Ibrance 75mg Tablets
It is used to treat breast cancer.
Drug Class
Antineoplastic agent
Pharmacologic Class
Cyclin-dependent kinase (CDK) 4/6 inhibitor
Pregnancy Category
Category D
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 get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food. Swallow the tablet whole - do not chew, break, or crush it. If the tablet 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 feeling well. If you vomit after taking a dose, do not take an extra dose. Instead, take your next dose at the usual time.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep it in its original container to maintain its quality.
What to Do If You Miss a Dose
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 to make up for the missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food. Swallow the tablet whole - do not chew, break, or crush it. If the tablet 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 feeling well. If you vomit after taking a dose, do not take an extra dose. Instead, take your next dose at the usual time.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep it in its original container to maintain its quality.
What to Do If You Miss a Dose
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 to make up for the missed one.
Lifestyle & Tips
- Take Ibrance with food, preferably with a meal, to help your body absorb the medicine better and reduce stomach upset.
- Take your dose at approximately the same time each day.
- Swallow tablets whole; do not chew, crush, or split 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, as they can increase the amount of Ibrance in your body.
- Avoid St. John's Wort, as it can decrease the amount of Ibrance in your body.
- Report any signs of infection (fever, chills, sore throat) immediately, as Ibrance can lower your white blood cell count.
- Use effective contraception during treatment and for at least 3 weeks after the last dose for women, and for 14 weeks after the last dose for men.
- Avoid donating blood or sperm during treatment and for a period after.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
125 mg orally once daily for 21 consecutive days, followed by 7 days off treatment, for a 28-day cycle. The 75 mg tablet is a dose reduction strength.
Dose Range:
75 - 125 mg
Condition-Specific Dosing:
HR+, HER2- advanced or metastatic breast cancer:
125 mg orally once daily for 21 days, followed by 7 days off, in combination with an aromatase inhibitor or fulvestrant.
Dose Reduction for Adverse Reactions:
First reduction: 100 mg daily for 21 days, 7 days off. Second reduction: 75 mg daily for 21 days, 7 days off. Discontinue if further reduction is needed.
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 are limited.
Dialysis:
No specific recommendation; clinical data are limited. Monitor closely.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A)
Moderate:
Reduce dose to 75 mg once daily (Child-Pugh B)
Severe:
Reduce dose to 75 mg once daily (Child-Pugh C)
Pharmacology
Mechanism of Action
Palbociclib is a highly selective, 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 regulating cell cycle progression from G1 to S phase. In many cancers, including hormone receptor-positive (HR+) breast cancer, CDK4/6 are overactive, leading to uncontrolled cell proliferation. By inhibiting CDK4/6, palbociclib prevents retinoblastoma protein (Rb) phosphorylation, thereby blocking cell cycle progression and inhibiting tumor cell growth.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 46%
Tmax:
6 to 12 hours
FoodEffect:
High-fat, high-calorie food increases palbociclib exposure (AUC and Cmax) by 21% and 26%, respectively, compared to fasting. Low-fat food increases AUC by 12% and Cmax by 9%. Palbociclib should be taken with food.
Distribution:
Vd:
Approximately 2583 L (apparent volume of distribution)
ProteinBinding:
Approximately 85%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 29 hours
Clearance:
Not available (apparent oral clearance is 17.3 L/hr)
ExcretionRoute:
Feces (74%), urine (17%)
Unchanged:
2.2% in feces, 1.9% in urine
Pharmacodynamics
OnsetOfAction:
Not precisely defined for clinical effect, but cellular effects (Rb phosphorylation inhibition) occur rapidly.
PeakEffect:
Not precisely defined for clinical effect.
DurationOfAction:
Related to dosing cycle (21 days on, 7 days off).
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
+ 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 from the gums
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruises that get bigger
+ 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
Signs of a blood clot, including:
+ 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're bothered by any of the following side effects or if they don't go away, contact your doctor or seek medical help:
Hair loss
Hair thinning
Mouth irritation or mouth sores
Feeling tired or weak
Dry skin
Change in taste
Diarrhea
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 if they bother you, don't improve, or are severe.
Reporting Side Effects
This list doesn't include all possible 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
+ 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 from the gums
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruises that get bigger
+ 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
Signs of a blood clot, including:
+ 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're bothered by any of the following side effects or if they don't go away, contact your doctor or seek medical help:
Hair loss
Hair thinning
Mouth irritation or mouth sores
Feeling tired or weak
Dry skin
Change in taste
Diarrhea
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 if they bother you, don't improve, or are severe.
Reporting Side Effects
This list doesn't include all possible 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
- Cough
- Painful urination
- Unusual bleeding or bruising
- Severe fatigue
- Severe nausea, vomiting, or diarrhea
- New or worsening shortness of breath or cough (could be signs of lung problems)
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, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. Certain medications, such as those used to treat HIV, infections, seizures, and other conditions, should not be taken with this drug. There are many medications that interact with this drug, so it is crucial to disclose all medications you are taking.
* If you are breastfeeding or plan to breastfeed. You should not breastfeed while taking this medication and for 3 weeks after your last dose.
This list is not exhaustive, and it is crucial to discuss all your medications and health problems with your doctor and pharmacist to ensure safe use. You must verify that it is safe to take this medication with all your 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, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. Certain medications, such as those used to treat HIV, infections, seizures, and other conditions, should not be taken with this drug. There are many medications that interact with this drug, so it is crucial to disclose all medications you are taking.
* If you are breastfeeding or plan to breastfeed. You should not breastfeed while taking this medication and for 3 weeks after your last dose.
This list is not exhaustive, and it is crucial to discuss all your medications and health problems with your doctor and pharmacist to ensure safe use. You must verify that it is safe to take this medication with all your 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.
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 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 while taking this drug and for at least 3 weeks after your last dose. If you become pregnant, notify your doctor immediately.
If your sexual partner may become pregnant, use birth control while taking this medication 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 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 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 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 while taking this drug and for at least 3 weeks after your last dose. If you become pregnant, notify your doctor immediately.
If your sexual partner may become pregnant, use birth control while taking this medication and for 3 months after your last dose. If your partner becomes pregnant, inform the doctor right away.
Overdose Information
Overdose Symptoms:
- Exaggerated adverse reactions, particularly neutropenia and other hematologic toxicities.
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) for advice.
Drug Interactions
Major Interactions
- Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, grapefruit juice): Concomitant use should be avoided. If a strong CYP3A inhibitor cannot be avoided, reduce palbociclib dose to 75 mg once daily.
- Strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort): Concomitant use should be avoided as they can decrease palbociclib exposure and efficacy.
Moderate Interactions
- Moderate CYP3A inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole): Monitor for increased palbociclib toxicity. Dose reduction may be considered if toxicity occurs.
- Moderate CYP3A inducers (e.g., bosentan, efavirenz, etravirine, modafinil): Monitor for decreased palbociclib efficacy.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline hematologic parameters, especially neutrophil and platelet counts, 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, as palbociclib is metabolized in the liver and dose adjustments are needed for hepatic impairment.
Timing: Prior to the start of Ibrance treatment.
Renal Function Tests (RFTs)
Rationale: To assess baseline renal function, as palbociclib is excreted renally.
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: If ANC < 1000/mm³ or platelets < 50,000/mm³, hold dose until recovery to Grade ≤1 (ANC ≥1500/mm³, platelets ≥75,000/mm³), then resume at same dose or reduced dose based on severity and recurrence.
Liver Function Tests (LFTs)
Frequency: Periodically, or as clinically indicated.
Target: Within normal limits or stable for patient.
Action Threshold: Significant elevations may require dose modification or discontinuation.
Renal Function Tests (RFTs)
Frequency: Periodically, or as clinically indicated.
Target: Within normal limits or stable for patient.
Action Threshold: Significant decline may require dose modification or discontinuation.
Symptom Monitoring
- Fever (especially with neutropenia, indicating infection)
- Signs of infection (chills, sore throat, cough, painful urination)
- Unusual bleeding or bruising
- Fatigue
- Nausea
- Diarrhea
- Hair thinning or loss
- Mouth sores
- Rash
- Shortness of breath or new/worsening cough (potential 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, it is classified as Pregnancy Category D. Advise pregnant women of the potential risk to a fetus.
Trimester-Specific Risks:
First Trimester:
Potential for major birth defects due to interference with cell division.
Second Trimester:
Potential for developmental toxicity.
Third Trimester:
Potential for developmental toxicity.
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 (L5 - Contraindicated/Hazardous)
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 alone.
Clinical Information
Clinical Pearls
- Neutropenia is the most common and dose-limiting adverse event; close monitoring of CBC is crucial, especially during the first two cycles.
- Always advise patients to take palbociclib with food to optimize absorption and reduce variability.
- Educate patients on signs of infection and the importance of reporting fever immediately.
- Dose reductions are common and should be managed according to the prescribing information based on toxicity, not just neutropenia.
- Counsel patients on avoiding strong CYP3A inhibitors (including grapefruit) and inducers (including St. John's Wort).
Alternative Therapies
- Everolimus (Afinitor) + exemestane
- Chemotherapy regimens (e.g., capecitabine, eribulin)
- Other endocrine therapies (e.g., tamoxifen, other aromatase inhibitors, fulvestrant)
Cost & Coverage
Average Cost:
Highly variable, typically several thousand USD per 30 tablets
Insurance Coverage:
Specialty Tier (requires prior authorization, may have high co-pay/co-insurance)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with 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 overdose, including the medication taken, the amount, and the time it occurred.