"Straightforward conjugation of payloads to mAbs under mild reaction conditions"

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Pipeline

Currently the first Lx®-based targeted drugs are in the last phase of preclinical development and have met most criteria of Good Manufacturing Practice required for their use in clinical studies. LinXis has the ambition to introduce Lx® on the medical market from 2016 onwards, both as toolbox products (drug- Lx®-ligands) for customized ADC development and with currently developed proprietary ADCs.

The LinXis pipeline includes the following ADCs:

LxT-001. An antibody-tracer conjugate (ATC) in cooperation with the Tracer Center Amsterdam of VU Medical Centre.

LxC-001. Auristatin-F-Lx®-trastuzumab, an Lx®-ADC for the treatment of mamma carcinoma metastases with low HER2 expression.

LxL-001. An Lx®-ADC for the treatment of esophageal varices as a consequence of portal hypertension, in cooperation with the Department of Internal Medicine I of the University of Bonn and the Groningen Research Institute of Pharmacy (GRIP).

LxC-002. Auristatin-Lx®-HyB3 for the treatment of non-small cell lung cancer (NSCLC), in cooperation with APO-T (Netherlands) that provided the mAb targeting MAGE, a cancer-specific, MHC-1 expressed peptide present in a variety of cancers.

These products are in their pre-IND phase.

Product Molecule Indication Phase Start
LxT-001 89Zr-DFO-Lx®-trastuzumab targeted PET tracer HER2+ cells Pre-clinical 2014
LxC-001 AF-Lx®-trastuzumab HER2+ metastatic breast cancer Pre-IND 2014
LxL-001 Lx®-R1 Liver disease Pre-IND 2017
LxC-002 AF-Lx®-HyB3 NSCLC Pre-IND 2015

The LinXis Semifinal drug-Lx® products

Product portfolio also includes stable, water-soluble semi-final drug-Lx® ligands that comply with shelf life requirements and are used for ADC production and development purposes, for instance Lx-auristatin F and others.