Off-Target Screening of Biotherapeutics

Biotherapeutics cross-reactivity

Toxicity due to off-target binding is a leading cause of failure in drug development. Retrogenix’s Cell Microarray screening can provide an understanding of the off-target binding potential of novel biologic drug leads during discovery and early development. Building a picture of the ‘toxic liability’ of a candidate drug helps reduce risk through more informed safety assessment and can save considerable time and resources by allowing bad drugs to fail earlier. Retrogenix’s off target screening data has been used in regulatory submissions for clinical studies.


Retrogenix off target profiling:

  • Identifies specific plasma membrane off-targets
  • Provides supporting information for IND regulatory submissions
  • Is highly specific with very low numbers of false positives/negatives
  • Complements tissue cross reactivity (TCR) and immunohistochemistry studies
  • Can predict/explain reduced bioavailability due to off-target binding
  • Can inform pre-clinical tox model selection, reducing animal testing
  • Helps prioritise drug leads or avoid off-target activities in next-generation of molecules

Low false positive rate

Our highly specific screen typically reports one or two confirmed interactions rather than 100s of erroneous results that can often be seen with protein microarrays. This saves months of validation work and avoids unnecessary investigations that could stall progress with regulatory submissions.

Please contact us to discuss an off-target project.

Screen for off-targets of:

  • Antibodies & bispecifics
  • ADCs
  • ScFvs, Fabs or antibody derivatives
  • whole CAR T cells
  • Peptides
  • Protein ligands
  • Labelled small molecules

“Specificity screening of antibodies and related molecules using human cell microarray technology.”

Download our poster, presented at PEGS 2017, which describes how the cell microarray approach is being applied to identify specific and relevant off-targets with a very low rate of false positive results.

Download poster


FAQ: “What is the sensitivity of the Cell Microarray technology?”

Ligand-receptor interactions of around 10 micromolar can be detected in the absence of any amplification strategy. This is more than adequate for most studies, however, amplification strategies can be employed when needed in order to detect lower affinity interactions.

See more FAQs

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The University of Sheffield
Aveo Oncology - The Human Response
Theraclone Sciences
Bluebird Bio
The Center for Infectious Disease Research
Compugen Logo
The University of Copenhagen
Lund University
NIH - National Institutes of Health
The University of Pennsylvania
Scripps Florida - The Scripps Research Institute
Peptinnovate Ltd - Unlocking Nature's Potential
We are very pleased with the service Retrogenix provided to us. In less than two months they were able to identify and confirm the target specificity of multiple antibodies we provided to Retrogenix (over 70% of antibodies provided).This helped us to validate our internal technology development.
Head of Antibody Discovery, Bayer