Lostartan can reduce cigarette smoke-induced lung injury

Researchers from Johns Hopkins University, BaltimoreLostartan, lead by have found that, Dr.Enid R. Neptune Losartan a drug used widely in the clinic (e.g., to treat high blood pressure), reduced lung disease in mice caused by exposure to cigarette smoke. Losartan blocks the protein angiotensin receptor type 1, and its effects on cigarette smoke-induced lung injury were a result of the fact that blocking angiotensin receptor type 1 leads to a decrease in levels of the soluble molecule TGF-beta. The authors therefore suggest that other TGF-beta-targeted therapeutics might also be viable candidates for the treatment of  chronic obstructive pulmonary disease, COPD....

Ref : http://www.jci.org/articles/view/46215?search[article_text]=&search[authors_text]=Enid+Neptune

MK 1775 shows promise against sarcomas..........

   2-Allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6- (4-(4-methyl- piperazin-1-yl)phenylamino)-1H-pyra -zolo [3,4-d]pyrimidin-3(2H)-one.  

MK 1775 (see structure), a small, selective inhibitor molecule, has been found to be active against many sarcomas when tested by researchers at Moffitt Cancer Center in Tampa, Fla. Researchers found that MK1775 treatment induces apoptopic cell death in four sarcoma cell lines at clinically relevant doses.

To further prove that inhibition of Wee1 by MK1775 leads to mitotic cell death in sarcomas cells, the researchers performed additional studies, including studies on sarcomas related to mutations, such as with the p53 gene. They also showed that MK1775 was an active inhibitor of Wee1 regardless of the p53 mutation status of the tumors in the cell lines tested.

"The cytotoxic effect of Wee1 inhibition on sarcoma cells appears to be independent of p53 mutation status following our testing sarcoma cell lines with different p53 mutations," he said. "All of them were highly sensitive to MK1775, suggesting that Wee1 inhibition may represent a novel approach in the treatment of sarcomas."

Researchers concluded that their laboratory tests on sarcoma cell lines suggest that MK1775 is effective as a monotherapy even in the cell lines that include p53 wild, p53 null and p53 mutant statuses.

More... 

Oncolytics REOLYSIN-Gemzar combination Phase 2 pancreatic cancer clinical trial meets primary endpoint

In continuation of my update on gemcitabine

Oncolytics REOLYSIN-Gemzar combination Phase 2 pancreatic cancer clinical trial meets primary endpoint: Oncolytics Biotech Inc. announced the interim data from a Phase 2 clinical trial using intravenous administration of REOLYSIN® in combination with gemcitabine (Gemzar) in patients with advanced pancreatic cancer (REO 017) indicated that the clinical study had successfully reached its primary endpoint, and that the drug combination is active.

New Antibodies Treat Autoimmune Disease like Crohn's in Mice....

 Synthetic drugs treat (below structure)  Crohn's disease in mice.................

[zinc-binding motif (where X is any amino acid) in MMPs, a symmetrical tripodal tris-imidazol–zinc complex (Zn-tripod; ZnC₃₆H₅₉N₁₁O₈)]


New Antibodies Treat Autoimmune Disease in Mice
Ref : http://www.nature.com/nm/journal/vaop/ncurrent/full/nm.2582.html

Salk scientists develop new drug that improves memory and prevents brain damage in mice

A new drug candidate may be the first capable of halting the devastating mental decline of Alzheimer's disease, based on the findings by a research group of Salk's Cellular Neurobiology Laboratory.

When given to mice with Alzheimer's, the drug, known as J147 (see structure), improved memory and prevented brain damage caused by the disease. The new compound, developed by scientists at the Salk Institute for Biological Studies, could be tested for treatment of the disease in humans in the near future.

"J147 enhances memory in both normal and Alzheimer's mice and also protects the brain from the loss of synaptic connections," says David Schubert, the head of Salk's Cellular Neurobiology Laboratory, whose team developed the new drug. "No drugs on the market for Alzheimer's have both of these properties."

Although it is yet unknown whether the compound will prove safe and effective in humans, the Salk researchers' say their results suggest the drug may hold potential for treatment of people with Alzheimer's.

More.....

Notch inhibitor appears to treat breast cancer....

In a novel therapeutic approach to treating breast cancer, Loyola University Medical Center researchers are reporting positive results from a clinical trial of a drug that targets tumor stem cells. A pilot study at Loyola found that an experimental drug known as a "notch inhibitor" appears to block this process by turning off key genes. Prior to surgery, the patients received one of two commonly used drugs, tamoxifen or letrozole. These drugs work by blocking estrogen stimulation of breast cancer cells. In addition to tamoxifen or letrozole, patients also received the experimental notch-inhibitor drug, MK-0752 (see structure).

 "The notch inhibitor appears to be doing what it is intended to do," said Dr. Clodia Osipo....

There were minimal side effects from either the notch inhibitor or the estrogen-blocking drugs. One patient experienced puffy eyes and coughing and four patients experienced facial acne. No patients experienced diarrhea or surgical complications.

Ref : Loyola Medicine News Release

Zoledronic Acid Shows Long-Term Benefit in Survivorship for Premenopausal ER-Positive Breast Cancer

In continuation of my update on Zoledronic acid....

Zoledronic Acid Shows Long-Term Benefit in Survivorship for Premenopausal ER-Positive Breast Cancer

Scientists identify why African naked mole-rat feels no pain when exposed to acid

In continuation of my update  naked mole-rat

Scientists identify why African naked mole-rat feels no pain when exposed to acid: British researchers of the Max Delbr-ck Center for Molecular Medicine (MDC) Berlin-Buch have found out why the African naked mole-rat (Heterocephalus glaber), one of the world's most unusual mammals, feels no pain when exposed to acid.

Ref : http://www.mdc-berlin.de/en/news/2011/20111220-mdc_researchers__ion_channel_makes_african1/index.html

Drug Duo of Ixabepilone and sunitinib Kills Chemotherapy-resistant Ovarian Cancer Cells......

In continuation of Sunitinib...

The use of two drugs never tried in combination before in ovarian cancer resulted in a 70 percent destruction of cancer cells already resistant to commonly used chemotherapy agents, say researchers at Mayo Clinic in Florida. Research  suggests that this combination (ixabepilone and sunitinib), might offer a much needed treatment option for women with advanced ovarian cancer. When caught at late stages, ovarian cancer is often fatal because it progressively stops responding to the chemotherapy drugs used to treat it. The finding also highlights the importance of the role of a molecule, RhoB, that the researchers say is activated by the drug duo. Neither drug is approved for use in ovarian cancer. Ixabepilone is a chemotherapy drug that, like other taxane drugs, targets the microtubules and stops dividing cells from forming a spindle. It has been approved for use in metastatic breast cancer. Sunitinib, approved for use in kidney cancer, belongs to a class of tyrosine kinase inhibitors that stops growth signals from reaching inside cancer cells.

                                           

     Sunitinib                                  Ixabepilone

Ref : http://www.mayoclinic.org/news2011-jax/6573.html

Geron Initiates Phase 2 Trial of GRN1005 in Brain Metastases from Breast Cancer

In continuation of my update on Paclitaxel and drug discovery....

Geron Corporation, announced the initiation of GRABM-B (GRN1005 Against Brain Metastases - Breast Cancer), a Phase 2 clinical trial to evaluate GRN1005 in patients with brain metastases arising from breast cancer. GRN1005 is the company's lead LRP-directed peptide-drug conjugate (LRP-directed PDC) that consists of the cytotoxic drug, paclitaxel, linked to a peptide (Angiopep-2) that targets the LRP receptor to cross the blood-brain barrier (BBB) and to target tumors in the brain.

The purpose of the Phase 2 study is to assess the efficacy, safety and tolerability of GRN1005 in patients with brain metastases from breast cancer. The trial is designed to include 100 patients with HER2 positive or HER2 negative metastatic breast cancer (MBC) disease, who will be assessed in two separate cohorts of 50 patients each.....

More...

Ref : http://www.geron.com/media/pressview.aspx?id=1287

Drug combination highly effective for newly diagnosed myeloma patients......

A three-drug combination treatment for the blood cancer multiple myeloma compares favorably to the best established therapy for newly diagnosed patients, according to a multi-center study led by Andrzej Jakubowiak, MD, PhD, professor of medicine and director of the multiple myeloma program at the University of Chicago Medical Center.

( Carfilzomib)

 (Lenalidomide)

( Thalidomide)

The combination includes an investigational medicine called carfilzomib combined with two standard medications: lenalidomide, an analogue of thalidomide, and low-dose dexamethasone, an anti-inflammatory with anti-cancer properties.

"This combination appears to deliver everything we expected and more," said Jakubowiak, who came to the University of Chicago this fall from the University of Michigan. "We have seen excellent efficacy — the best reported to date — without the neurotoxicity that has been problematic with other drug combinations."

Ref : http://www.uchospitals.edu/news/2011/20111206-myeloma.html

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Synta's ganetespib shows potent in vitro and in vivo activity against multiple breast cancer types

Synta researchers  have reported that, Ganetespib (structure)  shows potent in vitro and in vivo activity against multiple types of breast cancer including HER2-positive, ER/PR positive, triple-negative, and inflammatory breast cancer. 

"These results demonstrating that ganetespib potently inhibits key signaling pathways involved in the growth and proliferation of multiple forms of breast cancer are encouraging, and supportive of the results presented earlier at this meeting showing single-agent, anti-tumor activity in patients with breast cancer who have progressed on or failed to respond to multiple prior therapies," said Vojo Vukovic, M.D., Ph.D., Chief Medical Officer, Synta. 

Researchers conclude that, the combined preclinical and clinical results create a strong rationale for advancing ganetespib development in both HER2-positive and triple-negative breast cancer.

More : http://phoenix.corporate-ir.net/phoenix.zhtml?c=147988&p=irol-newsArticle&ID=1638540&highlight=

Combination of bortezomib and panobinostat shows promise against advanced multiple myeloma

In co\continuation of  my update on Bortezomib...

A phase 2 clinical trial has shown that pairing bortezomib with an experimental drug, panobinostat: Panobinostat is a histone deacetylase (HDAC) inhibitor, a type of drug that blocks key processes involved in gene expression and protein degradation. Panobinostat clogs up a protein disposal mechanism in myeloma cells so that harmful byproducts accumulate and eventually cause programmed cell death.(see below structure), may be a promising new treatment for such patients, Dana-Farber Cancer Institute researchers say.

 The PANORAMA 2 trial included 53 patients with relapsed multiple myeloma who had undergone multiple rounds of prior treatment and, in more than half, also stem cell transplant. The researchers reported on 44 patients receiving the panobinostat-bortezomib-dexamethasone combination.

Results showed that in the first phase of the treatment, 9 of the patients had at least a partial response of their disease, and 2 of the 9 saw their myeloma almost disappear, a so-called near complete response. Another 7 patients experienced minimal response, which is also associated with clinical benefit. 

More : http://ash.confex.com/ash/2011/webprogram/Paper41145.html

Ruxolinitib reduces spleen size by 35% in patients with myelofibrosis

In continuation of my ruxolinitib

In a major advance in treatment, a multicenter study found that ruxolinitib did a better job than off-label chemotherapy drugs reducing the terrible symptoms associated with myelofibrosis, including pain, enlarged spleen, anemia, fever, chills, fatigue, and weight loss. 

Only about 10 percent of myelofibrosis patients are eligible for a bone marrow transplant and chemotherapy often falls short, Dr. Mesa says. A handful of off-label chemotherapy drugs have been modestly helpful, he says.

A randomized, double-blind clinical trial, known as the COMFORT-1 study, showed that ruxolinitib reduced spleen size by more than 35 percent in almost all of the 154 patients studied. An enlarged spleen, caused by sequestered over-proliferating blood cells, causes discomfort and can also lead to the need for blood transfusions and further medical complications for patients.

"The studies confirmed the drug is very effective. As a representative of a particular class of molecular inhibitors called JAK2 inhibitors, which are now being widely studied, ruxolinitib suggests this category will continue to be promising for myelofibrosis," Dr. Mesa says.

Ref : More...

American Friends of Tel Aviv University: Beating Superbugs with a High-Tech Cleanser

American Friends of Tel Aviv University: Beating Superbugs with a High-Tech Cleanser

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

UMass Amherst Researchers Test a Drug-Exercise Program Designed to Prevent Type 2 Diabetes

In continuation of my update on Metformin...

Kinesiology researcher Barry Braun of the University of Massachusetts Amherst and colleagues recently reported unexpected results of a study suggesting that exercise and one of the most commonly prescribed drugs for diabetes, metformin, each improves insulin resistance when used alone, but when used together, metformin blunted the full effect of a 12-week exercise program in pre-diabetic men and women.

Ref : http://www.umass.edu/newsoffice/newsreleases/articles/142505.php

Editorial: An apple a day keeps colitis away

In continuation on my update on the benefits of apple

Editorial: An apple a day keeps colitis away:

More : http://msuextension.org/publications/AgandNaturalResources/MT200812AG.pdf

'via Blog this'

European Commission approves Vyndaqel® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP)

We know that, Tafamidis (see structure) or Vyndaqel was discovered in the Jeffery W. Kelly Laboratory at The Scripps Research Institute using a structure-based drug design strategy and was developed at FoldRx pharmaceuticals, a biotechnology company led by Richard Labaudiniere that was acquired by Pfizer in 2010.

Tafamidis or Vyndaqel functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. In patients with FAP, this protein dissociates in a process that is rate limiting for aggregation including amyloid fibril formation, causing neurodegeneration and failure of the autonomic nervous system and/or the peripheral nervous system and/or the heart.

Now, European Commission has approved Vyndaqel^® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP) in adult patients with stage 1 symptomatic polyneuropathy.

More...

HSC NEWS - Bat plant could give some cancers a devil of a time

In a new study published this month in the Journal of the American Chemical Society, researchers with The University of Texas Health Science Center at San Antonio have pinpointed the cancer-fighting potential in the bat plant, or Tacca chantrieri......

HSC NEWS - Bat plant could give some cancers a devil of a time

FDA Approves Intermezzo.....

The U.S. Food and Drug Administration today approved Intermezzo (zolpidem tartrate sublingual tablets) for use as needed to treat insomnia characterized by middle-of-the-night waking followed by difficulty returning to sleep.

This is the first time the FDA has approved a drug for this condition. Intermezzo should only be used when a person has at least four hours of bedtime remaining. It should not be taken if alcohol has been consumed or with any other sleep aid....

More....

Coffee may protect against womb cancer: Study

 In continuation of my update on the benefits of coffee

A new study shows that regular intake of coffee may significantly lower risk for endometrial or womb cancer.

For the study the researchers looked at coffee consumption and endometrial cancer risk in more than 67,000 women aged between 34 and 59 enrolled in the long-running Nurses' Health Study. The researchers found that women who took more than four cups of coffee a day over a 26-year period were 25 percent less likely to get the cancer. Women who drank two to three cups a day were 7 percent less likely to get it. Drinking less than four cups a day was not associated with reduced risk. Furthermore drinking tea did not reduce the risk. Additionally drinking more than two cups of decaffeinated coffee a day was tied to a 22 percent reduced risk for endometrial cancer.

The benefit wasn't a complete surprise, since coffee has been shown to lower estrogen and insulin levels, and higher levels of these hormones have been associated with an increased risk of endometrial cancer. But the new findings do help to clarify how obesity, estrogen and coffee might interact in triggering tumors.

“It would be premature to make a recommendation that women drink coffee to lower their endometrial cancer risk,” study author Dr. Edward Giovannucci, professor of nutrition and epidemiology at Harvard School of Public Health...

Ref : http://cebp.aacrjournals.org/content/early/2011/10/03/1055-9965.EPI-11-0766.abstract?sid=d8d229ed-e4b4-4b7a-bc6a-f3f86cba4c0e

Cisplatin anti-cancer drug binds pervasively to RNA....

In continuation of my update on Cisplatin.....

An anti-cancer drug used extensively in chemotherapy binds pervasively to RNA -- up to 20-fold more than it does to DNA, a surprise finding that suggests new targeting approaches might be useful, according to University of Oregon researchers, lead by Victoria J. DeRose

Ref : http://uonews.uoregon.edu/archive/news-release/2011/11/cancer-drug-cisplatin-found-bind-glue-cellular-rna

Old drugs find new target for treating brain tumor

In continuation of erlotinib ................................

Old drugs find new target for treating brain tumor

Researchers discover new class of antimalarial compounds...

Researchers have discovered a group of chemical compounds that might one day be developed into drugs that can treat malaria infection in both the liver and the bloodstream. The study, which appears in the Nov. 18 issue of Science, was led by Elizabeth A. Winzeler, Ph.D., of the Scripps Research Institute in La Jolla, Calif., and was partially funded by the National Institute of Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health.

By screening more than 4,000 chemical compounds that had previously shown activity against blood-stage Plasmodium, the investigators searched for a compound that would also inhibit liver-stage parasites and whose protein structure would allow the modification necessary for future drug development. They found that a group of three related compounds, known collectively as the imidazolopiperazine (IP) cluster, fit these criteria. In addition, strains of Plasmodium that had acquired resistance to other malaria drugs were susceptible to the IP cluster.

Using the IP cluster as a foundation, the researchers designed a drug candidate, GNF179, that reduced levels of one Plasmodium species by 99.7 percent and extended survival by an average of 19 days when tested in malaria-infected mice. By examining infected cells, the researchers confirmed that GNF179 (see the structure) was active in the liver stage of infection. Rresearchers note that while additional studies will be needed to fully understand the drug's mechanism of action and its specific targets within the liver, this study provides a potential starting point for developing new dual-stage antimalarial drugs.....

More : http://www.sciencemag.org/content/early/2011/11/16/science.1211936.abstract

New efficient synthesis for Taxol ?

In continuation of my update on taxol....

Baran's group reports erecting that Rockefeller tree and adding the first few ornaments -- a molecule called taxadiene. A conventional taxadiene synthesis is inefficient and involves 26 steps to produce. The Baran group's method involves just 10 steps to produce many times what has been previously synthesized -- more than sufficient for planned research to find a way to efficiently produce Taxol®.

Innovation Leads to Access.....

The taxadiene synthesis is more than just a midway stop on the way to Taxol®. The current commercial Taxol® production method, which involves culturing cells from the yew tree, is more economical than any new synthesis is likely to be. Instead, Baran and his team are aiming to understand the processes used in nature to produce the compound, which are many times more efficient than those used by scientists to date. "It's my opinion that when there's a huge discrepancy between the efficiency of nature and humans, in the space between, there's innovation.

More specifically, lead researcher Phil Baran believes that, while developing an efficient synthesis for Taxol®, they will gain a fundamentally improved understanding of the chemistry involved and develop more widely applicable techniques. Such innovation could allow production of a whole range of taxanes currently inaccessible for drug discovery research either because the quantities researchers can produce are vanishingly small, or because they can't produce them at all. Control of the taxane oxidation process therefore offers the potential for discovering new and important drugs, perhaps even one or more that is better at fighting specific cancers than Taxol®.

Establishing the remaining steps between taxadiene and Taxol® or other more complex taxanes remains a challenging task that Baran estimates will take years.

"Nature has a choreography in the way she decorates the tree," he said. "It's a precise dance she has worked out over millennia. We have to figure out a way to bring that efficiency to the laboratory setting."

More... : http://www.nature.com/nchem/journal/vaop/ncurrent/full/nchem.1196.html

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF

In continuation of my up date on rivaroxaban.....

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF: The U.S. Food and Drug Administration today approved the anti-clotting drug Xarelto (rivaroxaban) to reduce the risk of stroke in people who have abnormal heart rhythm.

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

In continuation of my update on the benefits of nuts...

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

Crocin for multiple sclerosis?

Medical researchers at the University of Alberta have discovered that an active ingredient in the Persian spice saffron may be a potential treatment for diseases involving neuroinflammation, such as multiple sclerosis. Researchers found there is a compound in saffron, known as crocin (see the structure below), that exerts a protective effect in brain cell cultures and other models of MS. It prevented damage to cells that make myelin in the brain.

Lead researcher  Power said. "Myelin is insulation around nerves. MS is characterized by inflamed brain cells that have lost this protective insulation, which ultimately leads to neurodegeneration.......

More......

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

Ref : http://www.nature.com/ajg/journal/v106/n10/full/ajg2011201a.html

World's most efficient flexible organic light-emitting diodes created on plastic

World's most efficient flexible organic light-emitting diodes created on plastic

In continuation of my update on usefulness of benzodiazepine derivatives

Lundbeck Inc. presented interim data from its long-term, open-label extension study evaluating ONFI™ (clobazam see structure below) CIV for the adjunctive treatment of drop seizures associated with Lennox-Gastaut syndrome (LGS). Company claims that, these interim results support the reductions in drop seizure rates associated with ONFI when used as add-on therapy for adult and pediatric patients, two years of age or older, with a current or previous diagnosis of LGS. ....

More....

Biogen’s Multiple Sclerosis pill succeeds at a late phase clinical trial

Biogen Idec Inc. has reported success in a late stage clinical trial of its oral multiple sclerosis drug BG-12 (see below structure), a competitor's of Teva Pharmaceutical Industries’ Laquinimod. A 240-milligram dose of BG-12 administered two or three times a day significantly reduced the proportion of patients who relapsed by 49% and 50%, respectively, after two years compared with a placebo....

Company adds that, in addition to significantly reducing ARR, BG-12 met all secondary relapse and MRI endpoints for both dose regimens.....

Ref : http://www.biogenidec.com/PRESS_RELEASE_DETAILS.aspx?ID=5981&ReqId=1621631 

Leafy greens (broccoli and cabbage) protect the gut’s immune system

In continuation of my update on Broccoli and its usefulness 

Research from the Babraham Institute and the Medical Research Council (MRC), were able to prove that leafy greens protect a certain type of immune cell known as intra-epithelial lymphocytes (IELs). IELs play a crucial role in keeping the gut lining healthy and preventing ‘bad’ bacteria from entering the gut while maintaining the balance of ‘good’ bacteria which help us to break down our food. Researchers studied mice fed a diet containing many vitamins and minerals known to be essential for good health, but which lacked vegetables. Over three weeks the mice lost 70 to 80 per cent of IELs.

The research showed for the first time that mice fed a diet low in vegetables rapidly lose these specialised immune cells lining the intestinal tract, but not other immune cells. The team discovered that IELs depend on chemical signals from the digestive breakdown products of a substance called Indole-3-carbinol, high levels of which are found in vegetables like broccoli and cabbage.......

Ref :1. http://www.mrc.ac.uk/Newspublications/News/MRC008231
2.  http://www.sciencedirect.com/science/article/pii/S0092867411011366

INNOPHARMA Receives FDA Approval of Generic Levetiracetam Injection

In continuation of my update on Olanzapine......

INNOPHARMA Receives FDA Approval of Generic Levetiracetam Injection

Phase III Trial of Regorafenib in Metastatic Colorectal Cancer Meets Primary Endpoint of Improving Overall Survival...

Bayer HealthCare Pharmaceuticals, announced the results from its Phase III trial evaluating its investigational compound regorafenib (see structure below, BAY 73-4506) for the treatment of patients with metastatic colorectal cancer (mCRC) whose disease has progressed after approved standard therapies: The trial met its primary endpoint of statistically significant improvement in overall survival. 

This is the result of a pre-planned interim analysis conducted by an independent Data Monitoring Committee (DMC) of the CORRECT (Patients with metastatic colorectal cancer treated with regorafenib or placebo after failure of standard t herapy) trial. Per the recommendation of the DMC, the study has been unblinded and patients in the placebo arm will be offered treatment with regorafenib. In this trial, the safety and tolerability of regorafenib were generally as expected.

"These data are significant because they demonstrate that regorafenib increased overall survival in patients with heavily pretreated metastatic colorectal cancer, an area of high unmet medical need," said Kemal Malik .....

Ref : http://www.bayer.com/en/news-detail.aspx?newsid=15124

Researcher's compound disables bacteria instead of killing them

A microbiologist at the University of Wisconsin-Milwaukee (UWM) has discovered a different approach: Instead of killing the bacteria, why not disarm them, quashing disease without the worry of antibiotic resistance?

Ching-Hong Yang, associate professor of biological sciences, has developed a compound that shuts off the "valve" in a pathogen's DNA that allows it to invade and infect. The research is so promising that two private companies are testing it with an eye toward commercialization.

"Researchers analyzed the genomic defense pathways in plants to identify all the precursors to infection and  used the information to discover a group of novel small molecules that interrupt one channel in the intricate pathway system."..

Yang and collaborator Xin Chen, a professor of chemistry at Changzhou University in China, have tested the compound on two virulent bacteria that affect plants and one that attacks humans. They found it effective against all three and believe the compound can be applied to treatments for plants, animals and people.

Ref : Ching-Hong Yang et.al., 

WPI Research Shows How Cranberry Juice Fights Bacteria at the Molecular Level

The study tested proanthocyanidins or PACs, a group of flavonoids found in cranberries. Because they were thought to be the ingredient that gives the juice its infection-fighting properties, PACs have been considered a hopeful target for an effective extract. The new WPI report, however, shows that cranberry juice, itself, is far better at preventing biofilm formation, which is the precursor of infection, than PACs alone. The data is reported in the paper "Impact of Cranberry Juice and Proanthocyanidins on the Ability of Escherichia coli to Form Biofilms," which will be published on-line, ahead of print on Oct. 31, 2011, by the journal Food Science and Biotechnology.

WPI Research Shows How Cranberry Juice Fights Bacteria at the Molecular Level

New dual drug combinations in development for various cancers

New dual drug combinations in development for various cancers: A rarely used—and as yet largely unproven—approach to drug development has emerged as a significant tool in the effort to create high-impact new cancer drugs.

New data on novel gene-silencing oligonucleotide technology...

Idera announced new data on its novel gene-silencing oligonucleotide (GSO) technology at the Cell Symposium on Regulatory RNAs in Chicago, IL. In preclinical studies, systemic delivery of GSOs targeted to ApoB or PCSK9 mRNA caused a reduction in the level of the targeted mRNA and associated protein and resulted in a decrease in serum total cholesterol and LDL-cholesterol concentration. ApoB and PCSK9 are two validated targets associated with cardiovascular diseases.

In this study, Idera created 19mer GSOs for apolipoprotein B (ApoB) and proprotein convertase subtilisin/kexin type 9 (PCSK9) mRNA and evaluated their in vivo activity in mice following subcutaneous administration. The data demonstrate that treatment with each GSO led to a significant reduction in the concentration of the target associated mRNAs and protein. The effects were specific, with no significant effects being observed on ABCA1, ABCG1 or LXR mRNA levels. In addition, treatment with GSOs for either ApoB or PCSK9 resulted in a decrease in total serum cholesterol and LDL-cholesterol. 

More...

Yawning May Help the Brain Chill Out

Yawning May Help the Brain Chill Out: Yawning may be a natural way of regulating brain temperature, a new study suggests.U.S. researchers examined the frequency of yawns among 80 people in the winter and another 80 people in the summer and found seasonal...

HSV1 drugs could slow progression of Alzheimer's disease

HSV1 drugs could slow progression of Alzheimer's disease: Antiviral drugs used to target the herpes virus could be effective at slowing the progression of Alzheimer's disease (AD), a new study shows.

New Alzheimer's Drug Shows Early Promise

An experimental Alzheimer's disease drug, gantenerumab, may help lower levels of amyloid plaque in the brains of people with the disease, an early clinical trial indicates. Researchers claims that, of 16 people with mild-to-moderate Alzheimer's disease, those who received two to seven infusions of the experimental drug every four weeks showed marked reductions in the amount of plaque in their brains via imaging tests that were conducted several months after their treatments.....

More...

Ginger Supplements Might Ease Inflammation Linked to Colon Cancer..

A small, preliminary study finds that ginger root supplements seem to reduce inflammation in the intestines  a potential sign that the pills might reduce the risk of colon cancer. Previous research in animals has suggested that ginger can reduce inflammation but isn't potentially toxic to the stomach like aspirin, Zick noted. And scientists have linked chronic inflammation in the gut to colon cancer, suggesting that easing this inflammation could reduce the risk of the disease.

In the new study, Zick's team randomly assigned 30 people to take pills containing 2 grams of ground ginger root extract or a "dummy" placebo pill each day for 28 days. They measured the level of inflammation in the participants' intestines before and after the test period. The researchers found that the level of inflammation in the subjects who took the ginger pills fell by an average of 28 percent, while staying about the same in those who took the placebo.

Ref : http://cancerpreventionresearch.aacrjournals.org/content/early/2011/10/07/1940-6207.CAPR-11-0224.abstract

Teriflunomide drug reduces relapse rate of people with MS

 In continuation of my update on  Teriflunomide
A new oral drug has been shown in a large international clinical trial to significantly reduce the relapse rate of people with multiple sclerosis and to slow the progression of the disease.

More....

First combination drug to treat type 2 diabetes and high cholesterol receives FDA approval

In continuation of my update on Simvastin

The U.S. Food and Drug Administration recently approved Juvisync (sitagliptin and simvastatin), a fixed-dose combination (FDC) prescription medication that contains two previously approved medicines in one tablet for use in adults who need both sitagliptin and simvastatin.....

More....

Blueberry powder may control triple negative breast cancer

In continuation of my update on blue berry's usefulness....

Blueberry powder may control triple negative breast cancer: In several studies recently conducted at the Beckman Research Institute at the City of Hope, Duarte, CA researchers found that feeding blueberry powder to mice significantly reduced the growth and spread of triple negative breast cancer cells, a very aggressive form of cancer.

Health Canada approves Trajenta (linagliptin) for type 2 diabetes

Linagliptin (below structure, BI-1356, trade name Tradjenta) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes.Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly. Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Both GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output. Thus, linagliptin stimulates the release of insulin in a glucose-dependent manner and decreases the levels of glucagon in the circulation.

Now Health Canada approves....

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Novel drug shows promise for MLL leukemia

Novel drug shows promise for MLL leukemia:

According to British scientists a potential new drug from GlaxoSmithKline could treat mixed-lineage leukemia (MLL). MLL is the most common form of leukemia in babies. The study appeared in the journal Nature where scientists from the British drugmaker collaborating with the charity Cancer Research UK (CRUK) and Cellzome AG found that the experimental drug, called I-BET151.

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Ref : http://www.nature.com/nature/journal/vaop/ncurrent/full/nature10509.html

Drug Shows Promise Against Deadly Lung Disease

 An experimental drug may offer a thin ray of hope to people suffering from the rapidly fatal lung disease known as idiopathic pulmonary fibrosis. The compound, currently known only as BIBF 1120 (see structure below : Vargatef™), seems to slow the disease, decrease exacerbations and improve quality of life for patients, according to a study funded by the drug's maker, Boehringer Ingelheim.

  "It improves the course of disease and, in my opinion, it's the first drug to significantly ameliorate the really devastating progression of the disease," 

said Dr. Norman Edelman, (chief medical officer for the American Lung Association, who noted that current treatments for the disease "are almost desperation attempts. There's very little evidence they work)..."

Authors don't claim [BIBF 1120] is going to reverse the disease. They claim it's going to slow it down, but even that is a major factor. 

Patients with IPF usually die within two to three years of diagnosis. While the disease used to be considered relatively rare, Edelman noted that doctors have been noticing an uptick in recent ears, especially among older men. Idiopathic pulmonary fibrosis (IPF) involves a relentless stiffening of the lungs due to overproduction of collagen, the "cement" that holds lung tissue together. 

More : http://www.nejm.org/doi/full/10.1056/NEJMoa1103690

Broccoli, Cabbage, and other Veggies May Protect Against Colon Cancer

In continuation of my update on the usefulness of broccoli 
Austrailian researchers examined the diets of 918 colorectal cancer patients and 1,021 people with no history of the disease and found that consumption of certain vegetables and fruits were associated with a decreased risk of cancer in the proximal and distal colon, that is, the upper and lower portions of the colon.

Consumption of brassica vegetables (also known as cole crops) such as broccoli, kale, cauliflower, turnips and cabbage, for example, appeared to reduce the risk of cancer in the upper colon, while both total fruit and vegetable intake (and total vegetable intake alone) reduced the risk of cancer in the lower colon.

They also found that eating more apples and dark, yellow vegetables was linked with a significantly reduced risk of lower colon cancer...


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