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市場調查報告書
腦血管障壁
Blood-Brain Barrier: Bridging Options for Drug Discovery and Development
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腦血管障壁 是由出版商Insight Pharma Reports在2008年05月所出版的。
這份英文市場調查報告書包含100 pages 價格從美金1250起跳。
本報告書內容包括：有效連結腦血管障壁的小分子及大分子藥物開發、設計、研發相關討論、奈米粒子技術應用、企業及學術界專家的意見、未來動向等。內容綱要摘記如下：
第1章 腦血管障壁：中樞神經藥物開發的課題
- 腦血管障壁瓶頸介紹
- 留有高度潛在需求的針對中樞神經疾病的藥
- 為克服腦血管障壁所需的新方針
第2章 腦血管障壁的生理學
- 特殊的腦部微血管成為擴散的障壁
- 為進行腦血管繞道手術的經頭蓋骨給藥
第3章 連結腦血管障壁的小分子藥物開發及設計
- 透過腦内皮細胞的被動擴散連結腦血管障壁
- 為阻止腦血管障壁滲透的流出輸送作用
- 為連結腦血管障壁的媒介傳送利用的小分子藥物設計
- 為評價腦血管障壁藥物滲透狀況的體内方法
- 掌握腦血管障壁滲透狀況的體外方法
- 為促使腦血管障壁滲透的奈米粒子技術利用
第4章 連結腦血管障壁的大分子藥物開發及設計
- 連結腦血管障壁之大分子藥物設計的受體運送方法探索
- 利用倣白喉毒做為腦血管障壁輸送的分子特洛伊木馬
- 利用倣嗜神經病毒糖蛋白類藥劑做為腦血管障壁輸送的分子特洛伊木馬
- 為探索連結腦血管障壁的大分子藥物之其他受體的基礎研究的必要性
第5章 藥物研發及新藥開發之腦血管障壁的課題預測
第6章 專家訪談
第7章 企業介紹
- Amgen
- Cellial Technologies
- GlaxoSmithKline
- Merck & Co.
- MethylGene
- Pfizer
- Wyeth
- XenoPort
附錄
Abstract
Topics covered include:
- Strategies to develop small- and large-mol-ecule CNS drugs capable of
crossing the blood-brain barrier (BBB)
- Interviews with leading researchers who are aggressively tackling the BBB
challenge in CNS drug discovery and development
- Analysis of results from a Blood-Brain Barrier Survey, responded to by a
range of companies involved in CNS research and drug discovery/development
CNS diseases are a major focus of the pharmaceutical industry, with CNS drugs
representing some of its most successful products. These include Pfizer' s
Zoloft (sertraline, for treatment of depression and certain types of anxiety
disorders), Lilly' s Cymbalta (duloxetine, for treatment of depression) and
Bristol-Myers Squibb' s/Otsuka' s Abilify (aripiprazole, for treatment of
bipolar disorder and schizophrenia). However, drug discovery and development
researchers experience difficulty developing CNS drugs that complete clinical
trials and win regulatory approval - especially drugs which meet major unmet
needs in the CNS area, such as Alzheimer' s disease. The vast majority of drugs
fail to cross the BBB, which is causing a major bottleneck in successful
development of CNS drug candidates.
This report reviews the discovery, design and development of small- and
large-molecule drugs that can efficiently cross the BBB. This includes more
traditional, medicinal chemistry-based methods, as well as approaches that
exploit carrier-mediated transport (CMT) and receptor-mediated transport
(RMT). Also covered in the report is use of nanoparticle technology to
enable BBB penetration. Further, the report presents in vitro and in vivo
assays as well as imaging methods to ascertain a drug' s ability to cross the
BBB and reach its target.
The report includes results of a survey of researchers and executives - from
corporate and academic organizations - who are active in the CNS drug
development area. The survey explores their involvement in BBB-related
technologies and programs. The survey results are discussed in terms of what
they reveal about the current state of BBB research and the future potential
for developing drugs that are able to cross it.
Table of Contents
Chapter 1
- THE BLOOD-BRAIN BARRIER: A CHALLENGE FOR CNS DRUG DEVELOPMENT
- 1.1. Introduction to the BBB Bottleneck
- 1.2. Dearth of Drugs for CNS Diseases with High Unmet Need
- Parkinson' s Disease
- Multiple Sclerosis
- 1.3. New Approaches Needed to Overcome the BBB Hurdle
- Tempting New CNS Targets...
- .....Belie an Underserved CNS Drug Market
Chapter 2
- PHYSIOLOGY OF THE BLOOD-BRAIN BARRIER
- 2.1. Specialized Brain Capillaries Present Barriers to Diffusion
- 2.2. Transcranial Delivery of Drugs to Bypass the BBB
Chapter 3
- DISCOVERY & DESIGN OF SMALL-MOLECULE DRUGS THAT CAN CROSS THE
BLOOD-BRAIN BARRIER
- 3.1. Crossing the BBB via Passive Diffusion across the Brain
Endothelium
- The "Rule of Five" for Determining "Drug-Like" Properties
- 3.2. Action of Efflux Transporters in Inhibiting BBB Penetration
- P-Glycoprotein (P-gp)
- Studies of P-gp Polymorphisms in Humans
- Discovery and Design of Drugs That Use Nutrient Transporters to Cross the
BBB
- Solute Carrier Transporters in Active Efflux from the BBB
- 3.3. Design of Small-Molecule Drugs That Use Carrier-Mediated Transport
to Cross the BBB
- Companies Involved in Developing Small-Molecule Drugs That Exploit
Transporter Biology
- 3.4. In Vivo Methods for Evaluating Drug Penetration of the BBB
- Traditional In Vivo Methods for Determining BBB Penetrance
- In Vivo Methods for Determining BBB Penetrance by Use of Imaging
- Positron Emission Tomography (PET)
- Magnetic Resonance Imaging (MRI)
- Functional Magnetic Resonance Imaging (fMRI)
- 3.5. In Vitro Methods for Determining BBB Penetrance
- Cell Culture Models of the BBB
- 3.6. Use of Nanoparticle Technology to Enable BBB Penetration
Chapter 4
- DISCOVERY & DESIGN OF LARGE-MOLECULE DRUGS THAT CAN CROSS THE
BLOOD-BRAIN BARRIER
- 4.1. Exploiting Receptor-Mediated Transport in Design of Large-Molecule
Drugs That Cross the BBB
- Molecular Trojan Horses
- 4.2. Use of a Diphtheria Toxin Mimetic as a Molecular Trojan Horse for
BBB Transport
- 4.3. Use of a Neurotropic Virus Glycoprotein Mimetic as a Molecular
Trojan Horse for BBB Transport
- 4.4. Need for Basic Research to Find Additional Receptors That Can Be
Exploited to Get Large-Molecule Drugs across the BBB
- Genomics and Proteomics Research Aimed at Discovery of Novel BBB
Transporters
Chapter 5
- OUTLOOK FOR MEETING THE CHALLENGE OF THE BLOOD-BRAIN BARRIER IN DRUG
DISCOVERY AND DEVELOPMENT
- 5.1. Blood-Brain Barrier Survey Results
- 5.2. Conclusions
Chapter 6
- 6.1. Pieter J. Gaillard, PhD
- Founder & Chief Executive Officer
- to-BBB, Leiden, The Netherlands
- 6.2. William M. Pardridge, MD
- Chairman & Chief Scientific Officer
- ArmaGen Technologies, Santa Monica, CA
- 6.3. Christopher L. Shaffer, PhD
- Senior Principal Scientist, Neuroscience
- Pharmacokinetics, Pharmacodynamics and Metabolism
- Pfizer, Groton, CT
- 6.4. Noa Zerangue, PhD
- Research Director
- XenoPort, Santa Clara, CA
Chapter 7
- SELECTED COMPANY PROFILES
- 7.1. Amgen
- 7.2. Cellial Technologies
- 7.3. GlaxoSmithKline
- 7.4. Merck & Co.
- 7.5. MethylGene
- 7.6. Pfizer
- 7.7. Wyeth
- 7.8. XenoPort
Appendix
- INSIGHT PHARMA REPORTS BLOOD-BRAIN BARRIER SURVEY - January 2008
References
Company Index with Web Addresses
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