Drug intelligence / Profile preview

AI-081

Development stage
Phase 2
Lead developer
OncoC4
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Vaccines & Immunotherapeutics, Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

AI-081 is a humanized bispecific monoclonal antibody designed to simultaneously target programmed cell death protein 1 (PD-1) and vascular endothelial growth factor (VEGF). It is constructed from proprietary high-affinity clinical-stage anti-PD1 (AI-025) and anti-VEGF (AI-011) antibodies using a head-and-tail bispecific configuration, with Fc silencing mutations to preserve immune effector cells. By binding PD-1, AI-081 blocks its interaction with ligands PD-L1 and PD-L2, thereby enhancing T-cell mediated immune responses against tumors. Concurrently, by targeting VEGF, it inhibits angiogenesis within the tumor microenvironment. Preclinical studies have shown that this dual blockade results in robust cooperative interactions and synergistic anti-tumor activity superior to other agents in its class. The drug is being developed for the treatment of advanced solid tumors and is currently undergoing Phase 1/2 clinical trials.

Other names
anti-PD-1/anti-VEGF bispecific antibody AI-081
02

Targets

VEGFA (Vascular endothelial growth factor A)PDCD1 (Programmed cell death protein 1 receptor)

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