Kisqali

Ribociclib may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• diarrhea
• constipation
• stomach pain
• headache
• hair loss
• back pain
• rash
• itching
• mouth sores
• swelling of the hands, feet, ankles, or lower legs
• difficulty falling asleep or staying asleep

Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately:

• fever, sore throat, chills, or other signs of infection
• rapid, irregular, or pounding heartbeat
• shortness of breath
• dizziness
• fainting
• yellowing of the skin or eyes
• dark or brown (tea-colored) urine
• tiredness
• loss of appetite
• pain in upper right side of stomach
• nausea
• vomiting
• bleeding or bruising more easily than normal

Ribociclib may decrease fertility in men. Talk to your doctor about the risks of taking ribociclib.

Ribociclib may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Kisqali is a prescription medication used to treat certain forms of breast cancer. 

Kisqali belongs to a group of drugs called kinase inhibitors. Kinase inhibitors work by slowing or preventing cancer cell growth. 

This medication comes in tablet form and is taken by mouth once daily, with or without food. Do not chew, divide, or break Kisqali tablets. Swallow tablets whole. 

Common side effects of Kisqali include nausea, fatigue, and diarrhea. 

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take: 

QT Prolonging Meds

• drugs that can cause an called Torsades des Point such as
  • certain medications including: procainamide, sotalol (Betapace), , dofetilide (Tikosyn), amiodarone (Nexterone, Pacerone, Cordarone), ibutilide (Corvert)
  • certain fluoroquinolone antibiotics including: levofloxacin (Levaquin), ciprofloxacin (Cipro), gatifloxacin (Zymar), moxifloxacin (Avelox)
  • certain macrolide antibiotics including: clarithromycin (Biaxin), erythromycin (EES, others)
  • certain azole antifungals including: ketoconazole (Nizoral), itraconazole (Sporanox, Onmel)
  • certain antidepressants including: amitriptyline, desipramine (Norpramin), imipramine ), doxepin (Silenor), fluoxetine (Prozac, Sarafem, Symbyax), sertraline (Zoloft), venlafaxine (Effexor XR)
  • certain antipsychotics including: haloperidol (Haldol), droperidol (Inapsine), quetiapine (Seroquel XR), thioridazine, ziprasidone (Geodon)
  • and other medications including: cisapride, sumatriptan (Treximet, Imitrex, Alsuma, Zecuity), zolmitriptan (Zomig, (Trisenox), dolasetron (Anzemet), and methadone (Methadone, Dolophine)

CYP3A4 Substrates

• medications that use the enzyme CYP3A4 such as budesonide (Entocort), cyclosporine (Neoral, Gengraf, Sandimmune), darifenacin (Enablex), dihydroergotamine (Migranal), fentanyl (Abstral, Fentora, Onsolis, Actiq), pimozide (Orap), quinidine (Cardioquin, Duraquin, Quinact), sirolimus (Rapamune), tacrolimus (Prograf), terfenadine (Seldane), fluticasone (Flovent HFA, Flonase), eletriptan (Relpax), lovastatin (Mevacor), quetiapine (Seroquel), sildenafil (Viagra, Revatio), and simvastatin (Zocor)

STRONG CYP3A4 inhibitors (blockers)

• medications that block a protein in the body (CYP3A4) such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), (Rescriptor), and

STRONG CYP3A4 inducers

• medications that increase the activity of the enzyme CYP3A4 such as carbamazepine (Tegretol, Equetro, Carbatrol), phenobarbital, phenytoin (Dilantin), rifampin (Rifadin), and St John's wort

This is not a complete list of Kisqali drug interactions. Ask your doctor or pharmacist for more information. 

Store Kisqali at room temperature: 68°F to 77°F (20°C to25°C). Keep this and all medicines out of the reach of children. 

Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

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.

Do not crush, chew, or break a ribociclib tablet. Swallow it whole.

You may take ribociclib with or without food. Take the medicine in the morning, at the same time each day.

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.

Your blood cells, liver function, and heart function will need to be tested before and during treatment. You will need frequent blood tests while taking ribociclib. Your heart function will be checked using an electrocardiograph or ECG (sometimes called an EKG). Your cancer treatments may be delayed based on the results of these tests.

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

In the U.S.

• Kisqali

Available Dosage Forms:

• Tablet

Therapeutic Class: Antineoplastic Agent

Pharmacologic Class: Cyclin-Dependent Kinase Inhibitor

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of ribociclib in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of ribociclib in the elderly.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Amifampridine
• Amisulpride
• Bepridil
• Cisapride
• Dronedarone
• Fluconazole
• Ketoconazole
• Mesoridazine
• Piperaquine
• Posaconazole
• Saquinavir
• Sparfloxacin
• Terfenadine
• Thioridazine
• Ziprasidone

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Alfentanil
• Alfuzosin
• Amiodarone
• Amitriptyline
• Anagrelide
• Apomorphine
• Aripiprazole
• Aripiprazole Lauroxil
• Arsenic Trioxide
• Asenapine
• Astemizole
• Atazanavir
• Azithromycin
• Bedaquiline
• Boceprevir
• Buserelin
• Carbamazepine
• Chloroquine
• Chlorpromazine
• Ciprofloxacin
• Citalopram
• Clarithromycin
• Clomipramine
• Clozapine
• Cobicistat
• Conivaptan
• Crizotinib
• Cyclobenzaprine
• Cyclosporine
• Dabrafenib
• Dasatinib
• Degarelix
• Delamanid
• Desipramine
• Deslorelin
• Dihydroergotamine
• Disopyramide
• Dofetilide
• Dolasetron
• Domperidone
• Donepezil
• Doxepin
• Droperidol
• Ebastine
• Efavirenz
• Enzalutamide
• Ergotamine
• Eribulin
• Erythromycin
• Escitalopram
• Everolimus
• Famotidine
• Felbamate
• Fentanyl
• Fingolimod
• Flecainide
• Flibanserin
• Fluoxetine
• Formoterol
• Foscarnet
• Fosphenytoin
• Galantamine
• Gatifloxacin
• Gemifloxacin
• Gonadorelin
• Goserelin
• Granisetron
• Halofantrine
• Haloperidol
• Histrelin
• Hydroquinidine
• Hydroxychloroquine
• Hydroxyzine
• Ibutilide
• Idelalisib
• Iloperidone
• Imipramine
• Indinavir
• Itraconazole
• Ivabradine
• Lapatinib
• Leuprolide
• Levofloxacin
• Lopinavir
• Lumacaftor
• Lumefantrine
• Mefloquine
• Methadone
• Methotrimeprazine
• Metronidazole
• Midazolam
• Mifepristone
• Mitotane
• Mizolastine
• Moricizine
• Moxifloxacin
• Nafarelin
• Nefazodone
• Nelfinavir
• Nilotinib
• Norfloxacin
• Octreotide
• Ofloxacin
• Olanzapine
• Ondansetron
• Oxycodone
• Paliperidone
• Panobinostat
• Papaverine
• Paroxetine
• Pasireotide
• Pazopanib
• Pentamidine
• Perphenazine
• Phenytoin
• Pimavanserin
• Pimozide
• Pipamperone
• Pitolisant
• Probucol
• Procainamide
• Prochlorperazine
• Promethazine
• Propafenone
• Protriptyline
• Quetiapine
• Quinidine
• Quinine
• Ranolazine
• Rifampin
• Risperidone
• Ritonavir
• Sertindole
• Sevoflurane
• Sirolimus
• Sodium Phosphate
• Sodium Phosphate, Dibasic
• Sodium Phosphate, Monobasic
• Solifenacin
• Sorafenib
• Sotalol
• St John's Wort
• Sultopride
• Sunitinib
• Tacrolimus
• Tamoxifen
• Telaprevir
• Telavancin
• Telithromycin
• Temsirolimus
• Tetrabenazine
• Tizanidine
• Tolterodine
• Toremifene
• Trazodone
• Trimipramine
• Triptorelin
• Vandetanib
• Vardenafil
• Vemurafenib
• Venlafaxine
• Vilanterol
• Vinflunine
• Voriconazole
• Vorinostat
• Zotepine
• Zuclopenthixol

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice
• Pomegranate
• Pomegranate Juice

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Angina (severe chest pain), unstable or
• Congestive heart failure or
• Electrolyte imbalance or
• Heart attack, recent or
• Heart rhythm problems (eg, long QT syndrome, slow heartbeat)—May cause side effects to become worse.

• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. If you are a woman who can bear children, your doctor may give you a pregnancy test before you start using this medicine to make sure you are not pregnant. Use an effective form of birth control to keep from getting pregnant during treatment and for at least 3 weeks after your last dose. If you think you have become pregnant while using the medicine, tell your doctor right away.

If you plan to have children, talk with your doctor before using this medicine. Some men using this medicine have become infertile (unable to have children).

Contact your doctor right away if you have any changes to your heart rhythm. You might feel dizzy or faint, or you might have a fast, pounding, or uneven heartbeat. Make sure your doctor knows if you or anyone in your family has ever had a heart rhythm problem such as QT prolongation.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, vomiting, or yellow eyes or skin. These could be symptoms of a serious liver problem.

Ribociclib can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

Tablet: 200 mg ribociclib (equivalent to 254.40 mg ribociclib succinate)

Film coated, light greyish violet, round, curved with beveled edges, debossed with “RIC” on one side and “NVR” on the other side.

     Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis studies have not been conducted with ribociclib.

Ribociclib was not mutagenic in an in vitro bacterial reverse mutation (Ames) assay or clastogenic in an in vitro human lymphocyte chromosomal aberration assay or an in vivo rat bone marrow micronucleus assay.

Fertility studies in animals have not been performed with ribociclib. In repeat-dose toxicity studies with oral administration of ribociclib daily for 3 weeks on /1 week off in rats up to 26 weeks duration and dogs up to 39 weeks duration, atrophic changes in testes were reported. Findings included degeneration of seminiferous tubular epithelia in the testes and hypospermia and luminal cellular debris in the epididymides of rats and dogs and vacuolation of epithelia in the epididymides of rats. These findings were observed at doses ≥75 mg/kg in rats and ≥1 mg/kg in dogs which resulted in systemic exposures that were 1.4 and 0.03 times the human exposure at the highest recommended daily dose of 600 mg/day based on AUC, respectively. These effects can be linked to a direct anti-proliferative effect on the testicular germ cells resulting in atrophy of the seminiferous tubules and showed a trend towards reversibility in rats and dogs after a four-week non-dosing period.

     Animal Toxicology and/or Pharmacology

In vivo cardiac safety studies in dogs demonstrated dose and concentration related QTc interval prolongation at an exposure similar to patients receiving the recommended dose of 600 mg. There is a potential to induce incidences of premature ventricular contractions (PVCs) at elevated exposures (approximately 5-fold the anticipated clinical Cmax).

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Get emergency medical help if you have signs of an allergic reaction to Kisqali: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• headache with chest pain and severe dizziness, fainting, fast or pounding heartbeats;

• low white blood cell counts - fever, swollen gums, painful mouth sores, pain when swallowing, skin sores, cold or flu symptoms, cough, trouble breathing; or

• liver problems - loss of appetite, upper stomach pain, tiredness, easy bruising or bleeding, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

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

Common Kisqali side effects may include:

• low white blood cells;

• nausea, vomiting;

• diarrhea, constipation;

• feeling tired;

• headache, back pain; or

• hair loss.

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 FDA at 1-800-FDA-1088.

Kisqali can cause a serious heart problem, especially if you use certain medicines at the same time, including antibiotics, antidepressants, antipsychotic medicines, stomach acid reducers, heart rhythm medicine, and medicines to treat cancer, malaria, HIV or AIDS.

Many drugs can interact with ribociclib. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Kisqali. Give a list of all your medicines to any healthcare provider who treats you.