Drug intelligence / Profile preview

(HE)3-ZHER3-ABD-mcDM1

Development stage
Preclinical
Lead developer
Uppsala University
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

(HE)3-ZHER3-ABD-mcDM1 is a preclinical-stage, HER3-targeted affibody-drug conjugate (AffiDC) developed by researchers at Uppsala University and KTH Royal Institute of Technology. The construct consists of a HER3-targeting affibody molecule (ZHER3) fused to an albumin-binding domain (ABD) for in vivo half-life extension, and an N-terminal (HE)3 tag (His-Glu-His-Glu-His-Glu) for site-specific radiolabeling (e.g., with technetium-99m). It is conjugated to the cytotoxic microtubule inhibitor payload DM1 (mertansine) via a non-cleavable maleimidocaproyl (mc) linker. In preclinical models of HER3-expressing cancers, such as pancreatic cancer and prostate cancer, the conjugate has demonstrated high binding specificity, efficient internalization, and potent cytotoxicity.

Other names
[99mTc]Tc-(HE)3-ZHER3-ABD-mcDM1[99mTc]Tc-ZHER3-ABD-mcDM1ZHER3-ABD-mcDM1ZHER-3-ABD-mcDM1ZHER 3-ABD-mcDM1
02

Targets

ERBB3 (Erb-b2 receptor tyrosine kinase 3)

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