Phase II results presented at the European Society for Medical Oncology (ESMO) 2012 Congress showed a 3.6-month improvement in progression-free survival (PFS) for patients receiving both the BRAF inhibitor dabrafenib and trametinib, a MEK inhibitor, compared to those receiving dabrafenib alone.

PFS was 9.4 months for patients who received dabrafenib plus trametinib compared to 5.8 months in patients who received dabrafenib alone (HR = 0.39, P < .0001), according to Georgina Long, MD, of the Westmead Hospital and the Melanoma Institute Australia at the University of Sydney, who presented the study at ESMO. Response rates were 75% for those in the combination group compared to 54% in the monotherapy group (P = .026). The median duration of response was 10.5 months with the combination compared to 5.6 months for the BRAF monotherapy. The results are published in the New England Journal of Medicine (NEJM).  Read More...

Melanoma comprises just 5% of all skin cancers but it is the most deadly. High unmet needs still persist for this tumor type and despite three decades of extensive R&D, five-year survival of advanced patients remains below 20%.
There are today 242 companies plus partners developing 273 drugs targeting melanoma in development. In addition, there are 3 suspended drugs and the accumulated number of ceased drugs over the last years amount to another 113 drugs. Melanoma Drug Pipeline Update lists all drugs and gives you a progress analysis on each one of them. Identified drugs are linked to 182 different targets. These targets are further categorized on in the software application by 57 classifications of molecular function and with pathway referrals to BioCarta, KEGG 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 242 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.

Developmental stage
This Drug Pipeline Update contains 273 drugs in development for the treatment of melanoma. In addition there are suspended and ceased drugs.

Pipeline Breakdown According to Number of Drugs
Marketed# 19
Pre-registration# 2
Phase III# 13
Phase II# 94
Phase I# 78
Preclinical# 66
No Data# 1
Suspended# 3
Ceased# 113

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

Indications
Included melanoma drugs are also in development for 181 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
Identified drugs are linked to more than 182 different targets, divided into 57 classifications of molecular function:
- Carboxy-lyase activity
- Carboxypeptidase activity
- Catalytic activity
- Cell adhesion molecule activity
- Chaperone activity
- Chemokine activity
- Cofactor binding
- Complement activity
- Cysteine-type peptidase activity
- Cytokine activity
- DNA binding
- DNA repair protein
- DNA topoisomerase activity
- DNA-directed DNA polymerase activity
- DNA-methyltransferase activity
- Extracellular ligand-gated ion channel activity
- Extracellular matrix structural constituent
- G-protein coupled receptor activity
- Growth factor activity
- GTPase activity
- Hydrolase activity
- Isomerase activity
- Kinase activity
- Kinase regulator activity
- Ligase activity
- Lipase activity
- Lipid kinase activity
- Metallopeptidase activity
- MHC class I receptor activity
- Molecular function unknown
- Motor activity
- Oxidoreductase activity
- Peptide hormone
- Protein binding
- Protein serine/threonine kinase activity
- Protein threonine/tyrosine kinase activity
- Protein tyrosine phosphatase activity
- Protein tyrosine/serine/threonine phosphatase activity
- Protein-tyrosine kinase activity
- Receptor activity
- Receptor binding
- Receptor signaling complex scaffold activity
- RNA binding
- RNA-directed DNA polymerase activity
- Serine-type peptidase activity
- Structural constituent of cytoskeleton
- 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
- Voltage-gated ion channel activity

Identified targets are categorized into 21 different primary and alternate sub-cellular localizations:
- Cell surface
- Centrosome
- Clathrin-coated vesicle
- Cytoplasm
- Cytoplasmic vesicle
- Cytoskeleton
- Cytosol
- Endoplasmic reticulum
- Endosome
- Extracellular
- Golgi apparatus
- Integral to membrane
- Lysosome
- Mitochondrion
- Nucleolus
- Nucleus
- Perinuclear vesicle
- Peroxisome
- Plasma membrane
- Secreted
- Secretory vesicle

Note: You are able to find and sort 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 244 protein expression profiles of 154 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 and NetPath.
- BioCarta# 221 Pathways
- KEGG# 111 Pathways
- NetPath# 25 Signaling 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 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

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)

Report cost $1,925.00

ABSTRACT: “Targeted therapy” is becoming the centerpiece of current therapeutic strategies, and is often mentioned as the desirable direction for future progress. Why and how it is replacing past approaches in the management of solid tumors is the subject of this two-part overview. Here, in Part I, we describe areas where major inroads were initially achieved by targeting angiogenesis (central to the biology of renal cell carcinoma and hepatocellular cancer) and by unraveling pathways in the heterogeneous tumors of mesenchymal origin—spurred by the identification of c-Kit–activating mutations in gastrointestinal stromal tumors (GIST) and the regressions that ensued when tumors harboring these mutations were exposed to the tyrosine kinase inhibitor imatinib (Gleevec). More recently, the successes in the treatment of the notoriously refractory malignant melanoma via the targeting of a specific BRAF mutation and via immune activation represent an unprecedented achievement of this new therapeutic direction. For each cancer discussed in the first part of our overview, as well as in Part II, which will deal with more common cancers, we briefly cover the tumor biology, how targeting was achieved, the introduction of immune modulation or immune-conjugates, and the impact these therapies are having in the disease. Read More...

A summary of the phase III BREAK-3 trial comparing the BRAF inhibitor dabrafenib with the chemotherapy agent dacarbazine (DTIC).

Patients taking dabrafenib had an improved progression-free survival (PFS) of 2.4 months compared with patients receiving chemotherapy. Read more...

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