Apoptosis in Oncology Drug Pipeline Update 2013

• Publication date: April 2013

Cancer cells frequently and possibly invariably possess apoptotic defects. In this context, apoptotic pathways provide exciting molecular targets for new therapeutic agents to specifically promote apoptosis of cancer cells. There are today 282 companies plus partners developing 277 apoptotic drugs in 1179 developmental projects in cancer. In addition, there are 9 suspended drugs and the accumulated number of ceased drugs over the last years am...

Cancer cells frequently and possibly invariably possess apoptotic defects. In this context, apoptotic pathways provide exciting molecular targets for new therapeutic agents to specifically promote apoptosis of cancer cells.
There are today 282 companies plus partners developing 277 apoptotic drugs in 1179 developmental projects in cancer. In addition, there are 9 suspended drugs and the accumulated number of ceased drugs over the last years amount to another 161 drugs. Apoptosis In Oncology Drug Pipeline Update lists all drugs and gives you a progress analysis on each one of them. Identified drugs are linked to 201 different targets. All included targets have been cross-referenced for the presence of mutations associated with human cancer. To date 173 out of the 194 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 54 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 282 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 277 apoptotic drugs in development, which have a total of 1179 developmental projects in cancer. In addition there are suspended and ceased drugs.

Pipeline Breakdown According to Number of Drugs
Marketed# 27
Registered# 1
Pre-registration# 1
Phase III# 42
Phase II# 117
Phase I# 130
Preclinical# 140
No Data# 3
Suspended# 9
Ceased# 161

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

Indications
Included apoptotic drugs are also in development for 156 other indications, where of 77 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 173 out of the 194 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 142 drug targets was retrieved from the RCSB Protein Databank for you to easily review the 2633 structures available today among drug targets.

Identified drugs are linked to more than 201 different targets, divided into 54 classifications of molecular function:
- Auxiliary transport protein activity
- Carboxy-lyase activity
- Caspase activator activity
- Catalytic activity
- Cell adhesion molecule activity
- Chaperone activity
- Chromatin binding
- Complement activity
- Cysteine-type peptidase activity
- Cytokine activity
- Deacetylase activity
- Defense/immunity protein activity
- DNA binding
- DNA topoisomerase activity
- G-protein coupled receptor activity
- Glutathione transferase activity
- Growth factor activity
- Growth factor binding
- GTPase activator activity
- GTPase activity
- Hydrolase activity
- Kinase activity
- Kinase binding
- Kinase regulator activity
- Ligand-dependent nuclear receptor activity
- Ligase activity
- Lipid kinase activity
- Metallopeptidase activity
- Molecular function unknown
- Motor activity
- Oxidoreductase activity
- Peptide hormone
- Phosphoric diester hydrolase activity
- Protein binding
- Protein serine/threonine kinase activity
- Protein-tyrosine kinase activity
- Receptor activity
- Receptor binding
- Receptor signaling complex scaffold activity
- Receptor signaling protein serine/threonine kinase activity
- RNA binding
- Serine-type peptidase activity
- Structural constituent of cytoskeleton
- Structural molecule activity
- Superoxide dismutase activity
- T cell receptor activity
- Transcription factor activity
- Transcription regulator activity
- Transferase activity
- Translation regulator activity
- Transmembrane receptor activity
- Transmembrane receptor protein tyrosine kinase activity
- Transporter activity
- Ubiquitin-specific protease activity

Sub-Cellular Localization
Identified targets are categorized into 24 different primary and alternate sub-cellular localizations:
- Cell surface
- Centrosome
- Clathrin-coated vesicle
- Cytoplasm
- Cytoskeleton
- Cytosol
- Endoplasmic reticulum
- Endosome
- Extracellular
- Golgi apparatus
- Integral to membrane
- Lysosome
- Microtubule
- Mitochondrial membrane
- Mitochondrion
- Nuclear membrane
- Nucleolus
- Nucleus
- Perinuclear region
- Peroxisome
- Plasma membrane
- Sarcoplasmic reticulum
- Secreted
- Secretory 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 302 protein expression profiles of 178 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# 220 Pathways
- KEGG# 163 Pathways
- NCI-Nature# 228 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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