Antibodies in Oncology: Drug Pipeline Update 2009

Table of Contents

Drug Pipeline Update at a Glance

Investigators

Includes 332 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 700 names

Developmental stage This Drug Pipeline Update contains 455 antibody drugs in active development and 889 developmental projects:

• #76 projects have reached market approval
• #3 projects have been registered
• #4 projects in pre-registration
• #39 projects in Phase III
• #272 projects in Phase II
• #201 projects in Phase I
• #268 projects in Preclinical
• #26 projects in other developmental stages
• Note: You are able to sort and find drugs according to developmental stage from drop-down menu in the application.

Indications

Included antibody drugs are in development for 181 different indications, where of 71 are different cancer indications. All antibodies 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 243 different targets, divided into 37 classifications of molecular function:

• ATPase activity
• Auxiliary transport protein activity
• Carboxypeptidase activity
• Catalytic activity
• Cell adhesion molecule activity
• Chaperone activity
• Chemokine activity
• Cofactor binding
• Complement activity
• Cysteine-type peptidase activity
• Cytokine activity
• Deacetylase activity
• DNA binding
• DNA topoisomerase activity
• DNA-directed DNA polymerase activity
• Extracellular ligand-gated ion channel activity
• Extracellular matrix structural constituent
• G-protein coupled receptor activity
• Growth factor activity
• Hormone activity
• Hydrolase activity
• Kinase activity
• Kinase binding
• Kinase regulator activity
• Ligand-dependent nuclear receptor activity
• Ligase activity
• Lipid kinase activity
• Metallopeptidase activity
• MHC class I receptor activity
• Molecular function unknown
• Motor activity
• Oxidoreductase activity
• Peptide hormone
• Peroxidase activity
• Protease inhibitor activity
• Protein binding
• Protein serine/threonine kinase activity
• Protein threonine/tyrosine kinase activity
• Protein-tyrosine kinase activity
• Receptor activity
• Receptor binding
• Receptor signaling complex scaffold activity
• Receptor signaling protein serine/threonine kinase activity
• Receptor signaling protein tyrosine phosphatase activity
• RNA-directed DNA polymerase activity
• Serine-type peptidase activity
• Structural constituent of cytoskeleton
• 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

Identified targets are categorized into 24 different primary and alternate sub-cellular localizations:

• Centrosome
• Clathrin-coated vesicle
• Cytoplasm
• Cytoplasmic vesicle
• Cytoskeleton
• Endoplasmic reticulum
• Endosome
• Extracellular
• Golgi apparatus
• Integral to membrane
• Lysosome
• Mitochondrial membrane
• Mitochondrion
• Nucleolus
• Nucleus
• Perinuclear region
• Perinuclear vesicle
• Plasma membrane
• Secreted
• Secretory granule
• Secretory vesicle
• Nuclear membrane
• Apical membrane
• Zymogen granule

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 211 protein expression profiles of 148 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 229 Pathways
• KEGG 78 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 269 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

• All antibody based

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 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)