Heterotandem bicyclic peptide complexes
AssigneeBicycleTx Limited
InventorsGemma Mudd, Punit Upadhyaya, Kevin McDonnell, Johanna Lahdenranta
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Abstract
The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to EphA2, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.
Claims8
A method of treating cancer in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a heterotandem bicyclic peptide complex, or pharmaceutically acceptable salt thereof, wherein the heterotandem bicyclic peptide complex comprises:
- (a) a peptide ligand that binds to EphA2 and has the amino acid sequence A[HArg]DC[HyP]LVNPLCLEP[d1Nal]WTC (SEQ ID NO:
- 1) conjugated via an N-(acid-PEG3)—N-bis(PEG3-azide) linker to
- (b) two peptide ligands, each of which binds to CD137 and has the amino acid sequence AcC[tBuAla]PE[dK(PYA)]PYCFADPY[Nle]CA (SEQ ID NO:
- 2),
- wherein each peptide ligand of (a) and (b) comprises a 1,1′,1″-(1,3,5-triazinane-1,3,5-triyl)triprop-2-en-1-one (TATA) molecular scaffold covalently bonded to the respective peptide ligand via each of the three cysteines of the amino acid sequence,
- wherein Ac represents acetyl, [HArg] is homoarginine, [HyP] is trans-4-hydroxy-L-proline, [d1Nal]d-1-naphthylalanine, [tBuAla] is t-butyl-alanine, [dK(PYA)] is d-lysine conjugated to 4-pentynoic acid, and [Nle] is norleucine, and
- wherein cells of the cancer express EphA2 and activated immune cells of the patient express CD137.
Dependencies are inferred from the claim text.