Yale scientists synthesize huperzine A to combat Alzheimer's

Scientists at Yale University have developed the first practical method to create a compound called huperzine A  (see structure below) in the lab. Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the plant firmoss Huperzia serrata. Huperzine A is also an Acetylcholinesterase inhibitor, which has a mechanism of action similar to donepezil, rivastigmine, and galantamine. In the US, Huperzine A is sold as a dietary supplement for memory support. The botanical has been used in China for centuries for the treatment of swelling, fever and blood disorders. Clinical trials in China have shown it to be effective in the treatment of Alzheimer's disease and enhancing memory in students. 

More at : http://opac.yale.edu/news/article.aspx?id=8796

FDA Approves Zelboraf - Potent New Melanoma Drug

Plexxikon Inc., a member of the Daiichi Sankyo Group, today announced that applications for market approval for vemurafenib ( PLX4032/RG7204, see below structure) for the treatment of metastatic melanoma have been submitted to the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA). The company had 

Phase 2 and 3 trials (BRIM2 and BRIM3) that evaluated vemurafenib in patients with BRAF ^V600 mutation-positive melanoma, as determined by the cobas 4800 BRAF ^V600 Mutation Test.

 Earlier this year, the company reported positive data from an interim analysis of BRIM3 which showed that the study met the pre-specified criteria for co-primary endpoints for BRIM3 for progression-free survival and overall survival, and that the safety profile was generally consistent with the previous vemurafenib studies. Based on these results, the data safety monitoring board for the trial recommended early termination of the trial and allowed dacarbazine-treated patients to immediately cross over to vemurafenib treatment. BRIM2 results reported earlier showed a 52 percent confirmed response rate, with tumor shrinkage in the majority of patients, consistent with results from earlier studies. 

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Green tea shows promise against two types of tumors, HHS

In continuation of my update on green tea

Researchers lead by  Dr. Thomas Smith at The Donald Danforth Plant Science Center and his colleagues at The Children’s Hospital of Philadelphia, have found that a compound found in green tea shows great promise for the development of drugs to treat two types of tumors and a deadly congenital disease. 

Dr. Smith and his colleagues discovered that two compounds found naturally in green tea are able to compensate for this genetic disorder by turning off GDH in isolated and when the green tea compounds were administered orally. The Smith lab also used X-ray crystallography to determine the atomic structure of these green tea compounds bound to the enzyme. With this atomic information, they hope to be able to modify these natural compounds to design and develop better drugs. 

Interestingly, two other research groups have validated and extended these findings to demonstrate that blocking GDH with green tea is very effective at killing two different kinds of tumors; glioblastomas, an aggressive type of brain tumor, and tuberous sclerosis complex disorder, a genetic disease that causes non-malignant tumors to grow on a number of organs. 

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EMA has accepted Pfizer's regulatory submissions for review of two investigational compounds crizotinib and bosutinib

European Medicines Agency (EMA) has accepted Pfizer's regulatory submissions for review of two investigational compounds  crizotinib, an oral first-in-class anaplastic lymphoma kinase (ALK) inhibitor, for the treatment of patients with previously treated ALK-positive advanced non-small cell lung cancer (NSCLC); and bosutinib for the treatment of adult patients with newly diagnosed Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase. 

Crizotinib

                                                                                               Bosutinib

Dr. Andreas Penk, president of Pfizer Oncology Europe, claims that,

"With the EMA submissions for crizotinib and bosutinib, we are one step closer to potentially bringing two promising agents to patient populations in areas of significant unmet medical need"......

Two Randomized Trials of Linaclotide for Chronic Constipation

We know that, Linaclotide (BELOW STRUCTURE) is an experimental peptide agonist of guanylate cyclase 2C that is undergoing clinical trials for use in treating abdominal pain in patients with irritable bowel syndrome (IBS) accompanied by constipation. The drug was developed by Ironwood Pharmaceuticals, based in Cambridge, Massachusetts. 

 Now researchers lead by, Dr. Anthony J. Lembo, an associate professor of medicine at Harvard Medical School and director of the GI Motility Center at Beth Israel Deaconess Medical Center in Boston, have come up with interesting claim  that "people who received the drug had improvement in symptoms, and the treatment was generally well-tolerated". 

Researchers conclude that, linaclotide significantly reduced bowel and abdominal symptoms in patients with chronic constipation (2 trials). Additional studies are needed to evaluate the potential long-term risks and benefits of linaclotide in chronic constipation...

Ref : http://www.nejm.org/doi/full/10.1056/NEJMoa1010863

Study Pits New Blood Thinner Against Warfarin For Irregular Heartbeat

A new drug, Rivaroxaban, (see structure) that lowers stroke risk among people with an irregular heartbeat may give the old standby, warfarin, some competition, a new study shows.

 We know that, Rivaroxaban (BAY 59-7939) is an oral anticoagulant invented and manufactured by Bayer; in a number of countries it is marketed as Xarelto. In the United States, it is marketed by Janssen Pharmaceutica. It is the first available orally active direct factor Xa inhibitor. Rivaroxaban is well absorbed from the gut and maximum inhibition of factor Xa occurs four hours after a dose. The effects lasts 8–12 hours, but factor Xa activity does not return to normal within 24 hours so once-daily dosing is possible. Now the  new trial pitted the newer drug, rivaroxaban, against warfarin in more than 14,000 patients who were randomly assigned either warfarin or rivaroxaban. Neither the patients nor the doctors knew who was taking which drug. As per the claim by the resarchers, new agent proved to be as effective as warfarin at reducing the risk of ischemic stroke -- the most common kind of stroke,  but it did not need to be monitored as closely as warfarin since it is given as a one-size-fits-all dose....

"a reasonable alternative to warfarin, with less intracranial or fatal bleeding." claims the lead researcher, Dr. Manesh R. Patel...

Ref : http://www.newsroom.heart.org/index.php?s=43&item=1191

Bear bile chemical could help keep hearts in rhythm

We know that, the compound, ursodeoxycholic acid (UDCA, see structure), is already used to lower cholesterol and help dissolve gallstones, and it's a key ingredient in many traditional Chinese medicines, which use bear bile. According to the latest research from Imperial College London it might also be able to treat abnormal heart rhythm, or arrhythmia, in fetuses and heart attack victims.

“These findings are exciting because the treatments we have now are largely ineffective at preventing arrhythmia in patients who develop an abnormal heart rhythm after a heart attack,” said Dr. Julia Gorelik...........

Ref : http://www3.imperial.ac.uk/newsandeventspggrp/imperialcollege/newssummary/news_2-8-2011-10-25-30

Positive results from combination drug trial for late-stage ovarian cancer

In continuation of my update on  carboplatin

Researchers from IU Medical Sciences Program-Bloomington  and Indiana University Melvin, have found that, an experimental two-drug combination (decitabine & carboplatin) for treating late-stage ovarian cancer continues to produce strong results, leading its Indiana University researchers to actively pursue the next step, conducting a larger clinical trial to test the therapy and to see how it compares with existing treatments for ovarian cancer.

The researchers have been investigating the addition of decitabine, which is marketed as Dacogen in the United States, because they suspect it reactivates tumor suppression genes that are turned off in ovarian cancer cells and improves cells' susceptibility to anti-cancer drugs like carboplatin.

"The science associated with the trial is novel and exciting and could have impact in the future," she said.....

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Diabetes drug rosiglitazone can reduce development of neuropathic pain..

In continuation of my update on Rosiglitazone,

The diabetes drug rosiglitazone (Avandia) can control inflammation leading to nerve damage and abnormal pain responses,  claims the researchers of  Juntendo University School of Medicine, Tokyo.

As per the claim by the researchers, Rosiglitazone works by blocking a specific pathway—called PPAR-gamma—which appears to play a critical role in the development of disabling neuropathic pain. Researchers  therefore propose PPAR-gamma regulation of the macrophage-mediated inflammatory response as a novel therapeutic target for treating neuropathic pain development.

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FDA Accepts NDA Filing for Ruxolitinib as a Treatment for Myelofibrosis

FDA Accepts NDA Filing for Ruxolitinib as a Treatment for Myelofibrosis

Taxoxifen combined with dasatinib reverses chemo-resistance in breast cancer cells

Researchers from Thomas Jefferson University Hospita,  found that taxoxifen combined with dasatinib, a protein-tyrosine kinase inhibitor, reverses the chemo-resistance caused by cancer-associated fibroblasts in the surrounding tissue by normalizing glucose intake and reducing mitochondrial oxidative stress, the process that fuels the cancer cells. 

In this study, researchers sought to better understand drug resistance by looking at the metabolic basis in an ER (+) cell line and cancer-associated fibroblasts.  Researchers claim that the  resistance to chemotherapeutic agents is a metabolic and stromal phenomenal  and the drug combination had an "antioxidant effect" in these types of cancer cells.  

Researchers showed that ER (+) cancer cells alone responded to tamoxifen but when co-cultured with human fibroblasts had little to no effect. Similarly, dasatinib, a chemotherapy drug used to treat leukemia patients who can no longer benefit from other medications, had no effect on fibroblasts alone or cancer cells. Together, however, the drugs prevented the cancer cells co-cultured with the fibroblasts from using high-energy nutrients from the fibroblasts. Researchers conclude that, 

"The drugs have no effect when they are used alone-it's in unison when they effectively kill the cancer cells in the presence of fibroblasts and combination resulted in nearly 80 percent cell death" 

Ref: http://www.jeffersonhospital.org/News/leukemia-drug-reverses-tamoxifen-resistance-in-breast-cancer-cells.aspx

New cough suppressant from cocoa

Researchers are carrying out the final stages of clinical trials of a drug that contains theobromine (see structure), an ingredient found in chocolate and cocoa. The drug could be in the market in another two years.

New cough suppressant from cocoa

Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

New three-drug combination may be effective for newly diagnosed blood cancer patients: Study

New three-drug combination may be effective for newly diagnosed blood cancer patients: Study

When Having the Blues is a Good Thing: Blueberries & Cancer Prevention

In continuation of my up date on the usefulness of blue berries.

Now researchers from the Department of Nutrition Sciences at the University of Alabama at Birmingham, lead by Laura Newton have come up with another interesting finding about blue berries, i.e., as little as a cup a day can help prevent cell damage linked to cancer.

As per the claim by the researchers, free radicals, atoms that contain an odd number of electrons and are highly reactive, can cause cellular damage, one of the factors in the development of cancer; many believe a diet filled with fruits and vegetables may help reduce the risk. 

Lead researcher says

"Studies suggest that antioxidants may help prevent the free-radical damage associated with cancer"

Researchers add that, Blueberries also are rich in vitamin C, which helps the immune system and can help the body to absorb iron. "Vitamin C also helps to keep blood vessels firm, offering protection from bruising. Blueberry juice and other products may be nutritious but often contain less fiber than the whole fruit, and added sugar or corn syrup may decrease their nutritional value. Consuming fresh, raw blueberries provides the most benefits; the average serving size of raw blueberries is one cup, which contains about 80 calories...

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