Reagent for tumor imaging and therapy
AssigneeAntisoma Limited
InventorAlan W. J. Stuttle
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Abstract
Novel oligopeptides are disclosed for in vivo tumor imaging and therapy. The novel oligopeptides are oligopeptides containing from 4 to 50 peptide units containing as a characteristic triplet therein the amino acid sequence leu-asp-val (LDV), which triplet provides the oligopeptide with a strong in vivo binding affinity for LDV binding sites on tumors and other tissues. For diagnostic purposes the oligopeptides are labelled with a radioactive label, e.g. .sup.125 I, whilst for therapeutic purposes the oligopeptides are chemically linked to or conjugated with a cytotoxin, such as the ricin A-chain.
Claims31
An oligopeptide consisting of from 4 to 50 peptide units containing as a triplet therein the amino acid sequence leu-asp-val (LDV) and as a result of which the oligopeptide is capable of binding in vivo with pathological tissues containing an LDV binding site, that oligopeptide having attached thereto or conjugated therewith a radioactive label or cytotoxin.
An oligopeptide comprising from 4 to 50 peptide units and containing the pentapeptide tyr-leu-asp-val-tyr, wherein the peptide is attached to a radioactive label or cytotoxin, and wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing an leu-asp-val (LDV) binding site.
An oligopeptide comprising from 4 to 50 peptide units and containing the nonapeptide leu-asp-val-gly-gly-gly-gly-ser-tyr, wherein the peptide is attached to a radioactive label or cytotoxin, and wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing an leu-asp-val (LDV) binding site.
An oligopeptide comprising the tridecapeptide having the sequence Tyr-Gly-Gly-Leu-Asp-Val-Gly-Leu-Asp-Val-Gly-Gly-Tyr (YGGLDVGLDVGGY) SEQ ID No. 2, wherein the oligopeptide is attached to a radioactive label or cytotoxin and wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing an leu-asp-val (LDV) binding site.
An oligopeptide comprising from 4 to 50 peptide units and containing the pentapeptide tyr-leu-asp-val-tyr, wherein the oligopeptide is labelled with a radioactive label, wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing an leu-asp-val (LDV) binding site.
An oligopeptide comprising from 4 to 50 peptide units and containing the nonapeptide leu-asp-val-gly-gly-gly-gly-ser-tyr, wherein the oligopeptide is labelled with a radioactive label, and wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing an leu-asp-val (LDV) binding site.
An oligopeptide comprising from 4 to 50 peptide units and containing the tridecapeptide SEQ ID No. 2, wherein the oligopeptide is labelled with a radioactive label, and wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing an leu-asp-val (LDV) binding site.
The radioactively labelled peptides:
- .sup.125 I-{tyr-leu-asp-val-tyr}
- .sup.125 I-{leu-asp-val-gly-gly-gly-gly-ser-tyr}
- and
- .sup.125 I-{SEQ ID No. 2}.
An anti-tumor therapeutic compound comprising an oligopeptide having from 4 to 50 peptide units and having as a triplet therein the amino acid sequence leu-asp-val (LDV), wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing a leu-asp-val (LDV) binding site and wherein the oligopeptide is chemically linked to or conjugated with a cytotoxin.
A diagnostic reagent for in vivo tumor imaging comprising an intravenously administrable liquid carrier containing an effective amount of a radioactively labelled oligopeptide having from 4 to 50 peptide units and having as a triplet the therein the amino acid sequence leu-asp-val (LDV), wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing a leu-asp-val (LDV) binding site.
An anti-tumor therapeutic reagent comprising an intravenously administrable liquid carrier comprising an effective amount of a cytotoxic oligopeptide having from 4 to 50 peptide units and having as a triplet therein the amino acid sequence leu-asp-val (LDV), wherein the oligopeptide is capable of binding in-vivo with pathological tissue containing leu-asp-val (LDV) binding sites, and wherein the oligopeptide is chemically linked to or conjugated with a cytotoxin.
A method of in vivo tumor imaging which comprises intravenously administering to the patient an effective amount of a radioactively labelled oligopeptide having from 4 to 50 peptide units and having as a triplet therein the amino acid sequence leu-asp-val (LDV), wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing a leu-asp-val (LDV) binding site and radiographically detecting the bound label.
A method of treating tumors in vivo which comprises intravenously administering to the patient an effective amount of a cytotoxic oligopeptide having from 4 to 50 peptide units and having as a triplet therein the amino acid sequence leu-asp-val (LDV), wherein the oligopeptide is capable of binding in-vivo with pathological tissues containing a leu-asp-val (LDV) binding site and wherein the oligopeptide is attached or conjugated with a cytotoxin.
Dependencies are inferred from the claim text.