Health Canada approves Trajenta (linagliptin) for type 2 diabetes

Linagliptin (below structure, BI-1356, trade name Tradjenta) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes.Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly. Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Both GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output. Thus, linagliptin stimulates the release of insulin in a glucose-dependent manner and decreases the levels of glucagon in the circulation.

Now Health Canada approves....

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Novel drug shows promise for MLL leukemia

Novel drug shows promise for MLL leukemia:

According to British scientists a potential new drug from GlaxoSmithKline could treat mixed-lineage leukemia (MLL). MLL is the most common form of leukemia in babies. The study appeared in the journal Nature where scientists from the British drugmaker collaborating with the charity Cancer Research UK (CRUK) and Cellzome AG found that the experimental drug, called I-BET151.

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Ref : http://www.nature.com/nature/journal/vaop/ncurrent/full/nature10509.html

Drug Shows Promise Against Deadly Lung Disease

 An experimental drug may offer a thin ray of hope to people suffering from the rapidly fatal lung disease known as idiopathic pulmonary fibrosis. The compound, currently known only as BIBF 1120 (see structure below : Vargatef™), seems to slow the disease, decrease exacerbations and improve quality of life for patients, according to a study funded by the drug's maker, Boehringer Ingelheim.

  "It improves the course of disease and, in my opinion, it's the first drug to significantly ameliorate the really devastating progression of the disease," 

said Dr. Norman Edelman, (chief medical officer for the American Lung Association, who noted that current treatments for the disease "are almost desperation attempts. There's very little evidence they work)..."

Authors don't claim [BIBF 1120] is going to reverse the disease. They claim it's going to slow it down, but even that is a major factor. 

Patients with IPF usually die within two to three years of diagnosis. While the disease used to be considered relatively rare, Edelman noted that doctors have been noticing an uptick in recent ears, especially among older men. Idiopathic pulmonary fibrosis (IPF) involves a relentless stiffening of the lungs due to overproduction of collagen, the "cement" that holds lung tissue together. 

More : http://www.nejm.org/doi/full/10.1056/NEJMoa1103690

Broccoli, Cabbage, and other Veggies May Protect Against Colon Cancer

In continuation of my update on the usefulness of broccoli 
Austrailian researchers examined the diets of 918 colorectal cancer patients and 1,021 people with no history of the disease and found that consumption of certain vegetables and fruits were associated with a decreased risk of cancer in the proximal and distal colon, that is, the upper and lower portions of the colon.

Consumption of brassica vegetables (also known as cole crops) such as broccoli, kale, cauliflower, turnips and cabbage, for example, appeared to reduce the risk of cancer in the upper colon, while both total fruit and vegetable intake (and total vegetable intake alone) reduced the risk of cancer in the lower colon.

They also found that eating more apples and dark, yellow vegetables was linked with a significantly reduced risk of lower colon cancer...


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Preclinical studies shows EmPAC more effective than Taxol

Cornerstone Pharmaceuticals, Inc. has announced the publication of data from preclinical studies on EmPAC™ (nanoparticle reformulation of paclitaxel). Company claims the data demonstrating improved safety and efficacy of EmPAC™ versus Taxol®, the generic formulation of paclitaxel and one of the most widely prescribed chemotherapies. EmPAC™ is a nanoemulsion formulation of Paclitaxel and is the lead product candidate of Cornerstone’s proprietary Emulsiphan™ cancer selective delivery nanotechnology platform. Taxol®, an injectable formulation of Paclitaxel, is currently used to treat a variety of cancers, including ovarian carcinomas, breast cancer, non-small cell lung cancer, and AIDS-related Kaposi’s sarcoma....

More : http://www.cornerstonepharma.com/wp-content/uploads/Empac-JNN-Release-FINAL-Sept_15_2011.pdf

Santarus, Inc. recently  announced that analysis of top-line safety data from a double blind, multicenter 12-month extended use study in patients treated daily with either the investigational drug budesonide (see structure) MMX^® 6 mg or placebo will be provided as support for the company's planned submission of a New Drug Application (NDA) for budesonide MMX 9 mg to the U.S. Food and Drug Administration (FDA) for the induction of remission of mild or moderate active ulcerative colitis. Santarus had previously announced results from two Phase III clinical studies that evaluated the safety and efficacy of budesonide MMX 9 mg over an eight week course of treatment for induction of remission of mild or moderate active ulcerative colitis.

Highlights (of the study of 123 patients) are: 

• The frequency of treatment related adverse events for budesonide MMX 6 mg (21.0%) was similar to placebo (21.3%).
• Mean morning plasma Cortisol levels remained within normal limits at all visits for both budesonide MMX 6 mg and placebo.
• There were no clinically meaningful differences in the numbers of patients with abnormal bone mineral density scans at baseline and end-of-study between budesonide MMX 6 mg and placebo. 

"Now that we have the top-line safety data from the extended use study, we are moving forward as planned to submit the NDA in December 2011 for budesonide MMX 9 mg for the induction of remission of mild to moderate active ulcerative colitis," said Gerald T. Proehl, CEO/President of the company...

More.: http://ir.santarus.com/releasedetail.cfm?ReleaseID=606515

We know that, Linagliptin (BI-1356, trade name Tradjenta) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes. Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly.

Now the companies have announced results of a 102 week Phase III study for linagliptin (trade name Trajenta® in Europe), which show meaningful and durable reductions in blood glucose for adults with type 2 diabetes (T2D). In the two-year study presented today at the 47^th Annual Meeting of the European Association for the Study of Diabetes (EASD), the DPP-4 inhibitor linagliptin showed a favourable safety profile and lowered HbA1c levels by 0.8% over the long term in those patients treated with linagliptin for the full study period. 

Researchers conclude that, these results show that the efficacy achieved by linagliptin is reliable and meaningful in a clinical setting, but also that it is durable over the long term. This is especially important in chronic conditions such as type 2 diabetes.

The data from these patients demonstrate the efficacy and tolerability of linagliptin as mono-, dual- (plus metformin or initial combination with pioglitazone) or triple (plus metformin and sulphonylurea) oral therapy over a period of 102 weeks. Reductions in HbA1c of 0.8% after 24 weeks of blinded treatment were seen to be durable over the additional 78 weeks. Overall, the rate of hypoglycaemic events was low and body weight remained unchanged.

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New drug cure nearly any viral infection?...

Could new drug cure nearly any viral infection? Technology shows promise against common cold, influenza and other ailments, researchers say

More : Broad-Spectrum Antiviral Therapeutics

In continuation of my update on H.Pylorihttp://www.med-chemist.com/search?q=pylori..

We know that,  stomach bacterium Helicobacter pylori is one of the biggest risk factors for the development of gastric cancer, the third most common cause of cancer-related deaths in the world. Molecular biologists from the University of Zurich have now identified a mechanism of Helicobacter pylori that damages the DNA of cells in the gastric mucosa and sets them up for malignant transformation.

 More at :

Biologists identify mechanism of H. pylori that damages DNA of gastric mucosal cells

In continuation of my updates on Rivaroxaban...

FDA Issues Complete Response Letter to Johnson & Johnson Pharmaceutical Research & Development Regarding New Drug Application for Tapentadol Extended Release....

Researchers rethink fenretinide for prevention of oral cancer

In continuation of my update on fenretinide...

For more than two decades, researchers have studied and used fenretinide, a synthetic vitamin A derivative. Fenretinide's capacity to induce both terminal differentiation and cell death yielded highly promising results with cultured human cancer cells. Likewise, studies in lung, breast skin, prostate and bladder animal cancer models re-enforced fenretinide's cancer-preventing effects at the in vivo level. However, when it came to prevention of oral cancer,  fenretinide efficacy wasn't what scientists expected. After multiple studies with lackluster results, oral cancer researchers moved away from fentretinide to look elsewhere for an answer. 

Now researchers lead by Dr. Susan Mallery started rethinking about the failure and  wanted to find  a way to circumvent issues with poor systemic uptake by delivering the compound directly to the lesion. 

Mallery found the answer in partnering with two University of Michigan pharmaceutical chemists (Steven Schwendeman and Kashappa Goud Desai) to develop a first of its kind patch that sticks to the inside of the mouth, and delivers a continuous therapeutic dose of fenretinide directly to the precancerous lesion. The patch consists of three layers: a disk saturated with fenretinide and polymers that make the lipid soluble fenretinide better adsorbed in a water-rich environment, a secondary adhesive ring to hold the disk in place, and a final backing layer that ensures the medication stays inside the area of the patch.

The research team has just completed a pharmacokinetic study in rabbits. Subsequent plans include an initial Phase zero study in humans, followed by a clinical trial to evaluate efficacy in patients with precancerous oral lesions. A companion formulation designed to prevent emergence of pre-cancerous cells within the entire mouth may also be used in the fenretinide patch clinical trial. 

Ref : http://cancer.osu.edu/mediaroom/releases/Pages/Oral-Patch.aspx

Redesigned Vancomycin As Potent Antimicrobial Activity Against Vancomycin-Resistant Bacteria...

In continuation of my update on vancomycin....

A team of scientists from The Scripps Research Institute has successfully reengineered an important antibiotic (Vancomycin)  to kill the   deadliest antibiotic-resistant bacteria. The researchers claim that compound could one day be used clinically to treat patients with life-threatening and highly resistant bacterial infections. The compound synthesized is  an  analogue of the well-known commercial antibiotic vancomycin.

Vancomycin normally works by grabbing hold of and sequestering the bacterial cell-wall making machinery, a peptidoglycan (carbohydrate and peptide containing molecule). Only Gram-positive bacteria have a cell wall, which is a membrane on the cell's outer surface. Unfortunately, bacteria have found a way to alter the peptidoglycan in such a way that the antibiotic can no longer grab hold. Researchers claim that,  the new vancomycin analogue can grab hold of the mutant peptidoglycan, and again prevent the bacteria from making the cell wall and killing the resistant bacteria. But what is so remarkable about the design is that the redesigned antibiotic maintains its ability to bind the wild type peptidoglycan as well.

New compound has an amidine (an iminium, RC=NH+ linked to a nitrogen, N) instead of an amide at a key position buried in the interior of the natural product. I appreciate the idea and the simplicity in achieving the target functional group.

Researchers add that, although it is still at its early stages and there is much work ahead.In my opinion it is a good beginning...

Ref : A Redesigned Vancomycin Engineered for Duald-Ala-d-Ala andd-Ala-d-Lac Binding Exhibits Potent Antimicrobial Activity Against Vancomycin-Resistant Bacteria

New class of anti-diabetic compound established

New class of anti-diabetic compound established

In continuation of my update on Valproic acid...

New research suggests brain tumor patients who take the seizure drug valproic acid on top of standard treatment may live longer than people who take other kinds of epilepsy medications to control seizures. The research is published in the August 31, 2011, online issue of Neurology®, the medical journal of the American Academy of Neurology.....

Ref : http://www.neurology.org/content/75/24/2229.abstract?sid=49b511a0-d597-4598-865c-297439b6eb39

Heat in Chili Peppers Can Ease Sinus Problems, Research Shows

In continuation of my update on the usefulness of   Casaicin...

We know that, Capsicum annum contains capsaicin, which is the main component of chili peppers and produces a hot sensation. Capsaicin is also the active ingredient in several topical medications used for temporary pain relief. It is approved for use by the U.S. Food and Drug Administration and is available over the counter.

Now researchers lead by  Jonathan A. Bernstein of University of Cincinnati College of Medicine, Cincinnati, Ohio, have come up with an interesting finding about Capsicum annum.  As per the claim by the researchers a nasal spray containing an ingredient derived from hot chili peppers (Capsicum annum) may help people "clear up" certain types of sinus inflammation. Researchers add that, study which showed that participants who used a nasal spray with Capsicum reported a faster onset of action or relief, on average within a minute of using the spray, than the control group and the spray is safe  and effective on non-allergic rhinitis.

Interestingly, this is the first controlled trial where capsaicin was able to be used on a continuous basis to control symptoms. It is considered a significant advance, because of the fact  that in  the previous trials the ingredient was too hot to administer without anesthesia.

Ref : http://www.annallergy.org/article/S1081-1206%2811%2900383-8/abstract