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US 11,306,123 B2Granted
Heterotandem bicyclic peptide complex
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 Nectin-4, 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.
Claims19
A heterotandem bicyclic peptide complex comprising:
- (a) a first peptide ligand which binds to Nectin-4 and which has the sequence CiP[1Nal][dD]CiiM[HArg]DWSTP[HyP]WCiii (SEQ ID NO:
- 1);
- conjugated via an N-(acid-PEG3)-N-bis(PEG3-azide) linker to
- (b) two second peptide ligands which bind to CD137 both of which have the sequence Ac-Ci[tBuAla]PE[D-Lys(PYA)]PYCiiFADPY[Nle]Ciii-A (SEQ ID NO:
- 2);
- or a pharmaceutically acceptable salt thereof,
- wherein each of said peptide ligands comprise a polypeptide comprising three reactive cysteine groups (Ci, Cii and Ciii), separated by two loop sequences, and a molecular scaffold which is 1,1′,1″-(1,3,5-triazinane-1,3,5-triyl)triprop-2-en-1-one (TATA) and which forms covalent bonds with the reactive cysteine groups of the polypeptide such that two polypeptide loops are formed on the molecular scaffold;
- wherein Ac represents acetyl, HArg represents homoarginine, HyP represents trans-4-hydroxy-L-proline, 1Nal represents 1-naphthylalanine, tBuAla represents t-butyl-alanine, PYA represents 4-pentynoic acid and Nle represents norleucine.
5 more elements
A heterotandem bicyclic peptide complex which is:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.