Tuesday, September 20, 2011

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 47th 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.

More..

Tuesday, September 13, 2011

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

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

Saturday, September 10, 2011

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

Friday, September 9, 2011

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...



Monday, September 5, 2011

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

Saturday, September 3, 2011

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