Cladribine-the first oral disease-modifying multiple sclerosis therapy ?

In my earlier blog, I have mentioned about the NDA (new drug application) of this drug Cladribine as drug to treat Multiple Sclerosis.  Now as per the report by Decision Resources, one of the world's leading research and advisory firms for pharmaceutical and healthcare issues, finds that a recent "refuse to file" (RTF) letter issued by the FDA regarding Merck Serono's oral cladribine has heightened the competition between oral cladribine and its primary competitor, Novartis/Mitsubishi Tanabe's FTY-720 (fingolimod), to be the first oral disease-modifying multiple sclerosis therapy to reach the market in the United States.

Although oral cladribine's first-to-market advantage over FTY-720 will be reduced as a result of a likely delay to market caused by the FDA's action, oral cladribine is still expected to launch in the U.S. in 2010 while FTY-720 remains on track to launch in early 2011. .....

Ref : http://www.decisionresources.com/News-and-Events/Press-Releases/Multiple-Sclerosis-010510

Imetelstat (GRN 163L) shows promising results against brain cancer glioblastoma and prostate cancer...

In continuation of my update on Telomerase inhibitors, I find this info really interesting and hence sharing here with. As mentioned in my earlier blog about imetelstat (GRN163L )  has been undergoing Phase I clinical trials designed to examine the safety, tolerability, pharmacokinetics and pharmacodynamics of the drug, alone or in combination, in solid tumors, chronic lymphoproliferative disease, multiple myeloma, lung and breast cancers and the company claims that Phase I objectives for imetelstat  (structure) have been achieved. Now  Dr. Jerry Shay, professor of cell biology of  The University of Texas Southwestern Medical Center at Dallas, claims that the same drug shows promise in fighting the brain cancer glioblastoma and prostate cancer.

Glioblastomas are the most common malignant brain tumors in adults, according to the American Cancer Society. They are difficult to treat with drugs because blood vessels in the brain have tightly constructed walls that allow only a few substances to pass through.

The researcher focused on cells called tumor-initiating cells. Some researchers believe that tumors contain a small subset of initiating cells – or cancer stem cells – that are able to initiate and drive tumors and that are often resistant to radiation therapy and chemotherapy.

In the glioblastoma study, Dr. Shay and his colleagues found that imetelstat blocked the action of telomerase in isolated tumor-initiating cells as well as the bulk of the tumor cells, eventually killing the cells. Combining imetelstat with radiation and a standard chemotherapy drug made imetelstat even more effective. When the researchers implanted human tumor-initiating cells into rodents, they found that imetelstat was able to enter brain tissue and inhibit telomerase activity.

In the prostate cancer study, the researchers isolated tumor-initiating cells from human prostate cancer cells. The cells showed significant telomerase activity. Imetelstat blocked the enzyme’s activity, and telomeres shortened greatly. As per Dr.Shay, since the drug attacks a mechanism that is active in most cancers, it might prove to be widely useful, especially when combined with other therapies.

Hope  Geron people must be really happy for these results  and conclusions.....

Ref : http://www.utsouthwestern.edu/utsw/cda/dept353744/files/570509.html

Liquorice root for antibiotic-resistant infections resulting from severe burns...

Liquorice root candy, or properly Glycyrrhiza glabra, is the dried root  of the liquorice plant (see pictures - credit : wikipedia), which is eaten as a candy. It is also used in traditional Chinese medicine, as well as in the traditional medicines of Japan, Korea, Vietnam, and other Asian nations (In India ಯಷ್ಠಿಮಧು/ಅತಿಮಧುರ (in kannada & मुलहठी in hindi). The extract of the liquorice root is one of the main ingredients in liquorice confectionery. Liquorice root can be shredded and added to boiling water to create liquorice root tea. Liquorice root has been traditionally used as a herbal remedy against different symptoms, such as cough and catarrh. People with heart conditions or high blood pressure should avoid ingesting extensive amounts of liquorice, as it can further heighten blood pressure and lead to stroke.

Though liquorice root has also been reported to speed the healing of canker sores, now researchers from University of Texas Medical Branch and Shriners Hospitals for Children have come up with more interesting findings, that is root can be used to treat antibiotic-resistant infections resulting from severe burns. They found that in burned mice, glycyrrhizin improved the ability of damaged skin to create small proteins that serve as the first line of defense against infection. These proteins, called antimicrobial peptides, work by puncturing the cell membranes of bacteria similar to how pins pop balloons. As per the claim by the researchers lead by Dr. Fujio Suzuki, more research is necessary to determine if this finding would have any implications for people with cystic fibrosis, who can develop Pseudomonas aeruginosa infections in their lungs.

Ref : http://www.jleukbio.org/cgi/content/abstract/87/1/35

Donepezil hydrochloride for Dementia Related to Alzheimer's Disease...

We know that, ARICEPT® [donepezil hydrochloride, see structure  (source-chemSpider) ] is a reversible inhibitor of the enzyme acetylcholinesterase, known chemically as (±)-2,3-dihydro-5,6-dimethoxy-2 -[[1-(phenylmethyl)-4-piperidinyl]- methyl]-1H-inden-1-one hydrochloride. Donepezil hydrochloride is commonly referred to in the pharmacological literature as E2020.

Acetylcholinesterase is the target of many Alzheimer's Dementia drugs , nerve gases, particularly the organophosphates (e.g. Sarin) and insecticides (e.g. carbaryl). These agents — known as cholinesterase inhibitors — block the function of acetylcholinesterase and thus cause excessive acetylcholine to accumulate in the synaptic cleft. The excess acetylcholine causes neuromuscular paralysis (i.e. interminable muscle contractions) throughout the entire body, leading to death by asphyxiation.

The U.S. Food and Drug Administration approved the first generic versions of Aricept (donepezil hydrochloride) orally disintegrating tablets on Dec. 11. Donepezil hydrochloride is indicated for the treatment of dementia related to Alzheimer's disease. Orally disintegrating tablets dissolve on the tongue, without having to be swallowed whole. This may make it easier to take the medication for older or disabled patients who have difficulty swallowing.

Alzheimer's disease :

Alzheimer's disease is an irreversible, progressive brain disease that slowly destroys memory and thinking skills and, eventually, the ability to carry out the simplest tasks of daily living. In most people with Alzheimer's disease, symptoms first appear after age 60. Alzheimer's disease is the most common cause of dementia among older people, but it is not a normal part of aging...

Ref : http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm194173.htm

Quetiapine fumarate (Seroquel XR) for Major Depressive Disorder (MDD)....

Quetiapine fumarate (see structure) is marketed by AstraZeneca as Seroquel or SeroquelXR and by Orion Pharma as Ketipinor, is an atypical antipsychotic schizophrenia used in the management of, bipolar I mania, bipolar II depression, bipolar I depression, and used off-label for a variety of other purposes, including insomnia and anxiety disorders.

It is sometimes used off-label, often as an augmentation agent, to treat such conditions as obsessive-compulsive disorder, post-traumatic stress disorder, restless legs syndrome, autism, alcoholism, depression, Tourette syndrome, and has been used by physicians as a sedative for those with sleep disorders or anxiety disorders.

Astra-Zeneca, recently  announced that the FDA has approved once-daily Seroquel XR (quetiapine fumarate) Extended Release Tablets as adjunctive (add-on) treatment to antidepressants in adults with Major Depressive Disorder (MDD). Seroquel XR is the only medication in its class approved by the FDA to treat both major depressive disorder as adjunctive therapy and acute depressive episodes associated with bipolar disorder as monotherapy. The company claims that this approval for Seroquel XR provides physicians with a new adjunctive treatment option for patients with MDD who have an inadequate response to their current antidepressant. FDAs approval of Seroquel XR is based on a clinical development program in MDD involving 939 patients randomized across two studies that assessed the efficacy and safety of once-daily treatment with Seroquel XR as adjunctive treatment to antidepressants.....

Ref : http://www.astrazeneca.com/media/latest-press-releases/2009/seroquel-us-MDD?itemId=7660757

Dabigatran etexilate a better drug than warfarin for VTE?.

We know that Dabigatran is an anticoagulant from the class of the direct thrombin inhibitors. It is being studied for various clinical indications and may replace warfarin as the preferred anticoagulant in many cases. It is orally administered as the prodrug dabigatran etexilate (marketed as Pradaxa since April 2008 in European countries and Pradax in Canada). It was developed by the pharmaceutical company Boehringer Ingelheim.

Now researchers lead by  Dr. Sam Schulman, a professor of medicine of the Michael G. DeGroote School of Medicine (McMaster University), who conducted a randomized, double-blind trial of 2,539 patients with acute VTE (venous thromboembolism) have found that dabigatran (see structure) is a safe and effective anticoagulant that does not require the routine monitoring or dose adjustments that are necessary with warfarin. In other words, patients can receive the same results in a more convenient manner. 

As per the claim by the researchers, the improvement seen in both groups from the treatments was similar. After six months of treatment, only 2.4 percent of the dabigatran etexilate group (30 patients) and 2.1 percent of the warfarin group (27 patients) experienced recurrent VTE. The safety of the two drugs was also comparable. In the dabigatran etexilate arm, 205 patients experienced bleeding (including 20 patients with major bleeding) versus 277 patients in the warfarin arm (including 24 with major bleeding). Other possible side effects, including death, acute coronary syndromes, and abnormalities in liver function tests, were infrequent in the two groups. Hope patients suffering from VTE will now breathe a sigh of relief....

Ref : http://dailynews.mcmaster.ca/story.cfm?id=6511

Engineered tobacco plants have more potential as a biofuel

Engineered tobacco plants have more potential as a biofuel

New RNA interference technique can silence up to five genes

New RNA interference technique can silence up to five genes

Nonanal (odour produced in humans and birds) - an attractant for the Culex mosquito ?

In continuation of my update on developments in mosquito repellents,  I  found this  interesting info. In  my earlier blog, I mentioned that carbon dioxide   emitted in human  breath  is  the main  attractant  for the    Culex mosquito to find people, aiding the transmission of these deadly diseases. Now scientists from University of California, Davis, have identified the dominant odor naturally produced in humans and birds that attracts the blood-feeding Culex mosquitoes, which transmit West Nile virus and other life-threatening diseases. As per the claim by the researchers, Nonanal (nonanaldehyde or pelargonaldehyde see below structure) is the powerful semiochemical that triggers the mosquitoes' keen sense of smell, directing them toward a blood meal. A semiochemical is a chemical substance or mixture that carries a message.The antennae of the Culex quinquefasciatus are highly developed to detect even extremely low concentrations of nonanal. Mosquitoes detect smells with the olfactory receptor neurons of their antennae.

The UC Davis researchers tested hundreds of naturally occurring compounds emitted by people and birds. They collected chemical odors from 16 adult human subjects, representing multiple races and ethnic groups. More interestingly, Leal and Syed found that nonanal acts synergistically with carbon dioxide, a known mosquito attractant.  Nonanal, in combination with carbon dioxide, increased trap captures by more than 50 percent, compared to traps baited with carbon dioxide alone. Hope this discovery will help those searching for cheaper, environment friendly  repellents.

Ref : http://www.news.ucdavis.edu/search/news_detail.lasso?id=9289 

Oleanolic acid capsules for Hepatitis B......

We  know that Oleanolic acid is a naturally occurring triterpenoid, widely  distributed in food and medicinal plants, related to betulinic acid. It can be found in Phytolacca americana (American pokeweed), and Syzygium spp, garlic, etc. It is relatively non-toxic, antitumor, and hepatoprotective (antihepatotoxic - protecting liver cells against toxins) as well as exhibiting antiviral properties.

Oleanolic acid was found to exhibit strong anti-HIV activity, the related compound betulinic acid was used to create the first commercial maturation inhibitor drug. It was first studied and isolated from several plants, including Rosa woodsii (leaves), Prosopis glandulosa (leaves and twigs), Phordendron juniperinum (whole plant), Syzygium claviflorum (leaves), Hyptis capitata (whole plant), and Ternstromia gymnanthera (aerial part). Other Syzygium species including java apple (Syzygium samarangense) and rose apples contain it.

Now Biostar Pharmaceuticals, Inc. has completed preparation to launch its flagship Xin Aoxing Oleanolic Acid ("Xin Aoxing") Capsules for the treatment of Hepatitis B in Beijing and Shanghai in early January 2010.....

Ref : http://www.biostarpharmaceuticals.com/newsdisp.asp?id=78