Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM in PBMC cell. It is an antiviral drug for the treatment of HIV infection. Emtricitabine has in vitro activity against both laboratory strains of HIV-1 and HIV-2 and clinical isolates of HIV-1. The 50% effective concentration (EC50) ranges from 0.002 to 1.5 µ mol/L, depending on the viral isolate and cell line used. Emtricitabine demonstrates in vitro synergy with zidovudine and stavudine and additive in vitro activity when combines with zalcitabine or didanosine[3]. Oral doses up to 1000 mg/kg/day provided daily area under the curve (AUC0→24) exposure to pregnant animals approximately 60- (mice) to 120-fold (rabbits) higher than that in humans at the recommended dose of 200 mg given once per day. In a mouse fertility study, emtricitabine had no effect on fertility, sperm count, or early embryonic development. There is no increased incidence of malformations in mouse and rabbit embryofetal toxicology studies. The development and fertility of F1 progeny are unaffected by emtricitabine in a mouse pre- and post-natal study. These data demonstrate a favorable pre-clinical reproductive safety profile for emtricitabine[4].
Emtricitabine 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
HeLa P4/R5 cells
Function assay
Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=0.17 μM
19596885
HepAD38 cell
Function assay
Inhibition of hepatitis B virus replication in the HepAD38 cell line, ED50=0.03 μM
11128652
HepG2 cells
Cytotoxicity assay
9 days
Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=27.7 μM
17888662
MDCK2 cells
10 μM
Function assay
Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay
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