Labelled adrenomedullin derivatives and their use for imaging and therapy.

摘要

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.

主权项

1. A method of determining a disease state in an organ in a mammal, the organ comprising adrenomedullin-receptor-bearing cells, the method comprising:
a) administering to the mammal a labelled adrenomedullin derivative in an effective amount to achieve binding between the labelled adrenomedullin derivative and the adrenomedullin-receptor-bearing cells; b) generating an image of the distribution of the labelled adrenomedullin derivative in the organ of the mammal; c) using the image of step b) to determine a labelling pattern of the adrenomedullin derivative in the organ; d) comparing the labelling pattern of step c) to a labelling pattern of a non diseased organ; and e) determining the disease state of the organ at least in part on the comparison of step d).