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市場調查報告書
離子通道調節劑產品線：開發標的及藥物
Ion Channel Modulator Pipelines: Targets and Agents in Development
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離子通道調節劑產品線：開發標的及藥物 是由出版商Insight Pharma Reports在2009年08月所出版的。
這份英文市場調查報告書包含154 pages 價格從美金3195起跳。
離子通道做為治療標的的未開發領域仍有許多發展的機會。目前有將近150種離子通道調節劑在臨床開發中。
本報告書內容包括：醫療實驗中的離子通道調節劑概要及發展潛力、離子通道的結構及細胞作用概要、高處理效率篩選、商業成功發展的未來預測等。內容綱要摘記如下：
第1章 介紹
第2章 標的分類
第3章 技術觀點
- 介紹
- 標的分布
- 離子通道的結構
- 標的
- 篩選的課題
- 非電力方法
- 高處理效率電力生理學
第4章 取得商業成功的離子通道調節劑
- 概要
- L型鈣通道阻斷藥
- 抗糖尿病KATP調節劑
- GABAa
- 抗心律不整藥（鉀通道阻斷藥）
- 抗痙癴藥（鈉通道阻斷藥）
- 5-HT3拮抗藥
- 尼古丁受體
- 其他離子通道調節劑
第5章 醫療實驗中的離子通道調節劑
第6章 企業介紹
第7章 未來預測
第8章 專家訪談
第9章 離子通道調查結果：2009年
參考資料
企業名錄（附網址）
Abstract
Ion channels represent a significant opportunity to address an underexploited
class of therapeutic targets. Nearly 150 novel ion channel modulators are
reported to be in clinical development. This report examines:
- Ion channel modulators in clinical development and their potential
- Improved molecular understanding of ion channel structure and cellular
activity
- High-throughput screening methods for identification of novel modulators
- Prospects for ion channel modulators and commercial successes to date"
Pipeline activities, expert views, and survey results
Ion Channel Modulator Pipelines: Targets and Agents in Development provides a
comprehensive analysis of the ion channel modulator pipeline, breaking it down
by company, ion channel type, and therapeutic indication. A number of
interesting trends are revealed: Major pharmaceutical companies currently only
account for just over one-third of all the ion channel modulators in
development. The range of channel types targeted by ion channel modulators in
development is relatively limited and heavily skewed toward a few channel
types. Eighty percent of these ion channel modulators are being developed for
diverse CNS indications.
This report also analyzes the approximately 100 ion channel modulators that
have been approved for clinical use. These drugs have generated considerable
revenues: Even though generic forms of many of these agents are now available,
sales of these branded drugs were around $20 billion in 2007. However,
relatively few of these were developed using channel-based screening
approaches, and many were identified with little or no knowledge of their
mechanism of action.
To date, ion channel modulators have been identified by various means,
relatively few of which have so far been focused on direct screening of
compounds for their activity on the channel(s) of interest. The past few years
have seen significant developments that facilitate the identification of novel
ion channel modulators. These improvements in screening methods should lead to
more selective agents being identified and progressing into clinical
development. We also examine other technical considerations when attempting to
modulate ion channels, such as target distribution throughout the body, and
the structure of ion channels and their multiple states (e.g., each state of
the ion channel offers a different conformation for a potential ligand to
recognize and thus any ion channel provides multiple potential targets).
Ion Channel Modulator Pipelines: Targets and Agents in Development concludes
with a commercial and scientific outlook, expert interviews, and results from
a survey gauging trends, current practices, and views on ion channel-focused
R&D activity.
Table of Contents
CHAPTER 1 INTRODUCTION 1
- 1.1. What Are Ion Channels?
- 1.2. Channel Activation
- Ligand-Gated
- Voltage-Gated
- Conformational States
- Accessory Proteins and Subunits
- Specificity and Function
- 1.3. Opportunity
CHAPTER 2 TARGET CLASSES
- 2.1. Overview
- 2.2. Classification
- 2.3. Voltage-Gated Channels
- Chloride
- ClC Channels
- ClCa
- CFTR
- Sodium
- Calcium
- Potassium
- KV Channels
- KCa Channels
- Kir Channels
- K2P Channels
- Degenerins
- Non-Specific Cation Channels
- 2.4. Ligand-Gated Channels
- Cyclic Nucleotide (CNGA, CNGB, and HCN)
- Nicotinic Receptors
- GABAA
- Glutamate
- NMDA
- AMPA
- Kainate
- Glycine
- 5-HT3 Receptors
- Purinergic
- Transient Receptor Potential Channels
- TRPV
- TRPM
- TRPA
CHAPTER 3 TECHNICAL CONSIDERATIONS
- 3.1. Introduction
- 3.2. Target Distribution
- 3.3. Ion Channel Structures
- 3.4. What to Target
- Multiple States
- Accessory Proteins
- The hERG Channel
- 3.5. Screening Issues
- 3.6. Non-Electrical Methods
- FLIPR Assays
- Isotopic Flux
- FRET
- 3.7. High-Throughput Electrophysiology
CHAPTER 4 COMMERCIALLY SUCCESSFUL ION CHANNEL MODULATORS
- 4.1. Overview
- 4.2. L-Type Calcium Channel Blockers
- 4.3. Antidiabetic KATP Modulators
- 4.5. GABA Analogs
- 4.6. Antiarrhythmic Agents (Potassium Channel Blockers)
- 4.7. Anticonvulsants (Sodium Channel Blockers)
- 4.8. 5-HT3 Antagonists
- 4.9. Nicotinic Receptors
- 4.10. Other Ion Channel Modulators
CHAPTER 5 ION CHANNEL MODULATORS IN CLINICAL DEVELOPMENT
- 5.1. Overview
- By Company
- Abbott
- AstraZeneca
- Eli Lilly
- GlaxoSmithKline
- Pfizer
- sanofi-aventis
- By Channel Type
- By Indication
- Late-Stage Development Compounds
- Tedisamil
- Vernakalant
- Dronedarone
- Eslicarbazepine
- Indiplon
- NGX-4010
- Zucapsaicin
- Amifampridine
- Fampridine
- SK-310
- 5.2. Phase III
- Gastrointestinal Disorders
- Arverapamil
- Crofelemer
- Anxiety
- TIK-101
- PD-332334
- Pagoclone
- Epilepsy
- Perampanel
- Retigabine
- Other CNS Indications
- Dimebolin
- RPI-78M
- Safinamide
- Cystic Fibrosis
- VX-770
- 5.3. Phase II
- CNS Conditions
- Alzheimer' s Disease
- Pain
- Schizophrenia
- Anxiety and Depression
- Parkinson' s Disease
- Epilepsy
- Other CNS Conditions
- Peripheral Conditions
- Inflammatory Diseases
- Cystic Fibrosis
- Cardiovascular Disease
- Gastrointestinal Disease
- Oncology
- Glaucoma and Tinnitus
- 5.4. Phase I
- GABA
- Glutamate Receptors
- Nicotinic Receptors
- Voltage-Gated Channels
- TRPV1
- Other
- 5.5. Outlook 93
CHAPTER 6 COMPANY PROFILES
- 6.1. Introduction
- 6.2. Leading Major Companies
- AstraZeneca
- Eli Lilly
- GlaxoSmithKline
- Merck & Co.
- Novartis
- Pfizer
- sanofi-aventis
- 6.3. Selected Biotechnology Companies
- Aurora Biomed
- CalciMedica
- Cellectricon
- CytoCentrics
- EPIX Pharmaceuticals
- Evotec
- Flyion
- Hydra Biosciences
- Icagen
- iOnGen
- Lectus Therapeutics
- Nanion Technologies
- Neurion Pharmaceuticals
- Neuromed Pharmaceuticals
- NeuroSearch
- Newron Pharmaceuticals
- Parion Sciences
- Targacept
- Xention
CHAPTER 7 OUTLOOK
- 7.1. Commercial Outlook
- 7.2. Scientific Outlook
CHAPTER 8 EXPERT INTERVIEWS
CHAPTER 9 RESULTS FROM INSIGHT PHARMA REPORTS' ION CHANNELS SURVEY, JULY 2009
- Question 1. Please classify your organization.
- Question 2. Under what functional area do your responsibilities fall?
- Question 3. What disease areas do you feel will see significant treatment
advances as a result of ion channel modulator development over the next five
years?
- Question 4. The major thrust of current efforts aimed at ion channel
modulators appears to be focused on CNS conditions, with some activity aimed
at heart disease and limited interest in other conditions. Is this overlooking
other potential targets?
- Question 5. There has been a recent explosion in interest in the
development of TRP channel modulators. Do you think that we are likely to see
many modulators of channels other than TRPV1 enter development in the near
term?
- Question 6. In your opinion, what type(s) of ion channels have the
greatest potential as drug targets?
- Question 7. My organization currently targets the following type(s) of ion
channels...
- Question 8. In what areas of ion channel development are further advances
going to be the most critical?
- Question 9. Has there been an upsurge of research activity on ion channel
targets since the emergence of improved knowledge of their molecular structure
and newer screening methods?
- Question 10. In your opinion, has the lack of reliable screening assays
been the major factor in decisions of large pharma to avoid the pursuit of
many ion channel targets?
- Question 11. In your opinion, what is currently the greatest barrier to
successful development of ion channel modulators?
- Question 12. Do you think that the low conductance of many types of ion
channels has been a major barrier to both their study and the
- identification of selective modulators?
- Question 13. How has your organization' s level of activity changed in the
past five years in terms of developing ion channel modulators?
- Question 14. Does your organization plan to change its level of
involvement with ion channels over the next three years?
- Question 15. Do you have any additional observations about the discovery
and development of ion channel modulators?
REFERENCES 133
COMPANY INDEX WITH WEB ADDRESSES 149
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