Claims
- 1. A method for the therapeutic treatment of tumours, having on their surface a high density of neurotensin receptor sites, in the body of a warm-blooded living being, which comprises administering to said being a composition comprising a peptide represented by the general formula:R1(1Pro)n—2Xaa—3Xbb—4Xcc—5Xdd—6Xee—7Leu—OH (1) (Seq ID 2). wherein:R1 is a C1-C3 alkanoyl group, an arylcarbonyl group, an aryl-(C1-C3) alkanoyl group, or a chelating group attached by an amide bond or through a spacing group to the peptide molecule; Xaa and Xbb are each individually Arg or Lys; Xcc is an unsubstituted or substituted cyclic amino acid, preferably selected from Pro and Hyp; Xdd is Tyr, Trp or Phe; Xee is Leu, Ile or tert-butlalanine; and n is 0 or 1; and wherein said peptide is labelled with a metal isotope, chelated by a chelating group R1 derived from ethylene diamine tetra-acetic acid (EDTA), diethylene triamine penta-acetic acid (DTPA), cyclohexyl 1,2-diamine tetra-acetic acid (CDTA), ethyleneglycol-O,O′-bis(2-aminoethyl)-N,N,N′,N′-tetra-acetic acid (EGTA), N,N-bis(hydroxybenzyl)-ethylenediamine-N,N-diacetic acid (HBED), triethylene tetramine hexa-acetic acid (TTHA), 1,4,7,10-tetraaacyclododecane-N,N′,N″N′″-tetra-acetic acid (DOTA), hydroxyethyldiamine triacetic acid (HEDTA), 1,4,8,11-tetra-azacyclotetradecane-N,N′,N″,N′″-tetra-acetic acid (TETA), substituted DTPA, substituted EDTA, or from a compound of the general formula wherein R is a branched or non-branched, optionally substituted hydrocarbyl radical, which may be interrupted by one or more hetero-atoms selected from N, O and S and/or by one or more NH groups, and Y is a group which is capable of reacting with an amino group of the peptide and which is preferably selected from the group consisting of carbonyl, carbimidoyl, N-(C1-C6)alkylcarbimidoyl, N-hydroxycarbimidoyl and N-(C1-C6)alkoxycarbimidoyl; andwherein said optionally present spacing group has the general formula wherein R5 is a C1-C10 alkylene group, a C1-C10 alkylidene group or a C2-C10 alkenylene group, and X is a thiocarbonyl group or a methylcarbonyl group;and wherein said metal isotope is selected from the group consisting of 186R 188Re, 77As, 90Y, 67Cu, 169Er, 121Sn, 127Te, 142Pr, 143Pr, 198Au, 199Au, 161Tb, 109Pd, 165Dy, 149Pm, 151Pm, 153Sm, 157Gd, 159Gd, 166Ho, 172Tm, 169Yb, 175Yb, 177Lu, 105Rh and 111Ag.
Priority Claims (1)
Number |
Date |
Country |
Kind |
94200409 |
Feb 1994 |
EP |
|
Parent Case Info
This application is a division of application 08/737,299 now U.S. Pat. No. 5,952,464 filed on Jul. 21, 1997, which is a 371 of PCT/US95/02131 filed Feb. 21, 1995.
Non-Patent Literature Citations (2)
Entry |
Gura, Science vol. 278, p. 1041, Nov. 1997. |
Johnson et al, Cancer Treatment Reviews vol. 2 p. 1, 1975. |