Labelled adrenomedullin derivatives and their use for...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/435 (2006.01) A61K 49/14 (2006.01) A61K 51/08 (2006.01)

Patent

CA 2567478

The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide chelated with at least one active agent. Examples of active agents include a paramagnetic element, a radioactive element and a fibrinolytic agent, among others. Paramagnetic agents have a distribution that is relatively easily shown through Magnetic Resonnance Imaging (MRI). Radioactive agents have applications in imaging and delivery of radiations, depending on the specific element included in the active agent. Delivery of fibrinolytic agents mainly to a specific organ, such as for example to the lungs, allows to substantially improve the specificity and efficacy of thrombolytic therapy by allowing local delivery of the fibrinolytic agent, thereby reducing the risks of major bleeding in the therapy of the organ. If the organ is the lungs, a non-limiting example of pathology treatable with the fibrinolytic is pulmonary embolus.

La présente invention concerne un dérivé d'adrénomédulline comprenant un peptide adrénomédulline chélaté avec au moins un agent actif. Des exemples d'agents actifs comprennent, notamment, un élément paramagnétique, un élément radioactif et un agent fibrinolytique. Les agents paramagnétiques ont une distribution qui est présentée de manière relativement facile par imagerie par résonance magnétique (IRM). Les agents radioactifs peuvent être utilisés en imagerie et pour l'application de rayons, selon l'élément spécifique inclus dans l'agent actif. L'administration d'agents fibrinolytiques principalement à un organe spécifique, tel que les poumons, par exemple, permet d'améliorer sensiblement la spécificité et l'efficacité de la thérapie thrombolytique, car elle permet d'administrer localement l'agent fibrinolytique et de réduire ainsi les risques d'hémorragies importantes lors de la thérapie. Les pathologies pulmonaires pouvant être traitées à l'aide de l'agent fibrinolytique comprennent, notamment, l'embolie pulmonaire.

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