In continuation of my update on Adempas (riociguat)....
Food and Drug Administration today approved Adempas (riociguat) to treat adults with two forms of pulmonary hypertension...
Med-Chemist : "Quintessential Medicinal Chemistry"
Monday, October 21, 2013
Friday, October 18, 2013
Psoriasis Drug May Help Treat Type 1 Diabetes: Report - Drugs.com MedNews
In continuation of my update on alefacept (Amevive)
A drug formerly used to treat the skin condition psoriasis shows promise in treating type 1 diabetes, according to a new study.
Both psoriasis and type 1 diabetes are autoimmune disorders. The drug alefacept (Amevive) is an immune-suppressing drug that was used to treat psoriasis but was withdrawn by its manufacturer in 2011. The drug maker, Astellas Pharma U.S., said at the time that "business needs" led to its decision to pull the drug from the market.
The new study included 49 type 1 diabetes patients at 14 medical centers in the United States. Thirty-three of the patients received weekly injections of alefacept for 12 weeks, followed by a break of 12 weeks and then another 12 weekly doses of the drug. Sixteen patients received a placebo on the same schedule.
The clinical trial's main outcome was a measure of how well the pancreas could secrete insulin in response to food, two hours after eating. Using this measure, the researchers found no significant differences between the two groups of patients.
Adempas drug gets FDA approval for treatment of pulmonary hypertension
The U.S. Food and Drug Administration today approved Adempas (riociguat) to treat adults with two forms of pulmonary hypertension. Pulmonary hypertension is caused by abnormally high blood pressure in the arteries of the lungs.
Wednesday, October 16, 2013
2013 Nobel Prize in Chemistry: Multiscale models for complex chemical systems
The work of Karplus, Levitt and Warshel is ground-breaking in that they managed to make Newton's classical physics work side-by-side with the fundamentally different quantum physics. Previously, chemists had to choose to use either or. The strength of classical physics was that calculations were simple and could be used to model really large molecules. Its weakness, it offered no way to simulate chemical reactions. For that purpose, chemists instead had to use quantum physics. But such calculations required enormous computing power and could therefore only be carried out for small molecules.
This year's Nobel Laureates in chemistry took the best from both worlds and devised methods that use both classical and quantum physics. For instance, in simulations of how a drug couples to its target protein in the body, the computer performs quantum theoretical calculations on those atoms in the target protein that interact with the drug. The rest of the large protein is simulated using less demanding classical physics.
Today the computer is just as important a tool for chemists as the test tube. Simulations are so realistic that they predict the outcome of traditional experiments.
Martin Karplus, U.S. and Austrian citizen. Born 1930 in Vienna, Austria. Ph.D. 1953 from California Institute of Technology, CA, USA. Professeur Conventionné, Université de Strasbourg, France and Theodore William Richards Professor of Chemistry, Emeritus, Harvard University, Cambridge, MA, USA.http://chemistry.harvard.edu/people/martin-karplus http://www-isis.u-strasbg.fr/biop/start
Michael Levitt, U.S., Brittish and Israeli citizen. Born 1947 in Pretoria, South Africa. Ph.D. 1971 from University of Cambridge, UK. Robert W. and Vivian K. Cahill Professor in Cancer Research, Stanford University School of Medicine, Stanford, CA, USA. http://med.stanford.edu/profiles/Michael_Levitt
Arieh Warshel, U.S. and Israeli citizen. Born 1940 in Kibbutz Sde-Nahum, Israel. Ph.D. 1969 from Weizmann Institute of Science, Rehovot, Israel. Distinguished Professor, University of Southern California, Los Angeles, CA, USA.http://chem.usc.edu/faculty/Warshel.html
Carbon's new champion: Carbyne, a simple chain of carbon atoms, strongest material of all?
Carbyne will be the strongest of a new class of microscopic materials if and when anyone can make it in bulk....
Carbon's new champion: Carbyne, a simple chain of carbon atoms, strongest material of all?
Carbon's new champion: Carbyne, a simple chain of carbon atoms, strongest material of all?
Phase 3 study of idelalisibin reports positive results in CLL patients
Gilead Sciences, Inc. (Nasdaq:GILD) today announced that its Phase 3 study (Study 116) evaluating idelalisib in previously-treated chronic lymphocytic leukemia (CLL) patients who are not fit for chemotherapy will be stopped early. This DMC recommendation is based on a predefined interim analysis showing highly statistically significant efficacy for the primary endpoint of progression-free survival in patients receiving idelalisib plus rituximab (see structures I and II respectively) compared to those receiving rituximab alone.
Two drugs in combination improve survival in patients with advanced pancreatic cancer
In continuation of my update on nab-paclitaxel (stands for nab-nanoparticle albumin-bound) and gemcitabine...
Investigators at the Vall d´Hebron University Hospital and the Vall d'Hebron Institute of Oncology (VHIO), have participated in an international phase III study, published in The New England Journal of Medicine. Results show that administering these two drugs in combination significantly improves one- and two-year survival in patients with advanced pancreatic cancer versus gemcitabine alone, the first-line treatment or most standard approach for this type of cancer to date.
The new drug is set to become a reference in advanced pancreatic cancer treatment. A multicentre phase III study, with centers participating from 11 countries in North America, Europe and Australia, shows that the drug combination nab-paclitaxel and gemcitabine is more effective in the treatment of patients with advanced pancreatic cancer than gemcitabine alone, which has been the standard treatment for these patients up until now.
The clinical trial, sponsored by Celgene Corporation, involved 861 patients, half of whom were administered the nab-paclitaxel/gemcitabine combination, while the other half received gemcitabine alone. Median overall survival was 8.5 months for nab-paclitaxel/gemcitabine versus 6.7 months for gemcitabine alone. One-year survival rates were 35% and 22%, respectively, and two-year survival rates were 9% and 4%, respectively. Similar side effects were found in the new drug and gemcitabine alike. The trial report therefore concluded that the nab-paclitaxel/gemcitabine combination significantly improves overall survival and response rate in patients with advanced pancreatic cancer.
Tuesday, October 15, 2013
Alkermes' ALKS 5461 drug gets FDA Fast Track status for major depressive disorder
Alkermes' ALKS 5461 drug gets FDA Fast Track status for major depressive disorder
(ALKS 33 -see structure in a combination with buprenorphine -see 2nd structure right- called ALKS 5461)
(ALKS 33 -see structure in a combination with buprenorphine -see 2nd structure right- called ALKS 5461)
Monday, October 14, 2013
Active ingredient of ipecac syrup inhibits growth of cancer cells
An old home remedy called ipecac syrup, once stocked in medicine cabinets in case of accidental poisoning, is showing promise as a new chemotherapy drug for bladder cancer.
Years ago, ipecac syrup was used to induce vomiting in poisoning cases. Now a Loyola University Medical Center study has found that the active ingredient of ipecac syrup effectively inhibits the growth of bladder cancer cells, especially when combined with a standard chemotherapy drug.
In the new study, Loyola researchers exposed cell lines of normal and cancerous bladder cells to emetine alone and to emetine plus cisplatin. (Cisplatin is the standard chemotherapy drug for advanced bladder cancer.)
- Emetine alone inhibits the proliferation of bladder cancer cell lines.
- Emetine acts synergistically with cisplatin to inhibit bladder cancer proliferation better than either drug does alone.
- Emetine has little effect on normal cells.
Bladder cancer is the fourth most common cancer in men and the 9th most common cancer in women. But even with aggressive surgery and chemotherapy, the five-year survival rate for patients with advanced Stage 4 bladder cancer is only 4 to 20 percent.
"There is an urgent need to develop new drug combinations," Dr. Gupta said. "Our study demonstrates that combining emetine with cisplatin is potentially beneficial, and merits further study in clinical trials."
Dr. Gupta is an assistant professor in the departments of Urology and Surgery and in the Oncology Research Institute of Loyola University Chicago Stritch School of Medicine. Dr. Foreman is an associate professor in the Department of Pathology and the Oncology Research Institute. Other authors are John Jesse III, a Stritch student, and Paul Kuo, MD, FACS, chair of Loyola's Department of Surgery and director of the Oncology Research Institute.
Ref : http://loyolamedicine.org/newswire/news/familiar-remedy-shows-promise-new-chemo-drug-bladder-cancer
Friday, October 11, 2013
FDA Approves Brintellix to Treat Major Depressive Disorder
We know that, Vortioxetine (vor-tye-ox-e-teen, trade name Brintellix, previously known as Lu AA21004) is a novel atypical antidepressant made byLundbeck and Takeda. On September 30, 2013, it was approved approved by the U.S. FDA for the treatment of major depressive disorder (MDD) in adults. Vortioxetine was also investigated as a treatment for generalized anxiety disorder (GAD).
Regulatory approval for the treatment of MDD for the European market has been filed in September 2012, for the United States in October 2012, and filing for Canada should follow. Filing for the Japanese market is expected in 2013.
The U.S. Food and Drug Administration recently approved Brintellix (vortioxetine) to treat adults with major depressive disorder.
Thursday, October 10, 2013
FDA Approves Duavee to Treat Hot Flashes and Prevent Osteoporosis
Bazedoxifene is a third generation selective estrogen receptor modulator (SERM), under development by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. Pfizer are seeking approval for bazedoxifene in the prevention and treatment ofpostmenopausal osteoporosis. Bazedoxfiene is the result of an exclusive research collaboration between Wyeth Pharmaceuticalsand Ligand Pharmaceuticals.
The U.S. Food and Drug Administration today approved Duavee (conjugated estrogens/bazedoxifene) for women who suffer from moderate-to-severe hot flashes (vasomotor symptoms) associated with menopause and to prevent osteoporosis after menopause....
Wednesday, October 9, 2013
Apple impregnated with tangerine juice reduces risk of cardiovascular disease in obese children
"It is not a product that induces weight loss in children, but it would help improve their quality of life. The modification of oxidative stress in adipose tissue (or fat tissue) can help in the prevention of cardiovascular risk associated with childhood obesity and in the long term prevent diseases such as atherosclerosis (hardening and narrowing of the arteries caused by the accumulation of fat, cholesterol and other substances)," said Dr. Pilar Codoñer, head of the Department of Paediatrics, University Hospital Doctor Peset and professor in the Department of Paediatrics at the Universitat de València.
To obtain the snack, researchers enriched apple slices with mandarin juice using a technology of impregnation developed and patented by the UPV team that allows incorporating additional ingredients to the structure of porous foods, as in the case of fruits and vegetables.
"After several years of work the product is ready to be marketed by private companies. Our snack has all the properties of two products as healthy as apples and tangerine and has no added ingredient. It is an alternative to snacks that exist in the market that contain oils and saturated fats and therefore are high in calories," says Noelia Betoret, principal researcher and professor at the School of Agricultural Engineering and Natural Environment.
Monday, October 7, 2013
New class of antidepressants appears potentially effective in combating deadly form of lung cancer
Jahchan tested the effect of a tricyclic antidepressant called imipramine (see structure) on human small-cell lung cancer cells grown in the laboratory and growing as tumors in laboratory mice. She found that the drug was able to potently activate a self-destruction pathway in the cancer cells and to slow or block metastases in the animals. The drug maintained its effectiveness regardless of whether the cancer cells had previously been exposed, and become resistant, to traditional chemotherapy treatments. Another drug, an antihistamine called promethazine, identified by the bioinformatics screen, also exhibited cancer-cell-killing abilities.
Although imipramine did not affect cells from another main type of lung cancer called non-small-cell lung adenocarcinoma, it did inhibit the growth of cells from other neuroendocrine tumors, including pancreatic neuroendocrine cancers, an aggressive skin cancer called Merkel cell carcinoma, and a pediatric cancer called neuroblastoma. (Neuroendocrine cells receive signals from the nervous system and secrete hormoneslike adrenaline into the blood to affect the body's function.)
Further investigation showed that the drugs appear to work through a class of molecule on the cancer cells' surfaces called G-protein-coupled receptors, but the researchers are continuing to investigate exactly how the drugs specifically kill neuroendocrine cancer cells.
"Our collaboration with the Butte lab allowed us to move very quickly from the initial idea to very convincing results," Sage said. "It was less than 20 months from the time of our first discussion to a clinical trial because the bioinformatics approach had been established and the drugs are FDA-approved. By focusing on diseases with little hope for the patient, it's easier to go forward fast."
Ref : http://cancerdiscovery.aacrjournals.org/content/early/2013/09/16/2159-8290.CD-13-0183.abstract
Saturday, October 5, 2013
Addition of walnuts to diet can protect against diabetes and heart disease in at-risk individuals
The research found that daily intake of 56g of walnuts improves endothelial function in overweight adults with visceral adiposity. The addition of walnuts to the diet does not lead to weight gain. Further study on the topic is still suggested. "The primary outcome measure was the change in flow-mediated vasodilatation (FMD) of the brachial artery," wrote the research group. "Secondary measures included serum lipid panel, fasting glucose and insulin, Homeostasis Model Assessment-Insulin Resistance values, blood pressure, and anthropometric measures. FMD improved significantly from baseline when subjects consumed a walnut-enriched diet as compared with the control diet. Beneficial trends in systolic blood pressure reduction were seen, and maintenance of the baseline anthropometric values was also observed. Other measures were unaltered."
Friday, October 4, 2013
Apple impregnated with tangerine juice reduces risk of cardiovascular disease in obese children
"It is not a product that induces weight loss in children, but it would help improve their quality of life. The modification of oxidative stress in adipose tissue (or fat tissue) can help in the prevention of cardiovascular risk associated with childhood obesity and in the long term prevent diseases such as atherosclerosis (hardening and narrowing of the arteries caused by the accumulation of fat, cholesterol and other substances)," said Dr. Pilar Codoñer, head of the Department of Paediatrics, University Hospital Doctor Peset and professor in the Department of Paediatrics at the Universitat de València.
To obtain the snack, researchers enriched apple slices with mandarin juice using a technology of impregnation developed and patented by the UPV team that allows incorporating additional ingredients to the structure of porous foods, as in the case of fruits and vegetables.
"After several years of work the product is ready to be marketed by private companies. Our snack has all the properties of two products as healthy as apples and tangerine and has no added ingredient. It is an alternative to snacks that exist in the market that contain oils and saturated fats and therefore are high in calories," says Noelia Betoret, principal researcher and professor at the School of Agricultural Engineering and Natural Environment.
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