Palbociclib
Generic Name: palbociclib
Brand Names:
Ibrance
11 DESCRIPTION IBRANCE capsules for oral administration contain 125 mg, 100 mg, or 75 mg of palbociclib, a kinase inhibitor. The molecular formula for palbociclib is C 24 H 29 N 7 O 2 . The molecular weight is 447.54 daltons.
Overview
11 DESCRIPTION IBRANCE capsules for oral administration contain 125 mg, 100 mg, or 75 mg of palbociclib, a kinase inhibitor. The molecular formula for palbociclib is C 24 H 29 N 7 O 2 . The molecular weight is 447.54 daltons.
Uses
1 INDICATIONS AND USAGE IBRANCE is indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer in combination with: • an aromatase inhibitor as initial endocrine-based therapy; or • fulvestrant in patients with disease progression following endocrine therapy. IBRANCE is indicated in combination with inavolisib and fulvestrant for the treatment of adult patients with endocrine-resistant, PIK3CA -mutated, HR-positive, HER2-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy.
Dosage
2 DOSAGE AND ADMINISTRATION IBRANCE capsules are taken orally with food in combination with an aromatase inhibitor, fulvestrant, or inavolisib and fulvestrant. ( 2 ) • Recommended starting dose: 125 mg once daily taken with food for 21 days followed by 7 days off treatment. ( 2.1 ) • Dosing interruption and/or dose reductions are recommended based on individual safety and tolerability. ( 2.2 ) 2.1 Recommended Dose and Schedule The recommended dose of IBRANCE is a 125 mg capsule taken orally once daily for 21 consecutive days followed by 7 days off treatment to comprise a complete cycle of 28 days. IBRANCE capsule should be taken with food [see Clinical Pharmacology (12.3) ] . Administer the recommended dose of an aromatase inhibitor when given with IBRANCE.
Side Effects
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: • Neutropenia [see Warnings and Precautions (5.1) ] • ILD/Pneumonitis [see Warnings and Precautions (5.2) ] Most common adverse reactions (incidence ≥20%) in combination with either letrozole or fulvestrant, including laboratory abnormalities, were white blood cell count decreased, neutrophils decreased, blood creatinine increased, hemoglobin decreased, platelets decreased, infections, aspartate aminotransferase increased, alanine aminotransferase increased, fatigue, nausea, stomatitis, diarrhea, and alopecia.
Interactions
7 DRUG INTERACTIONS Palbociclib is primarily metabolized by CYP3A and sulfotransferase (SULT) enzyme SULT2A1. In vivo, palbociclib is a time-dependent inhibitor of CYP3A. • CYP3A Inhibitors: Avoid concurrent use of IBRANCE with strong CYP3A inhibitors. If the strong inhibitor cannot be avoided, reduce the IBRANCE dose. ( 2.2 , 7.1 ) • CYP3A Inducers: Avoid concurrent use of IBRANCE with strong CYP3A inducers. ( 7.2 ) • CYP3A Substrates: The dose of sensitive CYP3A4 substrates with narrow therapeutic indices may need to be reduced when given concurrently with IBRANCE.
Warnings
5 WARNINGS AND PRECAUTIONS • Neutropenia: Monitor complete blood count prior to start of IBRANCE therapy and at the beginning of each cycle, as well as on Day 15 of the first 2 cycles, and as clinically indicated. ( 2.2 , 5.1 ) • Interstitial Lung Disease (ILD)/Pneumonitis: Severe and fatal cases of ILD/pneumonitis have been reported. Monitor for pulmonary symptoms of ILD/pneumonitis. Interrupt IBRANCE immediately in patients with suspected ILD/pneumonitis. Permanently discontinue IBRANCE if severe ILD/pneumonitis occurs. ( 5.2 ) • Embryo-Fetal Toxicity: IBRANCE can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, IBRANCE can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no available data in pregnant women to inform the drug-associated risk. In animal reproduction studies, administration of palbociclib to pregnant rats and rabbits during organogenesis resulted in embryo-fetal toxicity at maternal exposures that were ≥4 times the human clinical exposure based on AUC (see Data ) . Advise pregnant women of the potential risk to a fetus.
Storage
Store at 20 °C to 25 °C (68 °F to 77 °F); excursions permitted between 15 °C to 30 °C (59 °F to 86 °F) [see USP Controlled Room Temperature] .
Frequently Asked Questions
What is Palbociclib used for?▼
1 INDICATIONS AND USAGE IBRANCE is indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer in combination with: • an aromatase inhibitor as initial endocrine-based therapy; or • fulvestrant in patients with disease progression following endocrine therapy. IBRANCE is indicated in combination with inavolisib and fulvestrant for the treatment of adult patients with endocrine-resistant, PIK3CA -mutated, HR-positive, HER2-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy.
What are the side effects of Palbociclib?▼
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: • Neutropenia [see Warnings and Precautions (5.1) ] • ILD/Pneumonitis [see Warnings and Precautions (5.2) ] Most common adverse reactions (incidence ≥20%) in combination with either letrozole or fulvestrant, including laboratory abnormalities, were white blood cell count decreased, neutrophils decreased, blood creatinine increased, hemoglobin decreased, platelets decreased, infections, aspartate aminotransferase increased, alanine aminotransferase increased, fatigue, nausea, stomatitis, diarrhea, and alopecia.
Can I take Palbociclib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, IBRANCE can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no available data in pregnant women to inform the drug-associated risk. In animal reproduction studies, administration of palbociclib to pregnant rats and rabbits during organogenesis resulted in embryo-fetal toxicity at maternal exposures that were ≥4 times the human clinical exposure based on AUC (see Data ) . Advise pregnant women of the potential risk to a fetus.
What are the important warnings for Palbociclib?▼
5 WARNINGS AND PRECAUTIONS • Neutropenia: Monitor complete blood count prior to start of IBRANCE therapy and at the beginning of each cycle, as well as on Day 15 of the first 2 cycles, and as clinically indicated. ( 2.2 , 5.1 ) • Interstitial Lung Disease (ILD)/Pneumonitis: Severe and fatal cases of ILD/pneumonitis have been reported. Monitor for pulmonary symptoms of ILD/pneumonitis. Interrupt IBRANCE immediately in patients with suspected ILD/pneumonitis. Permanently discontinue IBRANCE if severe ILD/pneumonitis occurs. ( 5.2 ) • Embryo-Fetal Toxicity: IBRANCE can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception. 4 CONTRAINDICATIONS None. None. ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.