JNJ-42165279

JNJ-42165279 is a drug developed by Janssen Pharmaceutica which acts as a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 70 nM.[1] It is described as a covalently binding but slowly reversible selective inhibitor of FAAH.[2] JNJ-42165279 is being developed for the treatment of anxiety disorders and major depressive disorder. Clinical development has progressed as far as Phase II human trials with two studies in patients with mood disorders registered in ClinicalTrials.gov.[3][4]

JNJ-42165279
Clinical data
ATC code
  • None
Legal status
Legal status
Identifiers
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC18H17ClF2N4O3
Molar mass410.802 g/mol g·mol−1
3D model (JSmol)

In early 2016, a trial with a different FAAH inhibitor — Bial's BIA 10-2474 — resulted in a series of severe adverse events, including a death. In response, Janssen announced that it was temporarily suspending dosing in its two Phase II clinical trials with JNJ-42165279, describing the decision as "precautionary measure follows safety issue with different drug in class". Janssen was emphatic that no serious adverse events had been reported in any of the clinical trials with JNJ-42165279 to date. The suspension is to remain in effect until more information is available about the BIA 10-2474 study.[5] As of 2018, the trials had resumed.[6]

See also

References
  1. Keith, John M.; Jones, William M.; Tichenor, Mark; Liu, Jing; Seierstad, Mark; Palmer, James A.; Webb, Michael; Karbarz, Mark; Scott, Brian P.; Wilson, Sandy J.; Luo, Lin; Wennerholm, Michelle L.; Chang, Leon; Rizzolio, Michele; Rynberg, Raymond; Chaplan, Sandra R.; Breitenbucher, J. Guy (2015). "Preclinical Characterization of the FAAH Inhibitor JNJ-42165279". ACS Medicinal Chemistry Letters. 6 (12): 1204. doi:10.1021/acsmedchemlett.5b00353. PMC 4677372. PMID 26713105.
  2. JNJ-42165279: selective and slowly reversible FAAH inhibitor. Central and Peripheral PK/PD.
  3. "A Safety and Efficacy Study of JNJ-42165279 in Participants With Social Anxiety Disorder (NCT02432703)". ClinicalTrials.gov Registry. 29 April 2015. Retrieved 21 January 2016.
  4. "An Efficacy, Safety and Tolerability Study of JNJ-42165279 in Participants With Major Depressive Disorder With Anxious Distress (NCT02498392)". ClinicalTrials.gov Registry. 13 July 2015. Retrieved 21 January 2016.
  5. "Janssen Research & Development, LLC Voluntarily Suspends Dosing in Phase 2 Clinical Trials of Experimental Treatment for Mood Disorders". Janssen.com. 17 January 2016. Retrieved 21 January 2016.
  6. Postnov, Andrey; Schmidt, Mark E.; Pemberton, Darrel J.; de Hoon, Jan; van Hecken, Anne; van den Boer, Maarten; Zannikos, Peter; van der Ark, Peter; Palmer, James A.; Rassnick, Stef; Celen, Sofie; Bormans, Guy; van Laere, Koen (2018). "Fatty Acid Amide Hydrolase Inhibition by JNJ-42165279: A Multiple-Ascending Dose and a Positron Emission Tomography Study in Healthy Volunteers". Clinical and Translational Science. 11 (4): 397–404. doi:10.1111/cts.12548. ISSN 1752-8054. PMC 6039207.



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