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Redafamdastat

From Wikipedia, the free encyclopedia
Redafamdastat
Clinical data
Other namesJZP-150; JZP150; PF-04457845; PF-4457845; PF04457845; PF4457845
Routes of
administration
By mouth
ATC code
  • None
Legal status
Legal status
Pharmacokinetic data
MetabolismCY3A4
Identifiers
  • N-pyridazin-3-yl-4-[(3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl)methylidene]piperidine-1-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H20F3N5O2
Molar mass455.441 g·mol−1
3D model (JSmol)
  • n4ncccc4NC(=O)N(CC3)CC\C3=C/c2cc(ccc2)Oc(cc1)ncc1C(F)(F)F
  • InChI=1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32)
  • Key:BATCTBJIJJEPHM-UHFFFAOYSA-N

Redafamdastat (INNTooltip International Nonproprietary Name; developmental code names JZP-150, PF-04457845) is an inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50Tooltip half-maximal inhibitory concentration of 7.2 nM, and both analgesic and anti-inflammatory effects in animal studies comparable to those of the cyclooxygenase inhibitor naproxen.[1] It was being developed by Jazz Pharmaceuticals for the treatment of alcoholism, pain, and post-traumatic stress disorder (PTSD) and reached phase 2 clinical trials.[2][3] However, development of the drug was discontinued in December 2023.[2]

See also

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References

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  1. ^ Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, et al. (February 2011). "Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor". ACS Medicinal Chemistry Letters. 2 (2): 91–96. doi:10.1021/ml100190t. PMC 3109749. PMID 21666860.
  2. ^ a b "JZP 150". AdisInsight. 26 December 2023. Retrieved 16 August 2024.
  3. ^ "A Study of JZP150 in Adults With Posttraumatic Stress Disorder - Full Text View - ClinicalTrials.gov". clinicaltrials.gov.