Bayer Releases Riociguat Data

We  know that,  Riociguat (BAY 63-2521, below structure) is a novel drug that is currently in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase (sGC). At the moment Phase III clinical trials investigate the use of riociguat as a new approach to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat constitutes the first drug of a novel class of sGC stimulators. 

Bayer Releases Riociguat Data  

FDA Clears Eisai’s Epilepsy Drug Fycompa

We know that, Fycompa (see structure, perampanel) is a selective, non-competitive AMPA receptor antagonist discovered by the research teams at Eisai laboratories. The development of an AMPA antagonist compound with a favourable pharmacokinetic and safety profile arose after the AMPA receptor was identified as a promising target for drug development. The AMPA receptor is widely present in almost all excitatory neurons. It is believed to play a role in a large number of central nervous system diseases with similar neuropathology.

GEN | News Highlights:FDA Clears Eisai’s Epilepsy Drug Fycompa.

Inhibitory Effect of Carob (Ceratonia siliqua) Leaves Methanolic Extract on Listeria monocytogenes - Journal of Agricultural and Food Chemistry (ACS Publications)

We know that, Ceratonia siliqua, commonly known as the Carob tree and St John's-bread,  is a species of floweringevergreen shrub or tree in the pea family, Fabaceae. It is widely cultivated for its edible legumes, and as anornamental tree in gardens. The seed pod may be crushed and used as ersatz chocolate.

It is native to the Mediterranean region including Southern Europe, Northern Africa, the largerMediterranean islands; to the Levant and Middle-East of Western Asia into Iran; and to the Canary Islandsand Macaronesia

Inhibitory Effect of Carob (Ceratonia siliqua) Leaves Methanolic Extract on Listeria monocytogenes - Journal of Agricultural and Food Chemistry (ACS Publications)

Positive Results from Phase 2 Trial of Oral Calcitonin | News | Drug Discovery and Development Magazine

Tarsa Therapeutics Inc. announced that a Phase 2 trial of its oral recombinant salmon calcitonin in the prevention of postmenopausal osteoporosis was successfully concluded and yielded statistically significant, clinically relevant improvements in bone mineral density (BMD) at the lumbar spine.  These data were presented at the American Society for Bone and Mineral Research (ASBMR) 2012 Annual Meeting by Phase 2 investigator Neil Binkley, MD, who is an associate professor of endocrinology and Geriatrics at the University of Wisconsin School of Medicine and Public Health in Madison, Wisconsin.....

Positive Results from Phase 2 Trial of Oral Calcitonin | News | Drug Discovery and Development Magazine

T-DM1 Extends Overall Survival | News | Drug Discovery and Development Magazine

We know that,Trastuzumab emtansine (INN, also called trastuzumab-DM1 or trastuzumab-MCC-DM1, abbreviated T-DM1) is an antibody-drug conjugate consisting of the antibody trastuzumab (the active ingredient in Herceptin) linked to a cytotoxic agent that is a derivative of maytansine (DM1).

It is in clinical trials for breast cancer, especially of the HER2 positive type. Early results in Nov 2011 from an open-label phase II trial on 137 patients with HER2-positive advanced breast cancer were very encouraging.

EMILIA, a phase III trial of 991 people with HER2-positive unresectable locally advanced or metastatic breast cancer, comparing T-DM1 versus capecitabine plus lapatanib in patients previously treated with trastuzumab and a taxane chemotherapy, showed improved progression free survival in patients treated with T-DM1 (median 9.6 vs. 6.4 months) with an improved safety profile. The study sponsor reported in August 2012 that T-DM1 significantly improved survival in the EMILIA study and that the details will be reported at an upcoming medical meeting

T-DM1 Extends Overall Survival | News | Drug Discovery and Development Magazine

FDA Approves Oxtellar...

Oxtellar XR  is Oxcarbazepine Extended-Release Tablets...

We know that, Oxcarbazepine  is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. It is also used to treat anxiety and mood disorders, and benign motor tics. Oxcarbazepine is marketed as Trileptal by Novartis and available in some countries as a generic drug.

FDA Approves Oxtellar | News | Drug Discovery and Development Magazine

Astex Begins Phase 2 Cancer Trial | News | Drug Discovery and Development Magazine

Astex Begins Phase 2 Cancer Trial of  SGI-110 | News | Drug Discovery and Development Magazine

Empagliflozin Lowers Blood Pressure | News | Drug Discovery and Development Magazine

We know that, Empagliflozin (see structure) is a SGLT2 inhibitor which is being investigated in clinical trials for the oral treatment of type 2 diabetes by Boehringer Ingelheim and Eli Lilly and Company. It is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), which is found almost exclusively in the proximal tubules of nephronic components in the kidneys. SGLT-2 accounts for about 90 percent of glucose reabsorption into the blood. Blocking SGLT-2 causes blood glucose to be eliminated through the urine via the urethra...

Empagliflozin Lowers Blood Pressure | News | Drug Discovery and Development Magazine   ....

Aveo Files Tivozanib NDA | News | Drug Discovery and Development Magazine

We know that, Tivozanib (see structure below, AV-951) is an oral VEGF receptor tyrosine kinase inhibitor. It is undergoing clinical trial investigation for the treatment of renal cell carcinomas.An oral quinoline urea derivative, tivozanib suppresses angiogenesis by being selectively inhibitory against vascular endothelial growth factor. It was developed by AVEO Pharmaceuticals.It is designed to inhibit all three VEGF receptors. Phase III results on advanced renal cell carcinoma suggest a 30% or 3 months improvement in median PFS compared tosorafenib. 

Aveo Files Tivozanib NDA | News | Drug Discovery and Development Magazine

Cherry intake reduces risk of gout attacks

In continuation of my update on cherries

Cherry intake reduces risk of gout attacks