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url url url url
  2. Weltenzyklopädie
  3. سورافنیب - ویکی‌پدیا، دانشنامهٔ آزاد
سورافنیب - ویکی‌پدیا، دانشنامهٔ آزاد
از ویکی‌پدیا، دانشنامهٔ آزاد
سورافنیب
داده‌های بالینی
نام‌های تجاریNexavar
نام‌های دیگرNexavar
Sorafenib tosylate
AHFS/Drugs.commonograph
مدلاین پلاسa607051
داده‌ها
رده‌بندی داروهای
بارداری
  • AU: D
روش مصرف داروOral
کد ATC
وضعیت قانونی
وضعیت قانونی
داده‌های فارماکوکینتیک
زیست فراهمی۳۸–۴۹٪
پیوند پروتئینی۹۹٫۵٪
متابولیسمگلوکورونیداسیون و اکسیداسیون کبدی (توسط CYP3A4 و UGT1A9)
نیمه‌عمر حذف۲۵–۴۸ ساعت
دفعمدفوع (۷۷٪) و ادرار (۱۹٪)
شناسه‌ها
  • 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]
    phenoxy]-N-methyl-pyridine-2-carboxamide
شمارهٔ سی‌ای‌اس
پاب‌کم CID
IUPHAR/BPS
دراگ‌بنک
کم‌اسپایدر
UNII
KEGG
ChEBI
ChEMBL
لیگاند بانک داده پروتئین
CompTox Dashboard (EPA)
ECHA InfoCard100.110.083 ویرایش در ویکی‌داده
داده‌های فیزیکی و شیمیایی
فرمول شیمیاییC21H16ClF3N4O۳
جرم مولی464.825 g/mol g·mol−1
مدل سه بعدی (جی‌مول)
  • CNC(=O)c1cc(ccn1)Oc2ccc(cc2)NC(=O)Nc3ccc(c(c3)C(F)(F)F)Cl
  • InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,۲۸٬۲۹٬۳۱) ✔Y
  • Key:MLDQJTXFUGDVEO-UHFFFAOYSA-N ✔Y
  (صحت‌سنجی)

سورافنیب (انگلیسی: Sorafenib) با نام تجاری «Nexavar"[۱] یک داروی بازداندهٔ کیناز که جهت درمان سرطان پیشرفتهٔ کلیه، سرطان پیشرفته و اولیهٔ کبد، و سرطان تیروئید پیشرفتهٔ مقاوم به ید رادیواکتیو بکار می‌رود.[۲][۳][۴][۵]

این دارو در واقع بازدارندهٔ تعدادی از بازدارنده‌های تیروزین-کیناز از جمله گیرنده فاکتور رشد اندوتلیال عروقی، گیرنده فاکتور رشد مشتق از پلاکت و RAF کیناز (با تمایل بیشتر به c-Raf نسبت به BRAF) است[۶][۷][۸] و استفاده از آن، موجب القای پدیدهٔ اتوفاژی می‌شود[۹] که می‌تواند رشد سلول‌های سرطانی را مهار کند. البته این پدیده ممکن است خود منجر به بروز مقاومت دارویی شود.[۱۰]

عوارض شایع این دارو (با احتمال بروز بیش از ۱۰٪) عبارتند از: لنفوپنی، کاهش فسفات خون، خونریزی، فشار خون بالا، اسهال، راش، ریزش مو (در بیش از ۳۰٪ موارد)، قرمز شدنِ کف دست‌ها، خارش، اریتما، افزایش سطح آمیلاز، افزایش سطح لیپاز، خستگی، درد، تهوع و استفراغ.

منابع

  1. ↑ "FDA Approves Nexavar for Patients with Inoperable Liver Cancer" (Press release). FDA. November 19, 2007. Retrieved November 10, 2012.
  2. ↑ "Nexavar (sorafenib) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 26 December 2013.
  3. ↑ "NEXAVAR (sorafenib) tablet, film coated [Bayer HealthCare Pharmaceuticals Inc.]". DailyMed. Bayer HealthCare Pharmaceuticals Inc. November 2013. Retrieved 26 December 2013.
  4. ↑ "Nexavar 200mg film-coated tablets - Summary of Product Characteristics (SPC) - (eMC)". electronic Medicines Compendium. Bayer plc. 27 March 2013. Retrieved 26 December 2013.
  5. ↑ "PRODUCT INFORMATION NEXAVAR® (sorafenib tosylate)" (PDF). TGA eBusiness Services. Bayer Australia Ltd. 12 December 2012. Retrieved 26 December 2013.
  6. ↑ Smalley KS, Xiao M, Villanueva J, Nguyen TK, Flaherty KT, Letrero R, Van Belle P, Elder DE, Wang Y, Nathanson KL, Herlyn M (January 2009). "CRAF inhibition induces apoptosis in melanoma cells with non-V600E BRAF mutations". Oncogene. 28 (1): 85–94. doi:10.1038/onc.2008.362. PMC 2898184. PMID 18794803.
  7. ↑ Wilhelm SM, Adnane L, Newell P, Villanueva A, Llovet JM, Lynch M (October 2008). "Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling". Mol. Cancer Ther. 7 (10): 3129–40. doi:10.1158/1535-7163.MCT-08-0013. PMID 18852116.
  8. ↑ Keating GM, Santoro A (2009). "Sorafenib: a review of its use in advanced hepatocellular carcinoma". Drugs. 69 (2): 223–40. doi:10.2165/00003495-200969020-00006. PMID 19228077.
  9. ↑ Zhang Y (Jan 2014). "Screening of kinase inhibitors targeting BRAF for regulating autophagy based on kinase pathways". J Mol Med Rep. 9 (1): 83–90. doi:10.3892/mmr.2013.1781. PMID 24213221.
  10. ↑ Gauthier A (Feb 2013). "Role of sorafenib in the treatment of advanced hepatocellular carcinoma: An update." Hepatol Res. 43 (2): 147–154. doi:10.1111/j.1872-034x.2012.01113.x. PMC 3574194. PMID 23145926.
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