Abstract

Objective: To (I) provide an update of approved antibody drug conjugates (ADCs) and those registered with NMPA, (II) give an overview of HER2-targeting ADCs as a mono- or combination therapy in clinical development for breast cancer and the molecular mechanism of payloads of these molecules, (III) describe the pharmacokinetic profiles of ADCs using mostly exploited vcMMAE platform as an example, (IV) discuss future development strategies for ADC therapeutics in addressing substantially unmet medical needs, such as brain metastasis (BM) and drug resistance in patients with HER2-expressing advanced breast cancer.

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