Ibrance 125mg 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 breast cancer. It works by blocking specific proteins (CDK4 and CDK6) that help cancer cells grow and divide. By blocking these proteins, Ibrance helps to 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 Vomit After Taking a Dose
If you throw up after taking a dose, do not take an extra dose. Instead, wait until your next scheduled dose and take it as usual.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store it at room temperature in a dry place, away from the bathroom.
* Keep all medications in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, skip it and go back to your regular schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
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 Vomit After Taking a Dose
If you throw up after taking a dose, do not take an extra dose. Instead, wait until your next scheduled dose and take it as usual.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store it at room temperature in a dry place, away from the bathroom.
* Keep all medications in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, skip it and go back to your regular schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take Ibrance capsules whole with food, at approximately the same time each day.
- Do not chew, crush, or open the capsules.
- If you miss a dose or vomit after taking a dose, do not take an extra dose. Take the next dose at your regularly scheduled time.
- Avoid grapefruit and grapefruit products 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 women, and for at least 3 months after the last dose for men.
- Report any signs of infection (fever, chills, sore throat) immediately to your doctor.
- Report any new or worsening shortness of breath or 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 (28-day cycle). Administer with food.
Dose Range:
75 - 125 mg
Condition-Specific Dosing:
dose_reduction_due_to_toxicity:
First dose reduction: 100 mg orally once daily for 21 days on/7 days off. Second dose reduction: 75 mg orally once daily for 21 days on/7 days off. Discontinue if further dose reduction is required.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required (CrCl ≥90 mL/min)
Moderate:
No dose adjustment required (CrCl 60 to <90 mL/min)
Severe:
Reduce dose to 75 mg orally once daily (CrCl <30 mL/min)
Dialysis:
Not available (no data for patients requiring dialysis)
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A)
Moderate:
Reduce dose to 75 mg orally once daily (Child-Pugh B)
Severe:
Reduce dose to 75 mg orally once daily (Child-Pugh C)
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 phosphorylation of retinoblastoma protein (Rb), thereby blocking cell cycle progression and inhibiting tumor cell proliferation.
Pharmacokinetics
Absorption:
Bioavailability:
Not explicitly stated as a percentage, but well absorbed.
Tmax:
6 to 12 hours
FoodEffect:
Food increases palbociclib exposure (AUC and Cmax) by 21-24% and 10-12% respectively, compared to the fasted state. Administer with food.
Distribution:
Vd:
2583 L (apparent volume of distribution)
ProteinBinding:
Approximately 85% (primarily to human plasma proteins)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 29 hours
Clearance:
Not available
ExcretionRoute:
Fecal (74%), Renal (17%)
Unchanged:
2.3% (feces), 1.9% (urine)
Pharmacodynamics
OnsetOfAction:
Not precisely defined for chronic oncology treatment; sustained inhibition is the goal.
PeakEffect:
Not precisely defined for chronic oncology treatment.
DurationOfAction:
Not precisely defined for chronic oncology treatment; sustained inhibition is the goal.
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 other breathing difficulties
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 notice any of the following side effects, contact your doctor or seek medical attention if they bother you or persist:
Hair loss
Hair thinning
Mouth irritation or mouth sores
Fatigue or weakness
Dry skin
Changes in taste
Diarrhea
Nausea or vomiting
Upset stomach
Decreased appetite
These side effects are common with this medication. If you experience any of them, talk to your doctor about ways to manage them. Seek medical help immediately if any of these side effects are severe, worsen, or persist.
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 other breathing difficulties
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 notice any of the following side effects, contact your doctor or seek medical attention if they bother you or persist:
Hair loss
Hair thinning
Mouth irritation or mouth sores
Fatigue or weakness
Dry skin
Changes in taste
Diarrhea
Nausea or vomiting
Upset stomach
Decreased appetite
These side effects are common with this medication. If you experience any of them, talk to your doctor about ways to manage them. Seek medical help immediately if any of these side effects are severe, worsen, or persist.
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 (especially 100.4°F or higher) or chills
- Signs of infection (e.g., sore throat, cough, painful urination)
- Unusual bruising or bleeding
- Extreme tiredness or weakness
- Shortness of breath or difficulty breathing
- Persistent cough
- Severe nausea, vomiting, or diarrhea
- Mouth sores (stomatitis)
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 or health problems that may affect the use of this medication. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all your medications (prescription and OTC), natural products, vitamins, and health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
Never 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 or health problems that may affect the use of this medication. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all your medications (prescription and OTC), natural products, vitamins, and health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
Never 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.
You may also experience an increased 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 blood tests and other laboratory evaluations are crucial while taking this medication. Ensure that you adhere to the schedule recommended by your doctor for these tests.
This drug is often administered in conjunction with other medications. It is vital to understand the warnings, benefits, and risks associated with these additional drugs. If you have any questions or concerns, discuss them with your doctor.
Avoid consuming grapefruit and grapefruit juice during treatment with this medication.
Men taking this drug should be aware that it may affect their fertility. Discuss any concerns with your doctor.
For women, this drug may cause harm to an unborn baby. A pregnancy test will be conducted before initiating treatment to confirm that you are not pregnant. If you are capable of becoming pregnant, use effective birth control methods while taking this medication 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 while taking this drug 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.
You may also experience an increased 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 blood tests and other laboratory evaluations are crucial while taking this medication. Ensure that you adhere to the schedule recommended by your doctor for these tests.
This drug is often administered in conjunction with other medications. It is vital to understand the warnings, benefits, and risks associated with these additional drugs. If you have any questions or concerns, discuss them with your doctor.
Avoid consuming grapefruit and grapefruit juice during treatment with this medication.
Men taking this drug should be aware that it may affect their fertility. Discuss any concerns with your doctor.
For women, this drug may cause harm to an unborn baby. A pregnancy test will be conducted before initiating treatment to confirm that you are not pregnant. If you are capable of becoming pregnant, use effective birth control methods while taking this medication 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 while taking this drug and for 3 months after your last dose. If your partner becomes pregnant, contact the doctor right away.
Overdose Information
Overdose Symptoms:
- Increased severity of known adverse reactions, particularly myelosuppression (low white blood cell count, low platelet count).
What to Do:
There is no specific antidote for palbociclib overdose. Management should involve general supportive measures. Contact a poison control center (1-800-222-1222) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Strong CYP3A Inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, grapefruit juice): Significantly increase palbociclib exposure. Avoid concomitant use. If unavoidable, reduce palbociclib dose.
- Strong CYP3A Inducers (e.g., rifampin, phenytoin, carbamazepine, St. John's Wort): Significantly decrease palbociclib exposure. Avoid concomitant use.
Moderate Interactions
- Moderate CYP3A Inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole): May increase palbociclib exposure. Consider dose reduction if adverse reactions occur.
- Moderate CYP3A Inducers (e.g., bosentan, efavirenz, etravirine, modafinil, nafcillin): May decrease palbociclib exposure. Avoid if possible.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline hematologic parameters, especially neutrophil and platelet counts, as neutropenia and thrombocytopenia are common adverse reactions.
Timing: Prior to initiation of treatment
Liver Function Tests (ALT, AST, Bilirubin)
Rationale: To establish baseline liver function, as hepatic impairment may require dose adjustment and liver enzyme elevations can occur.
Timing: Prior to initiation of treatment
Routine Monitoring
Complete Blood Count (CBC) with differential
Frequency: Prior to the start of each cycle, on Day 15 of the first 2 cycles, and as clinically indicated.
Target: Neutrophils ≥1000/mm³, Platelets ≥50,000/mm³ for cycle initiation.
Action Threshold: Neutrophils <1000/mm³ or platelets <50,000/mm³ require dose interruption or reduction.
Liver Function Tests (ALT, AST, Bilirubin)
Frequency: Periodically, as clinically indicated.
Target: Within normal limits or stable.
Action Threshold: Significant elevations may require dose interruption or reduction.
Symptom Monitoring
- Fever or other signs of infection (e.g., chills, sore throat, cough)
- Unusual bruising or bleeding
- Fatigue or weakness
- Shortness of breath or cough (signs of interstitial lung disease/pneumonitis)
- Nausea, vomiting, diarrhea
- Stomatitis (mouth sores)
Special Patient Groups
Pregnancy
Ibrance can cause fetal harm when administered to a pregnant woman. Based on animal studies and its mechanism of action, palbociclib can cause embryo-fetal toxicity. 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. Advise males with female partners of reproductive potential to use effective contraception during treatment and for 3 months after the last dose.
Trimester-Specific Risks:
First Trimester:
High risk of embryo-fetal toxicity based on animal data.
Second Trimester:
High risk of embryo-fetal toxicity based on animal data.
Third Trimester:
High risk of embryo-fetal toxicity based on animal data.
Lactation
It is not known whether palbociclib is excreted in human milk. Because of the potential for serious adverse reactions in breastfed infants from palbociclib, advise lactating women not to breastfeed during 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 overall differences in safety or effectiveness were observed between patients ≥65 years of age and younger patients. No dose adjustment is required based on age.
Clinical Information
Clinical Pearls
- Always administer palbociclib with food to optimize absorption and reduce variability.
- Neutropenia is the most common adverse event and is typically reversible and manageable with dose interruptions and/or reductions. Close monitoring of CBC is crucial.
- Patients should be educated on the importance of reporting any signs of infection, fever, or respiratory symptoms immediately.
- Strict adherence to the 21-days-on/7-days-off dosing schedule is important for efficacy and managing side effects.
- Counsel patients to avoid strong CYP3A inhibitors (e.g., grapefruit) and inducers (e.g., St. John's Wort).
Alternative Therapies
- Other endocrine therapies (e.g., fulvestrant, aromatase inhibitors alone)
- Chemotherapy (e.g., capecitabine, eribulin, paclitaxel)
- Other targeted therapies (e.g., everolimus + exemestane, alpelisib + fulvestrant for PIK3CA-mutated HR+/HER2- breast cancer)
Cost & Coverage
Average Cost:
Highly variable, typically >$10,000 per 21 capsules (one cycle)
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high co-pays or co-insurance)
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.