PF-3052334(PF-3052334) - 药物靶点：HMG-CoA reductase_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

HMG-CoA reductase

作用机制

HMG-CoA reductase抑制剂(羟甲基戊二酰辅酶A合酶抑制剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

动脉粥样硬化

原研机构

Pfizer Inc.

在研机构-

非在研机构

Pfizer Inc.

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C28H34FN3NaO5

InChIKeyLYNATEDRTJYGMU-OHIDFYLOSA-N

CAS号887702-61-6

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关联

100 项与 PF-3052334 相关的临床结果

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100 项与 PF-3052334 相关的转化医学

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100 项与 PF-3052334 相关的专利（医药）

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1

项与 PF-3052334 相关的文献（医药）

2011-05-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: A bench-to-bedside case study on tissue selective drug distribution

4区 · 医学

Article

作者: Carine Boustany ; Mark R. Bush ; Richard Hutchings ; Mark Kowala ; Noe Erasga ; Jeffrey A. Pfefferkorn ; Emi Kimoto ; John Litchfield ; Ayman El-Kattan ; Andrew Robertson ; Renato Scialis ; David B. Duignan ; Rebecca Bakker-Arkema ; Theunis C. Goosen ; Gina Lu ; Catherine Sekerke ; Bruce Auerbach ; Zhiwu Lin ; Lisa Dillon ; Bradley D. Tait ; Paul Barclay ; Mark Milad ; Scott D. Larsen ; Vaishali Sahasrabudhe ; Erick Kindt ; Bo Feng ; Karen Atkinson ; Xue Min Cheng ; David C. Boyles ; Yurong Lai ; Jaap W. Mandema ; Robert Kennedy ; Bharat K. Trivedi ; Jeffrey C. Hanselman ; Karl Olsen ; Daniel M. Bowles ; Vu Le ; Chitase Lee ; Jonathan Chupka ; Yi An Bi ; Valerie Askew

The design of drugs with selective tissue distribution can be an effective strategy for enhancing efficacy and safety, but understanding the translation of preclinical tissue distribution data to the clinic remains an important challenge. As part of a discovery program to identify next generation liver selective HMG-CoA reductase inhibitors we report the identification of (3R,5R)-7-(4-((3-fluorobenzyl)carbamoyl)-5-cyclopropyl-2-(4-fluorophenyl)-1H-imidazol-1-yl)-3,5-dihydroxyheptanoic acid (26) as a candidate for treating hypercholesterlemia. Clinical evaluation of 26 (PF-03491165), as well as the previously reported 2 (PF-03052334), provided an opportunity for a case study comparison of the preclinical and clinical pharmacokinetics as well as pharmacodynamics of tissue targeted HMG-CoA reductase inhibitors.

100 项与 PF-3052334 相关的药物交易

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