Introduction: Besifovir (LB80380) is a relatively new oral acyclic nucleotide phosphonate. We reviewed the pharmacokinetic characteristics of LB80380 and discussed its role in the treatment of chronic hepatitis B infection.
Areas covered: LB80380 is a prodrug of LB80331 and LB80317. It is rapidly absorbed when taken orally. Escalating doses of besifovir produce linear increase of the plasma concentration. Doses above 60mg are effective for inhibiting HBV in human. Using 60mg as an example, the maximal concentration of LB80331 in plasma is 397 ng/mL. The time required to reach maximal concentration in plasma and elimination half-life are 2.0 and 3.0 h, respectively. Besifovir and its metabolites are mainly excreted via the kidneys. Its antiviral efficacy is non-inferior to ETV 0.5mg daily. It is generally safe in terms of renal and bone toxicity. The most common adverse event is carnitine depletion which affects almost all patients on besifovir requiring carnitine supplementation.
Expert opinion: Besifovir demonstrated predictable pharmacokinetic characteristics in human subjects. Few clinical studies on besifovir have been conducted. More data are expected particularly for special populations. The adverse events upon long term exposure should be monitored. Large scale head-to-head trials comparing besifovir with existing NA, especially tenofovir alafenamide, should be conducted. 相似文献
目的探讨玉蓝降糖联合二甲双胍治疗2型糖尿病患者的有效性和安全性。方法选取河北省第七人民医院2015年12月—2016年12月收治的2型糖尿病患者125例,随机分成对照组(62例)和治疗组(63例)。对照组患者口服盐酸二甲双胍片,2片/次,2次/d,根据病情适当调整剂量。治疗组在对照组基础上口服玉蓝降糖胶囊,4粒/次,3次/d。所有患者均治疗3个月。观察两组患者临床疗效,比较治疗前后两组患者空腹血糖(FPG)、餐后2 h血糖(2 h PG)和糖化血红蛋白(Hb A1c)以及临床指标水平和不良反应情况。结果治疗后,对照组临床总有效率为82.26%,显著低于治疗组的96.83%,两组比较差异具有统计学意义(P0.05)。治疗后,两组患者血清FPG、2 h PG和Hb A1c水平显著降低(P0.05);且治疗组患者FPG、2 h PG和Hb A1c水平明显低于对照组(P0.05)。治疗后,两组患者BMI指数、收缩压(SBP)、尿酸(UA)和三酰甘油(TG)水平均显著降低(P0.05);且治疗组患者各指标改善情况均要明显低于对照组(P0.05)。治疗期间,对照组不良反应发生率为19.35%,明显高于治疗组的4.76%,两组比较差异具有统计学意义(P0.05)。结论玉蓝降糖联合二甲双胍治疗2型糖尿病疗效好,安全性高,具有一定的临床推广应用价值。 相似文献