Drug intelligence / Profile preview

T-APN-Gal-MMAE

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

Overview

T-APN-Gal-MMAE is a **novel antibody-drug conjugate (ADC)** created by conjugating ADPN-modified trastuzumab (a monoclonal antibody targeting ERBB2/HER2) with a cytotoxic payload, *monomethyl auristatin E (MMAE)*, via a β-galactosidase-cleavable linker[1]. The ADPN functional group enables stable rebridging to reduced trastuzumab, while the β-galactosidase-cleavable linker allows for selective drug release within cancer cells. Upon binding and internalization into HER2-positive cancer cells, the linker is cleaved by intracellular β-galactosidase, releasing MMAE, which inhibits tubulin polymerization leading to cell cycle arrest and apoptosis[1][13]. This design provides enhanced specificity and potent cytotoxicity for HER2-positive cancers, showing efficacy comparable to trastuzumab emtansine (T-DM1) and strong selectivity versus HER2-negative cells in preclinical models[1]. The molecule is an experimental candidate developed for targeted therapy in HER2-positive cancers.

Brand names
T-APN-Gal-MMAE
Other names
T-ADPN-Gal-MMAE
02

Targets

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

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