Your Health, We Care
Another Name帕博西尼、哌柏西利、IBRANCE、LuciPalbo
IndicationsBreast Cancer
Reg No.08 L 1162/24
Inspection NO.
Palbociclib is primarily used for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor-2 (HER2)-negative locally advanced or metastatic breast cancer.
In specific applications, it can be used as initial endocrine therapy for postmenopausal women in combination with aromatase inhibitors.
Palbociclib is a targeted drug for breast cancer, which has significant efficacy and certain side effects. During use, it is necessary to strictly follow the doctor's instructions and pay attention to monitoring the changes in the patient's condition.
Palbociclib
It is suitable for adult patients with HR-positive and HER2-negative advanced or metastatic breast cancer. Pregnant and lactating women, as well as the elderly and children, should take the drug under the guidance of a doctor.
Based on findings from animal studies and its mechanism of action, Palbociclib can cause fetal harm when administered to a pregnant woman. 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 . Advise pregnant women of the potential risk to a fetus.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%-4% and 15%-20%, respectively.
There is no information regarding the presence of palbociclib in human milk, its effects on milk production, or the breastfed infant. Because of the potential for serious adverse reactions in breastfed infants from Palbociclib, advise a lactating woman not to breastfeed during treatment with Palbociclib and for 3 weeks after the last dose.
Based on animal studies, Palbociclib can cause fetal harm when administered to a pregnant woman. Females of reproductive potential should have a pregnancy test prior to starting treatment with Palbociclib.
The safety and efficacy of Palbociclib in pediatric patients have not been studied.
Altered glucose metabolism (glycosuria, hyperglycemia, decreased insulin) associated with changes in the pancreas (islet cell vacuolation), eye (cataracts, lens degeneration), kidney (tubule vacuolation, chronic progressive nephropathy) and adipose tissue (atrophy) were identified in a 27 week repeat-dose toxicology study in rats that were immature at the beginning of the studies and were most prevalent in males at oral palbociclib doses ≥30 mg/kg/day (approximately 11 times the adult human exposure [AUC] at the recommended dose). Some of these findings (glycosuria/hyperglycemia, pancreatic islet cell vacuolation, and kidney tubule vacuolation) were present with lower incidence and severity in a 15 week repeat-dose toxicology study in immature rats. Altered glucose metabolism or associated changes in the pancreas, eye, kidney and adipose tissue were not identified in a 27-week repeat-dose toxicology study in rats that were mature at the beginning of the study and in dogs in repeat-dose toxicology studies up to 39 weeks duration.
Toxicities in teeth independent of altered glucose metabolism were observed in rats. Administration of 100 mg/kg palbociclib for 27 weeks (approximately 15 times the adult human exposure [AUC] at the recommended dose) resulted in abnormalities in growing incisor teeth (discolored, ameloblast degeneration/necrosis, mononuclear cell infiltrate). Other toxicities of potential concern to pediatric patients have not been evaluated in juvenile animals.
Of 444 patients who received Palbociclib in Study 1, 181 patients (41%) were ≥65 years of age and 48 patients (11%) were ≥75 years of age. Of 347 patients who received Palbociclib in Study 2, 86 patients (25%) were ≥65 years of age and 27 patients (8%) were ≥75 years of age. No overall differences in safety or effectiveness of Palbociclib were observed between these patients and younger patients.
No dose adjustment is required in patients with mild or moderate hepatic impairment (Child-Pugh classes A and B). For patients with severe hepatic impairment (Child-Pugh class C), the recommended dose of Palbociclib is 75 mg once daily for 21 consecutive days followed by 7 days off treatment to comprise a complete cycle of 28 days . Based on a pharmacokinetic trial in subjects with varying degrees of hepatic function, the palbociclib unbound exposure (unbound AUCINF) decreased by 17% in subjects with mild hepatic impairment (Child-Pugh class A), and increased by 34% and 77% in subjects with moderate (Child-Pugh class B) and severe (Child-Pugh class C) hepatic impairment, respectively, relative to subjects with normal hepatic function. Peak palbociclib unbound exposure (unbound Cmax) increased by 7%, 38% and 72% for mild, moderate and severe hepatic impairment, respectively, relative to subjects with normal hepatic function .
Review the Full Prescribing Information for the aromatase inhibitor or fulvestrant for dose modifications related to hepatic impairment.
No dose adjustment is required in patients with mild, moderate, or severe renal impairment (CrCl >15 mL/min).
Based on a pharmacokinetic trial in subjects with varying degrees of renal function, the total palbociclib exposure (AUCINF) increased by 39%, 42%, and 31% with mild (60 mL/min ≤ CrCl <90 mL/min), moderate (30 mL/min ≤ CrCl <60 mL/min), and severe (CrCl <30 mL/min) renal impairment, respectively, relative to subjects with normal renal function. Peak palbociclib exposure (Cmax) increased by 17%, 12%, and 15% for mild, moderate, and severe renal impairment, respectively, relative to subjects with normal renal function.
The pharmacokinetics of palbociclib have not been studied in patients requiring hemodialysis.
There is no known antidote for Palbociclib. The treatment of overdose of Palbociclib should consist of general supportive measures.
Store at 20o C to 25o C (68o F to 77o F); excursions permitted between 15o C to 30o C (59o F to 86o F). Store in the original blister pack.
The pharmacokinetics (PK) of palbociclib were characterized in patients with solid tumors including advanced breast cancer and in healthy subjects.
from FDA，2022.12
