IGF-1R ANTIBODY-DRUG-CONJUGATE AND ITS USE FOR THE TREATMENT OF CANCER

摘要

The present invention relates to an antibody-drug-conjugate capable of binding IGF-1R. From one aspect, the invention relates to an antibody-drug-conjugate comprising an antibody capable of binding to IGF-1R, said antibody being conjugated to at least one drug selected from derivatives of dolastatin 10 and auristatins. The invention also comprises method of treatment and the use of said antibody-drug-conjugate for the treatment of cancer.

主权项

1. An antibody-drug-conjugate of the following formula (I):
Ab-(L-D)n  (I) or a pharmaceutically acceptable salt thereof, wherein Ab is an antibody, or an antigen binding fragment thereof, capable of binding to the human IGF-1R selected from i) an antibody which comprises the three heavy chain CDRs of sequence SEQ ID No. 1, 2 and 3 and the three light chain CDRs of sequence SEQ ID No. 4, 5 and 6; or ii) an antibody which competes for binding to IGF-1R with the antibody of i); or iii) an antibody which binds to the same epitope of IGF-1R as the antibody of i); L is a linker; D is a drug moiety of the following formula (II): wherein: R2 is COOH, COOCH3 or thiazolyl; R3 is H or (C1-C6)alkyl; R9 is H or (C1-C6)alkyl; m is an integer comprised between 1 and 8; the wavy line indicates the point of attachment to L; and n is 1 to 12.