Labelled adrenomedullin derivatives and their use for...

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/575 (2006.01) A61K 49/00 (2006.01) A61K 51/08 (2006.01) C07K 14/47 (2006.01)

Patent

CA 2686760

The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide, or a fragment thereof chelated or otherwise bound to 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 Resonance 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 agent is pulmonary embolus.

La présente invention porte sur un dérivé d'adrénomédulline comprenant un peptide adrénomédulline ou un fragment de celui-ci chélaté ou autrement lié à au moins un agent actif. Des exemples d'agents actifs comprennent un élément paramagnétique, un élément radioactif et un agent fibrinolytique, entre autres. Les agents paramagnétiques ont une distribution qui est montrée relativement facilement par une Imagerie par Résonance Magnétique (IRM). Les agents radioactifs ont des applications dans l'imagerie et la délivrance de rayons, en fonction de l'élément spécifique compris dans l'agent actif. L'administration d'agents fibrinolytiques principalement à un organe spécifique, tel que, par exemple, les poumons, permet d'améliorer de façon substantielle la spécificité et l'efficacité d'une thérapie thrombolytique en permettant une administration locale de l'agent fibrinolytique, réduisant ainsi les risques de saignement important lors de la thérapie de l'organe. Si l'organe est constitué par les poumons, un exemple non limitatif d'une pathologie qui peut être traitée par l'agent fibrinolytique, est l'embolie pulmonaire.

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