Drug intelligence / Profile preview

ASG-5ME

Development stage
Phase 1
Lead developer
Astellas Pharma
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

ASG-5ME is an investigational antibody-drug conjugate (ADC) designed for the treatment of solid tumors. It consists of a fully human monoclonal antibody targeting SLC44A4 (also known as AGS-5), which is highly expressed in prostate, pancreatic, and other cancers. The antibody is conjugated via a valine-citrulline linker to monomethyl auristatin E (MMAE), a potent microtubule-disrupting agent. Upon binding to SLC44A4 on tumor cells, ASG-5ME is internalized and MMAE is released through proteolytic cleavage inside the cell. MMAE then binds to tubulin and inhibits its polymerization, resulting in G2/M phase cell cycle arrest and apoptosis of the cancer cell[1][2][4][7]. The drug was co-developed by Agensys (an affiliate of Astellas Pharma) and Seattle Genetics for indications including metastatic castration-resistant prostate cancer, pancreatic cancer, and gastric cancer; however, further development was discontinued due to safety concerns related to its narrow therapeutic index[2][3].

Other names
anti-AGS-5 antibody-drug conjugateanti-AGS5 antibody-drug conjugateanti-AGS 5 antibody-drug conjugate
02

Targets

TUBB (Tubulin (alpha and beta subunits))SLC44A4 (Choline transporter-like protein 4)

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