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US 11,298,433 B2Granted
Radiolabelled antibody fragments for use in treating cancer
AssigneeVrije Universiteit Brussel
InventorsTony Lahoutte, Matthias D'Huyvetter, Jens De Vos, Nick Devoogdt
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Abstract
Provided herein are methods, kits, and compositions for stratifying and treating subjects, e.g., subjects having cancer. In some examples, the methods involve use of a radiolabelled heavy chain variable domain derived from a heavy chain antibody (VHH), or a functional fragment thereof, as both a screening agent and a treatment agent. In some examples, the VHH, or a functional fragment thereof, that is radiolabelled with a radioisotope that is both a γ-emitter and β-emitter.
Claims33
A method of treating a HER2-expressing cancer, the method comprising:
- (a) selecting a subject having cancer for treatment on the basis of detection in the subject of a screening dose of a radiolabelled, heavy chain variable domain derived from a heavy chain antibody (VHH), or a functional fragment thereof, which specifically binds to HER2 that is present on a cancer cell or solid tumor
- wherein the VHH or functional fragment thereof comprises
- a CDR1 comprising the amino acid sequence of SEQ ID NO:1,
- a CDR2 comprising the amino acid sequence of SEQ ID NO:2, and
- a CDR3 comprising the amino acid sequence of SEQ ID NO:3;
- and
- (b) administering to the subject a therapeutic dose of the radiolabelled VHH, or functional fragment thereof,
- wherein the VHH, or functional fragment thereof, of both the screening dose and the therapeutic dose is radiolabelled with Iodine-131 using N-succinimidyl-4-guanidinomethyl-3-[I-131] iodobenzoate ([I-131]-SGMIB).
5 more elements
A method of treating a HER2-expressing cancer, the method comprising:
- (a) selecting a subject having breast cancer for treatment on the basis of detection in the subject of a screening dose of between about 37 MBq and about 370 MBq of a radiolabelled, heavy chain variable domain derived from a heavy chain antibody (VHH), or a functional fragment thereof, which specifically binds to HER2 that is present on the cancer
- wherein the VHH or functional fragment thereof comprises
- a CDR1 comprising the amino acid sequence of SEQ ID NO:1,
- a CDR2 comprising the amino acid sequence of SEQ ID NO:2, and
- a CDR3 comprising the amino acid sequence of SEQ ID NO:3;
- and
- (b) administering to the subject a therapeutic dose of between about 3000 MBq and about 20000 MBq of the radiolabelled VHH, or functional fragment thereof,
- wherein the radiolabelled VHH, or functional fragment thereof, of both the screening dose and the therapeutic dose comprises N-succinimidyl-4-guanidinomethyl-3[I-131]iodobenzoate ([I-131]-SGMIB).
5 more elements
A method of treating a HER2-expressing breast cancer, the method comprising:
- (a) selecting a subject having breast cancer for treatment on the basis of detection in the subject of a screening dose of between about 37 MBq and about 370 MBq of a radiolabelled, heavy chain variable domain derived from a heavy chain antibody (VHH), or a functional fragment thereof, which specifically binds to HER2 that is present on the breast cancer;
- wherein the VHH or functional fragment thereof comprises
- a CDR1 comprising the amino acid sequence of SEQ ID NO:1,
- a CDR2 comprising the amino acid sequence of SEQ ID NO:2, and
- a CDR3 comprising the amino acid sequence of SEQ ID NO:3;
- and
- (b) administering to the subject a therapeutic dose of between about 3000 MBq and about 20000 MBq of the radiolabelled VHH, or functional fragment thereof,
- wherein the radiolabelled VHH, or functional fragment thereof, of both the screening dose and the therapeutic dose comprises N-succinimidyl-4-guanidinomethyl-3[I-131]iodobenzoate ([I-131]-SGMIB).
5 more elements
A method of treating a HER2-expressing gastric cancer, the method comprising:
- (a) selecting a subject having gastric cancer for treatment on the basis of detection in the subject of a screening dose of between about 37 MBq and about 370 MBq of a radiolabelled, heavy chain variable domain derived from a heavy chain antibody (VHH), or a functional fragment thereof, which specifically binds to HER2 that is present on the gastric cancer
- wherein the VHH or functional fragment thereof comprises
- a CDR1 comprising the amino acid sequence of SEQ ID NO:1,
- a CDR2 comprising the amino acid sequence of SEQ ID NO:2, and
- a CDR3 comprising the amino acid sequence of SEQ ID NO:3;
- and
- (b) administering to the subject a therapeutic dose of between about 3000 MBq and about 20000 MBq of the radiolabelled VHH, or functional fragment thereof,
- wherein the radiolabelled VHH, or functional fragment thereof, of both the screening dose and the therapeutic dose comprises N-succinimidyl-4-guanidinomethyl-3-[I-131]iodobenzoate ([I-131]-SGMIB).
5 more elements
Dependencies are inferred from the claim text.