The present Competitive Intelligence Report about Coagulation Factors provides a competitor evaluation in the field of plasma-derived and recombinant coagulation factors for topical or systemic administration to treat hereditary or acquired coagulation disorders as of October 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 present Competitive Intelligence Report about PDGF-R agonists and antagonists provides a competitor evaluation in the field of platelet derived growth factor receptor (PDGF-R) or PDGF targeting molecules for wound healing, bone formation or treatment of cancer as of October 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 present Competitive Intelligence Report about EGF-R agonists and antagonists provides a competitor evaluation in the field of epidermal growth factor receptor (EGF-R; ErbB1) targeting molecules for wound healing or treatment of cancer as of September 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 present Competitive Intelligence Report about Her2 receptor antagonists provides a competitor evaluation in the field of Her2 (ErbB2) receptor targeting molecules for treatment of cancer as of September 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.

Ras-Raf-MEK-ERK Inhibitors

Product description

The present Competitive Intelligence Report about Ras-Raf-MEK-ERK Inhibitors provides a competitor evaluation in the field of synthetic and biologic molecules targeting Ras-Raf-MEK-ERK pathway for treatment of cancer as of May 2009.

The mitogen activated protein kinases (MAPKs) are conserved proteins that regulate cell growth, division and death. Although activated in the cytosol, the MAPKs translocate to the nucleus upon activation and phosphorylate a large number of nuclear proteins. Investigating how Ras transmits extracellular growth signals, the MAPK pathway has emerged as the crucial route between membrane-bound Ras and the nucleus. The MAPK pathway represents a cascade of phosphorylation events including three pivotal kinases, namely Raf, MEK (MAP kinase kinase), and ERK (MAP kinase).

NGF Agonists & Antagonists

Product description

The present Competitive Intelligence Report about Nerve Growth Factor (NGF) Agonists & Antagonists provides a competitor evaluation in the field of investigational antibodies, small molecules and gene therapeutic approaches for treatment of chronic pain or Alzheimer’s disease and peripheral neuropathies as of May 2009.

Nerve growth factor (NGF) is the prototypical member of the family of neurotrophin growth factors that are involved in the growth and survival of nervous tissue. NGF and its receptors, the tyrosine-kinase receptor TrkA and the p75 NTR receptor are responsible for the survival and maintenance of specific subsets of peripheral neurons and basal forebrain cholinergic nuclei during development and maturation.

In the adult peripheral nervous system, NGF signaling plays a key role in pain transduction mechanisms. Furthermore, NGF levels are increased in inflammatory processes and administration of exogenous NGF leads to hyperalgesia, hypersensitivity to thermal stimulation and muscular pain. NGF plays a critical role in hyperalgesia and allodynia as established in animal models. Antagonists of NGF were able to prevent and even to treat neuropathic and inflammatory pain. Clinical proof of concept (PoC) has been demonstrated for antibodies against NGF. The most advanced molecule is currently being investigated in a broad phase III program of osteoarthritis pain with several phase II PoC studies in a broader range of pain conditions. Further anti-NGF antibodies are in the pipeline and small molecule inhibitors are emerging.

NGF is not only the target for antagonists but may also be used as an agonist to treat Alzheimer’s disease. NGF stimulates the function and prevents the death of an important cell type in the brain that degenerates in Alzheimer’s disease (the “cholinergic neuron”). In animal studies, NGF improved memory and prevents degeneration of cells resulting from injury, overproduction of amyloid, or aging. Several clinical studies were performed or are ongoing with intracerebral administration of the protein, the DNA of NGF or cells expressing NGF to evaluate its therapeutic role in patients with Alzheimer’s disease. Availability of small molecules increasing the availability of NGF in the peripheral nervous system allowed investigation of its effects on peripheral neuropathies in ongoing clinical trials.

Elastase Inhibitors

Product description

The present Competitive Intelligence Report about elastase inhibitors provides a competitor evaluation in the field of human plasma-derived, recombinant, transgenic, synthetic and gene therapeutic approaches for treatment of lung emphysema caused by congenital deficiency of antitrypsin or for treatment of chronic obstructive pulmonary disease (COPD) as of May 2009.

Neutrophil elastase (NE) is a serine protease, expressed mainly by neutrophils, that is capable of degrading a variety of structural proteins of the extracellular matrix. Infiltration of activated neutrophils and excessive NE activity have been implicated in several lung diseases, including acute lung injury, cystic fibrosis, pulmonary fibrosis and COPD. Thus, a NE inhibitor targeting excessive NE activity in lung tissue could have good therapeutic potential.

Novel Mitotic Kinase Inhibitors

Product description

The present Competitive Intelligence Report about Novel Mitotic Kinase Inhibitors provides a competitor evaluation in the field of synthetic molecules targeting polo-like kinase 1 (Plk-1), cyclin-dependent kinase (CDK) or aurora kinase for treatment of cancer as of June 2009.

Mitosis, a central event in tumor growth, is highly regulated to ensure accurate and equal segregation of genetic materials from parent cells to daughter cells. Main effectors of this process are mitotic spindles and centrosomes.157 Disruption of the process results in aneuploidy, and genomic instability renders the cellular condition optimal for apoptosis to occur. The rationale of targeting mitosis in cancer therapy is substantiated by the successful clinical development of tubulin-disrupting agents, such as vinca alkaloids and taxanes.

The coordination of progression through mitosis is mainly orchestrated by protein phosphorylation insured by several serine/threonine kinases of which the three main mitotic kinase families are the cyclin-dependent kinase CDKs), the polo-like kinases (Plks), and the Aurora kinases.

Attention-Deficit Hyperactivity Disorder (ADHD)

Product description

The present Competitive Intelligence Report about Attention-Deficit Hyperactivity Disoder (ADHD) provides a competitor evaluation in the field of approved and investigational drugs for treatment of ADHD as of March 2009.

Attention-deficit hyperactivity disorder (ADHD) is a common and highly heritable neurodevelopmental psychiatric disease. It is also an indication for commercially successful drugs. The major ADHD drugs posted 2008 sales of US$ 3.9 bln. The current generation of ADHD treatments are mostly CNS stimulants. Although the major classes such as amphetamine/lisdexamfetamine, methylphenidate and dexmethylphenidate have lost patent protection for the substance, the use of extended release or topical drug delivery formulations have maintained a rich source of revenues for major players J&J, Shire, Eli Lilly and Novartis. As many parents are concerned about the use of CNS stimulants for treatment of their kids due to their addictive properties, research is focused on new non-stimulant drug targets. Most of them are in clinical phase I and II evaluation and include reuptake inhibitors, glutaminerigic substances, histamine antagonists and nicotinic receptor agonists

Amyotrophic Lateral Sclerosis (ALS) / Lou Gehrig's disease

Product description

The present Competitive Intelligence Report about Amyotrophic Lateral Sclerosis (ALS) / Lou Gehrig’s disease provides a competitor evaluation about new treatments in the R&D pipeline of amyotrophic lateral sclerosis (ALS) / Lou Gehrig’s disease as of March 2009.

Amyotrophic lateral sclerosis (ALS, also called Lou Gehrig's disease) is a rapidly progressing, motor neuron disease characterized by the gradual degeneration and death of motor neurons. When muscles in the diaphragm and chest wall fail, patients lose the ability to breathe without ventilatory support. Most people with ALS die from respiratory failure. Approximately 120, 000 new cases are diagnosed each year. No cure has yet been found for ALS. There is one FDA approved drug, riluzole, that modestly slows the progression of ALS.

Sphingosine-1-Phosphate (S1P)

Product description

The present Competitive Intelligence Report about Sphingosine-1-Phosphate (S1P) provides a competitor evaluation in the field of molecules interacting with the sphingosine-1-phosphate pathway as of April 2009. Among these molecules are S1P and selective S1P1 receptor agonists or S1P lyase inhibitors for treatment of inflammatory disease such as multiple sclerosis, psoriasis, asthma and rheumatoid arthritis. Antibodies targeting S1P and inhibitors of sphingosine kinase have promise for treatment of cancer

Sphingosine-1-phospate (S1P) is a phospholipid released by platelets, mast and other cells. It is now known that S1P stimulates at least five different G-protein coupled receptors (GPCRs): S1P1, S1P2, S1P3, S1P4, and S1P5. Activation of these GPCRs mediates a complex variety of biological responses, such as lymphocyte migration, endothelial cell proliferation, blood vessel constriction, heart rate modulation and others. Selective S1P1 receptor agonists inhibit lymphocyte migration out of lymphoid tissue into the lymphatic and blood circulation, thereby reducing peripheral lymphocyte counts and preventing lymphocyte recruitment to sites of inflammation.

PARP Inhibitors

Product description

The present Competitive Intelligence Report about PARP Inhibitors provides a competitor evaluation in the field of investigational small molecules inhibiting poly-adenyl-ribose polymerase (PARP) for treatment of cancer as of April 2009.

Poly (ADP-ribose) polymerases (PARPs) are a family of nuclear enzymes implicated in the regulation of multiple physiological cellular functions, including DNA repair, gene transcription, protein modification and cell signaling. Over-activation of PARP results in pathologic alteration of cellular metabolism, activation of inflammatory pathways, perturbation of cellular energetics, and cell death through necrosis or apoptosis. Because of its involvement in DNA repair, PARP has been implicated in the development of anti-tumor drug resistance. Targeting PARP is an approach in solid tumor therapy for potentiating the effects of chemotherapy and of radiation therapy and for potentially reducing antitumor drug resistance or resensitizing resistant patients to antitumor therapies. The most advanced projects are in phase II studies of solid tumors.

Hypoxia-Inducible Factor (HIF)

Product description

The present Competitive Intelligence Report about Hypoxia-Inducible Factor (HIF) provides a competitor evaluation in the field of investigational small molecules and RNA inhibiting HIF-1alpha or HIF-2 for treatment of cancer or acting as HIF agonists to induce angiogenesis as of April 2009.

Hypoxia-inducible factor 1 (HIF-1) is a key regulator of angiogenic and glucose metabolism processes utilised by tumour cells for survival and growth under hypoxic conditions. While HIF-1α protein is found in a wide variety of human primary tumors, it is only produced at very low levels in normal tissue. Because of the important role that HIF-1α plays in regulating the response of growing tumors to hypoxia, the protein is expected to have substantial value as a target for therapeutic intervention. The protein is a key regulator of a large number of genes important in cancer biology, including genes that regulate angiogenesis, cell metabolism, cell proliferation, cell death (apoptosis) and cell invasion. The first molecules inhibiting HIF-1alpha have entered clinical development and others are to follow shortly including small molecules and RNA interfering agents.

CD3 Antagonists

Product description

The present Competitive Intelligence Report about CD3 Antagonists provides a competitor evaluation in the field of approved and investigational antibodies and other biologic constructs targeting CD3 for treatment of autoimmune diseases and cancer as of March 2009.

CD3 is a T lymphocyte receptor involved in normal cell signaling. Antagonists of CD3 are thought to work by blocking the function of T effector cells that attack the body’s tissues and cause autoimmune disease while inducing a subset of T cells known as T regulatory cells. It is thought that the T regulatory cells may protect against T effector cell damage well after the drug has been eliminated from the body. CD3 antagonist antibodies are currently being evaluated in number of inflammatory or autoimmune diseases, especially in type 1 diabetes but also in transplantation, psoriasis, Crohn’s disease and rheumatoid arthritis. The most advanced programs are in phase III.

EpCAM Antagonists

Product description

The present Competitive Intelligence Report about EpCAM Antagonists provides a competitor evaluation in the field of investigational antibodies and antibody-based constructs targeting epithelial cell adhesion molecule (EpCAM) for treatment of cancer as of April 2009.

Epithelial cell adhesion molecule (EpCAM; CD326) is a cell surface protein that is frequently expressed at high level on most solid tumor types, including prostate, breast, colon, gastric, ovarian, pancreatic and lung cancer. Overexpression of EpCAM has been shown to promote the proliferation, migration and invasiveness of breast cancer cells. Moreover, expression of EpCAM is associated with decreased survival in a number of cancer indications, including breast, gall bladder, bile duct, ovarian and ampullary pancreatic cancer. Most of the currently ongoing projects targeting EpCAM are antibodies or antibody-based constructs with an additional payload or effector function to enhance efficacy. Among these constructs are immunotoxins, immunocytokines and T-cell recruitment via CD3 targeting. Recently, the first EpCAM targeting antibody was recommended for approval in the European Union. Further molecules are being evaluated in ovarian cancer, gastric cancer, small-cell lung cancer, breast cancer and colorectal cancer.