Drug intelligence / Profile preview

trastuzumab-AJICAP-MMAE

Development stage
Preclinical
Lead developer
Ajinomoto
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Trastuzumab-AJICAP-MMAE is a site-specific antibody-drug conjugate (ADC) developed by Ajinomoto using their proprietary AJICAP (Fc-affinity guided chemical conjugation) technology. The drug consists of the anti-HER2 monoclonal antibody trastuzumab (Herceptin) conjugated to the cytotoxic payload monomethyl auristatin E (MMAE) via a cleavable maleimidocaproyl-valine-citrulline (MC-VC) linker. The conjugation occurs at a specific lysine residue (Lys248) in the Fc region of the antibody, resulting in a drug-to-antibody ratio (DAR) of approximately 1.6 to 2.0. This site-specific approach aims to improve the therapeutic index and pharmacokinetic profile compared to traditional stochastic ADCs by reducing heterogeneity. Preclinical studies in HER2-positive gastric cancer xenograft models and rat toxicology studies have demonstrated potent anti-tumor activity and a favorable safety profile.

Other names
AJICAP-ADCtrastuzumab-MMAE ADC (AJICAP)
02

Targets

TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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