Abstract
Product description
The present Competitive Intelligence Report about PI3K-AKT-mTOR Inhibitors
provides a competitor evaluation in the field of novel molecular entities
inhibiting members of the phosphatidyl-inositol-3 kinase (PI3K) / Akt /
mammalian target of rapamycin (mTOR) pathway for treatment of cancer or
inflammatory diseases as of July 2009. Purchase of the downloadable pdf report
includes a 6-month online access to the data of the report and any updates
since the publication date. Credentials to access the database will be sent by
e-mail and allow online work with the project data to print or export an
individual report.
The phosphatidylinositol-3-kinase (PI3K)/Akt/mammalian target of rapamycin
(mTOR) signaling pathway plays a critical role in the regulation of cellular
growth, survival, and proliferation. Dysregulation of this pathway, as a
result of genetic mutations and amplifications, is implicated in a variety of
human cancers. Therefore, each of the three components of the pathway alone
and in combination has emerged as a key target for the treatment of cancer.
While first generation therapeutic agents currently in clinical evaluation
preferably are pan-PI3K inhibitors, next generation selective PI3K inhibitors
are targeting one or several different subclasses.
However, only a short time ago, the paradigm existed that drugs targeted to
the four PI3K class I isoforms would be too toxic for use in cancer therapy
due to effects on physiologic signaling. Since that time, studies have
delineated the roles of these four isoforms in nonpathologic signaling as well
as their roles in cancer. An extensive effort has gone into developing agents
that inhibit one or more PI3K isoforms, e.g. alpha and beta, as well as
closely related proteins implicated in cancer. These agents have proved to be
tolerable and therapeutically beneficial in animal studies, and a number are
in clinical testing.
Numerous components of the PI3K pathway play an important role in the
expression and activation of inflammatory mediators, inflammatory cell
recruitment, immune cell function, airway remodelling and corticosteroid
insensitivity in asthma. More recently studies exploring the specific roles of
different PI3K catalytic subunit isoforms in asthma have been initiated.
Several of these have highlighted the importance of the delta isoform as a
novel target for therapeutic intervention in asthma.
Two mTOR complexes have been characterized, termed mTORC1 (mTOR complex-1) and
mTORC2. mTORC1 phosphorylates the hydrophobic motif of S6K, whereas mTORC2
phosphorylates the hydrophobic motif of Akt and SGK. The central role of mTOR
in controlling key cellular growth and survival pathways has sparked interest
in discovering mTOR inhibitors that bind to the ATP site and therefore target
both mTORC2 and mTORC1 (mTORC2 is resistant to rapamycin).
The report includes a compilation of current active projects in research and
development of PI3K-AKT-mTOR inhibitors in oncology and other indications. In
addition, the report lists company-specific R&D pipelines of PI3K-AKT-mTOR
inhibitors. Competitor projects are listed in a tabular format providing
information on:
- Drug Codes,
- Target / Mechanism of Action,
- Class of Compound,
- Company,
- Product Category,
- Indication,
- R&D Stage and
- additional comments with a hyperlink leading to the source of information.
Index
- Selective PI3K Inhibitors in Oncology Indications
- Selective PI3K Inhibitors in Inflammatory and Other Indications
- Non-Specific PI3K Inhibitors in Oncology Indications
- Dual PI3K/mTOR Inhibitors
- Selective mTOR Inhibitors in Oncology Indications
- Selective mTOR Inhibitors in Inflammatory and Other Indications
- Selective AKT Inhibitors in Oncology Indications
- AKT Dual Pathway Inhibitors in Oncology Indications
- Non-Specific AKT Inhibitors in Oncology Indications
Corporate PI3K-AKT-mTOR Inhibitor R&D Pipelines
- Abbott
- Abraxis Biosciences
- Aeterna Zentaris
- Ariad Pharmaceuticals
- Arno Therapeutics
- Astex Pharmaceuticals
- AstraZeneca
- Bayer Schering Pharma
- Biotica
- Calistoga Pharmaceuticals
- Cellzome
- CompleGen
- Eli Lilly
- Enzon Pharmaceuticals
- Exelixis
- Genentech
- GlaxoSmithKline (GSK)
- ICON
- Intellikine
- Isotechnika
- Keryx Biopharmaceuticals
- MacuSight
- Merck
- Novartis
- Oncothyreon
- OSI Pharmaceuticals
- Pfizer
- Piramal Life Sciences
- Roche
- S*Bio
- Samtheo Biopharma
- Sanofi-aventis
- Santen Pharmaceutical
- Semafore Pharmaceuticals
- SRI International
- Teva Pharmaceutical
- TopoTarget
- VioQuest Pharmaceuticals
- Wilex
- Wyeth
- Xcovery
- Zenyaku Kogyo
Table of Contents
- Selective PI3K Inhibitors in Oncology Indications
- Selective PI3K Inhibitors in Inflammatory and Other Indications
- Non-Specific PI3K Inhibitors in Oncology Indications
- Dual PI3K/mTOR Inhibitors in Oncology Indications
- Selective mTOR Inhibitors in Oncology Indications
- Selective mTOR Inhibitors in Inflammatory and Other Indications
- Selective AKT Inhibitors in Oncology Indications
- AKT Dual Pathway Inhibitors in Oncology Indications
- Non-Specific AKT Inhibitors in Oncology Indications
Corporate PI3K-AKT-mTOR Inhibitor R&D Pipelines
- Abbott
- Abraxis Biosciences
- Aeterna Zentaris
- Ariad Pharmaceuticals
- Arno Therapeutics
- Astex Pharmaceuticals
- AstraZeneca
- Bayer Schering Pharma
- Biotica
- Calistoga Pharmaceuticals
- Cellzome
- CompleGen
- Eli Lilly
- Enzon Pharmaceuticals
- Exelixis
- Genentech
- GlaxoSmithKline (GSK)
- ICON
- Intellikine
- Isotechnika
- Keryx Biopharmaceuticals
- MacuSight
- Merck
- Novartis
- Oncothyreon
- OSI Pharmaceuticals
- Pfizer
- Piramal Life Sciences
- Roche
- S*Bio
- Samtheo Biopharma
- Sanofi-aventis
- Santen Pharmaceutical
- Semafore Pharmaceuticals
- SRI International
- Teva Pharmaceutical
- TopoTarget
- VioQuest Pharmaceuticals
- Wilex
- Wyeth
- Xcovery
- Zenyaku Kogyo
