各靶点总图

υīСКī · 发表于 2014-3-29 23:46:41

收藏了慢慢研究

r12345j · 发表于 2014-3-31 21:22:41

只看图，没有说明很难理解啊

WXMPQ · 发表于 2014-4-14 19:05:07

2014年全球药物研发热门靶点（肿瘤部分）

靶点	适应症	在研药物
PI3K抑制剂	实体瘤、淋巴瘤、白血病	Idelalisib (filed), BKM120 (phase III), BYL719 (phase II), pictilisib (phase II), XL765 (phase II), PF-05212384 (phase II), PF-04691502 (phase II), GS-9820 (phase II), dactolisib (phase II), copanlisib (phase II), GDC-0941 (phase II), GSK2141795 (phase II), RG7422 (phase II), BGT226 (phase I/II), XL147 (phase I), SAR260301 (phase I), GSK2636771 (phase I), GSK2269557 (phase I), GSK2126458 (phase I), GSK1059615 (phase I, failed?), RG7604 (phase I), RG7666 (phase I), AMG 319 (phase I), MLN1117 (phase I), AZD5363 (phase I), AZD8186 (phase I), AZD6482 (phase I)
mTOR抑制剂	实体瘤	MK-8669 (phase II), XL765 (phase II), dactolisib (phase II), PF-05212384 (phase II), PF-04691502 (phase II), BGT226 (phase I/II), GSK1059615 (phase I, failed?), AZD8055 (phase I)
Akt抑制剂	实体瘤	MK-2206 (phase II), ipatasertib (phase II), GSK2110183 (phase I), GSK2141795 (phase I), GSK690693 (phase I, failed?), RG7440 (phase I)
Raf抑制剂	黑素瘤	Vemurafenib (approved), Dabrafenib (approved), LGX818 (phase II), RG7304 (phase I), MLN2480 (phase I)
MEK1/2抑制剂	黑素瘤、卵巢癌	Trametinib (approved), MEK162 (phase III), pimasertib (phase II), RG7167 (phase I), TAK-733 (phase I)
EGFR/HER2抑制剂	非小细胞肺癌、乳腺癌	Gefitinib (approved), erlotinib (approved), afatinib (approved), lapatinib (approved), dacomitinib (phase III, failed), AZD8931 (phase II), AEE788 (phase I/II, failed?), AZD9291 (phase I/II)
FGFR抑制剂	实体瘤	BGJ398 (phase II), LY2874455 (phase II), AZD4547 (phase II)
多靶点RTK抑制剂	实体瘤	TKI258 (phase III), nintedanib (phase III), motesanib (phase III)
Syk抑制剂	类风湿性关节炎、肿瘤	Fostamatinib (phase III, failed), GS-9973 (phase II), TAK-659 (phase I)

WXMPQ · 发表于 2014-4-14 19:06:17

Aurora激酶抑制剂	白血病、淋巴瘤	MLN8237 (phase III), AZD1152 (phase II/III), tozasertib (phase II, failed?), AMG 900 (phase I), MK-5108 (phase I, failed?), TAK-901 (phase I, failed?), GSK1070916 (phase I, failed?), PF-03814735 (phase I, failed?)
ALK抑制剂	非小细胞肺癌	Crizotinib (approved), LDK378 (phase III), RG7853 (phase II)
Bcl-2抑制剂	白血病、淋巴瘤	RG7601 (phase II), ABT-199 (phase II), ABT-737 (phase II), ABT-263 (phase II)
HDM2/p53抑制剂	实体瘤	SAR405838 (phase I), RG7388 (phase I), JNJ-26854165 (phase I)
JAK1/2/3抑制剂	类风湿性关节炎、银屑病、骨髓增殖性肿瘤	Tofacitinib (approved), ruxolitinib (approved), momelotinib (phase III), baricitinib (phase III), LY2784544 (phase II), GSK2586184 (phase II), GLPG0634 (phase II), AZD1480 (phase I, failed)
c-Met抑制剂	实体瘤	Crizotinib (approved), foretinib (phase II), LY2801653 (phase II), SAR125844 (phase I), AMG 208 (phase I), AMG 337 (phase I)
HDAC抑制剂	多发性骨髓瘤、淋巴瘤	Vorinostat (approved), romidepsin (approved), LBH589 (phase III), JNJ-26481585 (phase II)
Hedgehog通路抑制剂	基底细胞癌、急性粒细胞白血病	Vismodegib (approved), erismodegib (phase II), BMS-833923 (phase II), LY2940680 (phase II), PF-04449913 (phase I)
ChK1抑制剂	实体瘤、淋巴瘤	MK-8776 (phase II), LY2603618 (phase II, failed), RG7741 (phase I), AZD7762 (phase I, failed)
PARP抑制剂	乳腺癌、卵巢癌	Veliparib (phase III), olaparib (phase III), rucaparib (phase III), niraparib (phase III), AZD2461 (phase I, failed), iniparib (phase III, failed)
CDK抑制剂	乳腺癌	Palbociclib (phase III), dinaciclib (phase III), LEE011 (phase II), LY2835219 (phase II), BAY 1000394 (phase I/II), AZD5438 (phase I, failed?)
p38 MAPK抑制剂	急性冠脉综合征、慢性阻塞性肺病、急性肺损伤、肿瘤	losmapimod (phase II), dilmapimod (phase II), LY2228820 (phase II)
Notch通路抑制剂	实体瘤	MK-0752 (phase I/II, failed?), PF-03084014 (phase I), LY3039478 (phase I)
癌症免疫疗法（PD1/PDL1、CTLA4、CAR）	黑素瘤、非小细胞肺癌、淋巴瘤	Ipilimumab (approved), MK-3475 (phase III), nivolumab (phase III), MPDL3280A (phase I), AMP-514 (phase I), AMP-224 (phase I), CTL019 (phase I)
Anti-EGFR, HER2, HER3, PDGFR, VEGF(R), Tie2, c-Met, CSF-1R, TGF(R), IGF-1R单抗	实体瘤、AMD	Bevacizumab (approved), pertuzumab (approved), ranibizumab (approved), cetuximab (approved), panitumumab (approved), ramucirumab (filed), onartuzumab (phase III), necitumumab (phase III), olaratumab (phase II), icrucumab (phase II), LJM716 (phase II), trebananib (phase II), RG7597 (phase II), fresolimumab (phase II), SAR256212 (phase II), LY3016859 (phase II), LY2382770 (phase II), cixutumumab (phase II), icrucumab (phase II), RG7116 (phase I), AMG 780 (phase I), RG7155 (phase I), RG7221 (phase I), SAR307746 (phase I)
Anti-CD19, CD20, CD32, CD38, CD319单抗	淋巴瘤、白血病、自身免疫性疾病	Rituximab (approved), ibritumomab (approved), ofatumumab (approved), obinutuzumab (approved), ocrelizumab (phase III), elotuzumab (phase III), SAR3419 (phase II), SAR650984 (phase I), AMG 729 (phase I)
抗体偶联药物	肿瘤	SGN-35 (approved), T-DM1 (approved), RG7593 (phase II), RG7596 (phase II), ABT-414 (phase I/II), AMG 172 (phase I), RG7450 (phase I), RG7458 (phase I), RG7598 (phase I), RG7599 (phase I), RG7600 (phase I), RG7636 (phase I), AMG 172