1 1 2 1 1 1 1 100730 2 100700 EGFR-TKI 2005 2007 EGFR-TKI EGFR-TKI Ⅲ ~ Ⅳ 7 1 SD NSCLC R979. 1 A 1003-3734 2013 14-1676 - 05 Successful treatment of one patient with advanced non-small cell lung cancer with icotinib hydrochloride in replacement of gefitinib ZHANG Li 1 GUAN Qiu-hong 2 ZHAO Yan-wei 1 XIA Ying 1 XIAO Yi 1 1 Dongzhimen Hospital Affiliated to Beijing University of Chinese Medicine Beijing 100730 China 2 Chinese Academy of Medical Science Peking Union Medical College Hospital Beijing 100005 China Abstract Common adverse reactions of epidermal growth factor receptor tyrosine kinase inhibitor EGFR- TKI due to drug toxicity are rash and diarrhea. Positive curative effect has been observed after gefitinib Iressa ZD1839 and erlotinib Tarceva Ro50-8231 were introduced into China in 2005 and 2007 respectively. However some patients who were likely to benefit from the therapy might not accept EGFR-TKIs because of severe adverse event AE during the treatment. Conmana icotinib hydrochloride BPI-2009H is a newly developed and highly specific EGFR-TKI that is designed in China with independent intellectual property right. In this case the patient experienced III ~ IV-level diarrhea after taking gefitinib and antidiarrheal drugs were ineffective. The intolerable AE led to drug withdrawal. Treatment was then transformed into icotinib therapy and had been on for 7 months without apparent AE observed. After the first cycle of icotinib 30 days objective responses were evaluated to be SD physical conditions and the quality of life were improved. This suggests that icotinib is effective and well-tolerated in advanced NSCLC patients and superior to gefitinib and erlotinib in terms of curative effectiveness and safety among Chinese patients. Key words epidermal growth factor receptor tyrosine kinase inhibitor non-small cell lung cancer icotinib hydrochloride severe diarrhea 张力, 女, 硕士生导师, 主任医师, 教授, 主要从事呼吸系统肿瘤的研究联系电话 : ( 010) 69158206,E-mail: zhanglipumch@ yahoo. com. cn 关秋红, 女, 博士, 副主任医师, 主要从事中西医结合防治肺癌联系电话 : ( 010) 84013136,E-mail: guanqh1969@ yahoo. com. cn 张力 和关秋红为并列第一作者 1676
non-small-cell lung cancer NSCLC 2011 4 15 CT 85% 1 2011 4 16 CT MRI + 2 - NSCLC 3 1. 5 cm 2 cm EGFR TKI T2 EGFR-TKI EGFR 2011 4 28 3 2011 6 9 Ⅲ ~ Ⅳ 38 121 mmol L - 1 2011 6 13 CT 1 2 cm 3. 1 cm 1a ~ d 2011 6 14 MRI 1. 9 cm 0. 9 cm 72 2011 3 1. 4 cm 2 a ~ c 2011 6 14 CT Exon21 L858R 2573T > G 2011 6 16 117 mmol L - 1 24 h 198 mmol L - 1 scorpions amplification refractory mutation system SARMS EGFR 234. 08 μg 250 mmol L - 1 24 h UFC ACTH 1677
17. 8 pg ml - 1 0. 27 ng ml - 1 < 1 000 ml d - 1 3% 500 ml 20 mg 2011 6 22 SIADH 2011 6 27 124 mmol L - 1 250 mg qd 600 mg 2011 8 16 po qd 2011 7 2 600 mg 2 10 2011 9 2 1 g tid 2011 7 4 2011 125 mg 7 18 10 2008L11932 125 mg po qd 2011 9 4 4 mg 6 h 1 2 mg 72 h 2011 7 21 2011 7 27 75 g L - 1 201 10 9 L - 1 420 mg tid 2011 9 11 20 27 0. 5 g tid 2 mg tid 3 g tid 2011 7 28 24 h U-K 65. 1 mol L -1 U-Na 388 mol L -1 U-Cl 234 mol L -1 599 mosm kg -1 H 2 O 2011 8 11 MRI T2 2011 9 8 125 mg po bid 2011 9 9 WBC 2. 41 10 9 L -1 0. 71 10 9 L -1 400 mg iv 2011 9 28 125 mg po tid 2011 10 CT 28 CT 3a ~ d MRI PD 2011 8 10 4a ~ c SD 2012 1 11 CT SD 2012 4 9 CT 1678
PD 2012 4 10 NCCN 77. 42% EGFR-TKI NSCLC 80. 95% EGFR-TKI 85 EGFR 3 IC 50 5 2. 5 27 81 4 EGFR-TKI nmol L - 1 IC 50 50 20 80 ~ 90 nmol L - 1 60 mg kg - 1 52% 56% 38% 5-6 7 Ⅲ ~ Ⅳ ADH SIADH EGFR Exon21 L858R 2573 T > G SIADH 1 120 mmol L - 1 1 2 < 3 125 mg qd 1 4 125 mg bid 1 SIADH 125 mg tid 7 1 CT SD 2012 1 11 CT Ⅳ NSCLC 8 ~ 10 PFS 7 8 PFS 6 9 7 1 IV PFS 47 125 mg qd 1 7 125 mg bid 1 125 mg tid PFS 3 ~ 4 SAE 10 EGFR-TKI 7 11 I ~ III 2 12 2011 7 28 CT 3 NSCLC III 60. 5% 1679
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