The discovery and development of SU14813, a next-generation multitargeted tyrosine kinase inhibitor for the treatment of human malignancies.

Hu Lowe D; Brega N; Patyna S

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The discovery and development of SU14813, a next-generation multitargeted tyrosine kinase inhibitor for the treatment of human malignancies.

机译：SU14813的发现和开发，SU14813是用于治疗人类恶性肿瘤的下一代多靶点酪氨酸激酶抑制剂。

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SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), KIT, and fms-like tyrosine kinase 3 (FLT-3) (1). These receptors play a key role in angiogenesis and the growth and metastasis of solid and hematologic tumors. SU14813 was developed as a next-generation TKI agent following sunitinib (SU11248) designed to demonstrate optimized pharmacokinetic (PK) and tolerability profiles. Sunitinib malate (SUTENT) is approved multinationally for the treatment of gastrointestinal stromal tumor (GIST) after the failure of imatinib due to resistance or intolerance, advanced renal cell carcinoma (RCC), and unresect-able or metastatic, well-differentiated pancreatic neuro-endocrine tumors.

机译：SU14813是一种针对血管内皮生长因子受体（VEGFR），血小板衍生生长因子受体（PDGFR），KIT和fms样酪氨酸激酶3（FLT-3）的口服，多靶点酪氨酸激酶抑制剂（TKI）（1）。这些受体在实体瘤和血液肿瘤的血管生成以及生长和转移中起关键作用。 SU14813是继舒尼替尼（SU11248）之后开发的下一代TKI试剂，旨在证明其具有最佳的药代动力学（PK）和耐受性。苹果酸舒尼替尼（SUTENT）已因抗药性或不耐受性，晚期肾细胞癌（RCC）以及无法切除或转移性，分化良好的胰腺神经疾病而因伊马替尼失败而在国际上获批用于治疗胃肠道间质瘤（GIST）内分泌肿瘤。

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《Molecular cancer therapeutics》 |2011年第11期|共1页
作者
Hu Lowe D; Brega N; Patyna S;
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中图分类肿瘤学;
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1. The discovery and development of SU14813, a next-generation multitargeted tyrosine kinase inhibitor for the treatment of human malignancies. [J] . Hu Lowe D, Brega N, Patyna S Molecular cancer therapeutics . 2011,第11期

机译：SU14813的发现和开发，SU14813是用于治疗人类恶性肿瘤的下一代多靶点酪氨酸激酶抑制剂。
2. The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2, 3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents [J] . ZhangX., RaghavanS., IhnatM., Bioorganic and medicinal chemistry . 2014,第14期

机译：水溶性4-取代-2,6-二甲基呋喃并[2,3-d]嘧啶类多靶受体酪氨酸激酶抑制剂和微管靶向抗肿瘤药的设计与发现
3. Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor. [J] . Dai Y, Hartandi K, Ji Z, Journal of Medicinal Chemistry . 2007,第7期

机译：N-（4-（3-氨基-1H-吲唑-4-基）苯基）-N'-（2-氟-5-甲基苯基）脲（ABT-869）的发现，这是一种基于3-氨基吲唑的口服活性剂多靶受体酪氨酸激酶抑制剂。
4. Predictive Efficacy of Low Burden EGFR Mutation Detected by Next-Generation Sequencing on Response to EGFR Tyrosine Kinase Inhibitors in Non-Small-Cell Lung Carcinoma [C] . Yeul Hong Kim, Hye Sook Kim, Jae Sook Sung, Molecular Medicine TRI-CON. . 2014

机译：下一代测序对非小细胞肺癌抗蛋白酶激酶抑制剂进行下一代测序检测的低负荷EGFR突变的预测疗效
5. Computer-aided discovery of novel natural product inhibitors of receptor tyrosine kinases and their rational semisynthetic optimizations for multiple malignancies control. [D] . Mohyeldin, Mohamed M. 2016

机译：计算机辅助发现的受体酪氨酸激酶的新型天然产物抑制剂及其对多种恶性肿瘤的合理的半合成优化。
6. The Design and Discovery of Water Soluble 4-Substituted-26-dimethylfuro23-dpyrimidines as Multitargeted Receptor Tyrosine Kinase Inhibitors and Microtubule Targeting Antitumor Agents [O] . Xin Zhang, Sudhir Raghavan, Michael Ihnat, -1

机译：水溶性4-取代-26-二甲基呋喃23-d嘧啶作为多靶点受体酪氨酸激酶抑制剂和微管靶向抗肿瘤剂的设计与发现
7. The Discovery and Development of SU14813, a Next-Generation Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Human Malignancies [O] . Dana Hu-Lowe, Nicoletta Brega, Shem Patyna 2011

机译：SU14813的发现与发展，是治疗人恶性肿瘤的下一代多元酪氨酸激酶抑制剂

The discovery and development of SU14813, a next-generation multitargeted tyrosine kinase inhibitor for the treatment of human malignancies.

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