Ibrance 75mg Capsules
It is used to treat breast cancer.
Drug Class
Antineoplastic agent
Pharmacologic Class
Cyclin-dependent kinase (CDK) 4/6 inhibitor
Pregnancy Category
Not available
FDA Approved
Feb 2015
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ibrance is a medicine used to treat certain types of advanced breast cancer. It works by blocking specific proteins (CDK4 and CDK6) that help cancer cells grow and divide. By blocking these proteins, Ibrance helps slow down or stop the growth of cancer cells.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication with food to help your body absorb it properly.
Swallow the medication whole - do not chew, open, or crush it.
Check your medication before taking it. If it is broken, cracked, or looks damaged, do not take it.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
What to Do If You Miss a Dose or Have Trouble Taking Your Medication
If you vomit after taking a dose, do not take an extra dose. Instead, wait until your next scheduled dose and take it as usual.
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at the same time or take extra doses.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
* Keep all medications in a safe and secure location, out of the reach of children and pets.
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication with food to help your body absorb it properly.
Swallow the medication whole - do not chew, open, or crush it.
Check your medication before taking it. If it is broken, cracked, or looks damaged, do not take it.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
What to Do If You Miss a Dose or Have Trouble Taking Your Medication
If you vomit after taking a dose, do not take an extra dose. Instead, wait until your next scheduled dose and take it as usual.
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at the same time or take extra doses.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
* Keep all medications in a safe and secure location, out of the reach of children and pets.
Lifestyle & Tips
- Take Ibrance capsules whole, with food, at approximately the same time each day.
- Do not chew, crush, or open the capsules.
- Do not take Ibrance capsules that are broken, cracked, or otherwise damaged.
- Avoid grapefruit and grapefruit juice during treatment, as they can increase the amount of Ibrance in your body.
- Avoid St. John's wort during treatment.
- Use effective contraception during treatment and for at least 3 weeks after the last dose for females of reproductive potential, and for at least 3 months after the last dose for male patients with female partners of reproductive potential.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Report any new or worsening breathing problems (shortness of breath, cough).
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
125 mg orally once daily for 21 consecutive days, followed by 7 days off treatment, to comprise a 28-day cycle. Administer with food.
Dose Range:
75 - 125 mg
Condition-Specific Dosing:
HR+, HER2- advanced or metastatic breast cancer:
125 mg orally once daily for 21 consecutive days, followed by 7 days off treatment, to comprise a 28-day cycle. Administer with food. Dose reductions for adverse reactions are 100 mg, then 75 mg.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required.
Moderate:
No dose adjustment required.
Severe:
75 mg orally once daily for 21 consecutive days, followed by 7 days off treatment, to comprise a 28-day cycle.
Dialysis:
Not available. Avoid use in patients requiring hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A).
Moderate:
75 mg orally once daily for 21 consecutive days, followed by 7 days off treatment, to comprise a 28-day cycle (Child-Pugh B).
Severe:
75 mg orally once daily for 21 consecutive days, followed by 7 days off treatment, to comprise a 28-day cycle (Child-Pugh C).
Confidence:
Medium
Pharmacology
Mechanism of Action
Palbociclib is a reversible inhibitor of cyclin-dependent kinases (CDK) 4 and 6. These kinases are activated by binding to D-cyclins and play a crucial role in cell cycle progression from G1 to S phase. Inhibition of CDK4/6 by palbociclib prevents retinoblastoma protein (Rb) phosphorylation, thereby blocking cell cycle progression and inhibiting tumor cell proliferation.
Pharmacokinetics
Absorption:
Bioavailability:
46%
Tmax:
6 to 12 hours
FoodEffect:
Administration with food increases palbociclib exposure (AUC and Cmax) compared to the fasted state. High-fat food increases AUC by 21% and Cmax by 26%. Low-fat food increases AUC by 12% and Cmax by 15%. It is recommended to take palbociclib with food.
Distribution:
Vd:
2583 L (apparent volume of distribution)
ProteinBinding:
Approximately 85%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 29 hours
Clearance:
Not available (apparent oral clearance: 17.3 L/hr)
ExcretionRoute:
Fecal (74%), Renal (17%)
Unchanged:
2.1% (urine), 6.9% (feces)
Pharmacodynamics
OnsetOfAction:
Not precisely defined, related to cell cycle inhibition.
PeakEffect:
Not precisely defined, related to cell cycle inhibition.
DurationOfAction:
Related to drug half-life and continuous dosing schedule.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or changed sputum production
+ Painful urination
+ Mouth sores
+ Wounds that won't heal
Signs of bleeding, such as:
+ Vomiting or coughing up blood
+ Vomit that resembles coffee grounds
+ Blood in the urine
+ Black, red, or tarry stools
+ Bleeding gums
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruises that enlarge
+ Uncontrollable bleeding
Dizziness
Lung problems, which can be life-threatening. Seek medical help immediately if you experience:
+ Chest pain
+ Cough with or without mucus
+ Shortness of breath or difficulty breathing
Blood clots, which can be life-threatening. Seek medical help immediately if you experience:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, color change, or pain in a leg or arm
+ Difficulty speaking or swallowing
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or persist:
Hair loss
Hair thinning
Mouth irritation or mouth sores
Fatigue or weakness
Dry skin
Changes in taste
Diarrhea
Vomiting
Upset stomach
Decreased appetite
If you experience any of these side effects, talk to your doctor about ways to manage them. If they worsen, persist, or are severe, seek medical help.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or changed sputum production
+ Painful urination
+ Mouth sores
+ Wounds that won't heal
Signs of bleeding, such as:
+ Vomiting or coughing up blood
+ Vomit that resembles coffee grounds
+ Blood in the urine
+ Black, red, or tarry stools
+ Bleeding gums
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruises that enlarge
+ Uncontrollable bleeding
Dizziness
Lung problems, which can be life-threatening. Seek medical help immediately if you experience:
+ Chest pain
+ Cough with or without mucus
+ Shortness of breath or difficulty breathing
Blood clots, which can be life-threatening. Seek medical help immediately if you experience:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, color change, or pain in a leg or arm
+ Difficulty speaking or swallowing
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or persist:
Hair loss
Hair thinning
Mouth irritation or mouth sores
Fatigue or weakness
Dry skin
Changes in taste
Diarrhea
Vomiting
Upset stomach
Decreased appetite
If you experience any of these side effects, talk to your doctor about ways to manage them. If they worsen, persist, or are severe, seek medical help.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Fever (100.4°F or higher) or other signs of infection
- Chills
- Sore throat
- Unusual bleeding or bruising
- Extreme tiredness or weakness
- Shortness of breath
- Cough
- Chest pain
- Severe nausea, vomiting, or diarrhea
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins, that may interact with this medication. Certain medications used to treat HIV, infections, seizures, and other conditions should not be taken with this drug.
* If you are breastfeeding or plan to breastfeed. You should not breastfeed while taking this medication and for 3 weeks after your last dose.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications, health problems, and concerns with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins, that may interact with this medication. Certain medications used to treat HIV, infections, seizures, and other conditions should not be taken with this drug.
* If you are breastfeeding or plan to breastfeed. You should not breastfeed while taking this medication and for 3 weeks after your last dose.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications, health problems, and concerns with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
While taking this drug, you may be at a higher risk of developing infections, some of which can be severe or even life-threatening. To minimize this risk, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
Additionally, this medication may increase your tendency to bleed easily. To reduce the risk of injury, exercise caution in your daily activities and use a soft toothbrush and an electric razor for personal grooming.
Regular monitoring of your blood work and other laboratory tests is crucial, as directed by your doctor. This medication is often used in conjunction with other drugs, so it is vital to understand the benefits, risks, and warnings associated with these combination therapies. If you have any questions or concerns, discuss them with your doctor.
Certain foods and beverages, such as grapefruit and grapefruit juice, should be avoided while taking this medication.
Men taking this drug should be aware that it may affect their fertility. If you have concerns about fathering a child, consult your doctor.
For women of childbearing age, it is crucial to note that this medication may harm an unborn baby. A pregnancy test will be conducted before initiating treatment to confirm that you are not pregnant. If you may become pregnant, use effective birth control methods during treatment and for at least 3 weeks after your last dose. If you become pregnant, notify your doctor immediately.
If your partner may become pregnant, use birth control during your treatment and for 3 months after your last dose. If your partner becomes pregnant, contact the doctor right away.
While taking this drug, you may be at a higher risk of developing infections, some of which can be severe or even life-threatening. To minimize this risk, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
Additionally, this medication may increase your tendency to bleed easily. To reduce the risk of injury, exercise caution in your daily activities and use a soft toothbrush and an electric razor for personal grooming.
Regular monitoring of your blood work and other laboratory tests is crucial, as directed by your doctor. This medication is often used in conjunction with other drugs, so it is vital to understand the benefits, risks, and warnings associated with these combination therapies. If you have any questions or concerns, discuss them with your doctor.
Certain foods and beverages, such as grapefruit and grapefruit juice, should be avoided while taking this medication.
Men taking this drug should be aware that it may affect their fertility. If you have concerns about fathering a child, consult your doctor.
For women of childbearing age, it is crucial to note that this medication may harm an unborn baby. A pregnancy test will be conducted before initiating treatment to confirm that you are not pregnant. If you may become pregnant, use effective birth control methods during treatment and for at least 3 weeks after your last dose. If you become pregnant, notify your doctor immediately.
If your partner may become pregnant, use birth control during your treatment and for 3 months after your last dose. If your partner becomes pregnant, contact the doctor right away.
Overdose Information
Overdose Symptoms:
- Exaggerated adverse reactions, particularly myelosuppression (neutropenia, thrombocytopenia, anemia)
What to Do:
There is no specific antidote for Ibrance overdose. Management should include general supportive measures and treatment of symptoms. Call 1-800-222-1222 (Poison Control Center) for advice.
Drug Interactions
Major Interactions
- Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, grapefruit juice): Concomitant use significantly increases palbociclib exposure, increasing risk of adverse reactions. Avoid concomitant use. If unavoidable, reduce palbociclib dose to 75 mg once daily.
- Strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's wort): Concomitant use significantly decreases palbociclib exposure, potentially reducing efficacy. Avoid concomitant use.
Moderate Interactions
- Moderate CYP3A inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole): May increase palbociclib exposure. Monitor for adverse reactions and consider dose reduction if necessary.
- Moderate CYP3A inducers (e.g., bosentan, efavirenz, modafinil): May decrease palbociclib exposure. Monitor for reduced efficacy.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline counts before initiating treatment, as neutropenia is a common and dose-limiting adverse reaction.
Timing: Within 1 week prior to the start of treatment.
Liver Function Tests (LFTs)
Rationale: To establish baseline liver function, though severe hepatotoxicity is rare.
Timing: Prior to treatment initiation.
Routine Monitoring
Complete Blood Count (CBC) with differential
Frequency: Every 2 weeks for the first 2 cycles, then prior to the beginning of each of the subsequent cycles, and as clinically indicated.
Target: ANC ≥ 1000/mm³, Platelets ≥ 50,000/mm³
Action Threshold: For Grade 3 neutropenia (ANC 500 to <1000/mm³) or Grade 4 neutropenia (ANC <500/mm³), hold dose until recovery to Grade ≤2, then resume at reduced dose. For Grade 3 thrombocytopenia (platelets 25,000 to <50,000/mm³) or Grade 4 thrombocytopenia (platelets <25,000/mm³), hold dose until recovery to Grade ≤1, then resume at reduced dose.
Signs and symptoms of interstitial lung disease (ILD)/pneumonitis
Frequency: Throughout treatment
Target: N/A
Action Threshold: Monitor for new or worsening respiratory symptoms (e.g., hypoxia, cough, dyspnea). Interrupt IBRANCE in patients with new or worsening respiratory symptoms and consider ILD/pneumonitis. Permanently discontinue IBRANCE in patients with severe ILD/pneumonitis.
Symptom Monitoring
- Fever (especially with neutropenia, indicating infection)
- Chills
- Sore throat
- Unusual bleeding or bruising
- Fatigue
- Nausea
- Diarrhea
- Hair thinning/loss
- Rash
- New or worsening respiratory symptoms (e.g., shortness of breath, cough, chest pain)
Special Patient Groups
Pregnancy
Based on animal studies and its mechanism of action, Ibrance can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment and for at least 3 weeks after the last dose.
Trimester-Specific Risks:
First Trimester:
Potential for major birth defects and miscarriage due to interference with cell division.
Second Trimester:
Potential for fetal growth restriction and organ toxicity.
Third Trimester:
Potential for fetal growth restriction and adverse effects on developing organs.
Lactation
It is not known whether palbociclib is excreted in human milk. Because of the potential for serious adverse reactions in breastfed infants, advise lactating women not to breastfeed during Ibrance treatment and for 3 weeks after the last dose.
Infant Risk:
High (L5 - Contraindicated)
Pediatric Use
The safety and effectiveness of Ibrance in pediatric patients have not been established.
Geriatric Use
No dose adjustment is required for patients ≥65 years of age. Clinical studies did not reveal any overall differences in safety or effectiveness between these patients and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
Clinical Information
Clinical Pearls
- Always administer Ibrance with food to ensure consistent absorption and reduce variability.
- Emphasize strict adherence to the 21-days-on, 7-days-off schedule to allow for bone marrow recovery.
- Neutropenia is the most common adverse event; monitor CBCs closely, especially during the first two cycles. Dose reductions are frequently necessary.
- Educate patients on signs of infection and the importance of reporting fever immediately.
- Counsel patients on avoiding strong CYP3A inhibitors (including grapefruit) and inducers.
- Ibrance is typically given in combination with an aromatase inhibitor (e.g., letrozole) or fulvestrant for HR+, HER2- advanced breast cancer.
Alternative Therapies
- Endocrine therapy alone (e.g., aromatase inhibitors, fulvestrant)
- Chemotherapy (e.g., capecitabine, eribulin, paclitaxel)
- Everolimus + Exemestane (for HR+, HER2- advanced breast cancer after endocrine therapy)
Cost & Coverage
Average Cost:
Highly variable, typically >$10,000 - $15,000 per 21 capsules (one cycle)
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to step therapy)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.