Drug intelligence / Profile preview

R800-exatecan

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

Overview

R800-exatecan is an antibody-drug conjugate (ADC) developed by GO-therapeutics. It consists of a humanized monoclonal antibody, R800, conjugated to the topoisomerase 1 inhibitor payload, exatecan. The R800 antibody specifically targets truncated O-glycans (cancer-specific glycopeptide epitopes) that are expressed in various epithelial cancers but absent in healthy tissues. In preclinical studies, R800-exatecan has demonstrated potent anti-tumor activity across multiple solid tumor models, including triple-negative breast, lung, pancreatic, colorectal, and ovarian cancers. The drug leverages the high specificity of the R800 antibody to deliver the cytotoxic payload directly to tumor cells, aiming to enhance efficacy while minimizing off-target toxicity.

02

Targets

TOP1 (DNA Topoisomerase I)Tn/STn (Truncated O-linked N-acetylgalactosamine glycans (Tn/STn antigens))

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