Ester Imaging Agents

摘要

The present invention relates to contrast agents for optical imaging of oesophageal cancer and Barrett's oesophagus in patients. The contrast agents are esters of 5-aminolevulinic acid (5-ALA). They are useful in the diagnosis of oesophageal cancer and Barrett's oesophagus, for follow up of progress in disease development, and for follow up of treatment of oesophageal cancer and Barrett's oesophagus. The contrast agents are delivered by particular routes of administration.

主权项

1. A method of data acquisition useful in the diagnosis of a disease state of the oesophagus of the mammalian body in vivo, said method comprising:
(i) administration of a pharmaceutical composition comprising an ALA-ester of Formula (I) or a pharmaceutically acceptable salt thereof to a mammalian subject:R1 is C1-10 alkyl, C1-10 alkoxyalkyl, C1-10 hydroxyalkyl, C1-10 fluoroalkyl or —C3-6 aryl(C1-8 alkyl);
(ii) waiting for a period of time post-administration to allow:
(a) the ALA-ester from step (i) to accumulate at one or more areas of interest within the oesophagus; and/or(b) the ALA-ester from step (i) to be converted to protoporphyrin IX; (iii) illuminating said area of interest with an excitation light; (iv) detecting the light generated by fluorescence of the protoporphyrin IX from step (ii)(b), using a fluorescence detector;wherein the administration of step (i) is carried out by one or more of the following routes:
(A) oral administration of a composition further comprising sodium alginate; (B) oral administration of a lozenge which comprises the composition; (C) spraying of the composition as an aerosol onto the walls of the oesophagus; (D) direct contact of the composition as an aqueous, non-hydrogel solution with the walls of the oesophagus.