C07K14/595

Mini-gastrin analogue, in particular for use in CCK2 receptor positive tumour diagnosis and/or treatment
10953114 · 2021-03-23 · ·

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.sub.2, 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.

PROGASTRIN AS A BIOMARKER FOR IMMUNOTHERAPY
20200400675 · 2020-12-24 · ·

Methods for selecting patients responsive to immune checkpoint inhibitors are herein disclosed. Methods of treating cancer patients with an immune checkpoint inhibitor are also provided.

PROGASTRIN AS A BIOMARKER FOR IMMUNOTHERAPY
20200400675 · 2020-12-24 · ·

Methods for selecting patients responsive to immune checkpoint inhibitors are herein disclosed. Methods of treating cancer patients with an immune checkpoint inhibitor are also provided.

RADIOLABELED PROGASTRIN IN CANCER DIAGNOSIS
20200390913 · 2020-12-17 · ·

The present invention provides a radiotracer comprising a progastrin moiety, a chelating moiety and a radioisotope. Uses of said biomarker for imaging and detecting cancers in a subject are also provided. In one embodiment, the radiotracer is .sup.68Ga-NODAGA-Progastrin.

RADIOLABELED PROGASTRIN IN CANCER DIAGNOSIS
20200390913 · 2020-12-17 · ·

The present invention provides a radiotracer comprising a progastrin moiety, a chelating moiety and a radioisotope. Uses of said biomarker for imaging and detecting cancers in a subject are also provided. In one embodiment, the radiotracer is .sup.68Ga-NODAGA-Progastrin.

Methods and compositions for liver cancer therapy

The present disclosure provides methods of treating liver cancer and preventing liver cancer recurrence with anti-progastrin antibodies, methods of monitoring treatment efficacy of anti-progastrin therapy for liver cancer, and compositions useful therefore.

RADIOLABELED COMPOUNDS FOR IN VIVO IMAGING OF GASTRIN-RELEASING PEPTIDE RECEPTOR (GRPR) AND TREATMENT OF GRPR-RELATED DISORDERS

There is provided peptidic compounds of Formula I, A or B(R.sup.rad.sub.n6-[linker]-R.sup.L-Xaa.sup.1-Xaa.sup.2-Xaa.sup.3-Xaa.sup.4-Xaa.sup.5-Xaa.sup.6-Xaa.sup.7-Xaa.sup.8-?-Xaa.sup.9-NH.sup.2). Xaa.sup.1 is D-Phe, Cpa, D-Cpa, Nal, D-Nal, 2-Nal, or D-2-Nal; Xaa.sup.2 is Asn, Gln, Hse, Cit or His. Xaa.sup.3 is Trp, Bta, Trp(Me), Trp(7-Me), Trp(6-Me), Trp(5-Me), Trp(4-Me), Trp(2-Me), Trp(7-F), Trp(6-F), Trp(5-F), Trp(4-F), Trp(5-OH), or ?Me-Trp. Xaa.sup.4 is Ala or Ser. Xaa.sup.5 is Val, Cpg, or Tle. Xaa.sup.6 is Gly, NMe-Gly, or D-Ala. Xaa.sup.7 is His or NMe-His. Xaa.sup.8 is Leu or Phe. Xaa.sup.9-NH.sub.2 is a C-terminally amidated amino acid residue selected from Pro, 4-oxa-L-Pro, Me.sub.2 Thz, or Thz. ? represents a peptide bond or reduced peptide bond joining Xaa.sup.8 to Xaa.sup.9. R.sup.rad.sub.n6 is 1-5 radiolabeling groups. There is also provided the use of such compounds as imaging agents or therapeutic agents.

Peptide conjugates of GLP-1 receptor agonists and gastrin and their use

The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes related diseases or disorders.

Peptide conjugates of GLP-1 receptor agonists and gastrin and their use

The present invention relates, inter alia, to certain peptide conjugates, and to the use of the conjugates in the treatment of a variety of diseases or disorders, including diabetes (type 1 and/or type 2) and diabetes related diseases or disorders.

MINI-GASTRIN ANALOGUE, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT
20190240360 · 2019-08-08 · ·

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.sub.2, 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.