Jun 292013
FDA OKs Novartis’ Exelon Patch for Severe Alzheimer’s
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Jun 292013
Novartis Exelon® Patch now FDA approved to treat patients across all stages of Alzheimer’s disease
http://www.pharmalive.com/fda-oks-novartis-exelon-patch-for-alzheimers
Exelon Patch (rivastigmine transdermal system) contains rivastigmine, a reversible cholinesterase inhibitor known chemically as (S)- 3-[1-(dimethylamino) ethyl]phenyl ethylmethylcarbamate. It has an empirical formula of C14H22N2O2 as the base and a molecular weight of 250.34 (as the base). Rivastigmine is a viscous, clear, and colorless to yellow to very slightly brown liquid that is sparingly soluble in water and very soluble in ethanol, acetonitrile, n-octanol and ethyl acetate.
The distribution coefficient at 37°C in n-octanol/phosphate buffer solution pH 7 is 4.27.
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Exelon Patch is for transdermal administration. The patch is a four-layer laminate containing the backing layer, drug matrix, adhesive matrix and overlapping release liner (see Figure 1). The release liner is removed and discarded prior to use.
Figure 1: Cross Section of the Exelon Patch
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Layer 1: Backing Film
Layer 2: Drug Product (Acrylic) Matrix
Layer 3: Adhesive (Silicone) Matrix
Layer 4: Release Liner (removed at time of use)
Excipients within the formulation include acrylic copolymer, poly(butylmethacrylate, methylmethacrylate), silicone adhesive applied to a flexible polymer backing film, silicone oil, and vitamin E.
Navidea starts clinical trial for Alzheimer’s diagnostic drug
Phase 3 drug
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Jun 282013
Navidea Biopharmaceuticals hopes to bring an early diagnostic drug for Alzheimer’s disease to market.
AZD4694, NAV4694 STRUCTURE
Navidea starts clinical trial for Alzheimer’s diagnostic drug
Business First of Columbus
The Phase 3 trial for the Alzheimer’s agent, at the moment named NAV4694, will compare how well the drug displays the buildup of a damaging protein in the brain of patients believed to have Alzheimer’s compared with what’s found in the autopsy. There …
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http://www.bizjournals.com/columbus/news/2013/06/27/navidea-starts-clinical-trial-for.html
http://jnm.snmjournals.org/content/54/6/880.abstract
Navidea Biopharmaceuticals, a Dublin, Ohio biopharmaceutical company focused on precision diagnostics, earlier this week announced the completion of a study of its novel radiopharmaceutical NAV4694 as a biomarker for Alzheimer’s disease (AD).
NAV4694 is designed to aid visual detection and quantification of cerebral beta amyloid in diagnosing Alzheimer’s disease (AD). One hallmark of AD is the accumulation of beta amyloid plaques between nerve cells in the brain.
The study was designed and conducted by Navidea’s partner, AstraZeneca, to assess the safety and of the biomarker during PET scanning in subjects with AD and in healthy volunteers. Efficacy measures included binding parameters and overall image quality. The 16-patient trial was completed at Karolinska Institutet sites in Stockholm, Sweden.
DATE RAPE DRUGS-What is Rohypnol?
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Jun 272013
FLUNITRAZEPAM
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Rohypnol |  |
What is Rohypnol?“Roofies.” Sounds like a cartoon character or a piece of candy. However, nothing could be further from the truth about Roofies, also known as the drug Rohypnol.Rohypnol (Flunitrazepam) is a type of benzodiazepine, a class of drugs that depresses the central nervous system. You may have heard of Valium and Xanax. These are also benzodiazepines used as sedatives and antianxiety agents. Rohypnol was developed as a sleeping aid. It is also used in therapy settings to relax patients and to get them talking. Rohypnol is manufactured in Europe and Latin American and is sold in many countries around the world. However, it is illegal in the United States and Canada. The pills are round, white and smaller than aspirin. Because Rohypnol is inexpensive, it is becoming popular with high school and college students. In the US, Rohypnol is used mostly at parties, and usually taken with alcohol. It has a synergistic effect with other drugs such as alcohol. This means that one drug increases the effect of the other. |
Rohypnol Tablets Image courtesy of the U.S. Department of Justice |
Behavioral Effects of RohypnolRohypnol can produce amnesia (memory loss) and muscle relaxation and make people lower their inhibitions. An inhibition is when you feel like you can’t do something. When inhibitions are lowered, people feel as if an obstacle has been removed. Therefore, they can talk more freely and feel less shy. Continued, repeated use of Rohypnol may result in addiction and although Rohypnol is a sedative, it can cause aggressive behavior in some people. Withdrawal symptoms may occur and include headaches, sore muscles, hallucinations, convulsions, and possibly seizures 1-2 weeks after quitting the drug. Although overdoses are rarely fatal, emergency services are sometimes required because Rohypnol can cause a person to vomit, hallucinate, have trouble breathing and fall into a coma. When Rohypnol is combined with alcohol the outcome is usually worse. Street names for Rohypnol include rophies, ruffies, R2, roofenol, Roche, la rocha, rope, roopies, ropies, and rib. |
Because Rohypnol is colorless, odorless and flavorless, it can be slipped into drinks unnoticed. This is one reason this drug is so dangerous. People may consume it without knowing it. It dissolves quickly and takes effect in 20-30 minutes. Its effects can last 8-12 hours. Within the past few years, Rohypnol has become known as the “date rape” drug. People will come home from a party and have no idea what happened to them because they unknowingly ingested Rohypnol, passed out, and woke up several hours later with no memory of the evening. To address this new use, Congress passed the “Drug-Induced Rape Prevention and Punishment Act of 1996” to increase federal penalties for the use of any controlled substance to aid in a sexual assault.
Effects of Rohypnol on the BrainThe benzodiazepines influence behavior by interacting with receptors on neurons in the brain that use the neurotransmitter called GABA. When GABA binds to receptors, it usually inhibits a neuron and acts to reduce neuronal activity. When benzodiazepines attach to GABA receptors, they increase GABA binding to other receptors. In this way, benzodiazepines enhance the effects of GABA and reduce brain activity.The fact that there are receptors for benzodiazepines in the brain suggests that the brain makes its own type of benzodiazepine. The brain has been found to make its own morphine, the endorphins, but the brain’s own benzodiazepine has not yet been discovered.
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Vical and Astellas Announce Initiation of Phase 3 Trial of ASP0113 Cytomegalovirus Vaccine
VACCINE
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Jun 272013
Illustration of the CMV life cycle from viral entry to egress of new infectious virions.
Jun 25, 2013, Vical Incorporated and Astellas Pharma Inc. today announced the initiation of a multinational Phase 3 registration trial of ASP0113 (TransVax(TM)), in approximately 500 hematopoietic cell transplant (HCT) recipients. Vical and Astellas entered into exclusive worldwide license agreements in 2011 to develop and commercialize ASP0113, Vical’s investigational therapeutic vaccine designed to control cytomegalovirus (CMV) in transplant recipients. Astellas is conducting the trial, and Vical is providing development, regulatory and manufacturing support. The companies expect to begin a separate Phase 2 trial of ASP0113 in solid organ transplant (SOT) recipients later this year.
About ASP0113
ASP0113 is an investigational bivalent DNA vaccine containing plasmids (closed loops of DNA) encoding human CMV pp65 and gB antigens for induction of both cellular and humoral immune responses. ASP0113 is formulated with a proprietary poloxamer-based delivery system. ASP0113 has received orphan drug designation in the United States and Europe for HCT and SOT patients.
About CMV
CMV is a herpes virus that infects more than half of all adults in the United States by age 40, and is even more widespread in developing countries. A healthy immune system typically protects an infected person against CMV disease, but does not prevent or clear latent infection, and those whose immune systems are not fully functional are at high risk of CMV reactivation, potentially leading to severe illness or death. Those at greatest risk include transplant patients and infants born to mothers who first become infected during pregnancy. Vical is pursuing two distinct vaccine approaches for these separate market segments: ASP0113 for the transplant market and CyMVectin(TM) for the congenital disease market.
About Astellas
Astellas Pharma Inc., located in Tokyo, Japan, is a pharmaceutical company dedicated to improving the health of people around the world through the provision of innovative and reliable pharmaceutical products. Astellas has approximately 17,000 employees worldwide. The organization is committed to becoming a global category leader in Urology, Immunology (including Transplantation) and Infectious diseases, Oncology, Neuroscience and DM Complications and Kidney diseases. For more information on Astellas Pharma Inc., please visit www.astellas.com/en.
About Vical
Vical researches and develops biopharmaceutical products based on its patented DNA delivery technologies for the prevention and treatment of serious or life-threatening diseases. Potential applications of the company’s DNA delivery technology include DNA vaccines for infectious diseases or cancer, in which the expressed protein is an immunogen; cancer immunotherapeutics, in which the expressed protein is an immune system stimulant; and cardiovascular therapies, in which the expressed protein is an angiogenic growth factor. The company is developing certain infectious disease vaccines and cancer therapeutics internally. In addition, the company collaborates with major pharmaceutical companies and biotechnology companies that give it access to complementary technologies or greater resources. These strategic partnerships provide the company with mutually beneficial opportunities to expand its product pipeline and address significant unmet medical needs. Additional information on Vical is available at www.vical.com.
GSK presents data from five Phase III studies of albiglutide to treat type 2 diabetes
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Jun 272013
June 25, 2013, GlaxoSmithKline ( GSK ) recently presented data from five phase III studies (Harmony 1 to 5) on its once-daily diabetes candidate, albiglutide at the 73rd scientific session of American Diabetes Association.
In the five Harmony studies, albiglutide demonstrated significant efficacy in reducing HbA1c, an indicator of glucose level in the blood, versus placebo and/or active comparators (including insulin, a sulphonylurea, a thiazolidinedione and a dipeptidyl peptidase four inhibitor) after 1-2 years. The candidate met the primary efficacy endpoint in these studies.
Read more: http://www.nasdaq.com/article/glaxo-presents-albiglutide-data-analyst-blog-cm255791#ixzz2XNwNdQAR
Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist) drug under investigation by GlaxoSmithKline for treatment of type 2 diabetes. It is a dipeptidyl peptidase-4-resistantglucagon-like peptide-1 dimer fused to human albumin.
Albiglutide has a half-life of four to seven days, which is considerably longer than the other two GLP-1 analogs approved for market use, exenatide (Byetta) and liraglutide (Victoza).[1][2] GLP-1 drugs are currently only available for subcutaneous administration on a daily basis, so a GLP-1 drug with a longer half-life is desirable. Such a drug would only need to be injected biweekly or weekly instead of daily, reducing the discomfort and inconvenience of GLP-1 administration considerably.
It has not yet been determined whether albiglutide is as effective an antidiabetic agent as GLP-1 drugs currently on the market, and final data remain to be published regarding the incidence of adverse effects related to the drug. To evaluate the efficacy and safety of the drug, albiglutide is undergoing eight Phase III clinical trials.
New Fycompa® (perampanel) Data Presented at International Epilepsy Congress (IEC)
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Jun 272013
PERAMPANEL
New data provides additional evidence for use of Fycompa in partial-onset epilepsy
HATFIELD, England, June 26, 2013 /CNW/ – New data from 11 abstracts, including two oral presentations, presented at the 30th International Epilepsy Congress (IEC) in Montreal, Canada provide additional data on the safety, efficacy and impact on quality of life (QOL) of once daily Fycompa® (perampanel) as adjunct treatment in partial-onset epilepsy, the most common form of seizures.
Perampanel (trade name Fycompa) is an antiepileptic drug developed byEisai Co. that acts as a selective noncompetitive antagonist of AMPA receptors, the major subtype of ionotropic glutamate receptors.
Perampanel was found to be effective in the treatment of refractory partial-onset seizures in three pivotal (Phase 3) clinical trials and has been approved for marketing under the brand name Fycompa by the European Medicines Agency. The minimum effective dose is 4 mg once daily; doses of 8 mg and 12 mg daily provide a greater therapeutic benefit with a corresponding increase in adverse events. Dizziness and somnolence/sedation/fatigue are the most frequent dose-related adverse events. The drug is currently approved, for the control of partial-onset seizures, in those of both sexes who suffer from epilepsy and who are 12 years of age and older, by the Food and Drug Administration, and is considered to be a scheduled drug (an agent with the potential for addiction). Perampanel has been studied in other clinical indications includingParkinson’s disease.
Could “Magic” Mushrooms be used to treat anxiety and depression?
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Jun 252013
Emerging research indicates that low doses of the active chemical psilocybin can have positive psychiatric effects. Image via Wikimedia Commons/Dohduhdah
The latest study, published last week in Experimental Brain Research, showed that dosing mice with a purified form of psilocybin reduced their outward signs of fear. The rodents in the study had been conditioned to associate a particular noise with the feeling of being electrically shocked, and all the mice in the experiment kept freezing in fear when the sound was played even after the shocking apparatus was turned off. Mice who were given low doses of the drug, though, stopped freezing much earlier on, indicating that they were able to disassociate the stimuli and the negative experience of pain more easily.
Psilocybin is a naturally occurring psychedeliccompound produced by more than 200 species of mushrooms, collectively known aspsilocybin mushrooms. The most potent are members of the genus Psilocybe, such asP. azurescens, P. semilanceata, and P. cyanescens, but psilocybin has also been isolated from about a dozen other genera. As a prodrug, psilocybin is quickly converted by the body to psilocin, which has mind-altering effects similar to those of LSD, mescaline, and DMT. The effects generally include euphoria, visual and mental hallucinations, changes in perception, a distorted sense of time, and spiritual experiences, and can include possible adverse reactions such as nausea and panic attacks.
Psilocybin (O-phosphoryl-4-hydroxy-N,N-dimethyltryptamine or 4-PO-DMT) is a prodrug that is converted into the pharmacologicallyactive compound psilocin in the body by a dephosphorylation reaction. This chemical reaction takes place under strongly acidicconditions, or under physiological conditions in the body, through the action of enzymes called phosphatases.
Psilocybin is a tryptamine compound with a chemical structure containing an indole ring linked to an ethylamine substituent. It is chemically related to the amino acid tryptophan, and is structurally similar to the neurotransmitter serotonin. Psilocybin is a member of the general class of tryptophan-based compounds that originally functioned as antioxidants in earlier life forms before assuming more complex functions in multicellular organisms, including humans. Other related indole-containing psychedelic compounds includedimethyltryptamine, found in many plant species and in trace amounts in some mammals, and bufotenine, found in the skin ofpsychoactive toads. Biosynthetically, the biochemical transformation from tryptophan to psilocybin involves several enzyme reactions: decarboxylation, methylation at the N9 position, 4-hydroxylation, and O-phosphorylation. Isotopic labeling experiments suggest that tryptophan decarboxylation is the initial biosynthetic step and that O-phosphorylation is the final step. The precise sequence of the intermediate enzymatic steps is not known with certainty, and the biosynthetic pathway may differ between species.
A possible biosynthetic route to psilocybin. Although the order of the first (decarboxylation) and last (phosphorylation) steps are known with some certainty, the sequence of the two intermediate steps is speculative.
New aspects of natural products in drug discovery
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Jun 252013
Structures of compounds of microbial origin that are in development as anti-infective agents. Key to compounds: 1, arylomycin; 2, ECO-0501; 3, GE23077; 4, GE81112; 5, LBM415; 6, AC98–6446.
During the past 15 years, most large pharmaceutical companies have decreased the screening of natural products for drug discovery in favor of synthetic compound libraries. Main reasons for this include the incompatibility of natural product libraries with high-throughput screening and the marginal improvement in core technologies for natural product screening in the late 1980s and early 1990s. Recently, the development of new technologies has revolutionized the screening of natural products. Applying these technologies compensates for the inherent limitations of natural products and offers a unique opportunity to re-establish natural products as a major source for drug discovery. Examples of these new advances and technologies are described in this review.
http://www.sciencedirect.com/science/article/pii/S0966842X07000686
New aspects of natural products in drug discovery
- Nereus Pharmaceuticals Inc., 10480 Wateridge Circle, San Diego, CA 92121, USA
- Available online 11 April 2007
Jun 242013
LINAGLIPTIN
Phase III studies show linagliptin improved blood glucose control in Asian …
Wall Street Journal
RIDGEFIELD, Conn. and INDIANAPOLIS, June 22, 2013 /PRNewswire/ — Boehringer Ingelheim Pharmaceuticals, Inc. and Eli Lilly and Company (NYSE: LLY) today announced results from two phase III clinical studies that showed linagliptin in Asian adults, as …
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