	US 12,441,799 B2
	Activatable anti-CTLA-4 antibodies and uses thereof
Kimberly Ann Tipton, South San Francisco, CA (US); James William West, South San Francisco, CA (US); Shrikant Deshpande, Fremont, CA (US); and John J. Englehardt, El Cerrito, CA (US)
Assigned to Bristol-Myers Squibb Company, Princeton, NJ (US); and CytomX Therapeutics, Inc., South San Francisco, CA (US)
Filed by Bristol-Myers Squibb Company, Princeton, NJ (US); and CytomX Therapeutics, Inc., South San Francisco, CA (US)
Filed on Aug. 11, 2021, as Appl. No. 17/399,729.
Application 17/399,729 is a continuation of application No. 16/347,522, granted, now 11,117,968, previously published as PCT/US2017/059740, filed on Nov. 2, 2017.
Claims priority of provisional application 62/417,212, filed on Nov. 3, 2016.
Prior Publication US 2022/0089734 A1, Mar. 24, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. C07K 16/28 (2006.01); A61K 39/395 (2006.01)

CPC C07K 16/2818 (2013.01) [A61K 39/395 (2013.01); C07K 2317/24 (2013.01); C07K 2317/41 (2013.01); C07K 2317/50 (2013.01); C07K 2317/76 (2013.01); C07K 2317/92 (2013.01); C07K 2317/94 (2013.01)]

14 Claims

1. An activatable anti-human CTLA-4 antibody comprising a heavy chain and a light chain, wherein:

(i) the heavy chain comprises a heavy chain variable domain (VH) comprising CDRH1: SYTMH (SEQ ID NO: 557); CDRH2: FISYDGNNKYYADSVKG (SEQ ID NO: 558); and CDRH3: TGWLGPFDY (SEQ ID NO: 559); and

(ii) the light chain comprises:

(a) a light chain variable domain (VL) comprising CDRL1: RASQSVGSSYLA (SEQ ID NO: 560); CDRL2: GAFSRAT (SEQ ID NO: 561); and CDRL3: QQYGSSPWT (SEQ ID NO: 562);

(b) a cleavable moiety (CM); and

(c) a masking moiety (MM), wherein the MM comprises the amino acid sequence selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 9, SEQ ID NO: 23, SEQ ID NO: 24, SEQ ID NO: 35, SEQ ID NO: 39, SEQ ID NO: 41, SEQ ID NO: 51, SEQ ID NO: 53, SEQ ID NO: 55, SEQ ID NO: 60, SEQ ID NO: 61, SEQ ID NO: 62, SEQ ID NO: 63, SEQ ID NO: 64, and SEQ ID NO: 65,

wherein the light chain has the structural arrangement, from N-terminus to C-terminus, as follows: MM-CM-VL; and

wherein the activatable anti-human CTLA-4 antibody is nonfucosylated.