FIELD: radiopharmaceuticals.
SUBSTANCE: invention relates to gastrin-releasing peptide (GRPR) receptor-targeted pharmaceutical composition containing a radioactively labeled GRPR antagonist and a surfactant containing polyethylene glycol-15-hydroxystearate. The antagonist has the following formula: MС-S-P, where M is a radioactive metal and C is a chelator that binds M; S is an optional spacer covalently linked between the C and N-terminus of P; P is a peptide GRP receptor antagonist with the general formula: Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Z, where Xaa1 is the D-isomer of Phe; Xaa2 is Gln; Xaa3 is Trp; Xaa4 is Ala; Xaa5 is Val; Xaa6 is Gly; Xaa7 is His; Z is -NH-alkyl or Z is, where X is NH, and R1 and R2 are the same or different and are selected from proton or optionally substituted alkyl. The invention also relates to the use of the said pharmaceutical composition, a method for treating or preventing cancer, and a method for imaging a tumor.
EFFECT: invention makes it possible to obtain a stable pharmaceutical composition by preventing peptide adhesion.
13 cl, 8 dwg, 3 tbl, 2 ex
Title | Year | Author | Number |
---|---|---|---|
GRPR ANTAGONISTS FOR DETECTING, DIAGNOSING AND TREATING GRPR-POSITIVE ONCOLOGICAL DISEASE | 2013 |
|
RU2693465C2 |
GRPR ANTAGONISTS FOR DETECTING, DIAGNOSING AND TREATING GRPR-POSITIVE ONCOLOGICAL DISEASE | 2013 |
|
RU2821944C2 |
BOMBESIN ANALOGUE PEPTIDE ANTAGONIST CONJUGATES | 2009 |
|
RU2523531C2 |
THERAPEUTIC AGENTS AND USE THEREOF | 2012 |
|
RU2606773C2 |
NEW PSA-BINDING AGENTS AND THEIR USE | 2018 |
|
RU2787105C2 |
METHODS OF TREATING CANCER | 2019 |
|
RU2825637C2 |
ANTIBODIES POLYPEPTIDES AND USE THEREOF | 2014 |
|
RU2687163C1 |
COMPLEX CONTAINING A PSMA-TARGETING COMPOUND BOUND TO A LEAD OR THORIUM RADIONUCLIDE | 2018 |
|
RU2795398C2 |
PARAMINOHYPURIC ACID (PAH) AS A KIDNEY PROTECTOR | 2020 |
|
RU2804349C2 |
METHOD FOR UPREGULATING ANTIGEN EXPRESSION | 2014 |
|
RU2681953C2 |
Authors
Dates
2023-06-30—Published
2019-10-11—Filed