Drug intelligence / Profile preview

HER2xAPLP2-DM1

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

Overview

HER2xAPLP2-DM1 is a preclinical bispecific antibody-drug conjugate (ADC) developed by Regeneron Pharmaceuticals. It is designed to target HER2-expressing tumor cells, particularly those with intermediate levels of HER2 expression (IHC 2+) that are typically resistant to standard HER2-targeted therapies like trastuzumab emtansine (T-DM1). The bispecific antibody component consists of a high-affinity arm that binds to HER2 on tumor cells and a low-affinity arm that binds to amyloid-like protein 2 (APLP2), a rapidly internalizing receptor. Upon binding, the APLP2 arm facilitates rapid internalization and lysosomal trafficking of the ADC, leading to the release of the cytotoxic payload, emtansine (DM1), which inhibits microtubule assembly and induces cell death.

Other names
anti-HER2/anti-APLP2 bispecific antibody-drug conjugateanti-HER2xAPLP2 antibody drug conjugateanti-HER-2xAPLP2 antibody drug conjugateanti-HER 2xAPLP2 antibody drug conjugate
02

Targets

TUBB (Tubulin (alpha and beta subunits))APLP2 (Amyloid beta precursor-like protein 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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