by septillion

The number of kinase inhibitors entering clinical development has increased significantly in recent years. In addition to major pharmaceutical and biotech companies, an increasing number of emerging companies are focusing on their development. By 2020, small-molecule kinase inhibitors could generate annual revenues > billion.

This report assesses:

– R&D considerations specific to targeting kinases
– Current kinase inhibitor pipelines
– Commercial successes to date
– Near- and longer-term market outlook
– Corporate activities of firms involved with kinases

Kinases are now firmly established as a major class of drug targets. It was previously thought that kinases would be intractable drug targets due to the presumed need to compete with ATP and the assumption that sufficient selectivity would be unattainable. However, considerable progress has been made in understanding kinases and their function, and the past few years have seen a number of kinase inhibitors reach the market. Imatinib (Novartis’ Gleevec) is currently the most commercially successful, with sales reaching .7 billion in 2008. Erlotinib (OSI/Roche’s Tarceva) generated revenues of .1 billion the same year.

In recent years, there has been an explosion in the number of kinase inhibitors entering the clinic, and many more are in preclinical development. Kinase Therapeutics: Pipeline Assessment and Commercial Prospects identifies which kinase families and their respective members have attracted the greatest interest for therapeutic development and in which indications these kinases play a physiological or pathophysiological role and thus are most relevant for kinase inhibitor development.

TABLE OF CONTENTS

CHAPTER 1: KINASES
1.1. The Function of Kinases
1.2. The Human Kinome
1.3. Kinase Classification
AGC Family
CAMK Family
CMGC Family
CK1 Family
STE Family
TK Family
TKL Family
Atypical Protein Kinases
1.4. Kinase Structure
1.5. Kinases as Drug Targets

CHAPTER 2: INDICATIONS

2.1. Introduction
2.2. Cancer
2.3. Angiogenic Conditions
2.4. Inflammatory Diseases
2.5. Metabolic Disorders
2.6. CNS Conditions
2.7. Cardiovascular Disease

CHAPTER 3: R&D CONSIDERATIONS
3.1. Introduction
3.2. Kinase Selectivity
Profiling
Selectivity Profiles of Selected Inhibitors
How Selective?
3.3. Structural Features
X-Ray Structures and Multiple Conformations
3.4. Kinase Mutations
Bcr-Abl
Pharmacogenomics
3.5. Intellectual Property Issues

CHAPTER 4: CURRENT COMMERCIAL SUCCESSES
4.1. Introduction
4.2. Small Molecules
Overview
Abl Inhibitors
Gleevec (imatinib)
Tasigna (nilotinib) and Sprycel (dasatinib)
EGF Family Inhibitors
Tarceva (erlotinib) and Iressa (gefitinib)
Tykerb (lapatinib)
Multi-Kinase Inhibitors
Nexavar (sorafenib)
Sutent (sunitinib)
Palladia (toceranib) and Masivet (mastinib)
mTOR Inhibitors
Rapamune (sirolimus)
Torisel (temsirolimus), Afinitor/Certican (everolimus), Endeavor (zotarolimus)
Rho Inhibitor
Eril (fasudil)
4.3. Biological Agents

CHAPTER 5: CURRENT KINASE INHIBITOR PIPELINES
5.1. Introduction
5.2. Overview
5.3. Kinase Inhibitors in Phase III
Enzastaurin and Ruboxistaurin
Midostaurin
Pan-VEGFR Inhibitors
Votrient (pazopanib)
Cediranib
Motesanib
Axitinib
Aflibercept
Vandetanib
BIBW-2992
Neratinib
Pertuzumab
FGFR Inhibitors
BIBF-1120
Brivanib
Alvocidib
Bosutinib
Lestaurtinib
Ridaforolimus
Masitinib
BMS-907351
CP-690550
INCB-18424
5.4. Kinase Inhibitors in Phase II Development
5.5. Kinase Inhibitors in Phase I Development
5.6. Growth Factor Receptor Kinases
ErbB Family Kinases
ErbB2 and ErbB3
ErbB2 and EGFR
Pan-ErbB
Antibodies
FGF
IGF
VEGF
Multi-Kinase Inhibitors
Flt3
5.7. Popular Kinase Cascades
PI3K, Akt, mTOR, S6K
Perifosine
Triciribine
Archexin
Ras, Raf, MEK, ERK
Roche
Ardea Biosciences and Bayer
Array and AstraZeneca
JAK Family
5.8. Cell Cycle Inhibitors
Cyclic-Dependent Kinase (CDK)
Checkpoint Kinase (Chk)
Polo-Like Kinase (PLK)
BI-2536 and BI-6727
5.9. Popular Kinase Targets
Abl
p38
GSK-3
Protein Kinase C
Aurora
Broad Spectrum
Pan-Aurora
Aurora 1
Aurora 2
c-Met
Rho
JNK
Src Family
Kinases in Inflammatory Diseases
5.10. Other Kinases
Serine/Threonine Kinases
Tyrosine Kinases
Tyrosine-Like, CAMK, and Atypical Kinases
5.11. Outlook

CHAPTER 6: CORPORATE ACTIVITIES
6.1. Introduction
6.2. Major Companies
Abbott
Amgen
Astellas
AstraZeneca
Bayer
Boehringer Ingelheim
Bristol-Myers Squibb
Daiichi Sankyo
Eisai
Eli Lilly
GlaxoSmithKline
Johnson & Johnson
Merck & Co.
Merck Serono
Novartis
Pfizer
Roche
sanofi-aventis
Takeda
6.3. Specialist Companies
ACT Biotech
Advenchen
Array BioPharma
Avila Therapeutics
Calistoga Pharmaceuticals
Cellzome
Cyclacel Pharmaceuticals
Cylene Pharmaceuticals
Deciphera Pharmaceuticals
Emiliem
Exelixis
Intellikine
Kai Pharmaceuticals
Nerviano Medical Sciences
Oncalis
OSI Pharmaceuticals
Rigel Pharmaceuticals
S*Bio
Semafore Pharmaceuticals
SuperGen
TargeGen
Vertex Pharmaceuticals
6.4. Service Companies
Ambit Biosciences
Galapágos
Invitrogen
KINAXO Biotechnologies
ProQinase
SignalChem
Upstate (Millipore)

CHAPTER 7: MARKET OUTLOOK
7.1. Introduction
7.2. Near-Term Developments
7.3. Longer-Term Outlook

CHAPTER 8: EXPERT INTERVIEWS

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Video Rating: 5 / 5

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by jlinczak

Ever heard of wine tasting tours? Wine tasting has been tried out by many people over the years. This is an art that not everybody can master quickly and is only for those who truly appreciate the different types of wine that are available in the market today. From knowing the different kinds of wine, to being able to tell the difference between these wines and read the label on a bottle of wine properly, many consider it an enjoyable task and often spend time going on tours for this purpose, to the best wineries across the country. A lot of tourists too do not forget to add wine tasting tours to their travel plans as some countries are known for their excellent wineries.

If you are looking for such a wine tasting experience that may be closer to home for you, then why not consider visiting the wineries in Napa Valley? Napa Valley has several Napa wine tasting tours to suit the needs of each of its customers. If you are looking to combine wine tasting with adventure, there is a Napa wine tasting tour for that too.

Napa Valley is known the world over as one of the best wine regions. It has over 45000 acres of grape plantation, thereby guaranteeing that anyone wishing to go on a Napa wine tasting tour would have a wonderful experience.

Choose a Napa wine tasting tour that would work well for you. Consider what you are looking to gain out of this wine tasting experience and then choose which Napa tour for tasting wine you wish to go for. Lodging can be found easily, in and around the Napa valley. This makes it easier for you and your family to wake up just in time for your Napa wine tasting tour. Whether you wish to stay in an inn, hotel or motel, there is lodging to suit your pocket, while at the same time allowing you to enjoy the scenery.

You might also want to look at the list of activities and events that take place throughout the year on each Napa wine tasting tour, in order to make the most out of your experience. Either get a brochure, check out their website or sign-up for their newsletter to keep up-to-date with such events.

Visiting Napa Valley during specific festivals would be a great chance for you to taste different types of wine, whether you decide to take a biking tour or a simple picnic tour of the wineries.

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California is a land with rich wineries. It is an exquisite adventure to tour Californian wineries for a die hard wine lover. There are many ways to travel in the wine country. Napa Valley wine tour and Sonoma county tour operators provide extensive and memorable ways to travel. Read on to choose the one that suits you best.
Balloon
Napa Valley wine tours will be an adventurous experience for you if you choose to take a tour in one of the hot air balloons. The beautiful sunrise and the view of wineries from the top will be etched in your mind forever. There are complimentary breakfasts that come with the ride.
Train
Sonoma County and Napa Valley can be viewed by traveling in trains. The Napa wine train provides a unique travel experience. It is a 3 hour ride. There are various options to choose from. From dinner adventure to luncheon package the list is endless. Napa Valley wine tours through trains are another option to a memorable experience.

Car
This is the most common and easiest way to visit Sonoma County and Napa Valley. You can easily rent a car and grab few brochures of wineries and drive away to your destinations. You can consider traveling on jeeps to make your Napa Valley wine tours much easier. They drop you in the vineyards too!
Bus
This is one of the cheapest methods to tour the wine country. It is a stress free way to visit Napa Valley and Sonoma County.
Limo
It is a luxurious way to travel in the wine country. If you have money you can flaunt it. The tours can be custom made for you. Limos offer you hassle free wine tours. There is a driver who takes care of taking you to your preferred destination at the time you want him to. The only thing you are expected to do is to taste the wines.
Bike
There are 6 day itineraries that can allow you to peddle away to the wineries you want to visit. Many young people prefer to bike on Napa Valley as they can enjoy the climate and lazy away through the wineries as long as they can.
Foot
You can experience hiking too. There are 5 day itineraries that provide adventurous hiking experience. You can catch up the wine makers up close and gain knowledge from them at personal level.
Horseback
There are several itineraries that can take you around the country on horse back. This may eat your time too. So choose a less extensive type of itinerary that can keep you busy all the time.
It is recommended to choose the one hat will sit you best. Have a word with people who are accompanying you and then decide the travel method.

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