April 2014 – All About Drugs

Europe green light for GSK COPD drug Incruse (umeclidinium)

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Apr 302014

Europe green light for GSK COPD drug

Regulators in Europe have given the green light to GlaxoSmithKline’s new chronic obstructive pulmonary disease drug Incruse.

Specifically, the European Commission has granted marketing authorisation for Incruse (umeclidinium) as a once-daily treatment to relieve symptoms in adults with COPD. The drug is a once-daily long-acting muscarinic antagonist (LAMA) delivered by GSK’s Ellipta inhaler.

read

http://www.pharmatimes.com/Article/14-04-28/Europe_green_light_for_GSK_COPD_drug.aspx

5 Things You Should Know About MERS, The Deadly Virus That’s Now Breaking Out In Saudi Arabia

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Apr 252014

The MERS virus.

MERS (Middle Earth Respiratory Virus)

A new spike in cases of a deadly respiratory virus, in Saudi Arabia and the United Arab Emirates, is prompting new fears of an outbreak when the area’s population spikes during the annual Hajj pilgrimage.

The syndrome, called Middle East Respiratory Syndrome (MERS), is caused by a relatively new-to-humans virus that’s a close cousin of SARS, a virus that infected thousands of people worldwide in 2002-2004.

read at

http://www.businessinsider.in/5-Things-You-Should-Know-About-MERS-The-Deadly-Virus-Thats-Now-Breaking-Out-In-Saudi-Arabia/articleshow/34169304.cms

Illustration: http://yvpc.sph.umich.edu/

MERS, koronavirus that is still mysterious

http://medicmagic.net/mers-koronavirus-that-is-still-mysterious.html

MIT chemists design nanoparticles that can deliver three cancer drugs at a time.

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Apr 222014

Targeting Cancer with a Triple Threat | MIT Technology Review

MIT chemists design nanoparticles that can deliver three cancer drugs at a time.

Delivering chemotherapy drugs in nanoparticle form could help reduce side effects by targeting the drugs directly to the tumors. In recent years, scientists have developed nanoparticles that deliver one or two chemotherapy drugs, but it has been difficult to design particles that can carry any more than that in a precise ratio.

Now MIT chemists have devised a new way to build such nanoparticles, making it much easier to include three or more different drugs. In a paper published in the Journal of the American Chemical Society, the researchers showed that they could load their particles with three drugs commonly used to treat ovarian cancer.

read at

http://www.technologyreview.com/aroundmit/526711/targeting-cancer-with-a-triple-threat/

TECHNOLOGYREVIEW.COM

More and more companies are using fragment-based lead design as a drug discovery strategy

DRUG DESIGN Comments Off

Apr 222014

shaking hands

Small fragments that bind in nearby pockets can be connected to make a lead.

In the pursuit of new pharmaceuticals, many medicinal chemists want to start their leg of the drug discovery race with a drug-sized molecule that binds with a tenacious grip—we’re talking nanomolar potency—to its biological target. After all, there are so many molecular traits to optimize, such as reducing a drug lead’s toxicity and increasing its solubility in the body, that beginning with high-binding affinity seems like starting on the right foot. That’s why high-affinity hits are the primary aim of high-throughput screening (HTS), a bread-and-butter starting point for drug lead discovery.

But a growing number of medicinal chemists are leaving the high-affinity paradigm behind. These researchers are sidestepping some of the cherished tenets of HTS in favor of an emerging drug discovery strategy called fragment-based lead discovery (FBLD).

READ AT

http://cen.acs.org/articles/86/i29/Piece-Piece.html

Academic−Industrial Partnerships in Drug Discovery and Development

drugs Comments Off

Apr 222014

thumbnail image: Academic−Industrial Partnerships in Drug Discovery and Development

Author: Jonathan Faiz
Published: 22 April 2014
Copyright: Wiley-VCH Verlag GmbH & Co. KGaA
Source / Publisher: Angewandte Chemie International Edition
Associated Societies: Gesellschaft Deutscher Chemiker (GDCh), Germany
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The pharmaceutical industry is facing economic and strategic pressures to remain productive and profitable, and those involved in basic research in academia are encountering difficulties as funding is shifting toward more applied areas. Thus, the field of drug design and development can benefit from academic−industrial partnerships. In his Editorial, K. C. Nicolaou, Rice University, Houston, TX, USA, discusses the challenges and opportunities for such collaborations.

http://www.chemistryviews.org/details/news/6104841/AcademicIndustrial_Partnerships_in_Drug_Discovery_and_Development.html

One-Two Nanopunch For Difficult-To-Treat Breast Cancer Drug Delivery: Layered nanoparticles deliver a gene silencer and a drug to shrink tumors

cancer, drug delivery Comments Off

Apr 212014

Illustration of layer-by-layer synthesis of nanoparticles for treating breast cancer tumors

Double Duty

To deliver a one-two nanopunch to triple-negative breast cancer tumors, researchers start with a lipid-coated sphere filled with the chemotherapy drug doxorubicin (left). Then they add alternating layers of poly-L-arginine and an siRNA sequence (center), capped off by a layer of hyaluronic acid (right), which disguises the particle from the body’s immune system.

read at

http://cen.acs.org/articles/91/web/2013/10/One-Two-Nanopunch-DifficultTreat-Breast.html

Women with triple-negative breast cancer, a rare but aggressive form of the disease, often find that it is difficult to treat. An early diagnosis allows more treatment options, but women with this type of cancer generally have a lower survival rate than those with other types of breast cancers. To tackle the disease, a team of researchers has developed a nanomedicine that delivers a one-two punch to tumors that weakens their defenses and obliterates them (ACS Nano 2013, DOI: 10.1021/nn4047925).

Nanoparticles Deliver Three Cancer Drugs To Tumors Drug Delivery: Polymeric materials deliver specific amounts of multiple drugs to disease cells

nanotechnology Comments Off

Apr 212014

Graphic show that a nanoparticle with cisplatin core (green) is formed by polymerization of doxorubicin- and camptothecin-derivatized monomers and a cisplatin cross-linker.

CANCER KILLER

A drug-delivering nanoparticle with cisplatin core (green) is formed by polymerization of doxorubicin- and camptothecin-derivatized monomers and a cisplatin cross-linker.

http://cen.acs.org/articles/92/i16/Nanoparticles-Deliver-Three-Cancer-Drugs.html

The first polymer nanoparticles that carry a defined ratio of three cancer drugs and release them with three independent triggering mechanisms have been developed. The approach could provide a new way of delivering specific amounts of multiple drugs to patients and could help researchers optimize doses of such combination therapies.

The drug delivery nanoparticles were developed by Jeremiah A. Johnson of MIT and coworkers (J. Am. Chem. Soc. 2014, DOI: 10.1021/ja502011g).

read all this at

http://cen.acs.org/articles/92/i16/Nanoparticles-Deliver-Three-Cancer-Drugs.html

A highly efficient and recyclable ligand-free protocol for the Suzuki coupling reaction of potassium aryltrifluoroborates in water

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Apr 192014

A highly efficient and recyclable ligand-free protocol for the Suzuki coupling reaction of potassium aryltrifluoroborates in water

Green Chem., 2014, 16,2185-2189
DOI: 10.1039/C3GC42182A, Paper

Leifang Liu, Yan Dong, Nana Tang
A highly efficient, recyclable and ligand-free protocol was developed for the Suzuki coupling reaction of potassium aryltrifluoroborates in water.

http://pubs.rsc.org/en/Content/ArticleLanding/2014/GC/C3GC42182A?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

A highly efficient, recyclable and ligand-free protocol was developed for the Suzuki coupling of aryl halides with potassium aryltrifluoroborates in water using Pd(OAc)₂ as a catalyst and Na₂CO₃ as a base in air. The presence of poly(ethylene glycol) (PEG) was crucial to the efficiency of the protocol. A wide range of functional groups were tolerated under the optimized conditions. Furthermore, the protocol could be extended to the Suzuki coupling of heteroaryl halides with potassium phenyltrifluoroborate, delivering the desired products in moderate to excellent yields. After simple workup, Pd(OAc)₂–H₂O–PEG could be recycled at least eight times without significant loss in activity.

The role of modern drug discovery in the fight against neglected and tropical diseases

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Apr 192014

The role of modern drug discovery in the fight against neglected and tropical diseases

Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00011K, Review Article

Jeremy N. Burrows, Richard L. Elliott, Takushi Kaneko, Charles E. Mowbray, David Waterson
The future of drug discovery for neglected and tropical diseases will depend on the ability of those working in the area to collaborate and will require sustained resourcing and focus

http://pubs.rsc.org/en/Content/ArticleLanding/2014/MD/C4MD00011K?

utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FMD+%28RSC+-+Med.+Chem.+Commun.+latest+articles%29#!divAbstract

Neglected and tropical diseases affect a large proportion of the world’s population and impose a huge economic and health burden on developing countries. Despite this, there is a dearth of safe, effective, suitable medications for treatment of these diseases, largely as a result of an underinvestment in developing new drugs against these diseases by the majority of research-based pharmaceutical companies. In the past 12 years, the situation has begun to improve with the emergence of public-private product development partnerships (PDPs), which foster a collaborative approach to drug discovery and have established strong drug development pipelines for neglected and tropical diseases. Some large pharmaceutical companies have also now established dedicated research sites for developing world diseases and are working closely with PDPs on drug development activities. However, drug discovery in this field is still hampered by a lack of sufficient funding and technological investment, and there is a shortage of the tools, assays, and well-validated targets needed to ensure strong drug development pipelines in the future. The availability of high-quality chemically diverse compound libraries to enable lead discovery remains one of the critical bottlenecks. The pharmaceutical industry has much that it can share in terms of drug discovery capacity, know-how, and expertise, and in some cases has been moving towards new paradigms of collaborative pre-competitive research with the PDPs and partners. The future of drug discovery for neglected and tropical diseases will depend on the ability of those working in the area to collaborate together and will require sustained resourcing and focus.

Med. Chem. Commun., 2014, Advance Article

DOI: 10.1039/C4MD00011K

Boston Scientists Develop New Probiotic Supplement to Manage Weight

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Apr 192014

Boston Scientists Develop New Probiotic Supplement to Manage Weight

(Boston) – Healthcare experts continue to regard probiotics as one of the most powerful tools in the management of everything from constipation and bloating to diarrhea and skin health.

Historically, yogurt has been a primary source of probiotics, but yogurt products loaded with sugar have their own health implications for the tens of millions of Americans who are trying to lose weight. Sales of the healthier Greek-style yogurt were up 50% in 2012, showing that Americans are looking for healthier probiotic options. Unfortunately, even most Greek yogurt is loaded with sugar and calories.

So, how is the weight-conscious American supposed to get their probiotics?

http://www.howlifeworks.com/health_beauty/A_Simple_Way_to_Lose_Pounds_and_Relieve_Gas_and_Bloating_458?ag_id=1505&wid=8DC8FAB4-7586-49C7-938A-93851D50A3B9&did=5484&cid=1005&si_id=4193&pubs_source=mpt&pubs_campaign=20140418-1505