Pharmacology/ Therapeutics

• EuroHYP EU Grant Award for Stroke
  Proteome Sciences plc (“Proteome Sciences”) announces that Euro-HYP-1, a consortium of leading academic, clinical and industrial European partners in which it is a member, has been awarded a near €11m grant under the EU Framework 7 programme for new ground breaking research on the treatment of stroke.
• Rainforest remedy could spell end of dental pain
  An ancient Incan toothache remedy – for centuries handed down among an indigenous people in the rainforests of Peru – could be on the cusp of revolutionising worldwide dental practice.
• Brain network provides hope for tinnitus sufferers
  As Brain Awareness Week (12–18 March) gets underway in the UK, the preliminary findings from the latest tinnitus research suggest that hearing aids might help tinnitus sufferers; research is ongoing into the role the brain has, and how tinnitus symptoms are reflected in brain network activity.
• CRT unveils ‘screen test’ for potential drugs to treat oestrogen positive breast cancer
  Cancer Research UK and its commercial arm, Cancer Research Technology have developed a unique test to discover molecules that could lead to potential new treatments for oestrogen receptor (ER)-positive breast cancer.
• £10 million boost for neglected tropical disease research at Dundee
  The University of Dundee has received over £10 million from the Wellcome Trust in the fight against some of the world’s most neglected parasitic diseases, including support for a multi-million pound partnership with GlaxoSmithKline (GSK) to discover new drug treatments.

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25 Hottest Articles

• The growing impact of click chemistry on drug discovery • Review article
  Drug Discovery Today, Volume 8, Issue 24, December 2003, Pages 1128-1137 | Kolb, H.C.; Sharpless, K.B.
• What makes a good drug target? • Review article
  Drug Discovery Today, Volume 16, Issue 23-24, January 2011, Pages 1037-1043 | Gashaw, I.; Ellinghaus, P.; Sommer, A.; Asadullah, K.
• The road ahead for large pharma: long-term science and innovation • Editorial
  Drug Discovery Today, Volume 14, Issue 9-10, May 2009, Pages 439-441 | Lundberg, J.M.; Reilly, C.
• The impact of aromatic ring count on compound developability - are too many aromatic rings a liability in drug design? • Review article
  Drug Discovery Today, Volume 14, Issue 21-22, November 2009, Pages 1011-1020 | Ritchie, T.J.; Macdonald, S.J.F.
• Learning lessons from drugs that have recently entered the market • Review article
  Drug Discovery Today, Volume 16, Issue 9-10, May 2011, Pages 398-411 | Teague, S.J.

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Drug trials

Latest News

• Drug combination domino effect destroys pancreatic cancer cells
  Cancer Research UK scientists have revealed how a combination of two very different drugs, currently being tested in clinical trials, amplifies the destruction of pancreatic cancer cells, according to research published in the Journal of Experimental Medicine, today (Monday).
• Convergence Pharmaceuticals announces start of Phase II study for CNV1014802
  Convergence Pharmaceuticals today announced that the Phase II proof of concept study with CNV1014802 for treating pain associated with lumbosacral radiculopathy (LSR) has started.
• Mental health problems after miscarriage continue after healthy birth
  Women who experience depression and anxiety after a miscarriage continue to experience these symptoms even if they subsequently go on to have a healthy child.
• AstraZeneca and Pfizer Join Cancer Research UK’s Stratified Medicine Programme
  CANCER RESEARCH UK will be supported by AstraZeneca and Pfizer in a multimillion pound initiative to examine how genetic tests to improve cancer diagnosis can be best rolled out across the NHS.Cancer Research UK’s pioneering “Stratified Medicine Programme”* will also promote research into new targeted treatments by building a database of genetic information about tumours, treatments and survival rates that will enable researchers to design more effective cancer treatments in future.
• GSK and Prosensa announce start of Phase III study of investigational Duchenne Muscular Dystrophy medication
  GlaxoSmithKline (GSK) and Prosensa today announced that the first patient has commenced treatment in the Phase III study investigating GSK2402968, in ambulant boys with Duchenne Muscular Dystrophy (DMD), who have a dystrophin gene mutation amenable to an exon 51 skip

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The value of in silico chemistry in the safety assessment of chemicals in the consumer goods and pharmaceutical industries

In this article Sandeep Modi, Michael Hughes, Andrew Garrow and Andrew White discuss limitations and strengths of in silico tools. Additionally, they look at different parameters that are necessary to make the best use of these tools, and also how to gain acceptance outside the modelling community and into the regulatory arena.

The authors propose an integrated workflow for combined use of data extraction, quantitative structure activity relationships and read-across methods. They discuss how the recent advances in this field can enable transition to a new paradigm of the discovery process, as exemplified by the Toxicity Testing in the 21st Century initiative.

Use of magnetic emulsion as a novel drug carrier for chemotherapeutic agents

Magnetic guidance of magnetic emulsion for site specific delivery was investigated in vitro and in vivo. The magnetic emulsion was characterized in vitro for its magnetic responsiveness using a constant flow apparatus, and its high retention by magnetic field was confirmed. After intravenous injection in rat, magnetic emulsions were localized to the predetermined site (lungs) by application of an electromagnet to the lungs. Similarly, 1-(2-chloroethyl)-3-(trans-4-methylcyclohexyl)-1-nitrosourea (methyl-CCNU) contained in the dispersed oily phase of the emulsions, was also concentrated at the target-site. Such preferential localization by magnetic means suggested that magnetic emulsions could become effective drug carriers with site specificity for the delivery of chemotherapeutic agents in cancer chemotherapy.

Keywords

• Drugs, drug delivery, magnetic emulsion;
• electromagnet;
• methyl-CCNU;
• cancer chemotherapy

Copyright © 1983 Published by Elsevier Ltd.

Read more: http://pharmakokon.blogspot.com/2012/04/use-of-magnetic-emulsion-as-novel-drug.html#ixzz1s4vcZnJt

Pharma cology & clinical Ebooks

1. KDT OF PHARMACOLOGY-
2. Medical Pharmacology At A Glance 
3. Wiley (2003) Fundamentals of Psychopharmacology, Third Edition 
4. ) Lippincots Illustrated Reviews_pharmacology_2nd edition 
5. Behavioral Pharmacology of Human Drug Dependence 
6. Modern Pharmacology With Clinical Applications 6th Ed. 
7. The Pharmacological Basis of Therapeutics by Goodman & Gilman  
8. Rang and Dales Pharmacology  
9. Basic & Clinical Pharmacology_Bertram G. Katzung.pdf  
10. Basic & Clinical Pharmacology_10th edition Bertram G. Katzung.pdf 
11. Roach Introductory Clinical Pharmacology 
12. Bioequivalence and Statistics in Clinical Pharmacology by Patterson 
13. ) Pharmaceutical Statistics Practical and Clinical Applications 
14. Clinical Pharmacokinetics Concepts and Applications. 
15. Pharmaceutical and Clinical Calculations  

Pharma Connections Worldwide

Pharma Connections Worldwide

Responding to the Radiation Threat

— The New York Times recently reported that in the darkest moments of the triple meltdown last year of the Fukushima Daiichi nuclear power plant, Japanese officials considered the evacuation of the nearly 36 million residents of the Tokyo metropolitan area. The consideration of so drastic an action reflects the harsh fact that in the aftermath of a major radiation exposure event, such as a nuclear reactor accident or a "dirty bomb" terrorist attack, treatments for mass contamination are antiquated and very limited.
See Also:
Health & Medicine

Pharmacology
Infectious Diseases
Diseases and Conditions

Matter & Energy

Weapons Technology
Nuclear Energy
Chemistry

Reference

Actinide
Heavy metals
Plutonium
Uranium

The only chemical agent now available for decontamination -- a compound known as DTPA -- is a Cold War relic that must be administered intravenously and only partially removes some of the deadly actinides -- the radioactive chemical elements spanning from actinium to lawrencium on the periodic table -- that pose the greatest health threats.

Scientists at the U.S. Department of Energy (DOE)'s Lawrence Berkeley National Laboratory (Berkeley Lab) are developing a much more effective alternative that decontaminates a large number of the actinides likely to be part of the radiation exposure from a nuclear plant or weapon, including plutonium, americium, curium, uranium and neptunium. Furthermore, the Berkeley Lab treatment can be administered orally in the form of a pill, a necessity for prompt treatment in the event of mass contamination. Depending on the level of radiation exposure and how soon treatment can start, one of these pills would result in the excretion of approximately 90-percent of the actinide contaminants within 24 hours. Taking one pill daily for two weeks should be enough to remove virtually all of the actinide contaminants.

"With the expanding use of nuclear power and unfortunate possibility of nuclear weapon use, there is an urgent need to develop and implement an improved therapy for actinide contamination of a large population," says Rebecca Abergel, a chemist who leads the Bioactinide Group at Berkeley Lab's Glenn T. Seaborg Center. "We are now in the process of demonstrating that our actinide-specific decontaminating agents are ready for clinical development."

Once actinides are ingested or inhaled, their radioactivity and cancerous interactions with cells and tissue demand they be immobilized and removed from the body as soon as possible. Abergel and her group are part of an effort at Berkeley Lab that began more than two decades ago under the leadership of Ken Raymond, a chemist who holds joint appointments with Berkeley Lab and the University of California (UC) Berkeley, where he is the Chancellor's Professor of Chemistry, in collaboration with the late Patricia Durbin. The primary goal of this project has been to identify sequestering agents that can encapsulate actinides into tightly bound cage-like chemical complexes for transport out of the body. The early focus of this research was on plutonium, the alpha particle-emitting actinide discovered by Berkeley Lab Nobel laureate Glenn Seaborg, and natural chelators, the crablike molecules that specifically bind with iron and other metal ions.

"Since the biochemical properties of plutonium(IV) and iron(III) are similar, we modeled our sequestering agents after the chelating unit found in siderophores," Raymond says. Siderophores are small molecules secreted by bacteria to extract and solubilize iron. "This biomimetic approach enabled us to design multidentate hydroxypyridonate ligands that are unrivaled in terms of actinide-affinity, selectivity and efficiency."

The two best candidate hydroxypyridonate ligands -- nicknamed HOPO -- developed by Abergel and her colleagues are a tetradentate, which has four chelating arms, and an octadentate, which has eight chelating arms. The "arms" in this case are atoms with pairs of electrons available for covalent bonding with an actinide.

"We've advanced our two candidate ligands through the initial phases of pre-clinical development by successfully scaling up synthesis to the 5-kilograms level and establishing baseline preparation and analytical methods suitable for manufacturing larger amounts under good manufacturing practice guidelines," Abergel says.

The team has also carried out extensive studies in animal models and human cell lines that established the two HOPO candidates as being highly effective and non-toxic at the tested doses. As for comparisons between the two, each has its own merits.

"A single octadentate HOPO can form a full actinide complex and results in more total actinide excretion," Abergel says. "However, it is easier for the smaller tetradentate HOPO to pass through biological membranes and access desired target sites in the body. Both warrant further development for emergency use in the case of a radiological event."

Abergel says the basic research and development phase of these two candidates has been completed and she and her group have started the process with the U.S. Food and Drug Administration (FDA) to determine what further data is needed to move into clinical trials. Typically at this stage of development a private pharmaceutical company would step in but it is difficult to attract private investors for a drug that will hopefully never be needed.

"As we move further along with the FDA process it should be easier to convince private pharmaceutical companies to get involved," Abergel says.

In addition to Abergel, Raymond and Durbin, other researchers who are or have been involved in this project include Dahlia An, Kathleen Bjornstad, Eleanor Blakely, Deborah Bunin, Polly Chang, Shirley Ebbe, Erin Jarvis, Birgitta Kullgren, Chris Rosen, David Shuh, Manuel Sturzbecher-Hoehne and Jide Xu.

There have been several scientific papers published about this work with the most recent being "Multidentate terephthalamidate and hydroxypyridonate ligands: towards new orally active chelators," in the journal Hemoglobin. It was written by Abergel and Raymond.

This research was primarily supported by the National Institutes of Health through the National Institute of Allergy and Infectious Diseases and the Rapid Access to Interventional Development Program. Support also came from the DOE Office of Science.

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