JNJ-42165279
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| Formula | C18H17ClF2N4O3 |
| Molar mass | 410.81g·mol−1 |
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JNJ-42165279is a drug developed byJanssen Pharmaceuticawhich acts as a potent and selective inhibitor of the enzymefatty acid amide hydrolase(FAAH), with an IC50of 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 ofanxiety disordersandmajor depressive disorder.Clinical development has progressed as far as Phase II humantrialswith two studies in patients with mood disorders registered inClinicalTrials.gov.[3][4]
In early 2016, a trial with a different FAAH inhibitor —Bial'sBIA 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
[edit]References
[edit]- ^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.PMC4677372.PMID26713105.
- ^"JNJ-42165279: selective and slowly reversible FAAH inhibitor. Central and Peripheral PK/PD"(PDF).Archived fromthe original(PDF)on 2016-01-27.Retrieved2016-01-19.
- ^Clinical trial numberNCT02432703for "A Safety and Efficacy Study of JNJ-42165279 in Participants With Social Anxiety Disorder" atClinicalTrials.gov
- ^Clinical trial numberNCT02498392for "An Efficacy, Safety and Tolerability Study of JNJ-42165279 in Participants With Major Depressive Disorder With Anxious Distress" atClinicalTrials.gov
- ^"Janssen Research & Development, LLC Voluntarily Suspends Dosing in Phase 2 Clinical Trials of Experimental Treatment for Mood Disorders".Janssen.com. 17 January 2016. Archived fromthe originalon 25 January 2016.Retrieved21 January2016.
- ^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.PMC6039207.PMID29575526.
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