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标题: Ciclofilin制药应邀在剑桥大学Healthtech研究所的第十一届年会药 [打印本页]

作者: StephenW 时间: 2016-4-20 10:48 标题: Ciclofilin制药应邀在剑桥大学Healthtech研究所的第十一届年会药

Ciclofilin Pharmaceuticals Invited to Present Hepatitis B Drug Data at Cambridge Healthtech Institute’s Eleventh Annual Drug Discovery Chemistry Conference

                        Tuesday, April 19, 2016 1:00 PM UTC

SAN DIEGO, April 19, 2016 -- Ciclofilin Pharmaceuticals Inc. ("Ciclofilin" or the "Company"), a privately held biotech, announced today that it will discuss important new data for its cyclophilin inhibitor, CPI-431-32, during a presentation at the Cambridge Healthtech Institute’s Eleventh Annual Drug Discovery Chemistry Conference to be held April 19-22, 2016 at the Hilton San Diego Resort in San Diego, CA. CPI-431-32 is Ciclofilin’s lead drug candidate for the treatment of hepatitis B virus (“HBV”) infection.

  Ciclofilin’s CEO, Robert T. Foster, PharmD, PhD, will present findings that demonstrate CPI-431-32 is a best-in-class host-targeting antiviral drug. To date, CPI-431-32 in vitro completely suppresses HBsAg, suppresses HBeAg, and suppresses intracellular HBV DNA by greater than 90%, while also inhibiting viral uptake by blocking NTCP transporter activity. CPI-431-32 also reduces HBV DNA in the HBV1.3 transgenic mouse model. In contrast to other cyclophilin inhibitors, CPI-431-32 demonstrated a wide selective index (“SI”) as measured by the toxicity:efficacy ratio (CC50:IC50), which is sufficient for clinical development in HBV.
  “We have almost three decades worth of experience in cyclosporine chemistry.  Drawing upon this experience in structure-activity relationships, we have learned that relatively small and selective changes to the chemical structure of the cyclosporine backbone can have very dramatic consequences in pharmacology,” commented Dr. Foster. “With that in mind, we have discovered a compound that has demonstrated a significant shift in both the efficacy against the hepatitis B virus and cytotoxicity profiles in a way that provides for a clear and meaningful separation of these two properties.  This degree of separation, known as selective index, is something we have not seen with other known cyclophilin inhibitors, making CPI-431-32 extremely unique and compelling.”
  About Ciclofilin:
Ciclofilin is a privately held life sciences company based in San Diego, California, with R&D facilities in Edmonton, Canada. The company's lead oral drug candidate, CPI-431-32, is being developed as a treatment for chronic HBV infection. CPI-431-32 interferes with the ability of the HBV to infect cells, propagate, and cause disease primarily by preventing HBV interaction with host cell cyclophilins. CPI-431-32 also demonstrates anti-fibrotic activity in the liver, and may offer clinical benefits to patients in addition to anti-HBV activity.  CPI-431-32 has a wide selective index, allowing for HBV clinical development

作者: StephenW 时间: 2016-4-20 10:48

Ciclofilin制药应邀在剑桥大学Healthtech研究所的第十一届年会药物发现化学会议将出席乙肝药物数据

周二，2016年4月19日下午1:00 UTC

圣迭戈，2016年4月19日 - Ciclofilin制药公司（“Ciclofilin”或“公司”），一家私人持有的生物科技，今天宣布，将讨论新的重要数据，其亲环蛋白抑制剂，CPI-431-32，期间在剑桥Healthtech研究所的第十一届年会药物发现化学大会介绍到在希尔顿圣地亚哥度假村加利福尼亚州圣迭戈举行的2016年4月19-22日， CPI-431-32是Ciclofilin对乙型肝炎病毒（“乙肝”）感染的治疗铅候选药物。

Ciclofilin的CEO，罗伯特·福斯特T.药学博士，博士，将目前演示CPI-431-32是最好的一流的主机靶向抗病毒药物的发现。迄今为止，CPI-431-32体外完全抑制HBsAg和抑制HBeAg的，并且抑制由大于90％的细胞内HBV-DNA的同时，也通过阻断NTCP转运蛋白活性抑制病毒的摄取。 CPI-431-32也减少了HBV1.3全长转基因小鼠模型的HBV DNA。与其它亲环蛋白抑制剂，CPI-431-32表现出广泛选择指数由毒性测定（“SI”）：功效比（CC 50：IC 50），这是足够用于HBV的临床开发。

“我们有将近三十年的价值环孢素化学经验。在吸取的构效关系这方面的经验，我们了解到的环孢素骨干的化学结构相对较小，选择性的变化可以在药理学有非常严重的后果，“福斯特博士说。 “考虑到这一点，我们已经发现，已经证明在两个对中，提供了这两个属性的一个明确的和有意义的分离的一种方式的乙型肝炎病毒和细胞毒性型材功效的显著转变的化合物。这种程度的分离，被称为选择指数，是我们还没有与其他已知的亲环蛋白抑制剂看出，使得CPI-431-32非常独特而富有吸引力“。

关于Ciclofilin：
Ciclofilin是总部设在加利福尼亚州圣迭戈一家私人持有的生命科学公司，在加拿大埃德蒙顿的研发设施。公司的主导口服候选药物，CPI-431-32，正在发展为慢性HBV感染治疗。 CPI-431-32干扰了乙肝病毒的通过防止与宿主细胞亲环HBV的相互作用主要感染细胞，传播和引起疾病的能力。 CPI-431-32也显示在肝脏抗纤维化活性，并且可以提供除了抗HBV活性的患者的临床益处。 CPI-431-32具有广泛的选择性指标，允许乙肝临床开发

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