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Protein Kinase Inhibitors in Oncology Drug Pipeline Update 2013
Bioseeker, April 2013
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 288 companies plus partners developing 563 PKI drugs in 1918 developmental projects in cancer. In addition, there are 8 suspended drugs and the accumulated number of ceased drugs over the last years amount to another 301 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 224 different targets. All included targets have been cross-referenced for the presence of mutations associated with human cancer. To date 202 out of the 222 studied drug targets so far have been recorded with somatic mutations. The software application lets you narrow in on these mutations and links out to the mutational analysis for each of the drug targets for detailed information. All drugs targets are further categorized on in the software application by 46 classifications of molecular function and with pathway referrals to BioCarta, KEGG. NCI-Nature and NetPath.
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 downloadable application, which requires no installation on your computer. Please read more about application features and system requirements below.
Drug Pipeline Update at a Glance
Includes more than 288 principal companies plus their collaborators. There is direct access from inside the application to web pages of all principal companies.
Note: You are able to sort and find drugs according to companiess and partners from drop-down menus in the application. You may also sort and find drugs according to country of companies.
Drug name & Synonyms
Lists commercial, generic and code names for drugs.
This Drug Pipeline Update contains 563 PKI drugs in development, which have a total of 1918 developmental projects in cancer. In addition there are suspended and ceased drugs.
Pipeline Breakdown According to Number of Drugs
Phase III# 50
Phase II# 172
Phase I# 233
No Data# 3
Note: You are able to sort and find drugs according to developmental stage from drop-down menu in the application.
Included PKI drugs are also in development for 155 other indications, where of 90 are different cancer indications.
Note: You are able to find and sort drugs according to type of indication from drop-down menu in the application.
All targets are cross-referenced with the Catalogue of Somatic Mutations in Cancer (COSMIC). It is designed to store and display somatic mutation information and related details and contains information relating to human cancers. To date 202 out of the 222 studied drug targets so far have been recorded with somatic mutations and the software application lets you narrow in on these mutations and links out to the mutational analysis for each of the drug targets for detailed information.
The identity of available biological structures on 170 drug targets was retrieved from the RCSB Protein Databank for you to easily review the 2978 structures available today among drug targets.
Identified drugs are linked to more than 224 different targets, divided into 46 classifications of molecular function:
- Antigen binding
- ATPase activity
- Carboxy-lyase activity
- Catalytic activity
- Cell adhesion molecule activity
- Chaperone activity
- Cysteine-type peptidase activity
- Cytokine activity
- Cytoskeletal protein binding
- DNA binding
- DNA topoisomerase activity
- DNA-directed DNA polymerase activity
- Extracellular ligand-gated ion channel activity
- G-protein coupled receptor activity
- Growth factor activity
- GTPase activator activity
- GTPase activity
- Hydrolase activity
- Ion channel activity
- Isomerase activity
- Kinase activity
- Kinase binding
- Kinase regulator activity
- Ligase activity
- Lipid kinase activity
- Lipid phosphatase activity
- Molecular function unknown
- Oxidoreductase activity
- Peroxidase activity
- Protease inhibitor 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
- Structural constituent of cytoskeleton
- Structural molecule activity
- Transcription factor activity
- Transcription regulator activity
- Translation regulator activity
- Transmembrane receptor protein tyrosine kinase activity
- Transporter activity
Identified targets are categorized into 38 different primary and alternate sub-cellular localizations:
- Basolateral membrane
- Cell junction
- Cell projection
- Cell surface
- Clathrin-coated vesicle
- Cytoplasmic vesicle
- Endoplasmic reticulum
- Golgi apparatus
- Golgi membrane
- Integral to membrane
- Membrane fraction
- Mitochondrial membrane
- Nuclear membrane
- Perinuclear region
- Perinuclear vesicle
- Plasma membrane
- Sarcoplasmic reticulum
- Secretory vesicle
- Soluble fraction
- Synaptic vesicle
Note: You are able to find and sort drugs according to target gene name, protein name, molecular function of target, target localization, presence of mutations and availability of biological structures of target from drop-down menus in the application.
Target Expression Profile
Direct links are provided from inside the application to 330 protein expression profiles of 200 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
Identified targets have been cross referenced against their involvement in different cellular pathways, according to BioCarta, KEGG, NCI-Nature and NetPath.
- BioCarta# 225 Pathways
- KEGG# 145 Pathways
- NCI-Nature# 246 Pathways
- NetPath# 25 Pathways
Note: You are able to find and sort drugs according to targeted pathways from drop-down menus in the application.
In total there are different drug mechanism of action represented in this Drug Pipeline Update.
Note: You are able to find and sort drugs according to mechanism of action from drop-down menu in the application.
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.
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 Company & Partners
Presentation of principal company and partners
Target and Molecular Function of Target
Described target(s) is/are presented with:
Official Gene Symbol – Chromosome Location – Gene & Protein Name – Molecular Function
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
All targets are cross-referenced with the Catalogue of Somatic Mutations in Cancer (COSMIC). It is designed to store and display somatic mutation information and related details and contains information relating to human cancers.
The identity of available biological structures on drug targets was retrieved from the RCSB Protein Databank for you to easily review what available structures of drug targets exist.
Described target(s) is/are matched for the involvement in cellular pathways according to BioCarta, KEGG, NCI-Nature and NetPath.
Drug mechanism of action
Summary field of developmental projects for the drug, including indication, developmental stage and status.
Cancer, myeloma – Phase II Clinical Trial – Active
Cancer, prostate – Phase III Clinical Trial – Ceased
Short introduction to drug
Compound type, Chemical name, CAS Number and molecular weight
Available patent information related to the drug is presented here.
Fillings and Approvals
Approvals and submissions
Deals & Licensing
Collaborations and deals
Availability for licensing
Phase IV Data
Available Phase IV development data, developmental history and scientific data.
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.
Phase 0 Data
Available Phase 0 development data, developmental history and scientific data.
Available preclinical development data, developmental history and scientific data.
Available discovery development data, developmental history and scientific data.
Search, Find and Filter Panel with Initial Result Presentation
With this panel you can define your selectivity in each drug search with up to 24 different drug specific parameters. Each parameter has multi-select options to them and can be used as either an inclusion parameter or exclusion parameter.
The initial result table is a dynamic sortable table which gives you a fast overview of found results and can be narrowed down further by your own additional keywords.
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, NCI-Nature, NetPath etc.
- Direct links to company web pages of companies
Dynamic Report Generator
Our dynamic report generator lets you with ease and speed generate html reports directly in your web browser (Internet Explorer and FireFox), whether it is a single drug profile or an entire search you want have a report of.
- Operating system: Windows (2000/XP/Vista/7) and Mac OS X 10.6 (Snow Leopard) and OS X 10.7 (Lion)
- Browser Application (Internet Explorer)
- Internet access (to access related internet resources)
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