[1] 陈万青, 郑荣寿, 曾红梅, 等.2011年中国恶性肿瘤发病和死亡分析[J].中国肿瘤, 2015, 24(1):1-10.DOI:10.11735/j.issn.1004-0242.2015.01.A001.
Chen WQ, Zheng RS, Zeng HM, et al.Report of cancer incidence and mortality in China, 2011[J].China Cancer, 2015, 24(1):1-10.  doi: 10.11735/j.issn.1004-0242.2015.01.A001
[2] Cataldo VD, Gibbons DL, Pérez-Soler R, et al.Treatment of non-small-cell lung cancer with erlotinib or gefitinib[J].N Engl J Med, 2011, 364(10):947-955.DOI:10.1056/NEJMct0807960.
[3] Mendelsohn J, Baselga J.Status of epidermal growth factor receptor antagonists in the biology and treatment of cancer[J].J Clin Oncol, 2003, 21(14):2787-2799.DOI:10.1200/JCO.2003.01.504.
[4] Rudin M, Weissleder R.Molecular imaging in drug discovery and development[J].Nat Rev Drug Discov, 2003, 2(2):123-131.DOI:10.1038/nrd1007.
[5] Green MR.Targeting targeted therapy[J].N Engl J Med, 2004, 350(21):2191-2193.DOI:10.1056/NEJMe048101.
[6] Gridelli C, Marinis F, Maio M, et al.Gefitinib as first-line treatment for patients with advanced non-small-cell lung cancer with activating epidermal growth factor receptor mutation:Review of the evidence[J].Lung Cancer, 2011, 71(3):249-257.DOI:10.1016/j.lungcan.2010.12.008.
[7] Jian G, Songwen Z, Ling Z, et al.Prediction of epidermal growth factor receptor mutations in the plasma/pleural effusion to efficacy of gefitinib treatment in advanced non-small cell lung cancer[J].J Cancer Res Clin Oncol, 2010, 136(9):1341-1347.DOI:10.1007/s00432-010-0785-z.
[8] Bai H, Mao L, Wang HS, et al.Epidermal growth factor receptor mutations in plasma DNA samples predict tumor response in Chinese patients with stages IIIB to IV non-small-cell lung cancer[J].J Clin Oncol, 2009, 27(16):2653-2659.DOI:10.1200/JCO.2008.17.3930.
[9] Johnström P, Fredriksson A, Thorell JO, et al.Synthesis of[methoxy-11C]PD153035, a selective EGF receptor tyrosine kinase inhibitor[J].J Labelled Comp Radiopharm, 1998, 41(7):623-629.DOI:10.1002/(SICI)1099-1344(199807)41:73.0.CO;2-Q.
[10] Fredriksson A, Johnström P, Thorell JO, et al.In vivo evaluation of the biodistribution of 11C-labeled PD153035 in rats without and with neuroblastoma implants[J].Life Sci, 1999, 65(2):165-174.DOI:10.1016/S0024-3205(99)00233-7.
[11] Samén E, Thorell JO, Fredriksson A, et al.The tyrosine kinase inhibitor PD153035:implication of labeling position on radiometabolites formed in vitro[J].Nucl Med Biol, 2006, 33(8):1005-1011.DOI:10.1016/j.nucmedbio.2006.09.008.
[12] Samén E, Arnberg F, Lu L, et al.Metabolism of epidermal growth factor receptor targeting probe[11C]PD153035:impact on biodistribution and tumor uptake in rats[J].J Nucl Med, 2013, 54(10):1804-1811.DOI:10.2967/jnumed.113.120493.
[13] Wang H, Yu JM, Yang GR, et al.Further characterization of the epidermal growth factor receptor ligand 11C-PD153035[J].Chin Med J(Engl), 2007, 120(11):960-964.
[14] Wang H, Yu J, Yang G, et al.Assessment of 11C-labeled-4-N-(3-bromoanilino)-6, 7-dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression[J].Cancer Sci, 2007, 98(9):1413-1416.DOI:10.1111/j.1349-7006.2007.00562.x.
[15] Liu N, Li M, Li X, et al.PET-based biodistribution and radiation dosimetry of epidermal growth factor receptor-selective tracer 11C-PD153035 in humans[J].J Nucl Med, 2009, 50(2):303-308.DOI:10.2967/jnumed.108.056556.
[16] Meng X, Loo BW Jr, Ma L, et al.Molecular imaging with 11C-PD153035 PET/CT predicts survival in non-small cell lung cancer treated with EGFR-TKI:a pilot study[J].J Nucl Med, 2011, 52(10):1573-1579.DOI:10.2967/jnumed.111.092874.
[17] DeJesus OT, Murali D, Flores LG, et al.Synthesis of[F-18]-ZD1839 as a PET imaging agent for epidermal growth factor receptors[J].J Labelled Comp Radiopharm, 2003, 46(S1):S1-S9.DOI:10.1002/jlcr.750.
[18] Murali D, Flores LG, Converse AK, et al.Evaluation of[F-18] Iressa as a PET agent for tumor overexpressing epidermal growth factor (EGFR) receptors[J].J Labelled Comp Radiopharm, 2005, 48(s1):1-11.DOI:10.1002/jlcr.968.
[19] Seimbille Y, Phelps ME, Czernin J, et al.Fluorin-18 labeling of 6, 7-distributed anilinoquinazoline derivatives for positron emission tomography(PET) imaging of tyrosine kianse receptors:synthesis of 18F-Iressa and related molecular probes[J].J Labelled Comp Radiopharm, 2005, 48(11):829-843.DOI:10.1002/jlcr.998.
[20] Su H, Seimbille Y, Ferl GZ, et al.Evaluation of[18F] gefitinib as a molecular imaging probe for the assessment of the epidermal growth factor receptor status in malignant tumors[J].Eur J Nucl Med Mol Imaging, 2008, 35(6):1089-1099.DOI:10.1007/s00259-007-0636-6.
[21] Läppchen T, Vlaming ML, Custers E, et al.Automated synthesis of[18F] gefitinib on a modular system[J].Appl Radiat Isot, 2012, 70(1):205-209.DOI:10.1016/j.apradiso.2011.09.005.
[22] Holt DP, Ravert HT, Dannals RF, et al.Synthesis of[11C] gefitinib for imaging epidermal growth factor receptor tyrosine kinase with positron emission tomography[J].J Labelled Comp Radiopharm, 2006, 49(10):883-888.DOI:10.1002/jlcr.1104.
[23] Wang JQ, Gao M, Miller KD, et al.Synthesis of[11C] Iressa as a new potential PET cancer imaging agent for epidermal growth factor receptor tyrosine kinase[J].Bioorg Med Chem Lett, 2006, 16(15):4102-4106.DOI:10.1016/j.bmcl.2006.04.080.
[24] Zhang MR, Kumata K, Hatori A, et al.[11C]Gefitinib([11C] Iressa):radiosynthesis, in vitro uptake, and in vivo imaging of intact murine fibrosarcoma[J].Mol Imaging Biol, 2010, 12(2):181-191.DOI:10.1007/s11307-009-0265-5.
[25] Kawamura K, Yamasaki T, Yui J, et al.In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using[11C] gefitinib[J].Nucl Med Biol, 2009, 36(3):239-246.DOI:10.1016/j.nucmedbio.2008.12.006.
[26] Vlaming ML, Läppchen T, Jansen HT, et al.PET-CT imaging with[18F]-gefitinib to measure Abcb1a/1b(P-gp)and Abcg2(Bcrp1)mediated drug-drug interactions at the murine blood-brain barrier[J].Nucl Med Biol, 2015, 42(11):833-841.DOI:10.1016/j.nucmedbio.2015.07.004.
[27] Memon AA, Jakobsen S, Dagnaes-Hansen F, et al.Positron emission tomography(PET) imaging with[11C]-labeled erlotinib:a micro-PET study on mice with lung tumor xenografts[J].Cancer Res, 2009, 69(3):873-878.DOI:10.1158/0008-5472.CAN-08-3118.
[28] Memon AA, Weber B, Winterdahl M, et al.PET imaging of patients with non-small cell lung cancer employing an EGF receptor targeting drug as tracer[J].Br J Cancer, 2011, 105(12):1850-1855.DOI:10.1038/bjc.2011.493.
[29] Weber B, Winterdahl M, Memon A, et al.Erlotinib accumulation in brain metastases from non-small cell lung cancer:visualization by positron emission tomography in a patient harboring a mutation in the epidermal growth factor receptor[J].J Thorac Oncol, 2011, 6(7):1287-1289.DOI:10.1097/JTO.0b013e318219ab87.
[30] Petrulli JR, Sullivan JM, Zheng MQ, et al.Quantitative analysis of[11C]-erlotinib PET demonstrates specific binding for activating mutations of the EGFR kinase domain[J].Neoplasia, 2013, 15(12):1347-1353.DOI:10.1593/neo.131666.
[31]

Abourbeh G, Itamar B, Salnikov O, et al.Identifying erlotinib-sensitive non-small cell lung carcinoma tumors in mice using[11C]erlotinib PET[J/OL].EJNMMI Res, 2015, 5:4[2016-08-16].https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4385014.DOI:10.1186/s13550-014-0080-0.

[32] Traxl A, Wanek T, Mairinger S, et al.Breast Cancer Resistance Protein and P-Glycoprotein Influence in Vivo Disposition of 11C-Erlotinib[J].J Nucl Med, 2015, 56(12):1930-1936.DOI:10.2967/jnumed.115.161273.
[33] Bahce I, Smit EF, Lubberink M, et al.Development of[11C]erlotinib positron emission tomography for in vivo evaluation of EGF receptor mutational status[J].Clin Cancer Res, 2013, 19(1):183-193.DOI:10.1158/1078-0432.CCR-12-0289.
[34] Yaqub M, Bahce I, Voorhoeve C, et al.Quantitative and simplified analysis of 11C-Erlotinib studies[J].J Nucl Med, 2016, 57(6):861-866.DOI:10.2967/jnumed.115.165225.
[35]

Bahce I, Yaqub M, Errami H, et al.Effects of erlotinib therapy on[11C]erlotinib uptake in EGFR mutated, advanced NSCLC[J/OL].EJNMMI Res, 2016, 6(1):10[2016-08-16].https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4746207.DOI:10.1186/s13550-016-0169-8.

[36]

黄顺, 王全师, 郑希, 等.一种EGFR正电子示踪剂及其制备方法和应用:中国, 201510114513.X[P].2015-08-05.

Huang S, Wang QS, Zhen X, et al.The preparation and application of an EGFR positron tracer:CN, 201510114513.X[P].2015-08-05.

[37] Basuli F, Wu H, Li C, et al.A first synthesis of 18F-radiolabeled lapatinib:a potential tracer for positron emission tomographic imaging of Erbb1/Erbb2 tyrosine kinase activity[J].J Labelled Comp Radiopharm, 2011, 54(9):633-636.DOI:10.1002/jlcr.1898.
[38]

Saleem A, Searle GE, Kenny LM, et al.Lapatinib access into normal brain and brain metastases in patients with HER-2 overexpressing breast cancer[J/OL].EJNMMI Res, 2015, 5:30[2016-08-16].https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4424224.DOI:10.1186/s13550-015-0103-5.

[39] Gao M, Lola CM, Wang M, et al.Radiosynthesis of[11C]Vandetanib and[11C]chloro-Vandetanib as new potential PET agents for imaging of VEGFR in cancer[J].Bioorg Med Chem Lett, 2011, 21(11):3222-3226.DOI:10.1016/j.bmcl.2011.04.049.
[40] Li F, Jiang S, Zu Y, et al.A tyrosine kinase inhibitor-based high-affinity PET radiopharmaceutical targets vascular endothelial growth factor receptor[J].J Nucl Med, 2014, 55(1):1525-1531.DOI:10.2967/jnumed.114.138925.
[41]

Samén, E, Li L, Mulder J, et al.Visualization of angiogenesis during cancer development in the polyoma middle T breast cancer model:molecular imaging with(R)-[11C]PAQ[J/OL].EJNMMI Res, 2014, 4(1):17[2016-08-16].https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3986910.DOI:10.1186/2191-219X-4-17.

[42] Murakami H, Tamura T, Takahashi T, et al.Phase I study of continuous afatinib(BIBW 2992) in patients with advanced non-small cell lung cancer afterprior chemotherapy/erlotinib/gefitinib (LUX-Lung 4)[J].Cancer Chemother Pharmacol, 2012, 69(4):891-899.DOI:10.1007/s00280-011-1738-1.
[43] Slobbe P, Windhorst AD, Stigter-van Walsum M, et al.Development of[18F] afatinib as new TKI-PET tracer for EGFR positive tumors[J].Nucl Med Biol, 2014, 41(9):749-757.DOI:10.1016/j.nucmedbio.2014.06.005.
[44]

Slobbe P, Windhorst AD, Stigter-van Walsum M, et al.A comparative PET imaging study with the reversible and irreversible EGFR tyrosine kinase inhibitors[11C]erlotinib and[18F]afatinib in lung cancer-bearing mice[J/OL].EJNMMI Res, 2015, 5(1):14[2016-08-16].https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4385286.DOI:10.1186/s13550-015-0088-0.

[45] Pal A, Glekas A, Doubrovin M, et al.Molecular imaging of EGFR kinase activity in tumors with 124I-labeled small molecular tracer and positron emission tomography[J].Mol Imaging Biol, 2006, 8(5):262-277.DOI:10.1007/s11307-006-0049-0.
[46] Tian M, Ogawa K, Wendt R, et al.Whole-body biodistribution kinetics, metabolism, and radiation dosimetry estimates of 18F-PEG6-IPQA in nonhuman primates[J].J Nucl Med, 2011, 52(6):934-941.DOI:10.2967/jnumed.110.086777.
[47] Yeh HH, Ogawa K, Balatoni J, et al.Molecular imaging of active mutant L858R EGF receptor(EGFR) kinase-expressing nonsmall cell lung carcinomas using PET/CT[J].Proc Natl Acad Sci U S A, 2011, 108(4):1603-1608.DOI:10.1073/pnas.1010744108.
[48] Pal A, Balatoni JA, Mukhopadhyay U, et al.Radiosynthesis and initial in vitro evaluation of[18F]F-PEG6-IPQA-a novel PET radiotracer for imaging EGFR expression-activity in lung carcinomas[J].Mol Imaging Biol, 2011, 13(5):853-861.DOI:10.1007/s11307-010-0408-8.
[49] Medina OP, Pillarsetty N, Glekas A, et al.Optimizing tumor targeting of the lipophilic EGFR-binding radiotracer SKI 243 using a liposomal nanoparticle delivery system[J].J Control Release, 2011, 149(3):292-298.DOI:10.1016/j.jconrel.2010.10.024.
[50]

Yeh SH, Lin CF, Kong FL, et al.Molecular imaging of nonsmall cell lung carcinomas expressing active mutant EGFR kinase using PET with[124I]-morpholino-IPQA[J/OL].Biomed Res Int, 2013, 2013:549359[2016-08-16].https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3730369.DOI:10.1155/2013/549359.

[51] Bonasera TA, Ortu G, Rozen Y, et al.Potential 18F-labeled biomarkers for epidermal growth factor receptor tyrosine kinase[J].Nucl Med Biol, 2001, 28(4):359-374.DOI:10.1016/S0969-8051(01)00200-1.
[52] Ortu G, Ben-David I, Rozen Y, et al.Labeled EGFr-TK irreversible inhibitor(ML03):in vitro and in vivo properties, potential as PET biomarker for cancer and feasibility as anticancer drug[J].Int J Cancer, 2002, 101(4):360-370.DOI:10.1002/ijc.10619.
[53] Ben-David I, Rozen Y, Ortu G, et al.Radiosynthesis of ML03, a novel positron emission tomography biomarker for targeting epidermal growth factor receptor via the labeling synthon:[11C]acryloyl chloride[J].Appl Radiat Isot, 2003, 58(2):209-217.DOI:10.1016/S0969-8043(02)00301-9.
[54] Mishani E, Abourbeh G, Rozen Y, et al.Novel carbon-11 labeled 4-dimethylamino-but-2-enoic acid[4-(phenylamino)-quinazoline-6-yl]-amides:potential PET bioprobes for molecular imaging of EGFR-positive tumors[J].Nucl Med Biol, 2004, 31(4):469-476.DOI:10.1016/j.nucmedbio.2003.12.005.
[55] Dissoki S, Laky D, Mishani E.Fluorine-18 labeling of ML04-presently the most promising irreversible inhibitor candidate for visualization of EGFR in cancer[J].J Label Compd Radiopharm, 2006, 49(6):533-543.DOI:10.1002/jlcr.1071.
[56] Abourbeh G, Dissoki S, Jacobson O, et al.Evaluation of radiolabeled ML04, a putative irreversible inhibitor of epidermal growth factor receptor, as a bioprobe for PET imaging of EGFR-overexpressing tumors[J].Nucl Med Biol, 2007, 34(1):55-70.DOI:10.1016/j.nucmedbio.2006.10.012.
[57] Shaul M, Abourbeh G, Jacobson O, et al.Novel iodine-124 labeled EGFR inhibitors as potential PET agents for molecular imaging in cancer[J].Bioorg Med Chem, 2004, 12(13):3421-3429.DOI:10.1016/j.bmc.2004.04.044.
[58] Dissoki S, Aviv Y, Laky D, et al.The effect of the[18F]-PEG group on tracer qualification of[4-(phenylamino)-quinazoline-6-YL]-amide moiety-an EGFR putative irreversible inhibitor[J].Appl Radiat Isot, 2007, 65(10):1140-1151.DOI:10.1016/j.apradiso.2007.04.014.
[59] Dissoki S, Eshet R, Billauer H, et al.Modified PEG-anilinoquinazoline derivatives as potential EGFR PET agents[J].J Labelled Compd Radiopharm, 2009, 52(2):41-52.DOI:10.1002/jlcr.1569.
[60] Pantaleo MA, Mishani E, Nanni C, et al.Evaluation of modified PEG-anilinoquinazoline derivatives as potential agents for EGFR imaging in cancer by small animal PET[J].Mol Imaging Biol, 2010, 12(6):616-625.DOI:10.1007/s11307-010-0315-z.
[61] Vasdev N, Dorff PN, Gibbs AR, et al.Synthesis of 6-acrylamido-4-(2-[18F]fluoroanilino) quinazoline:a prospective irreversible EGFR binding probe[J].J Labelled Compd Radiopharm, 2005, 48(2):109-115.DOI:10.1002/jlcr.903.
[62] Vasdev N, Dorff PN, O'neil JP, et al.Metabolic stability of 6, 7-dialkoxy-4-(2-, 3-and 4-[18F]fluoroanilino) quinazolines, potential EGFR imaging probes[J].Bioorg Med Chem, 2011, 19(9):2959-2965.DOI:10.1016/j.bmc.2011.03.032.
[63] Kobus D, Giesen Y, Ullrich R, et al.A fully automated two-step synthesis of an 18F-labelled tyrosine kinase inhibitor for EGFR kinase activity imaging in tumors[J].Appl Radiat Isot, 2009, 67(11):1977-1984.DOI:10.1016/j.apradiso.2009.07.018.
[64] Wang M, Gao M, Zheng QH.The first radiosynthesis of[11C]AZD8931 as a new potential PET agent for imaging of EGFR, HER2 and HER3 signaling[J].Bioorg Med Chem Lett, 2014, 24(18):4455-4459.DOI:10.1016/j.bmcl.2014.07.092.
[65] Neto C, Fernandes C, Oliveira MC, et al.Radiohalogenated 4-anilinoquinazoline-based EGFR-TK inhibitors as potential cancer imaging agents[J].Nucl Med Biol, 2012, 39(2):247-260.DOI:10.1016/j.nucmedbio.2011.09.001.
[66]

齐传民, 李石磊, 王潇, 等.新型18F标记取代喹唑啉类化合物及其制备方法和肿瘤PET显像应用:中国, 201210036262.4[P].2013-08-21.

Qi CM, Li SL, Wang X, et al.The preparation of 18F labeled quinazoline compound and its PET imaging application:CN, 201210036262.4[P].2013-08-21.

[67]

齐传民, 陈玉蓉, 冯曼, 等.新型18F标记4-氨基喹唑啉类衍生物及其制备方法和肿瘤PET显像应用:中国, 201210036250.1[P].2013-08-21.

Qi CM, Chen YR, Feng M, et al.The preparation of 18F labeled 4-amino quinazoline derivatives and application of tumour PET imaging:CN, 201210036250.1[P].2013-08-21.

[68]

申宝忠.一种18F标记的喹唑啉类不可逆性EGFR正电子示踪剂及其制备方法和应用:中国, 201310711310.

X[P].2014-03-26.Shen BZ.The preparation and application of 18F labeled quinazoline class irreversibility EGFR PET tracer:CN, 201310711310.X[P].2014-03-26.

[69]

申宝忠.18F标记的喹唑啉类EGFR正电子示踪剂及其制备方法和应用:中国, 201310711309.7[P].2014-03-26.

Shen BZ.The preparation and application of 18F labeled quinazoline class EGFR PET tracer:CN, 201310711309.7[P].2014-03-26.

[70]

刘振峰, 董孟杰, 王国林, 等.2-氟代苯胺喹唑啉类肿瘤正电子显像剂及制备和应用:中国, 201310256474.8[P].2013-09-18.

Liu ZF, Dong MJ, Wang GL, et al.The preparation and application of 2-fluoroaniline quinazoline class tumor positron imaging agent:CN, 201310256474.8[P].2013-09-18.

[71] Pisaneschi F, Nguyen QD, Shamsaei E, et al.Development of a new epidermal growth factor receptor positron emission tomography imaging agent based on the 3-cyanoquinoline core:synthesis and biological evaluation[J].Bioorg Med Chem, 2010, 18(18):6634-6645.DOI:10.1016/j.bmc.2010.08.004.