维莫非 尼
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读音 | /ˌvɛməˈræfənɪb/ VEM-ə-RAF-ə-nib |
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其他 | PLX4032, RG7204, RO5185426 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a612009 |
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给药 | |
ATC碼 | |
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识别 | |
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CAS | 918504-65-1 |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
PDB | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.287.801 |
C23H18ClF2N3O3S | |
489.92 g·mol−1 | |
3D | |
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维莫
批准 [编辑]
维莫
维莫
2012
2017
作用 机 制 [编辑]
维莫
维莫
耐 药性[编辑]
癌 细胞开始过度表 达细胞表面 蛋白 PDGFRB,从而产生了 另一种生存 途 径 。第 二 个称为NRAS的 癌 基 因 发生突变,重 新 激 活 正常 的 BRAF生存 途 径 。[11]基 质细胞分泌 肝 细胞生 长因子 。[12][13]
临床试验[编辑]
2010
2011
计划进行进
2015
副作用 [编辑]
2013
参考 文献 [编辑]
- ^ 1.0 1.1 Bollag, Gideon; Hirth, Peter; Tsai, James; Zhang, Jiazhong; Ibrahim, Prabha N.; Cho, Hanna; Spevak, Wayne; Zhang, Chao; Zhang, Ying; Habets, Gaston; Burton, Elizabeth A. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature. 2010-09-30, 467 (7315) [2022-06-12]. ISSN 1476-4687. PMC 2948082
. PMID 20823850. doi:10.1038/nature09454. (
原始 内容 存 档于2022-01-05). - ^ FDA Approves Zelboraf (Vemurafenib) and Companion Diagnostic for BRAF Mutation-Positive Metastatic Melanoma, a Deadly Form of Skin Cancer. Genentech: Press Releases. 2011-08-17 [2022-06-12]. (
原始 内容 存 档于2016-11-07). - ^ Notice of Decision for Zelboraf. Health Canada. 2012-02-15 [2022-06-12]. (
原始 内容 存 档于2012-05-02). - ^ Hofland, Peter. First Personalized Cancer Medicine Allows Patients with Deadly Form of Metastatic Melanoma to Live Significantly Longer. Onco'Zine. 2012-02-20 [2022-06-12]. (
原始 内容 存 档于2012-04-11). - ^ Commissioner, Office of the. FDA approves first treatment for certain patients with Erdheim-Chester Disease, a rare blood cancer. FDA. 2020-03-24 [2022-06-12]. (
原始 内容 存 档于2022-06-18) (英 语). - ^ Diamond, Eli L.; Subbiah, Vivek; Lockhart, A. Craig; Blay, Jean-Yves; Puzanov, Igor; Chau, Ian; Raje, Noopur S.; Wolf, Jurgen; Erinjeri, Joseph P.; Torrisi, Jean; Lacouture, Mario. Vemurafenib for BRAF V600-Mutant Erdheim-Chester Disease and Langerhans Cell Histiocytosis: Analysis of Data From the Histology-Independent, Phase 2, Open-label VE-BASKET Study. JAMA oncology. 2018-03-01, 4 (3) [2022-06-12]. ISSN 2374-2445. PMC 5844839
. PMID 29188284. doi:10.1001/jamaoncol.2017.5029. (
原始 内容 存 档于2022-06-16). - ^ Sala, Elisa; Mologni, Luca; Truffa, Silvia; Gaetano, Carlo; Bollag, Gideon E.; Gambacorti-Passerini, Carlo. BRAF silencing by short hairpin RNA or chemical blockade by PLX4032 leads to different responses in melanoma and thyroid carcinoma cells. Molecular cancer research: MCR. 2008-05, 6 (5) [2022-06-12]. ISSN 1541-7786. PMID 18458053. doi:10.1158/1541-7786.MCR-07-2001. (
原始 内容 存 档于2022-06-23). - ^ Maverakis, Emanual; Cornelius, Lynn A.; Bowen, Glen M.; Phan, Tiffany; Patel, Falin B.; Fitzmaurice, Sarah; He, Young; Burrall, Barbara; Duong, Christopher; Kloxin, April M.; Sultani, Hawa. Metastatic melanoma - a review of current and future treatment options. Acta Dermato-Venereologica. 2015-05, 95 (5) [2022-06-12]. ISSN 1651-2057. PMID 25520039. doi:10.2340/00015555-2035. (
原始 内容 存 档于2022-06-15). - ^ Hatzivassiliou, Georgia; Song, Kyung; Yen, Ivana; Brandhuber, Barbara J.; Anderson, Daniel J.; Alvarado, Ryan; Ludlam, Mary J. C.; Stokoe, David; Gloor, Susan L.; Vigers, Guy; Morales, Tony. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature. 2010-03-18, 464 (7287) [2022-06-12]. ISSN 1476-4687. PMID 20130576. doi:10.1038/nature08833. (
原始 内容 存 档于2022-06-22). - ^ Halaban, Ruth; Zhang, Wengeng; Bacchiocchi, Antonella; Cheng, Elaine; Parisi, Fabio; Ariyan, Stephan; Krauthammer, Michael; McCusker, James P.; Kluger, Yuval; Sznol, Mario. PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells. Pigment Cell & Melanoma Research. 2010-04, 23 (2) [2022-06-12]. ISSN 1755-148X. PMC 2848976
. PMID 20149136. doi:10.1111/j.1755-148X.2010.00685.x. (
原始 内容 存 档于2022-06-16). - ^ Nazarian, Ramin; Shi, Hubing; Wang, Qi; Kong, Xiangju; Koya, Richard C.; Lee, Hane; Chen, Zugen; Lee, Mi-Kyung; Attar, Narsis; Sazegar, Hooman; Chodon, Thinle. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature. 2010-12-16, 468 (7326) [2022-06-12]. ISSN 1476-4687. PMC 3143360
. PMID 21107323. doi:10.1038/nature09626. (
原始 内容 存 档于2022-06-20). - ^ Straussman, Ravid; Morikawa, Teppei; Shee, Kevin; Barzily-Rokni, Michal; Qian, Zhi Rong; Du, Jinyan; Davis, Ashli; Mongare, Margaret M.; Gould, Joshua; Frederick, Dennie T.; Cooper, Zachary A. Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion. Nature. 2012-07-26, 487 (7408) [2022-06-12]. ISSN 1476-4687. PMC 3711467
. PMID 22763439. doi:10.1038/nature11183. (
原始 内容 存 档于2022-06-12). - ^ Wilson, Timothy R.; Fridlyand, Jane; Yan, Yibing; Penuel, Elicia; Burton, Luciana; Chan, Emily; Peng, Jing; Lin, Eva; Wang, Yulei; Sosman, Jeff; Ribas, Antoni. Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors. Nature. 2012-07-26, 487 (7408) [2022-06-12]. ISSN 1476-4687. PMC 3724525
. PMID 22763448. doi:10.1038/nature11249. (
原始 内容 存 档于2022-06-24). - ^ Drug hope for advanced melanoma. BBC News. 2009-06-02 [2022-06-12]. (
原始 内容 存 档于2009-06-05) (英国 英 语). - ^ Harmon, Amy. A Roller Coaster Chase for a Cure. The New York Times. 2010-02-22 [2022-06-12]. ISSN 0362-4331. (
原始 内容 存 档于2017-02-10) (美国 英 语). - ^ Garber, Ken. Cancer research. Melanoma drug vindicates targeted approach. Science (New York, N.Y.). 2009-12-18, 326 (5960) [2022-06-12]. ISSN 1095-9203. PMID 20019269. doi:10.1126/science.326.5960.1619. (
原始 内容 存 档于2022-06-20). - ^ Flaherty, K.; Puzanov, I.; Sosman, J.; Kim, K.; Ribas, A.; McArthur, G.; Lee, R. J.; Grippo, J. F.; Nolop, K.; Chapman, P. Phase I study of PLX4032: Proof of concept for V600E BRAF mutation as a therapeutic target in human cancer. Journal of Clinical Oncology. 2009-05-20, 27 (15_suppl) [2022-06-12]. ISSN 0732-183X. doi:10.1200/jco.2009.27.15_suppl.9000. (
原始 内容 存 档于2022-06-15) (英 语). - ^ Flaherty, Keith T.; Puzanov, Igor; Kim, Kevin B.; Ribas, Antoni; McArthur, Grant A.; Sosman, Jeffrey A.; O'Dwyer, Peter J.; Lee, Richard J.; Grippo, Joseph F.; Nolop, Keith; Chapman, Paul B. Inhibition of mutated, activated BRAF in metastatic melanoma. The New England Journal of Medicine. 2010-08-26, 363 (9) [2022-06-12]. ISSN 1533-4406. PMC 3724529
. PMID 20818844. doi:10.1056/NEJMoa1002011. (
原始 内容 存 档于2022-06-22). - ^ Plexxikon. A Study to Assess Safety, Pharmacokinetics, and Pharmacodynamics of PLX4032 in Patients With Solid Tumors. Roche Pharma AG. 2017-08-18 [2022-06-12]. (
原始 内容 存 档于2022-06-12). - ^ Hoffmann-La Roche. An Open-label Multicenter Study on the Efficacy of Continuous Oral Dosing of Vemurafenib on Tumour Response in Previously Treated Patients With Metastatic Melanoma. 2017-06-26 [2022-06-12]. (
原始 内容 存 档于2022-06-22). - ^ Press Releases. www.plexxikon.com. [2022-06-12]. (
原始 内容 存 档于2021-05-08). - ^ 22.0 22.1 Writer, GEN Staff. Plexxikon and Roche Report Positive Data from Phase III BRAF Mutation Melanoma Study. GEN - Genetic Engineering and Biotechnology News. 2011-06-06 [2022-06-12]. (
原始 内容 存 档于2022-06-12) (美国 英 语). - ^ Cobimetinib. Exelixis. 2015-02-04 [2022-06-12]. (
原始 内容 存 档于2015-02-04). - ^ Lawrence, Leah. MEK/BRAF Inhibitor Combo Reduces Death by One-Third in Melanoma. Cancer Network. [2022-06-12]. (
原始 内容 存 档于2020-11-28) (英 语). - ^ News, Oncology & Biotech. BRIM-2 Upholds Benefits Emerging with Vemurafenib in Melanoma. Oncology & Biotech News. July 2011. 2011-07-25, 5 (7) (
英 语). - ^ Getting close and personal. The Economist. [2022-06-12]. ISSN 0013-0613. (
原始 内容 存 档于2022-06-12).
延伸 阅读[编辑]
- Dean, Laura. Vemurafenib Therapy and BRAF and NRAS Genotype. Pratt, Victoria M. (编). Medical Genetics Summaries. Bethesda (MD): National Center for Biotechnology Information (US). 2012 [2022-06-12]. PMID 28809522. (
原始 内容 存 档于2022-02-03).
外部 链接[编辑]
- U.S. National Library of Medicine - Quick Access to Quality Drug Information. [2022-06-12]. (
原始 内容 存 档于2022-06-12) (英 语).
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