Her-2 binding antagonists

Details Her-2 binding antagonists Her-2 binding antagonists

A - Human Necessities

61

K

A61K 39/00 (2006.01) A61K 39/395 (2006.01) C07H 21/02 (2006.01) C07H 21/04 (2006.01) C07K 14/71 (2006.01) C12N 5/00 (2006.01) C12N 5/02 (2006.01) C12N 15/00 (2006.01) C12N 15/09 (2006.01) C12N 15/63 (2006.01) C12N 15/70 (2006.01) C12N 15/74 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2361181

There is disclosed a pharmaceutical composition for treating solid tumors that overexpress HER-2, comprising an agent selected from the group consisting of (a) an isolated polypeptide having from about 50 to 79 amino acids taken from the sequence of SEQ ID NO. 1, wherein the polypeptide binds to the extracellular domain ECD of HER-2 at an affinity of at least 108, (b) an isolated and glycosylated polypeptide having from about 300 to 419 amino acids taken from the sequence of SEQ ID NO. 2, wherein the C terminal 79 amino acids are present, and wherein at least three N-linked glycosylation sites are present, (c) a monoclonal antibody that binds to the ECD of HER-2, and (d) combinations thereof, with the proviso that the agent cannot be the monoclonal antibody alone, and pharmaceutically acceptable carrier.

L'invention concerne une composition pharmaceutique servant à traiter des tumeurs solides surexprimant HER-2, et contenant un agent sélectionné dans le groupe constitué par (a) un polypeptide isolé possédant de 50 à 79 acides aminés pris dans le séquence de SEQ ID NO.1, dans laquelle le polypeptide se fixe au domaine extracellulaire ECD de HER-2 avec une affinité d'au moins 10?8¿, (b) un polypeptide isolé et glycosylé possédant de 300 à 419 acides aminés pris dans la séquence de SEQ ID NO.2, dans laquelle les acides aminés à terminaison C sont présents et dans laquelle au moins trois sites de glycosylation possédant une liaison N sont présents, (c) un anticorps monoclonal qui se fixe au ECD de HER-2 et (d) leurs combinaisons, cet agent ne pouvant pas être l'anticorps monoclonal seul, ainsi qu'un véhicule acceptable sur le plan pharmaceutique.

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