New insect repellant may be thousands of times stronger than DEET

In continuation of mosquito repellants and DEET

Researchers report the identification and characterization of an Orco family agonist, VUAA1, using the Anopheles gambiae coreceptor (AgOrco) and other orthologues. These studies reveal that the Orco family can form functional ion channels in the absence of an odor-binding OR, and in addition, demonstrate a first-in-class agonist to further research in insect OR signaling. In light of the extraordinary conservation and widespread expression of the Orco family, VUAA1 represents a powerful new family of compounds that can be used to disrupt the destructive behaviors of nuisance insects, agricultural pests, and disease vectors alike...

New insect repellant may be thousands of times stronger than DEET

Ref : http://www.pnas.org/content/early/2011/05/04/1102425108#aff-1

Novel two-drug combination cures young patient with extensively drug-resistant tuberculosis

The combination of meropenem (above structure)  with clavulanate (right structure-potassium salt)  has high antimycobacterial activity in vitro against extensively drug-resistant Mycobacterium tuberculosis strains. Researchers report the successful use of this combination in association with linezolid (below structure)  in the management of an advanced extensively drug-resistant tuberculosis disease with complex second-line drug resistance in a 14-year-old teenager.

Ref : 1.Meropenem/Clavulanate and Linezolid Treatment for Extensively Drug-Resistant Tuberculosis

    2. http://www.einstein.yu.edu/uploadedFiles/PHD/2010%20Faculty%20Research%20Book.pdf

Australian TGA approves Biogen Idec's FAMPYRA to improve walking ability in patients with MS

We know the recent development about 'FAMPYRA' by "European Medicines Agency".....

Australian TGA approves Biogen Idec's FAMPYRA to improve walking ability in patients with MS...

First EffRx NDA accepted for filing by the FDA...

EffRx Pharmaceuticals SA, an Epalinges/Lausanne, Switzerland based drug delivery company announces that the New Drug Application (NDA) for the company's lead development program EX101 has been accepted for filing by the US Food and Drug Administration. EX101 is a proprietary buffered effervescent dosage form of alendronate sodium administered once weekly for treatment of osteoporosis in postmenopausal women and to increase bone mass in men with osteoporosis. The EX101 formulation is the first and only effervescent bisphosphonate alternative to tablets. EX101 has a pleasant taste of strawberry and is quickly and completely dissolved. 

About Alendronate : Alendronic acid or alendronate sodium ( sold as Fosamax by Merck) is a bisphosphonate drug used for osteoporosis and several other bone diseases. It is marketed alone as well as in combination with vitamin D (2,800 U and 5600 U, under the name Fosamax+D). Merck's U.S. patent on alendronate expired in 2008 and Merck lost a series of appeals to block a generic version of the drug from being certified by the FDA. On February 6, 2008, the US FDA approved the first generic versions of alendronate, which were marketed by Barr Pharmaceuticals and Teva Pharmaceuticals USA. Teva Pharmaceuticals manufactures generic alendronate in 5-milligram, 10-milligram, and 40-milligram daily doses, and in 35-milligram and 70-milligram weekly doses, while Barr made generic alendronate in 70-milligram tablets, which were taken once weekly. Barr pharmaceuticals were subsequently acquired by Teva in July 2008...

Ref : http://www.effrx.com/firsteffrxnda.htm

Regenerating nerve cells: Research offers hope in new treatment for spinal cord injuries

Regenerating nerve cells: Research offers hope in new treatment for spinal cord injuries

Clinical study: Celecoxib drug may treat breast cancer

In continuation of m update on Celecoxib

Clinical study: Celecoxib drug may treat breast cancer

World's first urine-based tuberculosis diagnostics tool

World's first urine-based tuberculosis diagnostics tool

Temsirolimus with chemotherapy may serve as promising therapy for mesothelioma

We know that Temsirolimus (CCI-779) is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the FDA in late May 2007.

But researchers in Austria have found that temsirolimus also may slow the growth of malignant pleural mesothelioma cells. Mesothelioma, a cancer that is usually caused by exposure to asbestos and may not appear until 30 to 50 years after exposure, frequently resists chemotherapy and radiation treatment........

Temsirolimus with chemotherapy may serve as promising therapy for mesothelioma.

Pfizer RA Drug Meets Study Goals

We knew that,  Tofacitinib (see structure, formerly tasocitinib is a drug being investigated by Pfizer for the treatment of rheumatoid arthritis (RA), psoriasis,inflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection. It is an inhibitor of the enzyme Janus kinase 3 (JAK3), which means that it interferes with the JAK-STAT signaling pathway that transmits information outside the cell into the cell nucleus, influencing DNA transcription.

Now Pfizer now claims that the drug has   met its key goals of reducing signs and symptoms of the condition in separate studies on patients over a 12-month and six-month period. Rheumatoid arthritis is a chronic inflammatory disease typically affecting joints.

The company's Oral Standard study involved 717 patients over a 12-month period with moderate-to-severe rheumatoid arthritis who had an inadequate response to the drug methotrexate. Meanwhile, the Oral Step study involved 399 patients over a six-month period with moderate-to-severe rheumatoid arthritis who did not have an adequate response to TNF inhibitor drugs.  Pfizer said no new safety signals emerged in the Oral Standard and Oral Step studies. A more detailed analysis off the data will be submitted to a future scientific meeting. 

The most common side effects of treatment with tofacitinib have included bronchitis, headache, infections, and gastrointestinal symptoms like nausea, vomiting, and diarrhea. More serious side effects in a mid-stage trial included lower levels of a type of white blood cell called neutrophils, higher cholesterol levels and increased creatinine levels.

Tofacitinib is a key developing drug for Pfizer and is also being studied as a potential treatment for psoriasis, inflammatory bowel disease, and renal transplant. A topical version of the drug is being studied as a psoriasis treatment and a dry eye disease treatment....

Press Release...

New research shows honey fights drug-resistant germs

In continuation of my update on antibacterial activity of honey....
New research shows honey fights drug-resistant germs

Scientists develop new compound for multiple sclerosis treatment

Scientists from the Florida campus of The Scripps Research Institute have developed the first of a new class of highly selective compounds that effectively suppresses the severity of multiple sclerosis in animal models. The new compound could provide new and potentially more effective therapeutic approaches to multiple sclerosis and other autoimmune diseases that affect patients worldwide.

As per the claim by the researchers, SR1001, a high-affinity synthetic ligand (first in a new class of compound, that is specific to both RORα and RORγt and which inhibits T_H17 cell differentiation and function),  binds specifically to the ligand-binding domains of RORα and RORγt, inducing a conformational change within the ligand-binding domain that encompasses the repositioning of helix 12 and leads to diminished affinity for co-activators and increased affinity for co-repressors, resulting in suppression of the receptors’ transcriptional activity. SR1001 inhibited the development of murine T_H17 cells, as demonstrated by inhibition of interleukin-17A gene expression and protein production. 

Furthermore, SR1001 inhibited the expression of cytokines when added to differentiated murine or human T_H17 cells. Finally, SR1001 effectively suppressed the clinical severity of autoimmune disease in mice. These data demonstrate the feasibility of targeting the orphan receptors RORα and RORγt to inhibit specifically T_H17 cell differentiation and function, and indicate that this novel class of compound has potential utility in the treatment of autoimmune diseases.....

Ref : http://www.nature.com/nature/journal/v472/n7344/full/nature10075.html

FDA panel votes in favour of Sunitib (Sutent) for pancreatic tumors....

In continuation of my update on sutent/sunitib....

 Pfizer Inc. announced this Tuesday that its oral multi-kinase inhibitor "Sutent" (see structure)  was determined as having a favourable benefit-risk profile by an oncology advisory committee of the FDA for the treatment of unresectable pancreatic neuroendocrine tumors. The panel voted 8-2 in favour of Sutent – generically called Sunitib malate.

Advanced pancreatic neuroendocrine tumour or NET, is a rare, life-threatening and difficult-to-treat form of cancer that accounts for approximately 22-28 percent of all neuroendocrine tumours. Nearly 90 percent of patients are initially diagnosed with locally advanced or metastatic disease, or cancer that has spread to other organs. An unresectable tumour is one that cannot be removed or resected by surgery.

 More...

Sutent or sunitinib malate targets vascular endothelial growth factor receptor or VEGFR and platelet-derived growth factor receptor or PDGFR, both of which are expressed by many types of solid tumours. The two targets are involved in tumours acquiring blood vessels, oxygen and nutrients needed for growth. 

Sunitinib was approved in 2006 in the United States for treating locally advanced or metastatic renal cell carcinoma and for imatinib-refractory or -intolerant gastrointestinal stromal tumour (GIST). It was approved for treating PNET in 2010 in Europe. A decision on approval is expected by the end of 2011, according to a company spokesperson....

FDA approves new targeted therapy to treat men with advanced prostate cancer..

In continuation of my update on  Abiraterone ....

We know that, Abiraterone (tradename Zytiga) is a drug currently under investigation for use in castration-resistant prostate cancer (formerly hormone-resistant or hormone-refractory prostate cancer) (prostate cancer not responding to androgen deprivation or treatment with antiandrogens). 

It blocks the formation of testosterone by inhibiting CYP17A1 (CYP450c17), an enzyme also known as 17α-hydroxylase/17,20 lyase. This enzyme is involved in the formation of DHEA and androstenedione, which may ultimately be metabolized into testosterone.This drug was initially discovered at the Institute of Cancer Research in London. 

Recently  approved abiraterone. It improves, by nearly four months, the overall survival rate of men with metastatic chemotherapy- and castration-resistant prostate cancer. Since 2005, the Prostate Cancer Foundation invested $8.2 million in over six research projects to advance independent academic research for investigating abiraterone's mechanism of action and biomarkers to predict patient response...

More....

Ohio State biophysicist disrupts cellular messages through fragment-based drug design

In continuation of my update  on FBDD..

Ohio State biophysicist disrupts cellular messages through fragment-based drug design

Maxwell Biotech, Sequella enter license agreement to commercialize SQ109 for TB treatment

In continuation of my update on drug discovery on TB...
Maxwell Biotech, Sequella enter license agreement to commercialize SQ109 for TB treatment.....