The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Apr. 11, 2023

Filed:

Dec. 18, 2020
Applicant:

Paul Scherrer Institut, Villigen, CH;

Inventors:

Martin Behe, Gelterkinden, CH;

Roger Schibli, Baden, CH;

Assignee:

Paul Scherrer Institut, Villigen, CH;

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 51/08 (2006.01); A61K 38/22 (2006.01); C07K 14/575 (2006.01); C07K 14/595 (2006.01); C07B 59/00 (2006.01); C07K 1/13 (2006.01); C07K 7/08 (2006.01); G01N 33/574 (2006.01);
U.S. Cl.
CPC ...
A61K 51/088 (2013.01); A61K 38/2207 (2013.01); C07B 59/008 (2013.01); C07K 1/13 (2013.01); C07K 7/08 (2013.01); C07K 14/57572 (2013.01); C07K 14/595 (2013.01); G01N 33/57484 (2013.01); G01N 2333/726 (2013.01);
Abstract

A gastrin analogue shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine. This PP-F11N mini gastrin exhibits currently the best tumor-kidney-ratio and is the most promising candidate.


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