Enhanced in vivo targeting of radiolabelled peptides with the means of enzyme inhibitors

• US 10,449,260 B2
• Filed: 07/06/2012
• Issued: 10/22/2019
• Est. Priority Date: 07/08/2011
• Status: Active Grant

• Current Assignee: Berthold Artur Nock, Marion De Jong Hendriks, Theodosia Maina-Nock
• Original Assignee: Berthold Artur Nock, Marion De Jong Hendriks, Theodosia Maina-Nock
• Inventors: Maina-Nock, Theodosia, Nock, Berthold Artur, de Jong Hendriks, Marion
• Primary Examiner(s): Jones, D. L.
• Application Number:
  US14/131,573
• Publication Number:
  US 20150104381A1
• Time in Patent Office: 2,664 Days
• Field of Search: 424 111, 424 165, 424 169, 424 91, 424 92, 530300, 514 1, 514 11, 514 192, 514 193
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/265 of carbonic, thiocarbonic, or thiocarboxylic acids, e.g. thioacetic acid, xanthogenic acid, trithiocarbonic acid
• CPC Class Codes: A61K 31/7028 Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
• CPC Class Codes: A61K 31/7056 containing five-membered rings with nitrogen as a ring hetero atom
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 51/08 Peptides, e.g. proteins , carriers being peptides, polyamino acids, proteins
• CPC Class Codes: A61K 51/083 the peptide being octreotide or a somatostatin-receptor-binding peptide
• CPC Class Codes: A61K 51/085 the peptide being neurotensin
• CPC Class Codes: A61K 51/086 the peptide being alphaMSH, alpha melanocyte stimulating hormone
• CPC Class Codes: A61K 51/088 conjugates with carriers being peptides, polyamino acids or proteins antibodies A61K51/10
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The present invention relates to a compound that inhibits the activity of a degrading enzyme for use in combination with a therapeutic or diagnostic compound, preferably a moiety conjugated peptide, in the diagnosis and/or treatment of a disease, in particular cancer, to enhance targeting of the therapeutic or diagnostic compound to the disease site.

Claims

1. A composition comprising a radiolabeled biodegradable peptide analog and a neutral endopeptidase (NEP) inhibitor, wherein the radiolabeled biodegradable peptide analog is (¹¹¹In-DOTA)-MG11.

2. The composition of claim 1, wherein the neutral endopeptidase (NEP) inhibitor comprises phosphoramidon or racecadotril.

3. The composition according to claim 1, wherein the composition further comprises an angiotensin-converting enzyme (ACE) inhibitor.

4. The composition according to claim 3, wherein the ACE inhibitor is lisinopril.

5. The composition according to claim 2, wherein the composition further comprises an angiotensin-converting enzyme (ACE) inhibitor.

6. The composition according to claim 5, wherein the ACE inhibitor is lisinopril.