Drug intelligence / Profile preview

LPA003

Development stage
Preclinical
Lead developer
Henlius
Modality
Small Molecules
Administration
Intravenous
01

Overview

LPA003 is a medium-potency, camptothecin-based linker-payload developed by Shanghai Henlius Biotech as part of its Hanjugator platform. It is designed for use in antibody-drug conjugates (ADCs), specifically optimized to allow for higher clinical dosing and optimal receptor occupancy by utilizing a payload with tunable potency (approximately threefold lower than deruxtecan). LPA003 exhibits high hydrophilicity, superior stability, and bystander killing effects over 10-fold stronger than deruxtecan. Its mechanism of action involves topoisomerase I inhibition. LPA003 has been applied to an EGFR/cMet bispecific ADC, which demonstrated significant tumor regression in xenograft models (including colorectal and lung cancer models) and was well-tolerated in cynomolgus monkeys. An Investigational New Drug (IND) submission for the LPA003-conjugated EGFR/cMet ADC is anticipated in the first quarter of 2026.

02

Targets

TOP1 (DNA Topoisomerase I)

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