Drug intelligence / Profile preview

AK158D1

Development stage
Unknown
Lead developer
Akeso
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

AK158D1 is a first-in-class bispecific antibody-drug conjugate (ADC) developed by Akeso (Akesobio) that simultaneously targets Trophoblast cell-surface antigen 2 (Trop2) and Nectin-4. It is engineered using Akeso's proprietary Dual-Lock technology, which is designed to enhance tumor selectivity and reduce off-target toxicity by ensuring the ADC remains stable in systemic circulation and selectively releases its cytotoxic payload within the tumor microenvironment. Trop2 and Nectin-4 are frequently overexpressed in a variety of epithelial malignancies, including lung, breast, and urothelial cancers, and their co-expression provides a synergistic targeting opportunity. By binding to two distinct tumor-associated antigens, AK158D1 aims to improve therapeutic efficacy and overcome potential resistance mechanisms associated with monospecific ADC therapies. The drug is currently being evaluated in Phase 1/2 clinical trials for patients with advanced solid tumors.

Other names
Trop2/Nectin-4 bispecific ADCAkeso Trop2-Nectin-4 bispecific ADC
02

Targets

PVRL4 (Nectin cell adhesion molecule 4)TACSTD2 (Tumor-associated calcium signal transducer 2)

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