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Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474
Open accessAbstract
A clue to a drug's neurotoxicity?: The drug BIA 10-2474 inhibits fatty acid amide hydrolase (FAAH), a lipase that degrades a specific endocannabinoid. On the basis of this activity, BIA 10-2474 was being developed as a potential treatment for anxiety and pain. In a phase 1 trial of the drug, one subject died, and four others suffered brain damage. As an initial step in investigating whether inhibition of off-target proteins by BIA 10-2474 might contribute to its clinical neurotoxicity, van Esbroeck et al. used activity-based proteomic assays to identify proteins targeted by the drug. Studying human cells and brain samples from subjects not associated with the trial, they found that BIA 10-2474 targeted several different lipases in addition to FAAH. It also substantially altered lipid metabolism in cultured neurons. Science , this issue p. 1084
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“During the period of its suspension, it was revealed that these problems were due to off-target effects of this agent that led to alterations in lipid networks in the cortexeffects which were not observed in more specific FAAH inhibitors (van Esbroeck et al., 2017).”
From Novel pharmacological targets in drug development for the treatment of anxiety and anxiety-related disorders (2019) · cites this paper as van Esbroeck et al., 2017
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“In light of the death and adverse events in other subjects given repeated high doses of the FAAH inhibitor BIA-102474-101 in a clinical trial (Kerbrat et al, 2016), it is crucial to note that this drug has multitude of off-targets, including inhibition of essential blood-clotting factors thrombin and Factor VII (van Esbroeck et al, 2017;Molinski et al, 2017), which may contributed to its toxicity.”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as van Esbroeck et al, 2017
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Metadata
- Authors
- van Esbroeck, A. C. M., Janssen, A. P. A., Cognetta, A. B., Ogasawara, D., Shpak, G., van der Kroeg, M., Kantae, V., Baggelaar, M. P., de Vrij, F. M. S., Deng, H., Allarà, M., Fezza, F., Lin, Z., van der Wel, T., Soethoudt, M., Mock, E. D., den Dulk, H., Baak, I. L., Florea, B. I., Hendriks, G., De Petrocellis, L., Overkleeft, H. S., Hankemeier, T., De Zeeuw, C. I., Di Marzo, V., Maccarrone, M., Cravatt, B. F., Kushner, S. A., & van der Stelt, M.
- Affiliations
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC, Leiden, Netherlands.
- Leiden University (NL)
- Scripps Research Institute (US)
- Erasmus MC (NL)
- Department of Psychiatry, Erasmus University Medical Centre, 3000 CA, Rotterdam, Netherlands.
- Istituto di Chimica Biomolecolare (IT)
- University of Rome Tor Vergata (IT)
- Toxys B.V., Robert Boyleweg 4, 2333 CG, Leiden, Netherlands.
- Endocannabinoid Research Group, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche (CNR), Via Campi Flegrei 34, Comprensorio Olivetti, 80078 Pozzuoli, Italy.
- Department of Neuroscience, Erasmus Medical Centre, 3000 CA, Rotterdam, Netherlands.
- Università Campus Bio-Medico (IT)
- Corresponding author
- Janssen, Antonius P. A.
- Cognetta, Armand B.
- Ogasawara, Daisuke
- Kushner, Steven A.
- ORCID
- van Esbroeck, Annelot C. M.
- Janssen, Antonius P. A.
- Cognetta, Armand B.
- Ogasawara, Daisuke
- Shpak, Guy
- van der Kroeg, Mark
- Kantae, Vasudev
- Baggelaar, Marc P.
- Deng, Hui
- Allarà, Marco
- Fezza, Filomena
- Lin, Zhanmin
- van der Wel, Tom
- Soethoudt, Marjolein
- Mock, Elliot D.
- den Dulk, Hans
- Baak, Ilse L.
- Florea, Bogdan I.
- Hendriks, Giel
- De Petrocellis, Luciano
- Overkleeft, Herman S.
- Hankemeier, Thomas
- Di Marzo, Vincenzo
- Maccarrone, Mauro
- Cravatt, Benjamin F.
- Kushner, Steven A.
- van der Stelt, Mario
- Venue
- Science
- Published
- 2017-06-09
- Volume
- 356
- Issue
- 6342
- Pages
- 1084-1087
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- PMC
- PMC5641481
- OpenAlex
- W2621737540
- Cited by
- 332
- References
- 40
- Citations by year
- 2026: 23 · 2025: 20 · 2024: 33 · 2023: 25 · 2022: 27 · 2021: 33 · 2020: 63 · 2019: 50 · 2018: 47 · 2017: 10
- FWCI
- 32.45
- Type
- journal article
- Language
- en
- Open access
- green
- pure.eur.nl
- Licence
- other-oa
- Locations
- Science (publishedVersion)
- PubMed (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (publishedVersion, other-oa)
- KNAW Research Portal (The Royal Netherlands Academy of Arts and Sciences) (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Leiden Repository (Leiden University) (submittedVersion, other-oa)
- Data Archiving and Networked Services (DANS) (submittedVersion, other-oa)
- EUR Research Repository (Erasmus University Rotterdam) (submittedVersion, other-oa)
- RePub (Erasmus University Rotterdam) (submittedVersion, other-oa)
- Data Archiving and Networked Services (DANS) (submittedVersion)
- Cineca Institutional Research Information System (Tor Vergata University) (submittedVersion)
- Leiden Repository (Leiden University) (submittedVersion)
- RePub (Erasmus University Rotterdam) (submittedVersion)
- Archivio Istituzionale della Ricerca - Università degli Studi dell Aquila (submittedVersion)
- Funders
- National Institutes of Health (award304469, DA033760)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
- Keywords
- FAAH inhibitors, off-target effects, lipase inhibition, neurotoxicity, activity-based protein profiling, fatty acid amide hydrolase, lipid metabolism, cortical neurons, drug safety
- MeSH terms
- Fatty Acid Amide Hydrolases, Amidohydrolases, Analgesics, Cross Reactions, Cyclic N-Oxides, Humans, Neurons, Pyridazines, Pyridines, Anti-Anxiety Agents, Urea, Clinical Trials, Phase I as Topic, Cell Line, Tumor, Protein Interaction Maps
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