Abstract
Executive Summary
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
- 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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