Leptin Signaling Pathway in Oncology Drug Pipeline Update 2013

• Publication date: April 2013

The binding of Leptin to its receptor, LEPR induces various signaling modules such as JAK/STAT, RAS/RAF/MAPK, IRS/PI-3K and AMPK/ACC. There are today 246 companies plus partners developing 340 Leptin pathway targeting drugs in 1175 developmental projects in cancer. In addition, there is 1 suspended drug and the accumulated number of ceased drugs over the last years amount to another 150 drugs. Leptin Signaling Pathway In Oncology Drug Pipeline...

The binding of Leptin to its receptor, LEPR induces various signaling modules such as JAK/STAT, RAS/RAF/MAPK, IRS/PI-3K and AMPK/ACC.
There are today 246 companies plus partners developing 340 Leptin pathway targeting drugs in 1175 developmental projects in cancer. In addition, there is 1 suspended drug and the accumulated number of ceased drugs over the last years amount to another 150 drugs. Leptin Signaling Pathway In Oncology Drug Pipeline Update lists all drugs and gives you a progress analysis on each one of them. Identified drugs are linked to 164 different targets. All included targets have been cross-referenced for the presence of mutations associated with human cancer. To date 149 out of the 163 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 39 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

Investigators
Includes more than 246 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.

Developmental stage
This Drug Pipeline Update contains 340 Leptin pathway targeting drugs in development, which have a total of 1175 developmental projects in cancer. In addition there are suspended and ceased drugs.

Pipeline Breakdown According to Number of Drugs
Marketed# 30
Registered# 1
Pre-registration# 5
Phase III# 35
Phase II# 119
Phase I# 131
Preclinical# 187
No Data# 3
Suspended# 1
Ceased# 150

Note: You are able to sort and find drugs according to developmental stage from drop-down menu in the application.

Indications
Included Leptin pathway targeting drugs are also in development for 165 other indications, where of 86 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.

Targets
Mutations
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 149 out of the 163 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.

Biological Structures
The identity of available biological structures on 134 drug targets was retrieved from the RCSB Protein Databank for you to easily review the 2794 structures available today among drug targets.

Identified drugs are linked to more than 164 different targets, divided into 39 classifications of molecular function:
- ATPase activity
- Catalytic activity
- Cell adhesion molecule activity
- Chaperone activity
- Complement activity
- Cysteine-type peptidase activity
- Cytokine activity
- DNA repair protein
- DNA topoisomerase activity
- G-protein coupled receptor activity
- Growth factor activity
- GTPase activity
- Isomerase activity
- Kinase activity
- Ligand-dependent nuclear receptor activity
- Ligase activity
- Lipid kinase activity
- Lipid phosphatase activity
- Metallopeptidase activity
- Molecular function unknown
- Oxidoreductase activity
- Peroxidase activity
- Protein binding
- Protein serine/threonine kinase activity
- Protein threonine/tyrosine kinase activity
- Protein tyrosine 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 activity
- Transmembrane receptor protein tyrosine kinase activity
- Transporter activity

Sub-Cellular Localization
Identified targets are categorized into 24 different primary and alternate sub-cellular localizations:
- Centrosome
- Chromosome
- Clathrin-coated vesicle
- Cytoplasm
- Cytoplasmic vesicle
- Cytoskeleton
- Cytosol
- Endoplasmic reticulum
- Endosome
- Extracellular
- Golgi apparatus
- Golgi membrane
- Microtubule
- Mitochondrion
- Nuclear membrane
- Nucleolus
- Nucleus
- Perinuclear region
- Perinuclear vesicle
- Plasma membrane
- Ribosome
- Sarcoplasmic reticulum
- Secreted
- 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 262 protein expression profiles of 156 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 involvement in different cellular pathways, according to BioCarta, KEGG, NCI-Nature and NetPath.
- BioCarta# 229 Pathways
- KEGG# 149 Pathways
- NCI-Nature# 243 Pathways
- NetPath# 25 Pathways

Note: You are able to find and sort drugs according to targeted pathways from drop-down menus in the application.

Mechanism
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.

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 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

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

Mutation
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.

Biological Structures
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.

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

Fillings and Approvals
Approvals and submissions
Analyst comments

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.

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

Discovery Data
Available discovery development data, developmental history and scientific data.

Application Features
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.

System Requirements
- 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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