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url url url url
  2. Weltenzyklopädie
  3. بوزوتینیب - ویکی‌پدیا، دانشنامهٔ آزاد
بوزوتینیب - ویکی‌پدیا، دانشنامهٔ آزاد
از ویکی‌پدیا، دانشنامهٔ آزاد
بوزوتینیب
داده‌های بالینی
نام‌های تجاریBosulif
داده‌ها
روش مصرف داروخوراکی
کد ATC
وضعیت قانونی
وضعیت قانونی
داده‌های فارماکوکینتیک
پیوند پروتئینی94–96%
متابولیسمBy CYP3A4, to inactive metabolites
نیمه‌عمر حذف22.5±1.7 hours
دفعمدفوع (۹۱.۳%) و کلیه (۳%)
شناسه‌ها
  • 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
شمارهٔ سی‌ای‌اس
پاب‌کم CID
IUPHAR/BPS
دراگ‌بنک
کم‌اسپایدر
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.149.122 ویرایش در ویکی‌داده
داده‌های فیزیکی و شیمیایی
فرمول شیمیاییC26H29Cl2N5O3
جرم مولی۵۳۰٫۴۵ g·mol−1
مدل سه بعدی (جی‌مول)
  • Clc1c(OC)cc(c(Cl)c1)Nc4c(C#N)cnc3cc(OCCCN2CCN(CC2)C)c(OC)cc34
  • InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31) ✔Y
  • Key:UBPYILGKFZZVDX-UHFFFAOYSA-N ✔Y
 N✔Y (این چیست؟)  (صحت‌سنجی)

بوزوتینیب (انگلیسی: Bosutinib یک دارو و مولکول کوچک BCR-ABL و مهارکننده تیروزین کیناز src است که برای درمان لوسمی میلوژن مزمن (CML) به کار می‌رود.

سازوکار

این دارو یک مهارکننده تیروزین کیناز Bcr-Abl رقابتی با ATP با یک اثر بازدارنده اضافی روی کینازهای خانواده Src (از جمله Src، Lyn و Hck) است.[۲] همچنین فعالیتی در برابر گیرنده‌های فاکتور رشد مشتق از پلاکت و فاکتور رشد اندوتلیال عروقی نشان داده است.[۳] بوزوتینیب 16 شکل از 18 شکل مقاوم به ایماتینیب Bcr-Abl را که در رده های سلولی میلوئید موش بیان می‌شود مهار کرد، اما سلول‌های جهش یافته T315I و V299L را مهار نکرد.

بوزوتینیب از راه CYP3A4 متابولیزه می‌شود.

منابع

  1. ↑ "Prescription medicines: registration of new chemical entities in Australia, 2014". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 10 April 2023. Retrieved 10 April 2023.
  2. ↑ Daud AI, Krishnamurthi SS, Saleh MN, Gitlitz BJ, Borad MJ, Gold PJ, et al. (February 2012). "Phase I study of bosutinib, a src/abl tyrosine kinase inhibitor, administered to patients with advanced solid tumors" (PDF). Clinical Cancer Research. 18 (4): 1092–100. doi:10.1158/1078-0432.CCR-11-2378. PMID 22179664.
  3. ↑ Bosutinib. livertox.nih.gov. 2012. Archived from the original on 3 April 2018. Retrieved 2 April 2018.

پیوند به بیرون

در ویکی‌انبار پرونده‌هایی دربارهٔ بوزوتینیب موجود است.
آیکون خرد

این یک مقالهٔ خرد داروشناسی است. می‌توانید با گسترش آن به ویکی‌پدیا کمک کنید.

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