Invention Grant
- Patent Title: Mini-gastrin analogue, in particular for use in CCK2 receptor positive tumour diagnosis and/or treatment
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Application No.: US17127265Application Date: 2020-12-18
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Publication No.: US11623014B2Publication Date: 2023-04-11
- Inventor: Martin Behe , Roger Schibli
- Applicant: Paul Scherrer Institut
- Applicant Address: CH Villigen
- Assignee: Paul Scherrer Institut
- Current Assignee: Paul Scherrer Institut
- Current Assignee Address: CH Villigen
- Agent Laurence A. Greenberg; Werner H. Stemer; Ralph E. Locher
- Priority: EP13191807 20131106
- Main IPC: A61K51/08
- IPC: A61K51/08 ; A61K38/22 ; C07K14/575 ; C07K14/595 ; C07B59/00 ; C07K1/13 ; C07K7/08 ; G01N33/574

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-NH2, 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.
Public/Granted literature
- US20210145990A1 MINI-GASTRIN ANALOGUE, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT Public/Granted day:2021-05-20
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