A multicenter, open-label study was performed to evaluate the safety, anti-hepatitis B virus (anti-HBV) activity, and pharmacokinetics of emtricitabine therapy administered once daily for 8 weeks to patients infected with HBV. Clinical and virologic evaluations were completed at the baseline; at 7, 14, 28, 42, and 56 days during treatment; and at 24, 48, and 28 days posttreatment. Forty-nine patients were enrolled in five dose cohorts (doses of 25, 50, 100, 200, and 300 mg, all of which were administered once daily [q.d.]). Peak plasma emtricitabine concentrations occurred within 1.5 h following dosing. Plasma emtricitabine concentrations (maximum concentrations of drug in plasma and areas under the concentration-time curves) increased nearly dose proportionally over the 25-to 300-mg dose range, with relatively small intersubject variabilities. The plasma half-life of emtricitabine ranged from 6 to 9 h. HBV DNA levels were measured by the Digene HBV Hybrid Capture II assay. Viral suppression (reduction in log 10 serum HBV DNA levels) occurred in all dose cohorts. All doses demonstrated potent and rapid antiviral activities, with a trend toward a greater suppression with daily doses of 100 mg or greater. At 2 months, the median change in the serum HBV DNA level from the baseline level ranged from ؊1.7 log 10 for the 25-mg dose administered q.d. to ؊3.3 log 10 for the 300 mg dose administered q.d. Emtricitabine was well tolerated over the 2-month dosing period. These results support further clinical development of emtricitabine for the treatment of chronic hepatitis B infection.Chronic hepatitis B virus (HBV) infection is a common and often severe form of liver disease that affects approximately 1 million Americans and 350 million people worldwide (4,8,14). In addition to treatment with alpha interferon, major therapeutic advances have occurred with the discovery of new antiviral compounds that inhibit the reverse transcriptase activity of HBV DNA polymerase. Recently, lamivudine (3TC) has been approved for use in the treatment of chronic HBV infection. However, prolonged monotherapy with 3TC selects for resistance mutations at rates varying from 16 to 32% at 1 year in immune competent patients (4,5,7,12,13). Therefore, there is a need to develop additional anti-HBV drugs that may be used alone or in combination to alleviate the problem of resistance.Emtricitabine (FTC) is a deoxycytidine analog reverse transcriptase inhibitor that has been demonstrated to have potent and selective inhibitory activities against HBV and human immunodeficiency virus (HIV) (the structure of FTC is illustrated in Fig. 1). FTC is readily anabolized by cellular enzymes stepwise to form its monophosphate, diphosphate, and finally, triphosphate forms. The triphosphate form is the active intracellular moiety that completely inhibits HBV DNA polymerase. The anti-HBV activity of FTC has been demonstrated in a chimeric mouse model and against woodchuck hepatitis virus in naturally infected woodchucks (1, 2).In in vitro assays with HIV, FTC is...
Middle-age adults may be increasingly affected by chlamydia, gonorrhea and infectious syphilis. There is a need for sexual health information targeting Canada's middle-age adults and their health care providers.
Broadband near-infrared (NIR) phosphor-converted light-emitting diodes (pc-LEDs) are essential to integrate near-infrared spectrometers into mobile devices for the rapid and noninvasive detection of biological components. However, efficient broadband NIR phosphors with a peak emission wavelength longer than 800 nm are deficient. In this study, CaMgGe2O6:Cr3+ phosphor was prepared by a high-temperature solid-state reaction. The phosphor doped with 0.02Cr3+ showed an emission band at 845 nm with a broad bandwidth of 160 nm and a high quantum yield of 84% under 450 nm excitation. The broadband NIR pc-LED was fabricated using CaMgGe2O6:0.02Cr3+ phosphor based on a blue light-emitting diode (LED) chip. A photoelectric efficiency of 27.2% @ 10 mA and an NIR output power of 57.98 mW @ 100 mA were achieved, which are the highest values reported yet for broadband NIR pc-LEDs with a peak wavelength longer than 800 nm. Using the fabricated NIR pc-LED as the light source, the characteristic absorption spectra of some substances were obtained. All of the results indicated that the CaMgGe2O6:Cr3+ phosphor has considerable potential in near-infrared spectroscopic applications.
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