A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activity

Combinatorial strategies, such as targeting different immune checkpoint receptors, hold promise to increase the breadth and duration of the response to cancer therapy. Here we describe the preclinical evaluation of CTX-8371, a protein construct which combines PD-1 and PD-L1 targeting in one bispecif...

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Main Authors: Diana I. Albu, Benjamin J. Wolf, Yan Qin, Xianzhe Wang, Amy Daniel Ulumben, Mei Su, Vivian Li, Eirene Ding, Jose Angel Gonzalo, Jason Kong, Ruturaj Jadhav, Nelly Kuklin, Alberto Visintin, Bing Gong, Thomas J. Schuetz
Format: Article
Language:English
Published: Taylor & Francis Group 2024-12-01
Series:OncoImmunology
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Online Access:https://www.tandfonline.com/doi/10.1080/2162402X.2024.2316945
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author Diana I. Albu
Benjamin J. Wolf
Yan Qin
Xianzhe Wang
Amy Daniel Ulumben
Mei Su
Vivian Li
Eirene Ding
Jose Angel Gonzalo
Jason Kong
Ruturaj Jadhav
Nelly Kuklin
Alberto Visintin
Bing Gong
Thomas J. Schuetz
author_facet Diana I. Albu
Benjamin J. Wolf
Yan Qin
Xianzhe Wang
Amy Daniel Ulumben
Mei Su
Vivian Li
Eirene Ding
Jose Angel Gonzalo
Jason Kong
Ruturaj Jadhav
Nelly Kuklin
Alberto Visintin
Bing Gong
Thomas J. Schuetz
author_sort Diana I. Albu
collection DOAJ
description Combinatorial strategies, such as targeting different immune checkpoint receptors, hold promise to increase the breadth and duration of the response to cancer therapy. Here we describe the preclinical evaluation of CTX-8371, a protein construct which combines PD-1 and PD-L1 targeting in one bispecific, tetravalent antibody. CTX-8371 matched or surpassed the activity of anti-PD-1 and PD-L1 benchmark antibodies in several in vitro T cell activation assays and outperformed clinically approved benchmarks in the subcutaneous MC38 colon and the B16F10 lung metastasis mouse tumor models. Investigation into the mechanism of action revealed that CTX-8371 co-engagement of PD-1 and PD-L1 induced the proteolytic cleavage and loss of cell surface PD-1, which is a novel and non-redundant mechanism that adds to the PD-1/PD-L1 signaling axis blockade. The combination of CTX-8371 and an agonistic anti-CD137 antibody further increased the anti-tumor efficacy with long-lasting curative therapeutic effect. In summary, CTX-8371 is a novel checkpoint inhibitor that might provide greater clinical benefit compared to current anti-PD-1 and PD-L1 antibodies, especially when combined with agents with orthogonal mechanisms of action, such as agonistic anti-CD137 antibodies.
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spelling doaj-art-5e1ca35cffdd474daf5caef1c125a47e2025-08-20T02:50:37ZengTaylor & Francis GroupOncoImmunology2162-402X2024-12-0113110.1080/2162402X.2024.2316945A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activityDiana I. Albu0Benjamin J. Wolf1Yan Qin2Xianzhe Wang3Amy Daniel Ulumben4Mei Su5Vivian Li6Eirene Ding7Jose Angel Gonzalo8Jason Kong9Ruturaj Jadhav10Nelly Kuklin11Alberto Visintin12Bing Gong13Thomas J. Schuetz14Compass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACompass Therapeutics Inc, Boston, MA, USACombinatorial strategies, such as targeting different immune checkpoint receptors, hold promise to increase the breadth and duration of the response to cancer therapy. Here we describe the preclinical evaluation of CTX-8371, a protein construct which combines PD-1 and PD-L1 targeting in one bispecific, tetravalent antibody. CTX-8371 matched or surpassed the activity of anti-PD-1 and PD-L1 benchmark antibodies in several in vitro T cell activation assays and outperformed clinically approved benchmarks in the subcutaneous MC38 colon and the B16F10 lung metastasis mouse tumor models. Investigation into the mechanism of action revealed that CTX-8371 co-engagement of PD-1 and PD-L1 induced the proteolytic cleavage and loss of cell surface PD-1, which is a novel and non-redundant mechanism that adds to the PD-1/PD-L1 signaling axis blockade. The combination of CTX-8371 and an agonistic anti-CD137 antibody further increased the anti-tumor efficacy with long-lasting curative therapeutic effect. In summary, CTX-8371 is a novel checkpoint inhibitor that might provide greater clinical benefit compared to current anti-PD-1 and PD-L1 antibodies, especially when combined with agents with orthogonal mechanisms of action, such as agonistic anti-CD137 antibodies.https://www.tandfonline.com/doi/10.1080/2162402X.2024.2316945Cancer immunotherapyimmuno-oncology
spellingShingle Diana I. Albu
Benjamin J. Wolf
Yan Qin
Xianzhe Wang
Amy Daniel Ulumben
Mei Su
Vivian Li
Eirene Ding
Jose Angel Gonzalo
Jason Kong
Ruturaj Jadhav
Nelly Kuklin
Alberto Visintin
Bing Gong
Thomas J. Schuetz
A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activity
OncoImmunology
Cancer immunotherapy
immuno-oncology
title A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activity
title_full A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activity
title_fullStr A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activity
title_full_unstemmed A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activity
title_short A bispecific anti-PD-1 and PD-L1 antibody induces PD-1 cleavage and provides enhanced anti-tumor activity
title_sort bispecific anti pd 1 and pd l1 antibody induces pd 1 cleavage and provides enhanced anti tumor activity
topic Cancer immunotherapy
immuno-oncology
url https://www.tandfonline.com/doi/10.1080/2162402X.2024.2316945
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