US 11,833,211 B2
Methods of suppression and treatment of disease comprising administering bicycle peptide ligands specific for EphA2
Liuhong Chen, Cambridge (GB); Philip Huxley, Cambridge (GB); Silvia Pavan, Cambridge (GB); and Katerine Van Rietschoten, Cambridge (GB)
Assigned to BicycleTx Limited, Cambridge (GB)
Filed by BicycleTx Limited, Cambridge (GB)
Filed on Sep. 23, 2022, as Appl. No. 17/934,896.
Application 17/934,896 is a division of application No. 16/220,685, filed on Dec. 14, 2018, granted, now 11,484,602.
Claims priority of application No. 1721259 (GB), filed on Dec. 19, 2017; application No. 1804102 (GB), filed on Mar. 14, 2018; and application No. 1818603 (GB), filed on Nov. 14, 2018.
Prior Publication US 2023/0144799 A1, May 11, 2023
Int. Cl. A61K 47/64 (2017.01); A61P 35/00 (2006.01); A61K 47/65 (2017.01); A61K 38/10 (2006.01); A61K 38/05 (2006.01); A61K 47/62 (2017.01); C07K 7/08 (2006.01)
CPC A61K 47/6415 (2017.08) [A61K 38/05 (2013.01); A61K 38/10 (2013.01); A61K 47/62 (2017.08); A61K 47/64 (2017.08); A61K 47/65 (2017.08); A61P 35/00 (2018.01); C07K 7/08 (2013.01)] 20 Claims
OG exemplary drawing
 
1. A method for suppressing or treating a disease or disorder characterized by overexpression of EphA2 in diseased tissue in a patient, the method comprising administering to the patient a peptide ligand specific for EphA2 comprising a polypeptide comprising three cysteine residues, separated by two loop sequences, and a non-aromatic molecular scaffold which forms covalent bonds with the cysteine residues of the polypeptide, such that two polypeptide loops are formed on the molecular scaffold, wherein the peptide ligand comprises the amino acid sequence:
 
 (SEQ ID NO: 1)
 
 Ci(HyP)LVNPLCiiLHP(D-Asp)W(HArg)Ciii;
wherein HyP is hydroxyproline, HArg is homoarginine, and Ci, Cii, and Ciii represent first, second, and third cysteine residues, respectively, or a pharmaceutically acceptable salt thereof.