IP Library Granted Patent US 12,390,541
Granted Patent B2
US 12,390,541 · App. 17/278,869 · Granted Aug 19, 2025

Mutant variants of PD-1 receptor with selective binding to PD-L1 and uses thereof

Inventors: Andras Fiser (New York, NY); Rojan Shrestha (Bronx, NY); Steven C. Almo (Pelham, NY); Sarah C. Garrett (Bronx, NY)
Assignee: Albert Einstein College of Medicine
A61K51/08C07K14/70532C07K2319/30
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Quick Facts
Patent No.
US 12,390,541
App. No.
17/278,869
Granted
Aug 19, 2025
Kind
B2
Abstract

Disclosed are human Programmed Cell Death-1 (PD-1) receptor mutants having selectivity for PD-L1 compared to PD-L2, methods of obtaining the mutants, and uses of the mutants for treatment and imaging.

Claims (12)

1. A human Programmed Cell Death-1 (PD-1) receptor mutant comprising at least the first 149 consecutive amino acids of SEQ ID NO:1 with mutation Y68R or Y68K, wherein the mutant has selectivity for PD-LI compared to PD-L2 and wherein the mutant has undetectable PD-L2 binding.

2. A fusion polypeptide comprising the PD-1 receptor mutant of claim 1 fused to an immunoglobulin domain polypeptide.

3. The fusion polypeptide of claim 2 , wherein the mutant is fused to the immunoglobulin domain polypeptide by a peptide bond between a terminal amino acid of the mutant and a terminal amino acid of the immunoglobulin domain polypeptide.

4. The fusion polypeptide of claim 2 , wherein the immunoglobulin domain polypeptide comprises an immunoglobulin IgG1 Fc domain.

5. The fusion polypeptide of claim 4 , wherein the immunoglobulin IgG1 Fc domain is human.

6. A composition comprising the PD-1 receptor mutant of claim 4 , and a pharmaceutically acceptable carrier.

7. The PD-1 receptor mutant of claim 1 further comprising a radiolabel.

8. A method of imaging a PD-L1 positive tumor in a subject comprising administering the radiolabeled PD-1 receptor mutant of claim 7 to the subject, where the mutant binds to the tumor, and imaging the radiolabeled mutant bound to the tumor.

9. A method of stimulating T cell activation, treating a tumor, or treating an infection in a subject comprising administering to the subject a human Programmed Cell Death-1 (PD-1) receptor mutant comprising at least the first 149 consecutive amino acids of SEQ ID NO: 1 with mutation Y68R or Y68K, wherein the mutant has selectivity for PD-LI compared to PD-L2 and wherein the mutant has undetectable PD-L2 binding, or a fusion polypeptide comprising the PD-1 receptor mutant fused to an immunoglobulin domain polypeptide, or a composition comprising the PD-1 receptor mutant or the fusion polypeptide, in an amount effective to stimulate T cell activation, treat a tumor, or treat an infection, respectively, in a subject.

10. The method of claim 9 , wherein the T cell activation comprises cytokine secretion.

11. The method of claim 9 , wherein the subject has a tumor.

12. The method of claim 9 , wherein the subject has an infection.

Assignments (2)
LICENSE Recorded Nov 4, 2024
From: ALBERT EINSTEIN COLLEGE OF MEDICINE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 069292/0335 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 7, 2021
From: FISER, ANDRAS; SHRESTHA, ROJAN; ALMO, STEVEN C.; GARRETT, SARAH C.
To: ALBERT EINSTEIN COLLEGE OF MEDICINE
Reel/Frame 055848/0008 →
Continuity (2)
Provisional Application 62736477 · Sep 26, 2018
Related Publication 20220047729A1 · Feb 17, 2022
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