Mini-gastrin analogue, in particular for use in CCK2 receptor positive tumour diagnosis and/or treatment
US11623014B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 18, 2020 |
| Grant date | Apr 11, 2023 |
| Priority date | — |
| Expiry date | Oct 12, 2041 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2333/726
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.