Quantcast
Last updated on April 17, 2014 at 10:25 EDT

Reportlinker Adds Ion Channel Modulator Pipelines: Targets and Agents in Development

October 26, 2009

NEW YORK, Oct. 26 /PRNewswire/ — Reportlinker.com announces that a new market research report is available in its catalogue.

Reportlinker Adds Ion Channel Modulator Pipelines: Targets and Agents in Development

http://www.reportlinker.com/p0156556/Reportlinker-Adds-Ion-Channel-Modulator-Pipelines-Targets-and-Agents-in-Development.html#utm_source=prnewswire&utm_medium=pr&utm_campaign=prnewswire

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.

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

Structural Biology

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

Tables

Table 2.1. Families of Ion Channels

Table 2.2. Voltage-Gated Calcium Channels

Table 2.3. Old and New Nomenclatures of Glutamate-Gated Ion Channels

Table 4.1. L-Type Calcium Channel Blockers and 2007 Sales

Table 4.2. KATP Channel Modulators and 2007 Sales

Table 4.3. GABAA Channel Modulators and 2007 Sales

Table 4.4. Class I Antiarrhythmic Agents (Sodium Channel Blockers)

Table 4.5. Class III Antiarrhythmic Agents (Potassium Channel Blockers)

Table 4.6. Anticonvulsant Agents and 2007 Sales

Table 4.7. 5-HT3 Antagonists and 2007 Sales

Table 5.1. Ion Channel Modulators Awaiting Regulatory Approval

Table 5.2. Ion Channel Modulators in Phase III Studies

Table 5.3. Ion Channel Modulators in Phase II Studies for CNS Disorders

Table 5.4. Ion Channel Modulators for Non-CNS Conditions in Phase II Studies

Table 5.5. Ion Channel Modulators in Phase I Studies

Figures

Figure 5.1. Ion Channels Modulators in Development by Major Pharmaceutical Companies

Figure 5.2. Ion Channel Modulators in Development by Target Type

Figure 5.3. Ion Channel Modulators in Development by Indication

Figure 6.1. Ion Channel Modulator Patents Filed by Seven Major Companies Published Between January 2005 and March 2009

To order this report:

Reportlinker Adds Ion Channel Modulator Pipelines: Targets and Agents in Development

http://www.reportlinker.com/p0156556/Reportlinker-Adds-Ion-Channel-Modulator-Pipelines-Targets-and-Agents-in-Development.html#utm_source=prnewswire&utm_medium=pr&utm_campaign=prnewswire

More market research reports here!

Contact:

Nicolas Bombourg

Reportlinker

Email: nbo@reportlinker.com

US: (805)652-2626

Intl: +1 805-652-2626

SOURCE Reportlinker


Source: newswire