IP Library › Granted Patent US 12,721,914
Granted Patent B2
US 12,721,914 · App. 18/049,609 · Granted Sep 1, 2026

Radiolabeled anti-LAG3 antibodies for immuno-PET imaging

Inventors: Marcus Kelly (New York, NY); Dangshe Ma (Pleasantville, NY); William Olson (Yorktown Heights, NY); Gavin Thurston (Millerton, NY); Richard Tavare (Salt Lake City, UT)
Assignee: Regeneron Pharmaceuticals, Inc.
A61K51/1027A61K39/00A61K51/1039C07C259/00C07K16/2803C07K2317/21
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Quick Facts
Patent No.
US 12,721,914
App. No.
18/049,609
Granted
Sep 1, 2026
Kind
B2
Abstract

Radiolabeled anti-LAG3 antibodies and their use in immuno-PET imaging are provided herein. Included are methods of detecting the presence of LAG3 proteins in a patient or sample.

Claims (23)

1 . A method for identifying a candidate for anti-tumor therapy, the method comprising:

(i) administering a radiolabeled anti-LAG3 antibody conjugate to a patient with a solid tumor, wherein the radiolabeled anti-LAG3 antibody conjugate comprises an anti-LAG3 antibody or antigen-binding fragment thereof comprising:

three heavy chain complementarity determining regions (HCDRs) in a heavy chain variable region (HCVR), wherein the HCVR has an amino acid sequence selected from the group consisting of SEQ ID NOs: 2, 18, 34, 50, 66, 82, 98, 130, 146, 162, 178, 194, 210, 226, 242, 258, 274, 290, 322, 338, 354, 370, 386, 402, 418, 434, 458, 466, 474, 482, 490, 498, 506, 514, 538, and 554; and three light chain complementarity determining regions (LCDRs) in a light chain variable region (LCVR), wherein the LCVR has an amino acid sequence selected from the group consisting of SEQ ID NOs: 10, 26, 42, 58, 74, 90, 106, 122, 138, 154, 170, 186, 202, 218, 234, 250, 266, 282, 298, 314, 330, 346, 362, 378, 394, 410, 426, 442, 522, 530, 546, and 562;

(ii) visualizing LAG3 expression by positron emission tomography (PET) imaging,

wherein presence of the radiolabeled antibody conjugate in the tumor identifies the patient as a candidate for anti-tumor therapy.

2 . The method of claim 1 , wherein the radiolabeled anti-LAG3 antibody conjugate comprises an anti-LAG3 antibody or antigen-binding fragment thereof, a chelating moiety, and a positron emitter.

3 . The method of claim 2 , wherein the antibody or antigen-binding fragment thereof is covalently bonded to one or more moieties of Formula (A):

-L-M Z   (A)

wherein L is the chelating moiety; M is the positron emitter; and z, independently at each occurrence, is 0 or 1; and wherein at least one of z is 1.

4 . The method of claim 2 , wherein the chelating moiety comprises desferrioxamine.

5 . The method of claim 2 , wherein the positron emitter is 89 Zr.

6 . The method of claim 3 , wherein-L-Mis

wherein Zr is the positron emitter, 89 Zr.

7 . The method of claim 3 , wherein the antibody or antigen-binding fragment thereof is covalently bonded to one, two, or three moieties of Formula (A).

8 . The method of claim 2 , wherein the radiolabeled anti-LAG3 antibody conjugate comprises an antibody or antigen-binding fragment thereof having three heavy chain complementarity determining regions (HCDRs) and three light chain complementarity determining regions (LCDRs) within the heavy chain variable region (HCVR)/light chain variable region (LCVR) amino acid sequence pair selected from the group consisting of SEQ ID NOs: 2/10, 18/26, 34/42, 50/58, 66/74, 82/90, 98/106, 130/138, 146/154, 162/170, 178/186, 194/202, 210/218, 226/234, 242/250, 258/266, 274/282, 290/298, 322/330, 338/346, 354/362, 370/378, 386/394, 402/410, 418/426, 434/442, 458/522, 466/522, 474/522, 482/522, 490/522, 498/530, 506/530, 514/530, 538/546, and 554/562.

9 . The method of claim 8 , wherein the radiolabeled anti-LAG3 antibody conjugate comprises an antibody or antigen-binding fragment thereof comprising a set of three HCDRs and three LCDRs, wherein the set of CDRs is selected from the group consisting of SEQ ID NOs: 4/6/8/12/14/16, 20/22/24/28/30/32, 36/38/40/44/46/48, 52/54/56/60/62/64, 68/70/72/76/78/80, 84/86/88/92/94/96, 100/102/104/108/110/112, 132/134/136/140/142/144, 148/150/152/156/158/160, 164/166/168/172/174/176, 180/182/184/188/190/192, 196/198/200/204/206/208, 212/214/216/220/222/224, 228/230/232/236/238/240, 244/246/248/252/254/256, 260/262/264/268/270/272, 276/278/280/284/286/288, 292/294/296/300/302/304, 324/326/328/332/334/336, 340/342/344/348/350/352, 356/358/360/364/366/368, 372/374/376/380/382/384, 388/390/392/396/398/400, 404/406/408/412/414/416, 420/422/424/428/430/432, 436/438/440/444/446/448, 460/462/464/524/526/528, 468/470/472/524/526/528, 476/478/480/524/526/528, 484/486/488/524/526/528, 492/494/496/524/526/528, 500/502/504/532/534/536, 508/510/512/532/534/536, 516/518/520/532/534/536, 540/542/544/548/550/552, and 556/558/560/564/566/568, respectively.

10 . The method of claim 2 , wherein the radiolabeled anti-LAG3 antibody conjugate comprises an antibody or antigen-binding fragment thereof having three HCDRs in an HCVR of SEQ ID NO: 418; and three LCDRs in an LCVR of SEQ ID NO: 426.

11 . The method of claim 2 , wherein the radiolabeled anti-LAG3 antibody conjugate comprises an antibody or antigen-binding fragment thereof having an HCDR1 amino acid sequence comprising SEQ ID NO: 420; an HCDR2 amino acid sequence comprising SEQ ID NO: 422; and an HCDR3 amino acid sequence comprising SEQ ID NO: 424; an LCDR1 amino acid sequence comprising SEQ ID NO: 428; an LCDR2 amino acid sequence comprising SEQ ID NO: 430; and an LCDR3 amino acid sequence comprising SEQ ID NO: 432.

12 . The method of claim 1 , wherein the radiolabeled anti-LAG3 antibody conjugate is administered at a dose of about 20 mg or less.

13 . The method of claim 1 , wherein the anti-tumor therapy is selected from nivolumab, ipilimumab, pembrolizumab, and combinations thereof.

14 . The method of claim 1 , wherein the anti-tumor therapy is a LAG3 inhibitor.

15 . The method of claim 1 , wherein the anti-tumor therapy is an anti-LAG3 antibody.

16 . The method of claim 15 , wherein the anti-tumor therapy is an anti-LAG3 antibody or antigen-binding fragment thereof that binds specifically to LAG3 and comprises three heavy chain complementarity determining regions (HCDRs) and three light chain complementarity determining regions (LCDRs) within the heavy chain variable region (HCVR)/light chain variable region (LCVR) amino acid sequence pair, wherein the HCVR/LCVR amino acid sequence pair is selected from the group consisting of SEQ ID NOS: 2/10, 18/26, 34/42, 50/58, 66/74, 82/90, 98/106, 114/122, 130/138, 146/154, 162/170, 178/186, 194/202, 210/218, 226/234, 242/250, 258/266, 274/282, 290/298, 306/314, 322/330, 338/346, 354/362, 370/378, 386/394, 402/410, 418/426, 434/442, 450/522, 458/522, 466/522, 474/522, 482/522, 490/522, 498/530, 506/530, 514/530, 538/546, and 554/562.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2025
From: KELLY, MARCUS; MA, DANGSHE; OLSON, WILLIAM; THURSTON, GAVIN; TAVARE, RICHARD
To: REGENERON PHARMACEUTICALS, INC.
Reel/Frame 072882/0793 →
Continuity (4)
Continuation 17127618 · Dec 18, 2020
Division 15892440 · Feb 9, 2018
Provisional Application 62457287 · Feb 10, 2017
Related Publication 20230270894A1 · Aug 31, 2023
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