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标题: ContraVir制药公司宣布TXL™优化配方的数据 [打印本页]

作者: StephenW    时间: 2018-6-22 12:54     标题: ContraVir制药公司宣布TXL™优化配方的数据

ContraVir Pharmaceuticals Announces Data on Optimized Formulation of TXL™
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June 21, 2018 08:00 ET | Source: ContraVir Pharmaceuticals Inc.

EDISON, N.J., June 21, 2018 (GLOBE NEWSWIRE) -- ContraVir Pharmaceuticals, Inc. (NASDAQ:CTRV), a biopharmaceutical company focused on the development and commercialization of therapeutic drugs for the treatment of hepatitis B virus (HBV), announced today the company has chosen an optimized formulation of tenofovir exalidex (TXL™) and is ready to initiate dosing HBV patients in a dose-range finding study with the optimized formulation.

TXL™ has been designed to target the liver to deliver the active drug to the reservoir where the hepatitis B virus resides. TXL™ displayed a favorable safety and tolerability profile in a completed Phase 2a study of HBV patients at doses up to 100 mg. The Phase 2a study confirmed that TXL™ administration resulted in lower circulating levels of tenofovir (TFV), compared with levels observed after administration of Viread® (tenofovir disoproxil fumarate, TDF).  Higher circulating levels of TFV, associated with TDF, have previously been shown to cause kidney and bone toxicities. Importantly, TXL™ dosing reduced viremia (HBV DNA) to the same extent as TDF, while minimizing TFV levels associated with these well-known toxicities.

ContraVir undertook studies to optimize the formulation of TXL™ to allow for more efficient, predictable, and precise delivery to the target organ (i.e., liver), thereby potentially reducing drug burden while maintaining consistent efficacy. The optimization of TXL™ was additionally designed to diminish the impact of physiological variables allowing for more consistent delivery of the prodrug to the site of action. Consistent and predictable target organ delivery is necessary, especially as curative combination regimens are developed for a functional cure.

“The ultimate goal in enhancing drug formulation is to offer a potential therapeutic benefit that could allow for more precise and predictive dosing while remaining safe and well tolerated,” said James Sapirstein, Chief Executive Officer of ContraVir. “With future fixed-dose combinations in mind and positioning TXL™ as part of the backbone therapy, our goal was to further enhance the delivery of TXL™ to the liver, and ultimately achieve better results when testing TXL™ in combination with other agents active against HBV, including CRV431, our second investigational compound. We believe that with the current findings of TXL™ showing no food effect and no need for dosing adjustment in patients with decreased renal function, TXL™ has the potential to be the tenofovir of choice.”

The objective of the next clinical trial with TXL™ will be to characterize the pharmacokinetic profile of the new formulation in HBV patients, and to select the target dose to be advanced into a Phase 3 registration clinical development program.  

About ContraVir Pharmaceuticals
ContraVir is a biopharmaceutical company focused on the development and commercialization of targeted antiviral therapies with a specific focus on developing a potentially curative therapy for hepatitis B virus (HBV). The company is developing two novel anti-HBV compounds with complementary mechanisms of action. TXL™, a nucleoside analog lipid prodrug of tenofovir (TFV), is designed to deliver higher hepatic intracellular concentrations of the active tenofovir species (tenofovir diphosphate) while reducing concentrations of tenofovir outside the liver, causing fewer off-target toxicities and side-effects. CRV431, the other anti-HBV compound, is a next-generation cyclophilin inhibitor with a novel structure that increases its potency and selective index against HBV. In vitro and in vivo studies have thus far demonstrated that CRV431 reduces HBV DNA and other viral proteins, including surface antigen (HBsAg). For more information visit www.contravir.com.
作者: StephenW    时间: 2018-6-22 12:54

ContraVir制药公司宣布TXL™优化配方的数据
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2018年6月21日08:00 ET |来源:ContraVir制药公司

新泽西州艾迪逊,2018年6月21日电(GLOBE NEWSWIRE) - 一家专注于治疗乙型肝炎病毒(HBV)治疗药物开发和商业化的生物制药公司ContraVir Pharmaceuticals,Inc.(NASDAQ:CTRV)今天宣布,该公司选择了替诺福韦exalidex(TXL™)的优化配方,并准备在优化配方的剂量范围调查研究中开始给予HBV患者剂量。

TXL™的设计目标是让肝脏将活性药物输送到乙型肝炎病毒所在的水库。在剂量高达100mg的HBV患者完成的2a期研究中,TXL™显示出良好的安全性和耐受性。 2a期研究证实,TXL™给药导致替诺福韦(TFV)的循环水平较给药Viread®(替诺福韦二吡呋酯富马酸盐,TDF)后观察到的水平低。先前已经显示与TDF相关的更高的TFV循环水平导致肾和骨毒性。重要的是,TXL™给药减少病毒血症(HBV DNA)达到与TDF相同的程度,同时最小化与这些众所周知的毒性相关的TFV水平。

ContraVir进行了研究以优化TXL TM的配方,以允许更有效,可预测和精确递送至目标器官(即肝脏),由此潜在地减少药物负担,同时保持一致的效力。 TXL™的优化还旨在减少生理变量的影响,从而使前药更加一致地输送到作用部位。一致和可预测的靶器官输送是必要的,特别是当治疗性联合用药方案被开发用于功能性治疗时。

“Contravi公司首席执行官James Sapirstein表示:”增强药物制剂的最终目标是提供潜在的治疗益处,可以提供更精确,更有预见性的剂量,同时保持安全且耐受性良好。 “考虑到未来的固定剂量组合,并将TXL™作为骨干治疗的一部分,我们的目标是进一步加强TXL™向肝脏的转运,并最终在测试TXL™与其他药物联合使用时获得更好的结果对抗HBV,包括我们的第二个研究化合物CRV431。我们相信,根据目前TXL™的研究结果显示,没有食物影响,并且肾功能下降的患者不需要调整剂量,TXL™有可能成为替诺福韦的首选。“

下一个使用TXL™的临床试验的目的是描述HBV制剂中新制剂的药代动力学特征,并选择进入第三期临床开发项目的目标剂量。

关于ContraVir制药公司
ContraVir是一家生物制药公司,专注于针对性抗病毒治疗的开发和商业化,并专门致力于开发针对乙肝病毒(HBV)的潜在治愈性治疗。该公司正在开发两种具有互补作用机制的新型抗HBV化合物。 TXL™是替诺福韦(TFV)的核苷类似物脂质前药,旨在提供更高的肝细胞内浓度的活性替诺福韦物质(替诺福韦二磷酸盐),同时降低肝脏外替诺福韦的浓度,导致更少的脱靶毒性和副作用。另一种抗-HBV化合物CRV431是新一代亲环蛋白抑制剂,具有增强其对HBV的效力和选择性指标的新结构。迄今为止,体外和体内研究已经证明CRV431减少了HBV DNA和其他病毒蛋白,包括表面抗原(HBsAg)。欲了解更多信息,请访问www.contravir.com

作者: 灵魂不屈    时间: 2018-6-23 08:37

不知道这两种药联合用药效果如何,希望能治愈。
作者: 齐欢畅    时间: 2018-6-23 19:25

灵魂不屈 发表于 2018-6-23 08:37
不知道这两种药联合用药效果如何,希望能治愈。

应该会考虑联用。效果比但用肯定要好。
作者: 默然10    时间: 2018-6-25 08:58

药物是越来越先进了。祝愿早日能面向市场投入使用。




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