What question did this study set out to answer?

To evaluate the efficacy and safety of CS5007, a dual-targeting antibody-drug conjugate for treating cancers that overexpress EGFR and HER3.

April 5, 2026

Abstract 1823: Preclinical efficacy and safety of CS5007, an EGFR×HER3 dual-targeting antibody-drug conjugate with a topoisomerase 1 inhibitor payload.

Key Points

To evaluate the efficacy and safety of CS5007, a dual-targeting antibody-drug conjugate for treating cancers that overexpress EGFR and HER3.
Developed CS5007 with a topoisomerase 1 inhibitor payload and proprietary linker for stability.
Conducted in vitro testing on tumor cell lines, including osimertinib-resistant models.
Performed in vivo studies in xenograft models and assessed safety in cynomolgus monkeys.
CS5007 showed high-affinity binding to EGFR and HER3, leading to effective signaling inhibition.
Demonstrated potent cytotoxicity and induced cell killing in various tumor cell lines.
A single dose exhibited robust antitumor activity and superior efficacy compared to existing treatments.

Abstract

Abstract Background: EGFR and HER3, members of the ErbB receptor family, are key oncogenic drivers that are frequently co-overexpressed across a variety of human epithelial malignancies, Both EGFR and HER3 are clinically validated therapeutic targets for cancer therapies. Therefore, simultaneously targeting both EGFR and HER3 offers a promising strategy to overcome tumor heterogeneity and adaptive resistance commonly observed with single-target approaches. CS5007 is constructed with 1) functional EGFR 2) hydrophilic beta-glucuronide linker (our proprietary CSL20 linker) to ensure that the ADC has a mAb-like PK profile, stability and tumor selective cleavage; 3) potent, well-tolerated and clinically validated topoisomerase 1 inhibitor exatecan (Exa) conjugated to the antibody with a drug-to-antibody ratio (DAR) of 4. Methods Part 1 (Regular Abstracts); 2026 Apr 17-22; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2026;86(7 Suppl):Abstract nr 1823.

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