Study reports anti-cancer activity in mice treated with experimental drug TAK-733

Study reports anti-cancer activity in mice treated with experimental drug TAK-733

TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.

Ref: http://www.heemd.com/news/?md=1510006/
http://www.medchemexpress.com/TAK-733.html

Eribulin drug has minor added benefit in one patient group, indication of lesser benefit in others

In continuation of my update on Eribulin

Eribulin (trade name: Halaven) is approved for women with locally advanced or metastatic breast cancer in whom the disease has progressed despite prior drug therapy. The German Institute for Quality and Efficiency in Health Care (IQWiG) examined in a dossier assessment whether the drug offers an added benefit over the appropriate comparator therapy in these patient groups.

According to the findings, there are both positive and negative effects. There is proof of minor added benefit for one group of patients. For other groups, there are hints or indications of lesser benefit.

Second assessment of eribulin

IQWiG already presented a dossier assessment of eribulin in February 2012. The subsequent decision on the added benefit made by the Federal Joint Committee (G-BA) was limited until April 2014. In addition, the drug manufacturer meanwhile obtained approval for an expanded therapeutic indication: In March 2011 eribulin was only available for patients who have progressed further after at least two chemotherapeutic regimens. Since June 2014, however, the drug can already be used after one unsuccessful treatment attempt. Hence there were two reasons ─ independent from each other ─ for the reassessment of eribulin.

G-BA specified appropriate comparator therapies

When the G-BA specified the appropriate comparator therapy, it distinguished between several treatment situations: The first one refers to patients who are not eligible for further chemotherapy with a taxane or an anthracycline. In this situation, eribulin was to be compared with individual chemotherapy containing the drugs capecitabine or vinorelbine.

In patients for whom taxanes or anthracyclines are principally still an option, eribulin was to be compared with an individual chemotherapy containing a taxane or an anthracycline.

Eribulin drug has minor added benefit in one patient group, indication of lesser benefit in others

FDA Approves Dual-Chamber Syringe for Abilify Maintena (aripiprazole) for Schizophrenia

In continuation of my update on aripiprazole

We know that, Aripiprazole (brand names: Abilify, Aripiprex) is a atypical antipsychotic. It is primarily used in the treatment of schizophrenia, bipolar disorder, major depressive disorder (as an add on to other treatment),tic disorders, and irritability associated with autism. 

It was approved by the U.S. Food and Drug Administration (FDA) for schizophrenia on November 15, 2002 and the European Medicines Agency on 4 June 2004; for acute manic and mixed episodes associated with bipolar disorder on October 1, 2004; as an adjunct for major depressive disorder on November 20, 2007; and to treat irritability in children with autism on 20 November 2009.  Likewise it was approved for use as a treatment for schizophrenia by the TGA of Australia in May 2003.  It is a partial dopamine agonist

Aripiprazole was developed by Otsuka in Japan, and in the United States, Otsuka America markets it jointly with Bristol-Myers Squibb.

FDA Approves Dual-Chamber Syringe for Abilify Maintena (aripiprazole) for Schizophrenia

FDA Approves Ofev (nintedanib) for Idiopathic Pulmonary Fibrosis

In continuation of update on nintedanib

The U.S. Food and Drug Administration today approved Ofev (nintedanib) for the treatment of idiopathic pulmonary fibrosis (IPF).

Idiopathic pulmonary fibrosis is a condition in which the lungs become progressively scarred over time. As a result, patients with IPF experience shortness of breath, cough, and have difficulty participating in everyday physical activities. Current treatments for IPF include oxygen therapy, pulmonary rehabilitation, and lung transplant.

FDA Approves Ofev (nintedanib) for Idiopathic Pulmonary Fibrosis

FDA Approves Revised Indication for Ozurdex for the Treatment of Diabetic Macular Edema

In continuation of my update on dexamethasone

Allergan, Inc., announced today that the U.S. Food and Drug Administration (FDA) has approved Ozurdex (dexamethasone intravitreal implant) 0.7 mg, a sustained-release biodegradable steroid implant, for the treatment of diabetic macular edema (DME). Ozurdex was originally approved in June as a treatment for DME in adult patients who have an artificial lens implant (pseudophakic) or who are scheduled for cataract surgery (phakic). Based on ongoing review of clinical data demonstrating efficacy and safety, the FDA has now approved Ozurdex for use in the general DME patient population.

FDA Approves Revised Indication for Ozurdex for the Treatment of Diabetic Macular Edema

FDA Approves Esbriet (pirfenidone) for Idiopathic Pulmonary Fibrosis

Pirfenidone is a drug developed by several companies worldwide, including InterMune Inc. (now part of Roche), Shionogi Ltd., and GNI Group Ltd., for the treatment of idiopathic pulmonary fibrosis (IPF). In 2008, it was first approved in Japan for the treatment of IPF after clinical trials, under the trade name of Pirespa by Shionogi & Co. In October 2010, the Indian Company Cipla launched it as Pirfenex. In 2011, it was approved for use in Europe for IPF under the trade name Esbriet.  was approved in Canada in 2012 under the trade name Esbriet; and was approved in the United States in October 2014 under the same name. In September 2011, the Chinese State Food and Drug Administration provided GNI Group Ltd with new drug approval of pirfenidone in China,^[3] and later manufacture approval in 2013 under the trade name of Etuary. 

In continuation of my update on pirfenidone

FDA Approves Esbriet (pirfenidone) for Idiopathic Pulmonary Fibrosis

FDA Approves Ofev (nintedanib) for Idiopathic Pulmonary Fibrosis

In continuation of update on nintedanib

The U.S. Food and Drug Administration today approved Ofev (nintedanib) for the treatment of idiopathic pulmonary fibrosis (IPF).

Idiopathic pulmonary fibrosis is a condition in which the lungs become progressively scarred over time. As a result, patients with IPF experience shortness of breath, cough, and have difficulty participating in everyday physical activities. Current treatments for IPF include oxygen therapy, pulmonary rehabilitation, and lung transplant.

FDA Approves Ofev (nintedanib) for Idiopathic Pulmonary Fibrosis

An apple a day could keep obesity away

Sientists at Washington State University have concluded that non digestible compounds in apples -- specifically, Granny Smith apples  may help prevent disorders associated with obesity. The study, thought to be the first to assess these compounds in apple cultivars grown in the Pacific Northwest, appears in October's print edition of the journal Food Chemistry.

"We know that, in general, apples are a good source of these nondigestible compounds but there are differences in varieties," said food scientist Giuliana Noratto, the study's lead researcher. "Results from this study will help consumers to discriminate between apple varieties that can aid in the fight against obesity."

The tart green Granny Smith apples benefit the growth of friendly bacteria in the colon due to their high content of non-digestible compounds, including dietary fiber and polyphenols, and low content of available carbohydrates. Despite being subjected to chewing, stomach acid and digestive enzymes, these compounds remain intact when they reach the colon. Once there, they are fermented by bacteria in the colon, which benefits the growth of friendly bacteria in the gut.

The study showed that Granny Smith apples surpass Braeburn, Fuji, Gala, Golden Delicious, McIntosh and Red Delicious in the amount of nondigestible compounds they contain.

"The nondigestible compounds in the Granny Smith apples actually changed the proportions of fecal bacteria from obese mice to be similar to that of lean mice," Noratto said.

An apple a day could keep obesity away 

Researchers identify compounds that could lead to discovery of new drugs for African sleeping sickness

In early drug discovery, you need a starting point, says North­eastern Uni­ver­sity asso­ciate pro­fessor of chem­istry and chemical biology Michael Pollastri.

In a new research paper published Thursday in the journal PLOS Neglected Tropical Diseases, Pollastri and his colleagues present hun­dreds of such starting points for poten­tially treating African sleeping sick­ness, a deadly disease that claims thousands of lives annually.

Pol­lastri, who runs Northeastern's Lab­o­ra­tory for Neglected Dis­ease Drug Dis­covery, and co- collaborators at the Spanish National Research Council for Scientific Research worked with global health­care com­pany GlaxoSmithKline to screen and test more than 42,000 chem­ical com­pounds against the par­a­sites that cause African sleeping sickness. In their paper, they report iden­ti­fying nearly 800 com­pounds that rep­re­sent good options for early drug discovery.

"Having this many good starting points for discovery of new drugs for sleeping sick­ness is a big deal and could ultimately lead to a cure," Pol­lastri said.

Pol­lastri also high­lighted another exciting component to this project. Previously, he created a data- sharing portal where sci­en­tists and researchers can access and con­tribute to each other's work on neglected tropical diseases. This new research on African sleeping sickness will be the first data to be deposited on the portal, which was sup­ported by a crowd­funding campaign.

"This is a venue where other people, particularly medical chemists from around the world, can con­tribute to the project in one way or the other," Pollastri said.

Researchers identify compounds that could lead to discovery of new drugs for African sleeping sickness

MIT researchers develop new way to model effects of cancer-causing genetic mutations

Sequencing the genomes of tumor cells has revealed thousands of genetic mutations linked with cancer. However, sifting through this deluge of information to figure out which of these mutations actually drive cancer growth has proven to be a tedious, time-consuming process.

MIT researchers have now developed a new way to model the effects of these genetic mutations in mice. Their approach, based on the genome-editing technique known as CRISPR, is much faster than existing strategies, which require genetically engineering mice that carry the cancerous mutations.

"It's a very rapid and very adaptable approach to make models," says Thales Papagiannakopoulos, a postdoc at MIT's Koch Institute for Integrative Cancer Research and one of the lead authors of the paper, which appears in the Oct. 22 online edition ofNature. "With a lot of these mutations, we have no idea what their role is in tumor progression. If we can actually understand the biology, we can then go in and try targeted therapeutic approaches."

Led by Papagiannakopoulos, graduate student Francisco Sanchez-Rivera, the paper's other lead author, and Koch Institute director Tyler Jacks, the paper's senior author, the team used CRISPR to accurately reproduce the effects of two well-known lung cancer genes. They also modeled a gene called APC, whose role in lung cancer was not previously known.

This approach could be used to study nearly any gene in many different types of cancer, the researchers say. "There has to be a functional way of assessing the role of these cancer-gene candidates as they appear in sequencing studies," Sanchez-Rivera says. "The system we developed fills that gap immediately because you can do it very rapidly and very precisely."

Ref  http://newsoffice.mit.edu/2014/fast-modeling-cancer-mutations-1022

MIT researchers develop new way to model effects of cancer-causing genetic mutations

Scientists develop new drug as alternative to antibiotics

In a breakthrough, scientists have developed the first effective alternative to antibiotics that may aid the fight against drug-resistant infections. 

In a small patient trial, the drug was shown to be effective at eradicating the superbug Methicillin-resistant Staphylococcus aureus (MRSA). 

Researchers said it is unlikely that the infection could develop resistance against the new treatment, which is already available as a cream for skin infections. 

They hope to develop a pill or an injectable version of the drug within five years. 

The treatment marks "a new era in the fight against antibiotic-resistant bacteria," according to Mark Offerhaus, chief executive of the biotechnology company Micreos, which is behind the advance. 

The treatment attacks infections in an entirely different way from conventional drugs and, unlike them, exclusively targets the Staphylococcus bacteria responsible for MRSA, and leaves other microbes unaffected. 

The approach is inspired by naturally occurring viruses that attack bacteria using enzymes called endolysins. It uses a 'designer' endolysin, Staphefekt, which the scientists engineered to latch on to the surface of bacteria cells and tear them apart, 'The Times' reported. 

"Endolysins exist in nature, but we've made a modified version that combines the bit that is best at binding to the bacteria with another bit that is best at killing it," said Bjorn Herpers, a clinical microbiologist, who tested the drug at the Public Health Laboratory in Kennemerland, the Netherlands. 

Conventional antibiotics need to reach the inside of the cell to work, and part of the reason they are becoming less effective is that certain strains of bacteria, such as MRSA, have evolved impenetrable membranes. 

Scientists develop new drug as alternative to antibiotics  

Analgesics, anti-inflammatory drugs have beneficial effect on treatment of depression

Analgesics and anti-inflammatory drugs used against muscle pain and arthritis may have a beneficial effect on depression symptoms....

Ordinary over the counter painkillers and anti-inflammatory drugs purchased from pharmacies may also be effective in the treatment of people suffering of depression.

This is shown by the largest ever meta-analysis that has just been published by a research group from Aarhus University in the American scientific journal JAMA Psychiatry. The meta-analysis is based on 14 international studies with a total 6,262 patients who either suffered from depression or had individual symptoms of depression.

Up to 15 per cent of the Danish population can expect to suffer from depression at some point in their lives. The World Health Organisation (WHO) estimates that depression is one of the top five reasons for loss of quality of life and also life years. Thus, it is a very serious condition, one where researchers all over the world are constantly trying to find more effective treatments.

In recent years research has demonstrated a correlation between depression and physical illnesses, such as painful conditions or infections in the individual patient.

"The meta-analysis supports this correlation and also demonstrates that anti-inflammatory medication in combination with antidepressants can have an effect on the treatment of depression. When combined they give an important result which, in the long term, strengthens the possibility of being able to provide the individual patient with more personalized treatment options," says MD-student Ole Köhler, who is first author of the scientific article and a member of the research group from Aarhus University.

Analgesics, anti-inflammatory drugs have beneficial effect on treatment of depression

Walnuts may help prevent Alzheimer's disease, study finds

Animal study reveals potential brain-health benefits of a walnut-enriched diet. A new animal study published in the Journal of Alzheimer's Disease indicates that a diet including walnuts may have a beneficial effect in reducing the risk, delaying the onset, slowing the progression of, or preventing Alzheimer's disease.

Research led by Abha Chauhan, PhD, head of the Developmental Neuroscience Laboratory at the New York State Institute for Basic Research in Developmental Disabilities (IBR), found significant improvement in learning skills, memory, reducing anxiety, and motor development in mice fed a walnut-enriched diet.

The researchers suggest that the high antioxidant content of walnuts (3.7 mmol/ounce) may have been a contributing factor in protecting the mouse brain from the degeneration typically seen in Alzheimer's disease. Oxidative stress and inflammation are prominent features in this disease, which affects more than five million Americans.

More : http://www.j-alz.com/node/396

Walnuts may help prevent Alzheimer's disease, study finds

Afatinib active against NSCLC nervous system metastases

Incontinuation of my update on Afatinib

Afatinib active against NSCLC nervous system metastases

Nanoparticle-based invention moves new drugs closer to clinical testing

Penn State College of Medicine researchers have developed a nanoparticle to deliver a melanoma-fighting drug directly to the cancer.

Delivering cancer drugs directly to tumors is difficult. Scientists are working on new approaches to overcome the natural limitations of drugs, including loading them into nanoparticles.

"The drug is packaged into a lipid ball significantly smaller than the width of a hair to make it soluble in the blood stream and prevent negative side effects. The drug-containing nanoparticle ball then travels in the bloodstream to the tumor, where it accumulates and the drug is released in the tumor to kill the cancer cells," said Gavin Robertson, professor of pharmacology, pathology, dermatology, and surgery and director of the Penn State Hershey Melanoma Center.

In previous research, Robertson discovered the cancer-fighting characteristics of leelamine, a substance derived from pine bark. But leelamine cannot be given by mouth because of poor uptake in the gastrointestinal tract or be injected intravenously because it causes damage to red blood cells.

To address this issue, Robertson and his team developed a new nanoliposome that loads leelamine, called Nanolipolee-007. Nanolipolee-007 can be injected intravenously without causing damage to red blood cells. It then accumulates in tumors because of its small size where it releases the drug to kill the cancer cells.

Leelamine is the first of a new unique class of drugs that inhibits cholesterol movement around a cancer cell to shut down signals needed for cancer cell survival. As a result, protein pathways like the PI3K, MAPK and STAT3 that are highly active and help cancer cells multiply and spread, are turned off and the cancer cells die. Since normal cells are not addicted to the high levels of activity of these pathways that occur in cancer cells, the drug has a minor effect on them.

"This nanoparticle moves leelamine one step closer to the clinic," Robertson said. "We now have a drug that has the potential to be given to humans that could not be done before."

The researchers showed the results of Nanolipolee-007 on cells growing in culture dishes and in tumors growing in mice following intravenous injection. Leelamine inhibited tumor development in mice with no detectable side effects.

Nanoparticle-based invention moves new drugs closer to clinical testing