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 at least 360 protein kinase inhibitors in active development for the treatment of cancer, from early preclinical to marketed drugs. In addition, the accumulated number of ceased drugs over the last three years amount to another 135 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 134 different targets. These targets are further categorized on the CDROM by 31 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 proactive 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 CDROM 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 189 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 dropdown 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 361 PKI drugs in active development and 914 developmental projects:
#16 projects have reached market approval
#2 projects in preregistration
#42 projects in Phase III
#313 projects in Phase II
#303 projects in Phase I
#225 projects in Preclinical
#13 projects in other developmental stages
Note: You are able to sort and find drugs according to developmental stage from dropdown menu in the application.
Indications Included PKI drugs are in development for 110 different indications, where of 61 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 134 different targets, divided into 31 classifications of molecular function:
Carboxylyase activity
Catalytic activity
Cell adhesion molecule activity
Chaperone activity
Cysteinetype peptidase activity
Cytokine activity
DNA topoisomerase activity
Gprotein coupled receptor activity
Growth factor activity
Hydrolase activity
Kinase activity
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
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 25 different primary and alternate subcellular localizations:
Centrosome
Clathrincoated 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
Secretory vesicle
Vesicle
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 132 protein expression profiles of 93 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 201 Pathways
KEGG 54 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 180 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 dropdown 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 dropdown 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 email, file export (xls) or in print
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