发明名称 |
MINI-GASTRIN ANALOGUE, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT |
摘要 |
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. |
申请公布号 |
US2016256580(A1) |
申请公布日期 |
2016.09.08 |
申请号 |
US201415034943 |
申请日期 |
2014.10.23 |
申请人 |
PAUL SCHERRER INSTITUT |
发明人 |
BEHE MARTIN;SCHIBLI ROGER |
分类号 |
A61K51/08;C07B59/00;C07K14/595;C07K1/13;A61K38/22;C07K7/08 |
主分类号 |
A61K51/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
Villigen PSI CH |