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
IUPAC name
  • N-(4-Chloropyridin-3-yl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]piperazine-1-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC18H17ClF2N4O3
Molar mass410.81 g·mol−1
3D model (JSmol)
SMILES
  • c3c1OC(F)(F)Oc1ccc3CN4CCN(CC4)C(=O)Nc2cnccc2Cl
InChI
  • InChI=1S/C18H17ClF2N4O3/c19-13-3-4-22-10-14(13)23-17(26)25-7-5-24(6-8-25)11-12-1-2-15-16(9-12)28-18(20,21)27-15/h1-4,9-10H,5-8,11H2,(H,23,26)
  • Key:YWGYNGCRVZLMCS-UHFFFAOYSA-N

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 JM, Jones WM, Tichenor M, Liu J, Seierstad M, Palmer JA, et al. (December 2015). "Preclinical Characterization of the FAAH Inhibitor JNJ-42165279". ACS Medicinal Chemistry Letters. 6 (12): 1204–8. doi:10.1021/acsmedchemlett.5b00353. PMC 4677372. PMID 26713105.
  2. "JNJ-42165279: selective and slowly reversible FAAH inhibitor. Central and Peripheral PK/PD" (PDF). Archived from the original (PDF) on 2016-01-27. Retrieved 2016-01-19.
  3. Clinical trial number NCT02432703 for "A Safety and Efficacy Study of JNJ-42165279 in Participants With Social Anxiety Disorder" at ClinicalTrials.gov
  4. Clinical trial number NCT02498392 for "An Efficacy, Safety and Tolerability Study of JNJ-42165279 in Participants With Major Depressive Disorder With Anxious Distress" at ClinicalTrials.gov
  5. "Janssen Research & Development, LLC Voluntarily Suspends Dosing in Phase 2 Clinical Trials of Experimental Treatment for Mood Disorders". Janssen.com. 17 January 2016. Archived from the original on 25 January 2016. Retrieved 21 January 2016.
  6. Postnov A, Schmidt ME, Pemberton DJ, de Hoon J, van Hecken A, van den Boer M, et al. (July 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. PMC 6039207. PMID 29575526.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.