Title:
CRGD-ERLOTINIB CONJUGATE AND PREPARATION METHOD THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/152756
Kind Code:
A1
Abstract:
Provided are a cRGD-erlotinib/icotinib conjugate and a preparation method thereof, wherein the cRGD is a cyclic polypeptide. Erlotinib and icotinib are small molecule inhibitors of a epidermal growth factor receptor (EGFR) that interfere with the growth of cancer cells and are thus used to treat metastatic non-small cell lung cancer (NSCLC). The cRGD-erlotinib/icotinib conjugate synthesized by the present invention selectively delivers the erlotinib/icotinib to non-small cell lung cancer cells and improves the site delivery efficiency, while also reducing the side effects for cancer patients.
Inventors:
LI SHUPENG (CN)
ZHANG HAILONG (CN)
ZHANG HAILONG (CN)
Application Number:
PCT/CN2017/074384
Publication Date:
September 14, 2017
Filing Date:
February 22, 2017
Export Citation:
Assignee:
XUZHOU RUIKANG BIOTECH COMPANY (CN)
International Classes:
C07K7/64; A61K38/12; A61P35/00; C07K1/04; C07K1/13
Foreign References:
| CN105906692A | 2016-08-31 | |||
| US20140358116A1 | 2014-12-04 | |||
| US20030125243A1 | 2003-07-03 | |||
| US20140058061A1 | 2014-02-27 |
Other References:
MATTEO, C. ET AL.: "Click Chemistry for the Synthesis of RGD-Containing Integrin Ligands", MOLECULES, vol. 15, no. 1, 6 January 2010 (2010-01-06), pages 178 - 197, XP055422177, ISSN: 1420-3049
CARMEN, W. ET AL.: "Multimerization of cRGD Peptides by Click Chemistry: Synthetic Strategies, Chemical Limitations, and Influence on Biological Properties", CHENIBIOCHEM, vol. 11, no. 15, 9 September 2010 (2010-09-09), pages 2168 - 2181, XP055422186, ISSN: 1439-7633
CARMEN, W. ET AL.: "Multimerization of cRGD Peptides by Click Chemistry: Synthetic Strategies, Chemical Limitations, and Influence on Biological Properties", CHENIBIOCHEM, vol. 11, no. 15, 9 September 2010 (2010-09-09), pages 2168 - 2181, XP055422186, ISSN: 1439-7633
Attorney, Agent or Firm:
NANJING SUKE PATENT AGENT CO.,LTD. (CN)
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