藥碼
PIQ01
藥名
Alpelisib 錠劑 150 mg
英文商品名
臨採 Piqray 錠劑 150 mg
中文商品名
愛克利膜衣錠150mg
螢幕名
臨採 Piqray 膜衣錠 150 mg
劑型
Tab
規格
Alpelisib 150 mg film-coated tablets
成分
藥理分類
Anticancer- Monoclonal antibodies
健保碼
BC27995100
ATC碼
適應症
Breast cancer, advanced or metastatic, HR-positive, HER2-negative, PIK3CA-mutated
藥理
Antineoplastic Agent, Phosphatidylinositol 3-Kinase Inhibitor; Phosphatidylinositol 3-Kinase (PI3K) Inhibitor
Alpelisib is a small-molecule phosphatidylinositol-3-kinase (PI3K) inhibitor with selective (and strong) activity against PI3Kα. Mutations in the gene encoding the catalytic α-subunit of PI3K (PI3KCA) lead to activation of PI3Kα and Akt-signaling, cellular transformation, and tumor generation. Alpelisib inhibits phosphorylation of PI3K downstream targets (including Akt) and demonstrated activity in cell lines harboring a PIK3CA mutation.
Alpelisib is a small-molecule phosphatidylinositol-3-kinase (PI3K) inhibitor with selective (and strong) activity against PI3Kα. Mutations in the gene encoding the catalytic α-subunit of PI3K (PI3KCA) lead to activation of PI3Kα and Akt-signaling, cellular transformation, and tumor generation. Alpelisib inhibits phosphorylation of PI3K downstream targets (including Akt) and demonstrated activity in cell lines harboring a PIK3CA mutation.
藥動學
Absorption
Time to peak: 2 to 4 hours
Distribution
1. Vd:114 L
2. Protein binding: 89%
Metabolism
Primarily by chemical and enzymatic hydrolysis to form its metabolite BZG791, and to a lesser extent by CYP3A4.
Excretion
Following a single 400 mg dose: Feces: 81% (36% as unchanged drug, 32% as BZG791); Urine: 14% (2% as unchanged drug, 7% as BZG791).
Pharmakodynamics
1. Half-life Elimination: 8 to 9 hours
2. Clearance: 9.2 L/hour (under fed conditions)
Time to peak: 2 to 4 hours
Distribution
1. Vd:114 L
2. Protein binding: 89%
Metabolism
Primarily by chemical and enzymatic hydrolysis to form its metabolite BZG791, and to a lesser extent by CYP3A4.
Excretion
Following a single 400 mg dose: Feces: 81% (36% as unchanged drug, 32% as BZG791); Urine: 14% (2% as unchanged drug, 7% as BZG791).
Pharmakodynamics
1. Half-life Elimination: 8 to 9 hours
2. Clearance: 9.2 L/hour (under fed conditions)
禁忌症
Severe hypersensitivity to alpelisib or any component of the formulation.
懷孕分類
Based on the mechanism of action, and data from animal reproduction studies, in utero exposure to alpelisib may cause fetal harm.
哺乳分類
It is not known if alpelisib is present in breast milk. Due to the potential for adverse events in a breastfed infant, breastfeeding is not recommended during therapy and for 1 week after the last alpelisib dose.
副作用
Common(>10%):
Dermatologic: Alopecia (20%), pruritus (18%), skin rash (52%)
Endocrine & metabolic: Decreased serum calcium (27%), decreased serum glucose (26%), hyperglycemia (65%; including severe hyperglycemia), increased gamma-glutamyl transferase (52%), weight loss (27%)
Gastrointestinal: Decreased appetite (36%), diarrhea (58%; grade 3: 7%), increased serum lipase (42%), nausea (45%; grade 3: 3%), vomiting (27%; grade 3: <1%)
Hematologic & oncologic: Lymphocytopenia (52%; grades 3/4: 8%), prolonged partial thromboplastin time (21%; grades 3: <1%)
Hepatic: Increased serum alanine aminotransferase (44%)
Renal: Increased serum creatinine (67%)
1% to 10%
Genitourinary: Urinary tract infection (10%; including urinary tract infection with sepsis)
Hematologic & oncologic: Anemia (2%)
Neuromuscular & skeletal: Osteonecrosis of the jaw (4%)
Renal: Acute kidney injury (3%)
Respiratory: Pneumonitis (2%)
<1%:
Dermatologic: Stevens-Johnson syndrome
Endocrine & metabolic: Ketoacidosis
Hypersensitivity: Severe hypersensitivity reaction (grades 3/4)
Dermatologic: Alopecia (20%), pruritus (18%), skin rash (52%)
Endocrine & metabolic: Decreased serum calcium (27%), decreased serum glucose (26%), hyperglycemia (65%; including severe hyperglycemia), increased gamma-glutamyl transferase (52%), weight loss (27%)
Gastrointestinal: Decreased appetite (36%), diarrhea (58%; grade 3: 7%), increased serum lipase (42%), nausea (45%; grade 3: 3%), vomiting (27%; grade 3: <1%)
Hematologic & oncologic: Lymphocytopenia (52%; grades 3/4: 8%), prolonged partial thromboplastin time (21%; grades 3: <1%)
Hepatic: Increased serum alanine aminotransferase (44%)
Renal: Increased serum creatinine (67%)
1% to 10%
Genitourinary: Urinary tract infection (10%; including urinary tract infection with sepsis)
Hematologic & oncologic: Anemia (2%)
Neuromuscular & skeletal: Osteonecrosis of the jaw (4%)
Renal: Acute kidney injury (3%)
Respiratory: Pneumonitis (2%)
<1%:
Dermatologic: Stevens-Johnson syndrome
Endocrine & metabolic: Ketoacidosis
Hypersensitivity: Severe hypersensitivity reaction (grades 3/4)
劑量和給藥方法
Adiministration:
Oral
Dosage:
300 mg once daily (in combination with fulvestrant); continue until disease progression or unacceptable toxicity.
Oral
Dosage:
300 mg once daily (in combination with fulvestrant); continue until disease progression or unacceptable toxicity.
小兒調整劑量
It is not known if PIQRAY is safe and effective in children.
腎功能調整劑量
CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling.
肝功能調整劑量
Hepatic impairment at baseline: There are no dosage adjustments provided in the manufacturer's labeling.
安定性
Store at 20°C to 25°C, excursions permitted between 15°C and 30°C.
藥袋資訊
臨床用途
局部晚期或轉移性乳癌
主要副作用
高血糖、皮疹、發燒、潮紅、腹瀉等
泡製方法
儲存方式
請置於 15-30℃ 乾燥處儲存
注意事項
其他說明
門診 ADC |藥庫 管G
藥品外觀
顏色
01
形狀
03
剝痕
N
標記1
UL7 NVR
標記2
其他
健保藥價
28420
自費價
34104
仿單
資料庫
健保給付規定