Novel Drug Screening Method: Informative Swellings
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Med-Chemist : "Quintessential Medicinal Chemistry"
Monday, September 14, 2009
Lurasidone - positive results from phase 3 clinical trials !
I read about this compound few months back, that it is one of "atypical antipsychotic" drugs that are being tried and this drug has shown promising results in the phase II and is being studied clinically for phase III by a Japanese company.
As per the claims by the company 'Lurasidone, blocks D2- and 5-HT2A-receptors and the advantage is it causes less extrapyramidal side effects than current antipsychotics.
Yes the phase 3 results are really interesting, with Lurasidone 40 and 120 mg, taken once-daily, demonstrated significantly greater improvement versus placebo on the primary efficacy measure. A total of 53% of patients on lurasidone 40 mg/day and 47% of patients on lurasidone 120 mg/day demonstrated a 30% or more improvement on the PANSS total score from baseline versus 38% on placebo. Lurasidone was also well-tolerated with an overall discontinuation rate similar to placebo (40% vs. 39% placebo) and few adverse event-related discontinuations (9% for both the overall lurasidone group and placebo). Adverse events seen in the trial were generally mild.
Congrats for this achievement.
Ref : http://dsp-america.com/pdf/news/LurasidonePh3Results.pdf
Tigecycline- as antimalarial drug ?
As for my knowledge goes, 'Tigecycline' is being used as drug for the antibiotic resistant strain 'Staphylococcus aureus'. And this drug belongs to the class of "glycylcyclines" (similar to tetracyclines : central four-ring carbocyclic skeleton). The broad spectrum activity is attributed to the D-9 position substitution. It is a bacteriostatic and acts by the inhibition of protein synthesis. It has been found to be active against both Gram positive and Gram negative bacterii.
Now thanx to the researchers from the Medical University of Vienna, Austria, who have achieved something interesting feat, i.e., Tigecycline has significant antimalarial activity on its own and may also be effective against multi drug-resistant malaria when administered in combination with traditional antimalarial drugs.
Increasing resistance of Plasmodium falciparum to existing drugs has resulted in the search for new antimalarial therapies and I congratulate the team for this important achievement. More interestingly the drug is 6 times more active against P. falciparum than doxycycline. As the drug itself is an established one, its one more addition to the serendepity list. Congrats the team...
Ref : http://www.asm.org/index.php?option=com_content&view=article&id=91042
Sunday, September 13, 2009
How one can prepare for the H1N1 flu ......
We all should be thankful to the U.S. Department of Health and Human Services (HHS), for there effort in educating about the health problems. I find these webcasts very useful in understanding the H1N1 flu and how one can prepare for this pandemic. The efforts by the govt., is highly appreciable as there are many myths about this virus !.
Those interested can go through the webcast archives about the H1N1 flu.
Saturday, September 12, 2009
A single dose vaccine for Swine flu !.....
I am reading anything and everything about this H1N1, since it started in Mexico and there were so many different names (many names like - swine flu !, Mexican flu, ....). The deadly virus has caused panic in each and every country, where there are reports of infection of H1N1. The real concern is the use of antibiotics and the real black market for Tamiflu and so many falsely claimed drugs. Now thanx to Dr. Russell Basser and group who have found that a single 15-µg dose of 2009 H1N1 vaccine was immunogenic in adults, with mild-to-moderate vaccine-associated reactions. Congrats for for this important achievement.
A (H1N1) 2009 virus is responsible for the first influenza pandemic in 41 years. This itself shows how important the vaccine is. The results are really interesting and as per the claim by the researchers : by day 21 after vaccination, antibody titers of 1:40 or more were observed in 96.7% those who received the 15-µg dose and 93.3% who received the 30-µg dose. No deaths, serious adverse events, or adverse events of special interest were reported. Local discomfort (e.g., injection-site tenderness or pain) was reported by 46.3% of subjects, and systemic symptoms (e.g., headache) by 45.0% of subjects. Nearly all events were mild to moderate in intensity.
Hope the efforts by the Australian drug maker CSL, Ltd. has yielded a novel vaccine that could take care of the H1N1 pandemic. Congrats once again for this achievement.
Ref : http://content.nejm.org/cgi/content/full/NEJMoa0907413
Sunday, September 6, 2009
Discovery Of Natural Odors- a new way to develop cheaper mosquito repellents !..
Entomologists at the University of California, Riverside (Anandasankar Ray, an assistant professor in the Department of Entomology, and Stephanie Turner, his graduate student) working on fruit flies in the lab have discovered a novel class of compounds that could pave the way for developing inexpensive and safe mosquito repellents for combating West Nile virus and other deadly tropica.
The basis for the 'invention' though looks simple, but this finding is of great importance. As for my knowledge goes most of the mosquito repellents are cyclohalothrins, which are a costly affair to prepare [as a synthetic chemist, I know how difficult its to prepare cyclohalothrins (pyrethroids) e.g., Allethrin & Permethrin. When I was working in Rallis India Limited, one of my senior colleague was working on Permethrin and I know how difficult to introduce the halo group that too by using florochlorocarbons CFCs (banned chemicals !)]. Congrats Anandsankar Ray, for this interesting achievement.
When fruit flies undergo stress, they emit carbon dioxide (CO2) that serves as a warning to other fruit flies that danger or predators could be nearby. The fruit flies are able to detect the CO2 and escape because their antennae are equipped with specialized neurons that are sensitive to the gas.
But fruits and other important food sources for fruit flies also emit CO2 as a by-product of respiration and ripening. If the innate response of the fruit fly is to avoid CO2, how then does it find its way to these foods?. The researchers have have identified a new class of odorants – chemical compounds with smells – present in ripening fruit that prevent the CO2-sensitive neurons in the antennae from functioning. In particular two odors, hexanol and 2,3- butanedione, are strong inhibitors of the CO2-sensitive neurons in the fruit fly.
CO2 emitted in human breath is the main attractant for the Culex mosquito to find people, aiding the transmission of these deadly diseases," Ray said. In their experiments they identified hexanol, and a related odor, butanal, as strong inhibitors of CO2-sensitive neurons in Culex mosquitoes. These compounds can now be used to guide research in developing novel repellents and masking agents that are economical and environmentally safe methods to block mosquitoes.
Those interested can listen to Anandsankar
Fruits better than prviously thought !.......
Polyphenol content in fruits usually refers to extractable polyphenols, but a Spanish scientist working at the Institute of Food Research in Norwich analysed apple, peach and nectarine. She found that nonextractable polyphenol content is up to five times higher than extractable compounds. Its really interesting and that might be the reason why our forefathers used to insist to eat whole fruits (though they might not have studied so exhaustively... !).
The interesting findings like, "polyphenols need to be treated with acid to extract them from the cell walls of fruit in the lab" will help at least now onwards to collect all the useful polyphenols (proanthocyanidins, ellagic acid and catechin) which without this new findings might have gone as waste. Dr Paul Kroon from IFR explains: “In the human body these compounds will be fermented by bacteria in the colon, creating metabolites that may be beneficial, for example with antioxidant activity.
Hope these nonextractable polyphenols, (which mostly escape analysis and are not usually considered in nutritional studies), will play a major part of bioactive compounds in the diet in the days to come. Congrats Professor Saura-Calixto, for this achievement.....
Sunday, August 23, 2009
Wearable Artificial Kidney good bye to dialysis !
I have seen people who had kidney failure and how its difficult to get dailysis & to mentain the sterile conditions to avoid infections. Now thanx to a group of researchers from David Geffen School of Medicine at UCLA, who have come up with a novel idea of developing wearable artificial kidney!.
As per the claim by the researchers, the device—essentially a miniaturized dialysis machine, worn as a belt—weighs about 10 pounds and is powered by two nine-volt batteries. Patients don't need to be hooked up to a full-size dialysis machine, they are free to walk, work, or sleep while undergoing continuous, gentle dialysis that more closely approximates normal kidney function. Despite enduring long hours on dialysis every week—with major limitations in activities, diet, and other areas of life—dialysis patients face high rates of hospitalization and death and more over its a costly affair too.
The Wearable Artificial Kidney is successful in preliminary tests, including two studies in dialysis patients. The new study provides important information on the technical details that made these promising results possible. Though further studies like 'long-term effect' has to be established its a great achievement and hope the researchers will succeed in their endeavor....
Congrats, Victor Gura et.al.,
Launch of Cobroxin for chronic pain relief.....
I used to read in magazines that, there are people who sell Cobra venom (from India) for research purpose and there were many groups working on this field. Yes, now the dream has come true, Nutra Pharma Corp, a biotechnology company that is developing treatments for Adrenomyeloneuropathy (AMN), HIV and Multiple Sclerosis (MS), has announced recently that, it has launched an OTC- pain reliever, Cobroxin, for the treatment of Stage 2 (moderate to severe) chronic pain.
As per the claim by the company, Cobroxin is the first OTC pain reliever clinically proven to treat Stage 2 (moderate to severe) chronic pain. The drug, which was developed by Nutra Pharma’s wholly-owned drug discovery subsidiary, ReceptoPharm, will be available as an oral spray for treating lower back pain, migraines, neck aches, shoulder pain, cramps and neuralgia and as a topical gel for treating repetitive stress, arthritis, and joint pain. More over the claims by the company (All Natural;Non-Addictive ;Non-Narcotic ;Non-Opiate ;More Potent than Morphine ; Long Lasting) are really encouraging and hope will become an alternative to the presently available NSAIDs (which have many side effects).
The mode of action claimed by the researchers, (peptides from the cobra venom) has many ways superior to the current opiate-based analgesics and those containing acetaminophen & there by help to overcome the side effects.
Hope in the days to come the people suffering from chronic pain will have a relief....
For more details on cobroxin u can visit the site ...
Sunday, August 16, 2009
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