US 12,227,566 B2
Endothelin receptor type a activity regulating antibody
Sang Taek Jung, Gyeonggi-do (KR); Yeon Gyu Yu, Seoul (KR); Man-Seok Ju, Gyeonggi-do (KR); Jung-Hyun Na, Seoul (KR); Youn Jae Kim, Seoul (KR); Hye-Mi Ahn, Gyeonggi-do (KR); Byoung Joon Ko, Chungcheongbuk-do (KR); and Won Kyu Lee, Gyeonggi-do (KR)
Assigned to HEDGEHOG, INC., Seoul (KR)
Appl. No. 17/311,537
Filed by HEDGEHOG, INC., Seoul (KR)
PCT Filed Dec. 5, 2019, PCT No. PCT/KR2019/017110
§ 371(c)(1), (2) Date Jun. 7, 2021,
PCT Pub. No. WO2020/116963, PCT Pub. Date Jun. 11, 2020.
Claims priority of application No. 10-2018-0155319 (KR), filed on Dec. 5, 2018; and application No. 10-2019-0159941 (KR), filed on Dec. 4, 2019.
Prior Publication US 2022/0153831 A1, May 19, 2022
Int. Cl. C07K 16/28 (2006.01); A61K 39/00 (2006.01); A61P 35/00 (2006.01)
CPC C07K 16/28 (2013.01) [A61P 35/00 (2018.01); A61K 2039/505 (2013.01); C07K 2317/56 (2013.01); C07K 2317/565 (2013.01); C07K 2317/76 (2013.01)] 17 Claims
 
1. A monoclonal antibody or a fragment thereof that recognizes and binds specifically to endothelin receptor type A or its extracellular domain as an antigen wherein the monoclonal antibody or fragment thereof comprises a heavy chain variable region comprising a CDR1 of SEQ ID NO: 38 and a CDR2 of SEQ ID NO: 39 and a light chain variable region comprising a CDR1 of SEQ ID NO: 40, a CDR2 of SEQ ID NO: 41, and a CDR3 of SEQ ID NO: 42 and wherein the CDR3 of the heavy chain variable region comprises the amino acid sequence of SEQ ID NO: 43 or a mutation selected from the group consisting of: a substitution of the amino acid at position 4 in the sequence of SEQ ID NO: 43 to proline (P), a substitution of the amino acid at position 7 in the sequence of SEQ ID NO: 43 to leucine (L), a substitution of the amino acid at position 9 in the sequence of SEQ ID NO: 43 to valine (V), a substitution of the amino acid at position 10 in the sequence of SEQ ID NO: 43 to isoleucine (I) or histidine (H), a substitution of the amino acid at position 11 in the sequence of SEQ ID NO: 43 to phenylalanine (F) or glutamine (Q), a substitution of the amino acid at position 12 in the sequence of SEQ ID NO: 43 to glutamate (E), a substitution of the amino acid at position 13 in the sequence of SEQ ID NO: 43 to asparagine (N) or cysteine (C) or a substitution of the amino acid at position 14 in the sequence of SEQ ID NO: 43 to leucine (L).