Ibrance 100mg 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 to slow down or stop the growth of cancer cells. It is usually taken along with another hormone therapy medicine.
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 prescription and follow the instructions carefully.
Take your medication with food to help your body absorb it properly. Swallow the tablet whole - do not chew, open, or crush it.
Check your medication before taking it. If the tablet is broken, cracked, or looks damaged, do not take it.
Establish a routine by taking your medication at the same time every day.
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 effective and safe:
Store it at room temperature in a dry place, away from the bathroom.
* Keep all medications in a secure location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at once 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 prescription and follow the instructions carefully.
Take your medication with food to help your body absorb it properly. Swallow the tablet whole - do not chew, open, or crush it.
Check your medication before taking it. If the tablet is broken, cracked, or looks damaged, do not take it.
Establish a routine by taking your medication at the same time every day.
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 effective and safe:
Store it at room temperature in a dry place, away from the bathroom.
* Keep all medications in a secure location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at once or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take Ibrance with food, preferably at the same time each day.
- Swallow capsules whole; do not chew, crush, or open them.
- Do not take a missed dose if it is close to the next scheduled dose. Skip the missed dose and take the next dose at your regular time.
- 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.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Report any unusual bleeding or bruising.
- 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.
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 an aromatase inhibitor or fulvestrant.
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 75 mg dose is not tolerated.
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:
No dose adjustment required (CrCl 30 to <60 mL/min). For CrCl <30 mL/min, no dose adjustment is required based on population PK analysis, but clinical data is limited.
Dialysis:
No specific recommendations; limited data. Monitor closely.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A)
Moderate:
75 mg orally once daily for 21 days on/7 days off (Child-Pugh B)
Severe:
75 mg orally once daily for 21 days on/7 days off (Child-Pugh C)
Pharmacology
Mechanism of Action
Palbociclib is an orally bioavailable, selective 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 in estrogen receptor-positive (ER+) breast cancer cell lines.
Pharmacokinetics
Absorption:
Bioavailability:
Not directly reported, but good oral absorption
Tmax:
6 to 12 hours
FoodEffect:
High-fat, high-calorie food increases AUC and Cmax by 21% and 26% respectively, compared to fasting. Low-fat food increases AUC by 12% and Cmax by 15%. Palbociclib should be taken with food.
Distribution:
Vd:
2583 L (apparent volume of distribution)
ProteinBinding:
Approximately 85%
CnssPenetration:
Limited (not a primary target for CNS metastases, but some preclinical data suggests potential)
Elimination:
HalfLife:
Approximately 29 hours
Clearance:
Not directly reported, but apparent oral clearance is 119 L/hr
ExcretionRoute:
Feces (74%), Urine (17%)
Unchanged:
Approximately 2.2% in feces, 6.9% in urine
Pharmacodynamics
OnsetOfAction:
Not directly applicable (chronic therapy for tumor growth inhibition)
PeakEffect:
Not directly applicable (chronic therapy for tumor growth inhibition)
DurationOfAction:
Not directly applicable (chronic therapy for tumor growth inhibition)
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
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 right away:
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
+ Pain while urinating
+ 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 may not experience any side effects or may only have 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 worsen, persist, or are severe.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. 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 right away:
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
+ Pain while urinating
+ 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 may not experience any side effects or may only have 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 worsen, persist, or are severe.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. 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
- Easy bruising or bleeding
- Extreme tiredness or weakness
- Shortness of breath, cough, or chest pain (new or worsening)
- Severe diarrhea
- Nausea or vomiting that is severe or doesn't go away
- Yellowing of skin or eyes (jaundice)
- Dark urine
- Severe rash
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 your 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 your 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 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 bleeding, be cautious and avoid injuries. Use a soft-bristled toothbrush and an electric razor for shaving.
Regular blood tests and other laboratory evaluations are crucial while taking this medication. Ensure that you undergo these tests as directed by your doctor.
This drug is often administered in conjunction with other medications. It is vital to understand the warnings, benefits, and risks associated with these other drugs. If you have any questions or concerns, discuss them with your doctor.
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Men taking this drug should be aware that it may affect their fertility. Discuss any concerns with your doctor.
Women of childbearing age should note that this medication can cause harm to 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 while taking this drug 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, inform 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 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 bleeding, be cautious and avoid injuries. Use a soft-bristled toothbrush and an electric razor for shaving.
Regular blood tests and other laboratory evaluations are crucial while taking this medication. Ensure that you undergo these tests as directed by your doctor.
This drug is often administered in conjunction with other medications. It is vital to understand the warnings, benefits, and risks associated with these other drugs. If you have any questions or concerns, discuss them with your doctor.
Avoid consuming grapefruit and grapefruit juice while taking this medication.
Men taking this drug should be aware that it may affect their fertility. Discuss any concerns with your doctor.
Women of childbearing age should note that this medication can cause harm to 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 while taking this drug 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, inform the doctor right away.
Overdose Information
Overdose Symptoms:
- Increased severity of known adverse reactions, particularly myelosuppression (e.g., neutropenia, thrombocytopenia, anemia)
What to Do:
There is no specific antidote for Ibrance overdose. Management should involve general supportive measures and close monitoring of hematologic parameters. Call 1-800-222-1222 (Poison Control Center) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, grapefruit juice): Concomitant use significantly increases palbociclib exposure. Avoid co-administration. If co-administration cannot be avoided, reduce palbociclib dose to 75 mg once daily.
- Strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort, enzalutamide): Concomitant use significantly decreases palbociclib exposure, potentially reducing efficacy. Avoid co-administration.
Moderate Interactions
- Moderate CYP3A inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole): May increase palbociclib exposure. Monitor for increased adverse reactions.
- Moderate CYP3A inducers (e.g., efavirenz, bosentan, modafinil): May decrease palbociclib exposure. Monitor for decreased efficacy.
Minor Interactions
- Gastric pH elevating agents (e.g., proton pump inhibitors, H2-receptor antagonists, antacids): No clinically meaningful effect on palbociclib absorption.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline hematologic parameters, as neutropenia is a common and dose-limiting toxicity.
Timing: Prior to the start of Ibrance treatment.
Liver Function Tests (LFTs)
Rationale: To assess baseline hepatic function, especially given hepatic metabolism.
Timing: Prior to the start of Ibrance treatment.
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: Absolute Neutrophil Count (ANC) ≥1000/mm³, Platelets ≥50,000/mm³
Action Threshold: ANC <1000/mm³ or Platelets <50,000/mm³ (requires dose interruption or reduction); Febrile neutropenia (requires dose interruption or reduction).
Liver Function Tests (LFTs)
Frequency: Periodically, or as clinically indicated.
Target: Within normal limits or stable
Action Threshold: Significant elevations in AST/ALT or bilirubin (requires monitoring or dose adjustment).
Symptom Monitoring
- Signs of infection (fever, chills, sore throat)
- Unusual bleeding or bruising
- Fatigue
- Diarrhea
- Nausea/Vomiting
- Hair thinning/loss
- Mouth sores
- Shortness of breath or new/worsening cough (signs of interstitial lung disease/pneumonitis)
Special Patient Groups
Pregnancy
Ibrance can cause fetal harm when administered to a pregnant woman. Based on animal studies and its mechanism of action, Ibrance is contraindicated during pregnancy. Advise pregnant women of the potential risk to a fetus.
Trimester-Specific Risks:
First Trimester:
High risk of embryo-fetal toxicity due to interference with cell division.
Second Trimester:
High risk of fetal toxicity and developmental abnormalities.
Third Trimester:
High risk of fetal toxicity and developmental abnormalities.
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 risk of serious adverse reactions (e.g., myelosuppression, growth inhibition) due to potential excretion in breast milk and mechanism of action.
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 included a sufficient number of patients aged 65 and over to determine that efficacy and safety profiles are similar to younger patients.
Clinical Information
Clinical Pearls
- Neutropenia is the most common adverse reaction and is often dose-limiting. Close monitoring of CBC is crucial, especially during the first two cycles.
- Administer Ibrance with food to optimize absorption and reduce variability.
- Patients should be educated on signs of infection and instructed to report fever immediately.
- Strong CYP3A inhibitors and inducers must be avoided or managed with dose adjustments due to significant drug interactions.
- Ibrance is part of a combination therapy for HR+, HER2- advanced or metastatic breast cancer; it is not used as monotherapy in this setting.
- Interstitial Lung Disease (ILD)/Pneumonitis, though rare, is a serious adverse reaction. Patients should be monitored for new or worsening respiratory symptoms.
Alternative Therapies
- Everolimus (Afinitor) + Exemestane
- Chemotherapy regimens (e.g., capecitabine, eribulin, paclitaxel)
- Other endocrine therapies (e.g., tamoxifen, other aromatase inhibitors, fulvestrant)
Cost & Coverage
Average Cost:
$14,000 - $16,000 per 21 capsules (one cycle)
Insurance Coverage:
Specialty Tier (requires prior authorization, may have high co-pay/coinsurance)
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 this 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 medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.