Compositions and methods of therapy for cancers...

C - Chemistry – Metallurgy – 12 – N

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C12N 9/88 (2006.01) A61K 38/00 (2006.01) A61K 39/395 (2006.01) A61K 45/00 (2006.01) C07K 16/00 (2006.01) C07K 16/40 (2006.01) C12Q 1/527 (2006.01) G01N 33/573 (2006.01)

Patent

CA 2496572

Compositions and methods useful in inhibiting proliferation of CA IX + preneoplastic or neoplastic cells in a mammal are provided. The compositions are antagonist anti-CA IX antibodies and other inhibitory agents that target carbonic anhydrase activity of CA IX on these cells. The antagonist anti-CA IX antibodies or antigen-binding fragments thereof are specifically reactive with an inhibitory epitope of CA IX or biologically active variant thereof. Formation of an antibody-antigen complex between the antagonist anti-CA IX antibodies or antigen-binding fragments thereof and the respective inhibitory epitopes results in inhibition of carbonic anhydrase activity of CA IX or biologically active variant thereof. Other small molecule agents that inhibit carbonic anhydrase activity of CA IX or biologically active variant thereof and screening assays for identifying such agents are also provided. The antagonist anti-CA IX antibodies, antigen-binding fragments thereof, and other CA IX inhibitory agents identified herein are useful in the treatment of cancers characterized by the expression of the CA IX tumor-associated antigen.

L'invention concerne des compositions et des procédés utiles pour inhiber la prolifération de cellules prénéoplastique ou néoplastiques CA IX + chez un mammifère. Ces compositions sont des anticorps anti-CA IX et d'autres agents inhibiteurs qui ciblent l'activité d'anhydrase carbonique sur ces cellules. Ces anticorps anti-CA IX antagonistes ou fragments de liaison d'antigène de ces derniers réagissent de manière spécifique avec un épitope inhibiteur de CA IX ou un variant biologiquement actif de celui-ci. La formation d'un complexe anticorps-antigène entre les anticorps anti-CA IX antagonistes ou les fragments de liaison d'antigène de ce dernier et les épitopes inhibiteurs respectifs, entraîne l'inhibition de l'activité d'anhydrase carbonique de CA IX ou d'un variant biologiquement actif de ce dernier. L'invention porte sur d'autres agents à petites molécules qui inhibent l'activité d'anhydrase carbonique de CA IX ou d'un variant biologiquement actif de ce dernier et sur des dosages de criblage permettant d'identifier ces agents. Les anticorps anti-CA IX antagonistes, les fragments de liaison d'antigène de ce dernier, et d'autres agents inhibiteurs de CA IX susmentionnés sont utiles dans le traitement de cancers caractérisés par l'expression de l'antigène CA IX associé aux tumeurs.

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