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Protein Kinase Inhibitors in Oncology: Drug Pipeline Update 2008
Bioseeker, April 2008


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Protein kinase inhibitors such as Gleevec, Iressa and Tarceva have allowed the biotechnology industry to deliver on the promise of targeted cancer drugs. However, these three successful drugs are just the top of an emerging line of therapy. Given the fact that they all target tyrosine kinases and that kinase mutations can cause patients to become resistant to these drugs, there is plenty of room for more competition.

There are today more than 380 protein kinase inhibitors for the treatment of cancer, from early preclinical to marketed drugs. Protein Kinase Inhibitors in Oncology: Drug Pipeline Update lists all drugs and gives you a progress analysis on each one of them. Identified drugs are linked to 139 different targets. These targets are further categorized on the CD-ROM by 36 classifications of molecular function and with pathway referals to BioCarta, KEGG and NetPath. Read more below on how the Protein Kinase Inhibitors in Oncology: Drug Pipeline Update is organized.

How May Drug Pipeline Update Be of Use?

Show investors/board/management that you are right on top of drug development progress in your therapeutic area.
Find competitors, collaborations partners, M&A candidates etc.
Jump start competitive drug intelligence operations
Excellent starting point for world wide benchmarking
Compare portfolio and therapy focus with your peers
Speed up pro-active in-/out licensing strategy work
Fast and easy way of tracking drugs using search engines; just one click from inside the application and you may search the World Wide Web and PubMed for any drug.
Drug Pipeline Update is delivered to you as a CD-ROM application, which requires no installation on your computer. Please read more about application features and system requirements below.

Drug Pipeline Update at a Glance

Investigators Includes more than 190 principal investigators plus their collaborators. There is direct access from inside the application to web pages of all principal investigators.
Note: You are able to sort and find drugs according to investigators and partners from drop-down menus in the application. You may also sort and find drugs according to country of investigator.

Drug name & Synonyms Lists commercial, generic and code names for drugs. In all more than 500 names
Developmental stage This Drug Pipeline Update contains more than 380 PKI drugs in active development and more than 930 developmental projects:
15 marketed drugs
> 50 projects in Phase III
> 320 projects in Phase II
> 250 projects in Phase I
> 260 projects in Preclinical
Note: You are able to sort and find drugs according to developmental stage from drop-down menu in the application.

Indications Included PKI drugs are in development for over 90 indications, where of 50+ are different cancer indications. All PKIs are in development for the treatment of cancer.
Note: You are able to sort and find drugs according to type of indication from drop-down menu in the application.

Targets Identified drugs are linked to more than 139 different targets, divided into 36 classifications of molecular function:
- Carboxy-lyase activity
- Catalytic activity
- Cell adhesion molecule activity
- Chaperone activity
- Cysteine-type peptidase activity
- Cytokine activity
- DNA topoisomerase activity
- DNA-directed DNA polymerase activity
- Growth factor activity
- GTPase activity
- Hormone activity
- Hydrolase activity
- Kinase activity
- Kinase binding
- Kinase regulator activity
- Ligase activity
- Lipid kinase activity
- Lipid phosphatase activity
- Oxidoreductase activity
- Peroxidase activity
- Protein binding
- Protein serine/threonine kinase activity
- Protein threonine/tyrosine kinase activity
- Protein tyrosine/serine/threonine phosphatase activity
- Protein-tyrosine kinase activity
- Receptor activity
- Receptor binding
- Receptor signaling complex scaffold activity
- Receptor signaling protein serine/threonine kinase activity
- RNA binding
- Structural constituent of cytoskeleton
- Transcription factor activity
- Transcription regulator activity
- Translation regulator activity
- Transmembrane receptor protein tyrosine kinase activity
- Transporter activity

Identified targets are categorized into 18 different primary and alternate sub-cellular localizations:
- Centrosome
- Clathrin-coated vesicle
- Cytoplasm
- Cytoplasmic vesicle
- Cytoskeleton
- Cytosol
- Endoplasmic reticulum
- Endosome
- Extracellular
- Golgi apparatus
- Integral to membrane
- Lysosome
- Microtubule
- Mitochondrial membrane
- Mitochondrion
- Nuclear membrane
- Nucleolus
- Nucleus
- Perinuclear region
- Perinuclear vesicle
- Peroxisome
- Plasma membrane
- Secreted


Note: You are able to sort and find drugs according to target gene name, molecular function of target, and target localization from drop-down menus in the application.

Target Expression Profile Direct links are provided from inside the application to 92 protein expression profiles of 75 drug targets in various human tissues and cancer types, cell lines and primary cells, including up to:
- 48 different normal tissue types
- 20 different types of cancer
- 47 cell lines
- 12 samples of primary blood cells
Pathway Referals Identified targets have been cross referenced against their invovlement in different cellular pathways, according to BioCarta, KEGG and NetPath.
- BioCarta 207 Pathways
- KEGG 57 Pathways
- NetPath 20 Signaling Pathways
Note: You are able to sort and find drugs according to targeted pathways from drop-down menues in the application.

Mechanism In total there are more than 170 different drug mechanism of action represented in this Drug Pipeline Update.
Note: You are able to sort and find drugs according to mechanism of action from drop-down menu in the application.

Compound Identified drug compounds are described by:

Compound type, Chemical name, CAS Number and molecular weight

Note: You are able to sort and find drugs according to compound type from drop-down menu in the application.
Drug Profile Progress analysis and review of drug development. A typical drug profile reports on, depending on stage of development and available information:
Drug Name & Synonyms
Presentation of drug name and synonyms

Principal Investigator & Partners
Presentation of principal investigator and partners

Target and Molecular Function of Target
Described target(s) is/are presented with:
Official Gene Symbol - Official Gene Name [Species/Homo Sapiens] - Molecular Function

Target Localization
Described target(s) is/are presented with primary and alternate localizations.

Target Expression Profiles
Links to protein expression profile(s) of target(s) in various human tissues, cell lines and primary cells, including up to:
48 different normal tissue types
20 different types of cancer
47 cell lines
12 samples of primary blood cells

Targeted Pathways
Described target(s) is/are matched for the involvement in cellular pathways according to BioCarta, KEGG, and NetPath.

Mechanism
Drug mechanism of action

Developmental Projects
Summary field of developmental projects for the drug, including indication, developmental stage and status.
Example:
Cancer, myeloma - Phase II Clinical Trial - Active
Cancer, prostate - Phase III Clinical Trial - Ceased

Drug Description
Short introduction to drug

Compound Data
Compound type, Chemical name, CAS Number and molecular weight

Patent Data
Available patent information related to the drug is presented here.

Business & Markets
Collaborations and deals
Approvals and submissions
Analyst comments

Phase III Data
Available Phase III development data, developmental history and scientific data.

Phase II Data
Available Phase II development data, developmental history and scientific data.

Phase I Data
Available Phase I development data, developmental history and scientific data.

Preclinical Data
Available preclinical development data, developmental history and scientific data.

Licensing Information
Availability for licensing

Application Features Use 13 different parameters, available in drop-down menus, to find and sort among drugs
- Drug status
- Clinical Trial Status
- Principle Investigator
- Partners
- Indication
- Developmental Stage
- Compound Type
- Mechanism
- Target
- Molecular Function of Target
- Target Localization
- Targeted Pathways
- Free text search of entire drug profile contents
Direct linkage from inside the application to related internet resources
- Drug data is linked to search engines like Google and PubMed
- Drug target data is linked directly to BioCarta, Human Protein Atlas, KEGG, and NetPath
- Direct links to company web pages of principal investigators

Export and sharing of information
- Found information is easily shared with others over e-mail, file export (xls) or in print

System Requirements - AMD-Athlon/Pentium II PC
- Windows 98/NT4/2000/ME/XP/VISTA
- 8x-speed CD Rom drive
- SVGA 16 bit display. (32 bit recommended)
- 32 MB of available RAM (128 MB recommended)
- Internet access (for related internet resources)



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