News Column

Patent Issued for Antibodies Specifically Binding to the Epidermal Growth Factor Receptor

June 23, 2014



By a News Reporter-Staff News Editor at Clinical Trials Week -- According to news reporting originating from Alexandria, Virginia, by NewsRx journalists, a patent by the inventors Kim, Se-Ho (Yongin-si, KR); Chang, Ki Hwan (Yongin-si, KR); Hong, Kwang-Won (Yongin-si, KR); Shin, Yong-Won (Yongin-si, KR); Kim, Min-soo (Yongin-si, KR); Lee, Hae-Won (Yongin-si, KR); Shin, Yong Nam (Yongin-si, KR); Ryoo, Kyung Hwan (Yongin-si, KR); Seo, Dong Hyuck (Yongin-si, KR); Won, Jong-Hwa (Yongin-si, KR); Hur, Min-Kyu (Yongin-si, KR), filed on November 2, 2009, was published online on June 10, 2014 (see also Green Cross Corporation).

The assignee for this patent, patent number 8748175, is Green Cross Corporation (Yongin-Si, KR).

Reporters obtained the following quote from the background information supplied by the inventors: "The epidermal growth factor receptor (EGFR) is a 170 kDa type I transmembrane protein and is known to be overexpressed in many human tumors, e.g., carcinoma of the lung, breast, colon, stomach, brain, bladder, head, neck, ovaries and prostate. Its overexpression is frequently accompanied by the production of EGFR-ligands, TGF-.alpha. (transforming growth factor-.alpha.) and EGF (epidermal growth factor), and the binding of the ligands to EGFR was confirmed to induce cell proliferation and tumor growth. Blocking the interaction between such ligands and EGFR using an antibody against EGFR therefore can inhibit tumor growth, which has been proven effective by experiments that employed monoclonal antibodies against EGFR.

"Antibody C225 (trade name: Erbitux; ImClone, U.S), which is currently used in clinical trials for the treatment of metastatic colorectal cancers, is a chimeric antibody, comprising the mouse antibody variable regions linked to human antibody IgG1 constant regions (about 30% of mouse amino acid sequence is included therein). C225 has been shown to inhibit tumor cell growth, EGFR phosphorylation in vitro and tumor formation in a nude mouse, and also to completely eradicate human tumor xenografts in mice when used together with a specific chemotherapeutic agent. However, the antibody has the problem of inducing immune reactions in some (.about.10%) of the patients treated therewith. Accordingly, there exists a need for improved therapeutic antibodies against EGFR.

"Therapeutic agents for target therapy constitute about 50% of anticancer drugs recently approved by U.S. Food and Drug Administration (FDA). Such antibodies provide target specificity and a capability to effectively engage the immune system, which in combination with long biological half-lives thereof have alerted researchers to the therapeutic potentials thereof. As a result, the U.S. FDA has recently approved the use of several antibodies for cancer treatment. Antibodies play prominent roles in many therapeutic approaches to diseases, which has become even more attractive with the recent advent of technologies that allow the development of fully human antibodies.

"The present inventors have endeavored to develop novel, improved antibodies having new complementarity determining regions (CDRs) and have found that such antibodies can be used in cancer treatment by blocking the EGFR-mediated signal transduction."

In addition to obtaining background information on this patent, NewsRx editors also obtained the inventors' summary information for this patent: "Therefore, it is an object of the present invention to provide a novel antibody which specifically binds to the epidermal growth factor receptor.

"It is another object of the present invention to provide DNAs which respectively encode the heavy chain variable region and the light chain variable region of said antibody, and an expression vector comprising the same.

"It is still another object of the present invention to provide a cell line transformed with the expression vector.

"It is a further object of the present invention to provide a pharmaceutical composition for treating a cancer, comprising said antibody.

"In accordance with one aspect of the present invention, there is provided an antibody specifically binding to the epidermal growth factor receptor (EGFR), comprising: a) a heavy chain variable region comprising complementarity determining regions (CDRs) 1, 2, and 3 having the amino acid sequences of SEQ ID NOs: 1, 2, and 3, respectively; b) a light chain variable region comprising CDR 1, CDR 2, and CDR 3 having the amino acid sequences of SEQ ID NOs: 4, 5, and 6, respectively; c) a heavy chain constant region; and d) a light chain constant region.

"Further, there is provided an antibody specifically binding to the epidermal growth factor receptor (EGFR), comprising: a) a heavy chain variable region comprising CDR 1, CDR 2, and CDR 3 having the amino acid sequences of SEQ ID NOs: 1, 2, and 3, respectively; b) a light chain variable region comprising CDR 1, CDR 2, and CDR 3 having the amino acid sequences of SEQ ID NOs: 9, 5, and 6, respectively; c) a heavy chain constant region; and d) a light chain constant region.

"In accordance with another aspect of the present invention, there is provided a DNA encoding the heavy chain variable region or the light chain variable region of the antibody, and an expression vector comprising the same.

"In accordance with a still another aspect of the present invention, there is provided a cell line transformed with said expression vector.

"In accordance with a further aspect of the present invention, there is provided a composition for treating a cancer, comprising said antibody."

For more information, see this patent: Kim, Se-Ho; Chang, Ki Hwan; Hong, Kwang-Won; Shin, Yong-Won; Kim, Min-soo; Lee, Hae-Won; Shin, Yong Nam; Ryoo, Kyung Hwan; Seo, Dong Hyuck; Won, Jong-Hwa; Hur, Min-Kyu. Antibodies Specifically Binding to the Epidermal Growth Factor Receptor. U.S. Patent Number 8748175, filed November 2, 2009, and published online on June 10, 2014. Patent URL: http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=8748175.PN.&OS=PN/8748175RS=PN/8748175

Keywords for this news article include: Antibodies, Cancer, Oncology, Immunology, Amino Acids, Legal Issues, Therapeutics, Blood Proteins, Immunoglobulins, Membrane Proteins, Peptide Receptors, Green Cross Corporation, Growth Factor Receptors.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC


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Source: Clinical Trials Week


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