Drug intelligence / Profile preview

iso-nexatecan-based GGFG payload

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

Overview

The iso-nexatecan-based GGFG payload is a proprietary drug-linker technology developed by IntoCell Inc. for use in antibody-drug conjugates (ADCs). This construct consists of iso-nexatecan, a cytotoxic topoisomerase I inhibitor derived from camptothecin analogs, conjugated to a GGFG (glycyl-glycyl-phenylalanyl-glycine) tetrapeptide linker. The GGFG linker is designed to be protease-cleavable, maintaining high stability in systemic circulation but undergoing rapid enzymatic cleavage by lysosomal cathepsins once the ADC is internalized into tumor cells. Upon release, the iso-nexatecan payload inhibits topoisomerase I, leading to DNA strand breaks and subsequent cell death. In October 2025, IntoCell licensed this technology to Piramal Pharma Solutions to expand their bioconjugate development and manufacturing capabilities.

Other names
iso-nexatecan GGFG payloadiso-nexatecan-GGFG
02

Targets

TOP1 (DNA Topoisomerase I)

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