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US 2004/0001790 A1Published application
Methods for diagnosis and treatment of tumours
AssigneeSchering Corporation
InventorsChristoph-Stephan Hilger, Dietmar Berndorff, Ludger Dinkelborg, Dieter Moosmayer, Giovanni Neri
Life of this patent
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Abstract
The present invention relates to new methods for diagnosis and treatment of tumours, using novel peptides for binding radionuclides.
Claims21
A compound comprising
- a peptide comprising
- aa) an antigen-binding site for the extra domain B (ED-B) of fibronectin comprising complementarity-determining regions HCDR3 and/or LCDR3 as shown in Table 1 or a variation thereof that is a deletion, insertion and/or 0
- substitution of up to 5 amino acids for the HCDR3 region and up to 6 amino acids for the LCDR3 region which has the same function as a peptide according to Seq. Id. No. 1;
- ab) an antigen-binding site for the extra domain B(ED-B) of fibronectin comprising complementarity-determining regions HCDR1, HCDR2, HCDR3, LCDR1, LCDR2 and LCDR3 as shown in Table 1 or a variation thereof that is a deletion, insertion and/or substitution of up to 3 amino acids for the HCDR1 region, up to 8 amino acids for the HCDR2 region, up to 5 amino acids for the HCDR3 region, up to 6 amino acids for the LCDR1 region, up to 4 amino acids for the LCDR2 region and up to 6 amino acids for the LCDR3 region;
- which has the same function as a peptide according to Seq. Id. No. 1;
- or
- ac) a sequence according to Seq. Id. No. 1 (L19) or a variation of Seq. Id. No. 1 that is a deletion, insertion and/or substitution of up to 30 amino acids, an which has the same function as a peptide according to Seq. Id. No. 1,
- and
- ba) an amino acid sequence Xaa1-Xaa2-Xaa3-Cys (Seq. Id. No. 2), wherein Xaa1, Xaa2 and Xaa3 each independently represent any naturally occuring amino acid or
- bb) an amino acid sequence Xaa1-Xaa2-Xaa3-Cys-Xaa4(Seq. Id. No. 3), wherein Xaa1, Xaa2, Xaa3, and Xaa4 each independently represent any naturally occuring amino acid or
- bc) an amino acid sequence (His)n (Seq. Id. No. 4), wherein n stands for an integer from 4 to 6,
- wherein the C-terminus of aa), ab) or ac) is bound to the N-terminus of one of the sequences Seq. Id. No. 2, Seq. Id. No. 3 or Seq. Id. No. 4 via a peptide bond.
9 more elements
The compound according to claim 6 which is conjugated to a radioisotope selected from a radioisotope of Technetium, such as 94mTc, 99mTc, Rhenium, such as 186Re, 188Re, or other isotopes, such as 203Pb, 67Ga 68Ga, 43Sc, 44Sc, 47Sc, 110mIn, 111In, 97Ru, 62Cu, 64Cu, 67Cu, 68Cu, 86Y, 88Y, 90Y, 121Sn, 161Tb, 153Sm, 166Ho, 105Rh, 177Lu, 72As and 18F.
Use of a peptide comprising
- aa) an antigen-binding site for the extra domain B (ED-B) of fibronectin comprising complementarity-determining regions HCDR3 and/or LCDR3 as shown in Table 1 or a variation thereof that is a deletion, insertion and/or substitution of up to 5 amino acids for the HCDR3 region and up to 6 amino acids for the LCDR3 region which has the same function as a peptide according to Seq. Id. No. 1;
- ab) an antigen-binding site for the extra domain B(ED-B) of fibronectin comprising complementarity-determining regions HCDR1, HCDR2, HCDR3, LCDR1, LCDR2 and LCDR3 as shown in Table 1 or a variation thereof that is a deletion, insertion and/or substitution of up to 3 amino acids for the HCR1 region, up to amino acids for the HCDR2 region, up to 5 amino acids for the HCDR3 region, up to 6 amino acids for the LCDR1 region, up to 4 amino acids for the LCDR2 region and up to 6 amino acids for the LCDR3 region;
- which has the same function as a peptide according to Seq. Id. No. 1;
- or
- ac) a sequence according to Seq. Id. No. 1 (L19) or a variation of Seq. Id. No. 1 that is a deletion, insertion and/or substitution of up to 30 amino acids an which has the same function as a peptide according to Seq. Id. No. 1,
- and
- ba) an amino acid sequence Xaa1-Xaa2-Xaa3-Cys (Seq. Id. No.2), wherein Xaa1, Xaa2 and Xaa3 each independently represent any naturally occuring amino acid or
- bb) an amino acid sequence Xaa1-Xaa2-Xaa3-Cys-Xaa4(Seq. Id. No. 3), wherein Xaa1, Xaa2, Xaa3, and Xaa4 each independently represent any naturally occuring amino acid or
- bc) an amino acid sequence (His)n (Seq. Id. No. 4), wherein n stands for an integer from 4 to 6,
- wherein the C-terminus of aa), ab) or ac) is bound to the N-terminus of one of the sequences Seq. Id. No. 2, Seq. Id. No. 3 or Seq. Id. No. 4 via a peptide bond,
- for binding a radioisotope.
8 more elements
Dependencies are inferred from the claim text.