Daiichi Sankyo Company, Limited

Yusuke Ogitani

Takeshi Masuda

Hiroyuki Naito

Masao Yoshida

Yuji Kasuya

Takashi Nakada

Shinji Ashida

Yuki Abe

Koji Morita

Ichiro Hayakawa

As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L-L-L-NH—(CH)n-L-L-L- wherein the antibody is connected to the terminal of L, and the antitumor compound is connected to the terminal of Lwith the nitrogen atom of the amino group at position 1 as a connecting position.

Antibody-drug conjugate

As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L-L-L-NH&#x2014;(CH)n-L-(CH)n-C(&#x2550;O)&#x2014; wherein the anti-HER2 antibody is connected to the terminal L, and the antitumor compound is connected to the carbonyl group of the &#x2014;(CH)n-C(&#x2550;O)&#x2014; moiety with the nitrogen atom of the amino group at position 1 as the connecting position

Method for treating cancer comprising administration of anti-HER2 antibody-drug conjugate

As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L-L-L-NH&#x2014;(CH)n-L-L-L- wherein the antibody is connected to the terminal of L, and the antitumor compound is connected to the terminal of Lwith the nitrogen atom of the amino group at position 1 as a connecting position.

As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L-L-L-NH&#x2014;(CH)n-L-(CH)n-C(&#x2550;O)&#x2014; wherein the anti-HER2 antibody is connected to the terminal L, and the antitumor compound is connected to the carbonyl group of the &#x2014;(CH)n-C(&#x2550;O)&#x2014; moiety with the nitrogen atom of the amino group at position 1 as the connecting position. 

Method of treating cancer comprising administration of anti-HER2 antibody-drug conjugate

As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the formula: L-L-L-NH&#x2014;(CH)n-L-L-Lor -L-L-L- wherein the anti-HER2 antibody is connected to the terminal L, and the antitumor compound is connected to the terminal Lor Lwith the nitrogen atom of the amino group at position 1 as the connecting position. 

(Anti-HER2 antibody)-drug conjugate

As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula (I) is conjugated to an antibody via a linker having a structure represented by the following formula: -L-L-L-NH&#x2014;(CH)n-L-L-L- or -L-L-L- wherein the antibody is connected to the terminal of L, the antitumor compound is connected to the terminal of Lor L, and any one or two or more of linkers of L, L, and Lhas a hydrophilic structure.

Antibody-drug conjugate produced by binding through linker having hydrophilic structure

As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula:-L-L-L-NH&#x2014;(CH)-L-L-L-wherein the antibody is connected to the terminal of L, and the antitumor compound is connected to the terminal of Lwith the nitrogen atom of the amino group at position 1 as a connecting position.

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Tokyo, Japan

Yusuke Ogitani