Eribulin mesylate drug may help extend lives of women with advanced breast cancer..

We know that, Eribulin (see structure E7389) is an investigational  anticancer drug. Eribulin was previously known as E7389.  Eribulin is currently being investigated by Eisai Co. for the third-line treatment of advanced breast cancer in patients who have been previously treated with anthracyclines, taxanes and capecitabine, as well as a variety of other solid tumors, including non-small cell lung cancer, prostate cancer and sarcoma.

Structurally, eribulin is a fully synthetic macrocyclic ketone analogue of the marine sponge natural product halichondrin B a potent mitotic inhibitor with a unique mechanism of action found in the Halichondria genus of sponges. Eribulin is a mechanistically-unique inhibitor of microtubule dynamics, exerting its anticancer effects by triggering apoptosis of cancer cells following prolonged mitotic blockage. A new synthetic route to E7389 was published in 2009.

Now   research team at the University of Leeds and St James's Institute of Oncology led an international trial of the new chemotherapy drug, eribulin mesylate. As per the claim by the researchers, average survival was typically 25 per cent longer for women who took eribulin mesylate.

In the EMBRACE trial, 762 patients with advanced breast cancer received either eribulin or standard cancer treatment. All of the patients had already been heavily treated with conventional therapies, but their disease had returned or spread to other parts of the body.  Researchers concluded that those who took the new drug lived for 13.1 months, on average, compared with 10.7 months for those on conventional chemotherapy. The drug was also well-tolerated by most patients. Researchers hope that these results may establish eribulin as a new, effective treatment for women with late-stage metastatic breast cancer (either single drug or in combination with other anticancer drug). The drug is not yet available for routine clinical treatment and is awaiting regulatory approval in the European Union, the US and Japan.

"Until now, there hasn't really been a standard treatment for women with such advanced breast cancer. For those women who have already received all of the recognised treatments, these are promising results, claims the lead investigator Professor Christopher Twelves...

Ref : http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=74&abstractID=50309

Polyphenols in red wine and green tea halt prostate cancer growth, study suggests

In continuation of my update on Green Tea and EGCG........

"The profound impact that the antioxidants in red wine and green tea have on our bodies is more than anyone would have dreamt just 25 years ago," Weissmann added. "As long as they are taken in moderation, all signs show that red wine and green tea may be ranked among the most potent 'health foods' we know." ....

Polyphenols in red wine and green tea halt prostate cancer growth, study suggests

New evidence that drinking coffee may reduce the risk of diabetes

In continuation of my update on benefits of coffee....

New evidence that drinking coffee may reduce the risk of diabetes

Carbamazepine Reduces Hepatic Fibrosis.....

We know that Carbamazepine (CBZ see structure), is an  anticonvulsant and mood stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder, as well as trigeminal neuralgia. It is also used off-label for a variety of indications, including attention-deficit hyperactivity disorder (ADHD), schizophrenia, phantom limb syndrome, paroxysmal extreme pain disorder, and post-traumatic stress disorder.

Now researchers from University of Pittsburgh School of Medicine, have come up with interesting finding about this drug, i.e., the liver scarring of α1-antitrypsin (AT) deficiency, the most common genetic cause for which children undergo liver transplantation, might be reversed or prevented with carbamazepine.  The disease, which affects 1 in 3,000 live births, a gene mutation leads to an abnormal protein, dubbed ATZ, that unlike its normal counterpart is prone to aggregation. As per the claim by the researchers these aggregates of ATZ accumulate in the liver cells and eventually lead to scarring, or fibrosis, of the organ and set the stage for tumor development. The disease sometimes doesn't show itself until adulthood, when the liver starts to fail due to cirrhosis or cancer.

Encouraged by the fact that carbamazepine could enhance a natural cellular pathway called autophagy  or self-digestion, researchers thought that  it might be able to rid the cells of the toxic aggregated ATZ. For the study researchers treated an ATZ cell line with carbamazepine. They found that carbamazepine did indeed cause a marked decrease in ATZ because the abnormal proteins were degraded more quickly via autophagy, and so they did another experiment in a mouse model of AT deficiency.

The most amazing finding,  as per the claim by the researchers is  that the drug reversed the fibrosis in the livers of the mice and after two weeks of treatment the liver tissue resembled that of a healthy mouse...

The ability of carbamazepine and drugs like it to "soup up" the cell's autophagy machinery might have value in other disorders ― such as Alzheimer's disease, Huntington's disease and Parkinsonism ― that are thought to be caused by toxic effects of protein clumping in the brain. Dr. Perlmutter and his colleagues are now exploring these possibilities in preclinical studies. ....

Ref : http://www.sciencemag.org/cgi/content/abstract/science.1190354v1

Azithromycin as effective as penicillin for early-stage syphilis...

We know that azithromycin (structure) is one of the world's best-selling  antibiotics. It is derived from erythromycin; however, it differs chemically from erythromycin in that a methyl-substituted nitrogen atom is incorporated into the lactone ring, thus making the lactone ring 15-membered.  Azithromycin is being used to treat or prevent certain bacterial infections, most often those causing middle ear infections, tonsillitis, throat infections, laryngitis, bronchitis, pneumonia, Typhoid, certain urinary tract infections and venereal diseases, such as non-gonococcal urethritis, chlamydia, gonorrhea and cervicitis. and sinusitis. In recent years it has primarily been used to prevent bacterial infections in infants and those with weaker immune systems.

Now researchers lead by Dr. Edward W. Hook, III of University of Alabama at Birmingham have come up with an interesting finding, i.e., antibiotic pills (azithromycin) are as effective as penicillin injections in curing early-stage syphilis in HIV-negative volunteers. 

Although long-acting penicillin delivered by injection is recommended as the preferred treatment for early syphilis, the authors note that this therapy has shortcomings, particularly in resource-limited settings. Penicillin injections can cause allergic reactions, and the drug must be refrigerated and administrated by trained personnel. The orally administered azithromycin may provide a good alternative for treating HIV-negative people with early-stage syphilis, the scientists conclude. They note that there is a potential for syphilis-causing bacteria to acquire resistance to macrolide drugs such as azithromycin and they recommend continued research into this possibility..

Ref : http://www.niaid.nih.gov/news/newsreleases/2010/Pages/syphilis.aspx

Telomeres: Size matters when it comes to DNA

In continuation of my update on Telomerase and Telomerase inhibition....

Telomeres: Size matters when it comes to DNA

Lovastatin: A New Weapon Against Plague?

We know that, Lovastatin is a member of the drug class of statins,  used for lowering  cholesterol (hypolipidemic agent) in those with hypercholesterolemia and so preventing cardiovascular disease. Lovastatin is a naturally occurring drug found in food such as oyster mushrooms  and red yeast rice.

Now scientists at the Unité de Recherche sur les Maladies Infectieuses et Tropicales Emergentes (CNRS/Université Aix-Marseille 2), have found that Lovastatin protects animals against the deadly effects of plague.

After inoculating small rodents with the Yersinia pestis bacterium, the team led by Didier Raoult and Michel Drancourt at the URMITE (CNRS/Université Aix-Marseille 2) showed that animals treated with lovastatin presented fewer and less severe infections. Lovastatin therefore has preventive properties against plague mortality in an animal model. This experimental study also reveals that this statin has no direct antibiotic effect against Yersinia pestis but that it prevents the development of septicemia.  

Researchers conclude that Lovastatin had no in-vitro antibiotic effect against Y. pestis. The difference in the mortality between control mice (11/15; 73.5%) and lovastatin-treated mice (3/15; 20%) was significant (P<0.004; Mantel-Haenszel test). Dead mice exhibited Y. pestis septicemia and inflammatory destruction of lung and spleen tissues not seen in lovastatin-treated surviving mice. These data suggest that lovastatin may help prevent the deadly effects of plague, with a caution that field observations are warranted to assess the role of lovastatin in the prophylaxis of human plague....

Ref : http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0010928

FDA accepts Orexigen's Contrave NDA for treatment of obesity

Orexigen Therapeutics, Inc., a biopharmaceutical company focused on the treatment of obesity, recently anounced that the U.S. Food and Drug Administration (FDA) has accepted for filing the Company's New Drug Application (NDA) for Contrave(R) (see structrures below ; naltrexone SR   and bupropion SR), its investigational drug for the treatment of obesity. The NDA is based on a substantial body of evidence gathered through the Contrave Obesity Research (COR) clinical program, which included over 4,500 patients.....

"We are pleased the FDA has accepted our NDA for filing and look forward to working with the Agency during the review process," said Michael Narachi, President and CEO of Orexigen. "If approved, we believe Contrave will become an important therapeutic option for obese patients, making weight loss and weight maintenance an achievable cornerstone in the treatment of obesity and its common co-morbidities."

Ref : http://ir.orexigen.com/phoenix.zhtml?c=207034&p=irol-newsArticle&ID=1432740&highlight=

ACT Biotech's Telatinib receives orphan drug designation from FDA for treatment of gastric cancer

ACT Biotech's Telatinib receives orphan drug designation from FDA for treatment of gastric cancer..

Telatinib (see structure,  source : ChemBlink) :
(17-Demethoxy-17-allylaminogeldanamycin; Tanespimycin; 17-Allylaminogeldanamycin)

Bone drug (Zoledronic acid) suppresses wandering tumor cells in breast cancer patients

In continuation of my update on zoledronic acid, I find this info really  interesting.  Researchers from Washington University School of Medicine in St. Louis, have found that the bone-strengthening drug zoledronic acid (Zometa) can help fight metastatic breast cancer when given before surgery.

When the drug was given along with chemotherapy for three months before breast cancer surgery, it reduced the number of women who had tumor cells in their bone marrow at the time of surgery.

Tumors shed thousands of cells, which spread throughout the body and are referred to as disseminated tumor cells (DTCs). Breast cancer DTCs often lodge in bone marrow where bone growth factors help them survive.

Chemotherapy can increase bone turnover and bone growth factors, potentially exacerbating the problem of DTCs in the bone, which can resurface later to cause metastatic disease in cancer patients.

Researchers believe that zoledronic acid inhibits the release of growth factors that help support the growth of DTCs.

In this randomized phase II clinical trial, researchers split 109 women with newly diagnosed stage II or stage III breast cancer into two groups. The control group received chemotherapy alone, while the other received a combination treatment of chemotherapy and zoledronic acid. After three months of therapy, patients with DTCs in their bone marrow decreased from 43 percent to 30 percent in the combination group, compared with a decrease from 48 percent to 47 percent in the control group. This result approached statistical significance.

Zoledronic acid treatment with chemotherapy had additional benefits. Women in the combination group experienced significant gains in bone density after 12 months. This is helpful for breast cancer patients, who often develop osteoporosis as a side effect of chemotherapy and other breast cancer treatments.  

The study also suggested that zoledronic acid may help fight certain types of breast tumors directly. Aft speculates that the drug may stop the tumor from making its own blood supply, modify the immune system in a way that makes it harder for tumor cells to survive or even cause the cancer cells to commit suicide.....

Ref : http://www.ncbi.nlm.nih.gov/pubmed/20362507?dopt=Abstract