4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide

Product Name4-fluoro-3-((4-hydroxypiperidin-1-yl)sulfonyl)-N-(3,4,5-trifluorophenyl)benzamide
CAS1445790-55-5
MFC18H16F4N2O4S
MW432.39
EINECS
MOL File1445790-55-5.mol

Chemical Properties

solubility	DMSO: Soluble: =10 mg/mL Ethanol: Soluble: =10 mg/mL
form	Solid
color	White to off-white

Usage And Synthesis

Description

NVR 3-778 is the first capsid assembly modulator (CAM) that has demonstrated antiviral activity in hepatitis B virus (HBV)-infected patients. NVR 3-778 inhibited the generation of infectious HBV DNA-containing virus particles with a mean antiviral 50% effective concentration (EC50) of 0.40μM in HepG2.2.15 cells. The antiviral profile of NVR 3-778 indicates pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication.

Uses

NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity[1].

in vivo

NVR 3-778 (1.5mg/kg; i.g.) displays the mean C_max and AUC_0–inf values of 0.56μg/ml and 3.50μg·h/ml, respectively, in dogs following oral administration. And the mean oral bioavailability is determined to be 84.6%^[1].

Animal Model:	Dogs^[1]
Dosage:	1.5mg/kg (Pharmacokinetic Analysis)
Administration:	Oral gavage
Result:	The mean C_max and AUC_0–inf values are 0.56μg/ml and 3.50μg·h/ml and the oral bioavailability is 84.6%.

References

[1] Lam AM, et al. Preclinical Characterization of NVR 3-778, a First-in-Class Capsid Assembly Modulator against Hepatitis B Virus. Antimicrob Agents Chemother. 2018 Dec 21;63(1). DOI:10.1128/AAC.01734-18
[2] KLAUS KLUMPP . Efficacy of NVR 3-778, Alone and In Combination With Pegylated Interferon, vs Entecavir In uPA/SCID Mice With Humanized Livers and HBV Infection[J]. Gastroenterology, 2018, 154 3: Pages 652-662.e8. DOI: 10.1053/j.gastro.2017.10.017