoring sections

L - Disclaimer

Refer to the New Drug Funding Program or Ontario Public Drug Programs websites for the most up-to-date public funding information.
The information set out in the drug monographs, regimen monographs, appendices and symptom management information (for health professionals) contained in the Drug Formulary (the "Formulary") is intended for healthcare providers and is to be used for informational purposes only. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects of a particular drug, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for a given condition. The information in the Formulary is not intended to constitute or be a substitute for medical advice and should not be relied upon in any such regard. All uses of the Formulary are subject to clinical judgment and actual prescribing patterns may not follow the information provided in the Formulary.
The format and content of the drug monographs, regimen monographs, appendices and symptom management information contained in the Formulary will change as they are reviewed and revised on a periodic basis. The date of last revision will be visible on each page of the monograph and regimen. Since standards of usage are constantly evolving, it is advised that the Formulary not be used as the sole source of information. It is strongly recommended that original references or product monograph be consulted prior to using a chemotherapy regimen for the first time.
Some Formulary documents, such as the medication information sheets, regimen information sheets and symptom management information (for patients), are intended for patients. Patients should always consult with their healthcare provider if they have questions regarding any information set out in the Formulary documents.
While care has been taken in the preparation of the information contained in the Formulary, such information is provided on an “as-is” basis, without any representation, warranty, or condition, whether express, or implied, statutory or otherwise, as to the information’s quality, accuracy, currency, completeness, or reliability.
CCO and the Formulary’s content providers shall have no liability, whether direct, indirect, consequential, contingent, special, or incidental, related to or arising from the information in the Formulary or its use thereof, whether based on breach of contract or tort (including negligence), and even if advised of the possibility thereof. Anyone using the information in the Formulary does so at his or her own risk, and by using such information, agrees to indemnify CCO and its content providers from any and all liability, loss, damages, costs and expenses (including legal fees and expenses) arising from such person’s use of the information in the Formulary.

Info Sheet Name:

ribociclib (patient)

Info Sheet Introduction:

For treating a certain type of breast cancer. Ribociclib is given together with another medication.

Info Sheet Date: Vendredi, septembre 12, 2025 Info Sheet body:

ribociclib

Pronunciation:

rye-boe-SYE-klib

Other Name(s):

Kisqali™

Appearance:

Tablet

This handout gives general information about this cancer medication.

You will learn:

who to contact for help
what the medication is
how it is given
what to expect while on medication

This handout was created by Ontario Health (Cancer Care Ontario) together with patients and their caregivers who have also gone through cancer treatment. It is meant to help support you through your cancer treatment and answer some of your questions.

This information does not replace the advice of your health care team. Always talk to your health care team about your treatment.

Who do I contact if I have questions or need help?

My cancer health care provider is: _____________________________________________

During the day I should contact: _______________________________________________

Evenings, weekends and holidays: _____________________________________________

This page gives general information about this cancer medication.

You will learn:

who to contact for help
what the medication is
how it is given
what to expect while on this medication

This information was created by Ontario Health (Cancer Care Ontario) together with patients and their caregivers who have also gone through cancer treatment. It is meant to help support you through your cancer treatment and answer some of your questions.

This information does not replace the advice of your health care team. Always talk to your health care team about your treatment.

What is this treatment for?

For treating a certain type of breast cancer. Ribociclib is given together with another medication.

What should I do before I start this treatment?

Tell your health care team if you have or had significant medical condition(s), especially if you have / had:

heart problems (including irregular heartbeat or heart rate),
a family history of severe heart problems,
low salt levels in your blood (such as low calcium, magnesium, phosphorous, or potassium),
liver, kidney problems, or
any allergies.

Remember To:

Tell your health care team about all of the other medications you are taking.
Keep taking other medications that have been prescribed for you, unless you have been told not to by your health care team.

You will have a blood test to check for hepatitis B before starting treatment. See the Hepatitis B and Cancer Medications pamphlet for more information.

How is this treatment given?

This medication is usually taken once a day by mouth for 21 days followed by a 7 day break with no ribociclib treatment. Talk to your health care team about how and when to take your medication.
Take the dose at about the same time each day, preferably in the morning.
Swallow whole with a glass of water, with or without food.
Do not crush, chew or split the tablets.
If you miss a dose, skip this and take your next dose as you normally do. Do not take an extra dose to make up for the missed dose.
If you vomit (throw up) after taking your medication, do not take an extra dose. Take your next dose at the normal time.

Warning: If you take too much of this medication by accident, or if you think a child or a pet may have swallowed your medication, you must call the Ontario Poison Control Center right away at: 1-800-268-9017.

DO this while on treatment

DO check with your health care team before getting any vaccinations, surgery, dental work or other medical procedures.

DO NOT do this while on treatment

Stop Icon

DO NOT take any other medications, such as vitamins, over-the-counter (non-prescription) drugs or substances, or natural health products without checking with your health care team.

DO NOT start any complementary or alternative therapies, such as acupuncture or homeopathic products, without checking with your health care team.

DO NOT use tobacco products (such as smoking cigarettes or vaping) or drink alcohol while on treatment without talking to your health care team first. Smoking and drinking can make side effects worse and make your treatment not work as well.

DO NOT eat or drink grapefruit, starfruit, Seville oranges or their juices (or products that contain these) while on this treatment. These may increase the quantity of the medication in your blood and increase the side effects.

DO NOT drive, operate machinery or do any tasks that need you to be alert if you feel faint.

DO this while on treatment

Check Mark Icon

DO check with your health care team before getting any vaccinations, surgery, dental work or other medical procedures.

DO NOT do this while on treatment

Stop Icon

DO NOT take any other medications, such as vitamins, over-the-counter (non-prescription) drugs or substances, or natural health products without checking with your health care team.

DO NOT start any complementary or alternative therapies, such as acupuncture or homeopathic products, without checking with your health care team.

DO NOT use tobacco products (such as smoking cigarettes or vaping) or drink alcohol while on treatment without talking to your health care team first. Smoking and drinking can make side effects worse and make your treatment not work as well.

DO NOT eat or drink grapefruit, starfruit, Seville oranges or their juices (or products that contain these) while on this treatment. These may increase the quantity of the medication in your blood and increase the side effects.

DO NOT drive, operate machinery or do any tasks that need you to be alert if you feel faint.

Will this treatment interact with other medications or natural health products?

Yes, this medication can interact with other medications, vitamins, foods, traditional medicines and natural health products. Interactions can make this medication not work as well or cause severe side effects.

Tell your health care team about all of your:

prescription and over-the-counter (non-prescription) medications
other drugs and substances, such as cannabis/marijuana (medical or recreational)
natural health products such as vitamins, herbal teas, homeopathic medicines, and other supplements, or traditional medicines

Check with your health care team before starting or stopping any of them.

Talk to your health care team BEFORE taking or using these :

Anti-inflammatory medications such as ibuprofen (Advil^® or Motrin^®), naproxen (Aleve^®) or Aspirin^®.
Over-the-counter products such as dimenhydrinate (Gravol^®)
Natural health products such as St. John’s Wort
Traditional medicines
Supplements such as vitamin C
Grapefruit juice
Alcoholic drinks
Tobacco
All other drugs or substances, such as marijuana or cannabis (medical or recreational)

What to do if you feel unwell, have pain, a headache or a fever

Always check your temperature to see if you have a fever before taking any medications for fever or pain (such as acetaminophen (Tylenol^®) or ibuprofen (Advil^®)).
- Fever can be a sign of infection that may need treatment right away.
- If you take these medications before you check for fever, they may lower your temperature and you may not know you have an infection.

How to check for fever:

Keep a digital (electronic) thermometer at home and take your temperature if you feel hot or unwell (for example, chills, headache, mild pain).

You have a fever if your temperature taken in your mouth (oral temperature) is:
- 38.3°C (100.9°F) or higher at any time
OR
- 38.0°C (100.4°F) or higher for at least one hour.

If you do have a fever :

Try to contact your health care team. If you are not able to talk to them for advice, you MUST get emergency medical help right away.
Ask your health care team for the Fever pamphlet for more information.

If you do not have a fever but have mild symptoms such as headache or mild pain:

Ask your health care team about the right medication for you. Acetaminophen (Tylenol^®) is a safe choice for most people.

Talk to your health care team before you start taking ibuprofen (Advil^®, Motrin^®), naproxen (Aleve^®) or ASA (Aspirin^®), as they may increase your chance of bleeding or interact with your cancer treatment.

Talk to your health care team if you already take low dose aspirin for a medical condition (such as a heart problem). It may still be safe to take.

How will this treatment affect sex, pregnancy and breastfeeding?

Talk to your health care team about:

How this treatment may affect your sexual health
How this treatment may affect your ability to have a baby, if this applies to you

This treatment may harm an unborn baby. Tell your health care team if you or your partner are pregnant, become pregnant during treatment, or are breastfeeding.

If there is any chance of pregnancy happening, you and your partner together must use 2 effective forms of birth control at the same time until at least 21 days after your last treatment dose. Talk to your health care team about which birth control options are best for you.

Do not use hormonal birth control (such as birth control pills), unless your health care team told you that they are safe. Talk to your health care team about the safest birth control for you.

Do not breastfeed while on this treatment and for at least 21 days after your last dose.

How to safely store and handle this medication

Check with your pharmacist about whether you should store your ribociclib tablets at room temperature or in the refrigerator.
Keep the tablets in the original packaging.

Keep out of sight and reach of children and pets.

Do not throw out any unused ribociclib tablets at home. Bring them to your pharmacy to be thrown away safely.

How to safely touch oral anti-cancer medication

If you are a patient:

Wash your hands before and after touching your oral anti-cancer medication.
Swallow each pill whole. Do not crush or chew your pills.

If you are a caregiver:

Wear nitrile or latex gloves when touching tablets, capsules or liquids.
Wash your hands before putting on your gloves and after taking them off, even if your skin did not touch the oral anti-cancer medication.
Throw out your gloves after each use. Do not re-use gloves.
Do not touch oral anti-cancer medications if you are pregnant or breastfeeding.

What to do if anti-cancer medication gets on your skin or in your eyes

If medication gets on your skin:

Wash your skin with a lot of soap and water.
If your skin gets red or irritated, talk to your health care team.

If medication gets in your eyes:

Rinse your eyes with running water right away. Keep water flowing over your open eyes for at least 15 minutes.

What are the side effects of this treatment?

The following table lists side effects that you may have when getting ribociclib. The table is set up to list the most common side effects first and the least common last. It is unlikely that you will have all of the side effects listed and you may have some that are not listed.

Read over the side effect table so that you know what to look for and when to get help. Refer to this table if you experience any side effects while on ribociclib.

Very Common Side Effects (50 or more out of 100 people)
Side effects and what to do	When to contact health care team
Low neutrophils (white blood cells) in the blood (neutropenia) (May be severe) When neutrophils are low, you are at risk of getting an infection more easily. Ask your health care team for the Neutropenia (Low white blood cell count) pamphlet for more information. What to look for? If you feel hot or unwell (for example if you have chills or a new cough), you must check your temperature to see if you have a fever. Do not take medications that treat a fever before you take your temperature (for example, Tylenol®, acetaminophen, Advil® or ibuprofen). Do not eat or drink anything hot or cold right before taking your temperature. You have a fever if your temperature taken in your mouth (oral temperature) is: 38.3°C (100.9°F) or higher at any time OR 38.0°C (100.4°F) or higher for at least one hour. What to do? If your health care team has told you that you have low neutrophils: Wash your hands often to prevent infection. Check with your health care team before getting any vaccines, surgeries, medical procedures or visiting your dentist. Keep a digital thermometer at home so you can easily check for a fever. If you have a fever: If you have a fever, try to contact your health care team. If you are unable to talk to the team for advice, you must get emergency medical help right away.	If you have a fever, try to contact your health care team. If you are unable to talk to the team for advice, you MUST get emergency medical help right away.
Low platelets in the blood (May be severe) When your platelets are low, you are at risk for bleeding and bruising. Ask your health care team for the Low Platelet Count pamphlet for more information. What to look for? Watch for signs of bleeding: bleeding from your gums unusual or heavy nosebleeds bruising easily or more than normal black coloured stools (poo) or blood in your stools (poo) coughing up red or brown coloured mucus dizziness, constant headache or changes in your vision heavy vaginal bleeding red or pink coloured urine (pee) What to do? If your health care team has told you that you have low platelets: Tell your pharmacist that your platelet count may be low before taking any prescriptions or over-the-counter medication. Check with your healthcare team before you go to the dentist. Take care of your mouth and use a soft toothbrush. Try to prevent cuts and bruises. Ask your health care team what activities are safe for you. Your treatment may have to be delayed if you have low platelets. Your health care team may recommend a blood transfusion. If you have signs of bleeding: If you have a small bleed, clean the area with soap and water or a saline (saltwater) rinse. Apply pressure for at least 10 minutes. If you have bleeding that does not stop or is severe (very heavy), you must get emergency medical help right away.	Talk to your health care team if you have any signs of bleeding. If you have bleeding that doesn’t stop or is severe (very heavy), you MUST get emergency help right away.
Nausea and vomiting (Generally mild) What to look for? Nausea is feeling like you need to throw up. You may also feel light-headed. You may feel nausea within hours to days after your treatment. What to do? To help prevent nausea: It is easier to prevent nausea than to treat it once it happens. Drink clear liquids and have small meals. Get fresh air and rest. Do not eat spicy, fried foods or foods with a strong smell. Limit caffeine (like coffee, tea) and avoid alcohol. If you have nausea or vomiting: Take your rescue (as-needed) anti-nausea medication(s) as prescribed. Ask your health care team for the Nausea & Vomiting pamphlet for more information. Talk to your health care team if: nausea lasts more than 48 hours vomiting lasts more than 24 hours or if it is severe	Talk to your healthcare team if nausea lasts more than 48 hours or vomiting lasts more than 24 hours or if it is severe.

Common Side Effects (25 to 49 out of 100 people)
Side effects and what to do	When to contact health care team
Fatigue What to look for? Feeling of tiredness or low energy that lasts a long time and does not go away with rest or sleep. What to do? Be active. Aim to get 30 minutes of moderate exercise (you are able to talk comfortably while exercising) on most days. Check with your health care team before starting any new exercise. Pace yourself, do not rush. Put off less important activities. Rest when you need to. Ask family or friends to help you with things like housework, shopping, and child or pet care. Eat well and drink at least 6 to 8 glasses of water or other liquids every day (unless your health care team has told you to drink more or less). Avoid driving or using machinery if you are feeling tired. Ask your health care team for the Fatigue pamphlet for more information.	Talk to your health care team if it does not improve or if it is severe.
Diarrhea What to look for? Loose, watery, unformed stool (poo) that may happen days to weeks after you get your treatment. What to do? If you have diarrhea: Take anti-diarrhea medication if your health care team prescribed it or told you to take it. Do not eat foods or drinks with artificial sweetener (like chewing gum or ‘diet’ drinks), coffee and alcohol, until your diarrhea has stopped. Eat many small meals and snacks instead of 2 or 3 large meals. Drink at least 6 to 8 cups of liquids each day, unless your health care team has told you to drink more or less. Talk to your health care team if you can’t drink 6 to 8 cups of liquids each day when you have diarrhea. You may need to drink special liquids with salt and sugar, called Oral Rehydration Therapy. Talk to your health care team if your diarrhea does not improve after 24 hours of taking diarrhea medication or if you have diarrhea more than 7 times in one day. Ask your health care team for the Diarrhea pamphlet for more information.	Talk to your health care team if no improvement after 24 hours of taking diarrhea medication or if severe (more than 7 times in one day).
Hair thinning or loss (Generally mild) What to look for? Your hair may begin to become thin or fall out during or after treatment. In most cases, your hair will grow back after treatment, but the texture or colour may change. In very rare cases, hair loss may be permanent. What to do? Use a gentle soft brush. Do not use hair sprays, bleaches, dyes and perms.	Talk to your health care team if this bothers you.
Constipation What to look for? Having bowel movements (going poo) less often than normal. Small hard stools (poo) that look like pellets. The need to push hard and strain to have any stool (poo) come out. Stomach ache or cramps. A bloated belly, feeling of fullness, or discomfort. Leaking of watery stools (poo). Lots of gas or burping. Nausea or vomiting. What to do? To help prevent constipation: Try to eat more fiber rich foods like fruits with skin, leafy greens and whole grains. Drink at least 6 to 8 cups of liquids each day unless your health care team has told you to drink more or less. Be Active. Exercise can help to keep you regular. If you take opioid pain medication, ask your health care team if eating more fibre is right for you. To help treat constipation: If you have not had a bowel movement in 2 to 3 days you may need to take a laxative (medication to help you poo) to help you have regular bowel movements. Ask your health care team what to do. Ask your health care team for the Constipation Pamphlet for more information.	Talk to your health care team if it does not improve or if it is severe.
Headache; mild joint, muscle pain or cramps What to look for? A mild headache New pain in your muscles or joints, muscle cramps, or feeling achy. What to do? Take pain medication (acetaminophen or opioids such as codeine, morphine, hydromorphone, oxycodone) as prescribed. Read the above section: "What to do if you feel unwell, have pain, a headache or a fever?" before taking acetaminophen (Tylenol®), ibuprofen (Advil®, Motrin®), naproxen (Aleve®) or Aspirin. These medications may hide an infection that needs treatment or they may increase your risk of bleeding. Rest often and try light exercise (such as walking) as it may help. Ask your health care team for the Pain pamphlet for more information.	Talk to your health care team if it does not improve or if it is severe.

Less Common Side Effects (10 to 24 out of 100 people)
Side effects and what to do	When to contact health care team
Rash; dry, itchy skin (May be severe) What to look for? You may have cracked, rough, flaking or peeling areas of the skin. Your skin may look red and feel warm, like a sunburn. Your skin may itch, burn, sting or feel very tender when touched. What to do? To prevent and treat dry skin: Use fragrance-free skin moisturizer. Protect your skin from the sun and the cold. Use sunscreen with UVA and UVB protection and a SPF of at least 30. Avoid perfumed products and lotions that contain alcohol. Drink 6 to 8 cups of non-alcoholic, non-caffeinated liquids each day, unless your health care team has told you to drink more or less. Rash may be severe in some rare cases and cause your skin to blister or peel. If this happens, get emergency medical help right away.	Talk to your health care team if it does not improve or if it is severe.
Liver problems (May be severe) Your health care team may check your liver function with a blood test. The liver changes do not usually cause any symptoms. What to look for? Rarely, you may develop yellowish skin or eyes, unusually dark pee or pain on the right side of your belly. This may be severe. What to do? If you have any symptoms of liver problems, get emergency medical help right away.	Get emergency medical help right away.
Low appetite What to look for? Loss of interest in food or not feeling hungry. Weight loss. What to do? Try to eat your favourite foods. Eat small meals throughout the day. You may need to take meal supplements to help keep your weight up. Talk to your health care team if you have no appetite. Ask your health care team for the Loss of Appetite pamphlet for more information.	Talk to your health care team if it does not improve or if it is severe.
Mild swelling What to look for? You may have mild swelling or puffiness in your arms and/or legs. Rarely, this may be severe. What to do? To help prevent swelling: Eat a low-salt diet. If you have swelling: Wear loose-fitting clothing. For swollen legs or feet, keep your feet up when sitting.	Talk to your health care team if it does not improve or if it is severe.
Trouble Sleeping Your medications may cause trouble sleeping. It may get better once your body gets used to the medication or when your treatment ends. What to look for? You may find it hard to fall asleep or stay asleep. How well you sleep may change over your treatment. For example, you may have several nights of poor sleep followed by a night of better sleep. You may wake up too early or not feel well-rested after a night's sleep. You may feel tired or sleepy during the day. What to do? Talk to your health care team if it does not improve or if it is severe.	Talk to your health care team if it does not improve or if it is severe.
Cough and feeling short of breath (May be severe) What to look for? You may have a cough and feel short of breath. Symptoms that commonly occur with a cough are: Wheezing or a whistling breathing Runny nose Sore throat Heartburn Weight loss Fever and chills Rarely this may be severe with chest pain, trouble breathing or coughing up blood. What to do? Check your temperature to see if you have a fever. Read the above section "What to do if you feel unwell, have pain, a headache or a fever?". If you have a fever, try to talk to your health care team. If you are not able to talk to them for advice, you MUST get emergency medical help right away. If you have a severe cough with chest pain, trouble breathing or you are coughing up blood, get medical help right away.	Talk to your health care team. If you are not able to talk to your health care team for advice, and you have a fever or severe symptoms, you MUST get emergency medical help right away.
Mouth sores What to look for? Round, painful, white or gray sores inside your mouth that can occur on the tongue, lips, gums, or inside your cheeks. In more severe cases they may make it hard to swallow, eat or brush your teeth. They may last for 3 days or longer. What to do? To help prevent mouth sores: Take care of your mouth by gently brushing and flossing regularly. Rinse your mouth often with a homemade mouthwash. To make a homemade mouthwash, mix 1 teaspoonful of baking soda and 1 teaspoonful of salt in 4 cups (1L) of water. Do not use store-bought mouthwashes, especially those with alcohol, because they may irritate your mouth. If you have mouth sores: Avoid hot, spicy, acidic, hard or crunchy foods. Your doctor may prescribe a special mouthwash to relieve mouth sores and prevent infection. Talk to your health care team as soon as you notice mouth or lip sores or if it hurts to eat, drink or swallow. Ask your health care team for the Oral Care (Mouth Care) pamphlet for more information.	Talk to your health care team as soon as you notice mouth or lip sores or if it hurts to eat, drink or swallow.
Dry mouth What to look for? You may have a dry or sticky feeling in your mouth or throat, Your saliva may be thick and stringy. You may have cracks in your lips or at the corners of your mouth You may have difficulty chewing, tasting, swallowing or talking What to do? Use sugar-free gum or lozenges (e.g. those that contain xylitol) to help keep your mouth moist. Suck on ice chips or sugarless popsicles to help relieve dry mouth. Rinse your mouth often (every 1 to 2 hours) with a homemade mouthwash. To make a homemade mouthwash, mix 1 teaspoon of baking soda and 1 teaspoon of salt in 4 cups (1L) of water Do not use store-bought mouthwashes, especially those with alcohol because they may irritate dry your mouth Spray your mouth with water or artificial saliva products (e.g., Moi-Stir Spray®, Biotene® products) as needed to keep it moist. Apply mouth lubricant (like Biotene Oral balance gel®) after you brush your teeth, at bedtime, and as needed. Use a steam vaporizer at night to relieve nighttime dry mouth Speak to your health care team about the right product for you. See our Mouth Care pamphlet for more information. Talk to your health care team if your dry mouth does not improve or if it is severe.	Talk to your health care team if it does not improve or if it is severe.
Eye problems What to look for? Your eyes may feel dry, irritated, or painful. They may look red and have a lot of tears. They may feel sensitive to light and your vision may be blurry. What to do? Avoid wearing contact lenses. Wear sunglasses with UV protection. Use protective eyewear (goggles or helmet with face mask) when playing sports, mowing the lawn or doing anything that may get particles or fumes in your eyes. You may try artificial tears (eye drops) or ointment.	Contact your health care team as soon as possible.
Heartburn; stomach upset; bloating What to look for? Pain or burning in the middle or top part of your chest. It may get worse when you are lying down or bending over or when you swallow. A bitter or acidic taste in your mouth. What to do? Drink clear liquids and eat small meals. Do not eat acidic, fatty or spicy foods. Limit caffeine (like coffee, tea) and avoid alcohol. Avoid smoking or being around tobacco. Sit up or stand after eating. Do not lie down. Raise the head of your bed six to eight inches. You may need to use extra pillows to do this.	Talk to your health care team if it does not improve or if it is severe.
Taste changes What to look for? Food and drinks may taste different than usual. What to do? Eat foods that are easy to chew, such as scrambled eggs, pasta, soups, cooked vegetables. Taste foods at different temperatures, since the flavour may change. Try different forms of foods, like fresh, frozen or canned. Experiment with non-spicy foods, spices and seasonings.	Talk to your health care team if it does not improve or if it is severe.

Other rare, but serious side effects are possible with this treatment.

If you have any of the following, talk to your cancer health care team or get emergency medical help right away:

irregular heartbeat, shortness of breath, chest pain, fainting spells or swelling in your legs, ankles and belly
pain, swelling and hardening of the vein in an arm or leg
muscle spasms, cramping, weakness, twitching, seizures, confusion or blood pressure changes

For more information on how to manage your symptoms ask your health care provider, or visit: https://www.cancercareontario.ca/symptoms.

Notes

September 2025 Updated/Revised drug information sheet

The information set out in the medication information sheets, regimen information sheets, and symptom management information (for patients) contained in the Drug Formulary (the "Formulary") is intended to be used by health professionals and patients for informational purposes only. The information is not intended to cover all possible uses, directions, precautions, drug interactions or side effects of a certain drug, nor should it be used to indicate that use of a particular drug is safe, appropriate or effective for a given condition.

A patient should always consult a healthcare provider if he/she has any questions regarding the information set out in the Formulary. The information in the Formulary is not intended to act as or replace medical advice and should not be relied upon in any such regard. All uses of the Formulary are subject to clinical judgment and actual prescribing patterns may not follow the information provided in the Formulary.

Info Sheet (English):

ribociclib patient.pdf Info Sheet (French):

ribociclib pour le patient.pdf Monograph:

ribociclib.pdf Funding Program: Exceptional Access Program Funding Instance:

ribociclib - For the treatment of patients with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER 2)-negative, unresectable locally advanced or metastatic breast cancer in combination with an aromatase inhibitor or fulvestrant according to clinical criteria

Phonetic Spelling:

rye-boe-SYE-klib

Cancer Type: Breast Type of Content: Drug Monograph Status: Null Info Sheet Status: Null Global Date: Vendredi, septembre 12, 2025 Universal Date: 2025-09-12 00:00:00 AddThis: Title URL: ribociclib Drug Display Status: Active Revision Summary:
Drug Monograph: Updated Pharmacokinetics, Adverse Effects, Dosing, Administration Guidelines, Pregnancy/Lactation, Interactions, and Monitoring sections
Patient Info Sheet EN: Updated/Revised drug information sheet