拉帕替尼

拉帕替尼
臨床資料
商品名英语Drug nomenclatureTykerb, Tyverb, others
AHFS/Drugs.comMonograph
MedlinePlusa607055
核准狀況
懷孕分級
  • : C
给药途径By mouth (tablets)
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度Variable, increased with food
血漿蛋白結合率>99%
药物代谢Liver, mostly CYP3A-mediated (minor 2C19 and 2C8 involvement)
生物半衰期24 hours (repeated dosing), 14.2 hours (single dose)
排泄途徑Mostly Feces
识别信息
  • N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-
    [5-[(2-methylsulfonylethylamino)methyl]-2-furyl]
    quinazolin-4-amine
CAS号231277-92-2  checkY
388082-78-8  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB配體ID
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C29H26ClFN4O4S
摩尔质量581.06 g·mol−1
3D模型(JSmol英语JSmol
  • CS(=O)(=O)CCNCc1ccc(o1)c2ccc3c(c2)c(ncn3)Nc4ccc(c(c4)Cl)OCc5cccc(c5)F
  • InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35) checkY
  • Key:BCFGMOOMADDAQU-UHFFFAOYSA-N checkY

拉帕替尼INN諾華商品名TykerbTyverb泰嘉錠[1])是一种用于治疗乳腺癌和其他实体瘤的口服活性药物,以二甲苯磺酸拉帕替尼的形式使用。[2]它是一种双酪氨酸激酶抑制剂,可中断 HER2/neu和表皮生长因子受体通路。[3]它用于 HER2 阳性乳腺癌的联合治疗。 它用于治疗肿瘤过度表达 HER 的晚期或转移性乳腺癌患者。[4]

作用机制

拉帕替尼是小分子4-苯胺基喹唑啉类受体酪氨酸激酶抑制剂,抑制表皮生长因子受体(ErbB1)和人表皮因子受体2(ErbB2)。[5]

不良反应

拉帕替尼不良反应主要为胃肠道反应,包括恶心、腹泻、口腔炎和消化不良等,皮肤干燥、皮疹,其他有背痛、呼吸困难及失眠等。[5]

相互作用

在体外拉帕替尼在治疗浓度可抑制CYP3A4和CYP2C8,并且主要由CYP3A4代谢,抑制此酶活性的药物能显著提高拉帕替尼的血药浓度。[5]

参考文献

  1. ^ 用藥指導 LAPATINIB[失效連結]國軍高雄總醫院
  2. ^ Burris, Howard A. Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. The Oncologist. 2004,. 9 Suppl 3 [2022-06-13]. ISSN 1083-7159. PMID 15163842. doi:10.1634/theoncologist.9-suppl_3-10. (原始内容存档于2022-06-15). 
  3. ^ Higa, Gerald M.; Abraham, Jame. Lapatinib in the treatment of breast cancer. Expert Review of Anticancer Therapy. 2007-09, 7 (9) [2022-06-13]. ISSN 1744-8328. PMID 17892419. doi:10.1586/14737140.7.9.1183. (原始内容存档于2022-06-13). 
  4. ^ Breast cancer drug approved for new indication. Women's Health (London, England). 2010-03, 6 (2) [2022-06-13]. ISSN 1745-5065. PMID 20187722. doi:10.2217/whe.10.11. (原始内容存档于2022-06-18). 
  5. ^ 5.0 5.1 5.2 Lapatinib Uses, Side Effects & Warnings. Drugs.com. [2022-06-13]. (原始内容存档于2022-06-13) (英语). 

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