In continuation of my update on Dacogen
EU Approves Dacogen, Velcade Indications | News | Drug Discovery and Development Magazine
EU Approves Dacogen, Velcade Indications | News | Drug Discovery and Development Magazine
Med-Chemist : "Quintessential Medicinal Chemistry"
Thursday, November 1, 2012
Tuesday, October 30, 2012
Dulaglutide Fares Well in New Trials
Eli Lilly and Co.'s potential once-weekly treatment for type 2 diabetes fared better than three other drugs in lowering blood sugar levels, according to initial results from some late-stage research.
The Indianapolis drugmaker said that two doses of its injectable drug dulaglutide (see structure) delivered statistically superior reductions in blood sugar levels when compared to twice-daily injections of exenatide and the oral treatments metformin and sitagliptin. Lilly will present more details from the studies at scientific meetings next year and in 2014.
Lilly said it will submit the drug to regulators for approval next year. It said timing in the United States will depend on the completion of Food and Drug Administration requirements for an assessment of the drug's cardiovascular risk.
Monday, October 29, 2012
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.
Sunday, October 28, 2012
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.
Saturday, October 27, 2012
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
Friday, October 26, 2012
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.....
Thursday, October 25, 2012
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
Tuesday, October 23, 2012
FDA Approves Oxtellar...
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.
Monday, October 22, 2012
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 ....
Saturday, October 20, 2012
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.
Friday, October 19, 2012
Thursday, October 18, 2012
Synta announces results from ganetespib Phase 2b trial on NSCLC
In continuation of my update on Ganetespib....
"The preliminary results from GALAXY indicate that the addition of ganetespib to docetaxel is well tolerated and may improve outcomes in patients compared to docetaxel alone," said Dr. Ramalingam, a Principal Investigator of the study. "This includes promising improvements in survival seen across the broad adenocarcinoma population as well as in key predefined patient populations. A well-tolerated combination regimen that extends survival associated with salvage therapy in NSCLC will meet a much awaited need to improve the current standard of care."
As per the CEO's statement "the objective of the interim analysis was to identify the best choice of patient population and trial design for transitioning to the Phase 3 stage of the study. The broad-based activity seen in the results presented support advancing into the Phase 3 stage in alladenocarcinoma patients. The results have yielded a rich data set which we are using to optimize and de-risk the Phase 3 stage of the program. We are hopeful that this next stage of development will lead to a new treatment option for patients fighting this devastating disease."
Enrollment completion of the Phase 2b stage of the GALAXY trial and the transition to the Phase 3 stage are expected later this year. Based on current assumptions, the Company anticipates that Phase 3 will enroll approximately 500 adenocarcinoma patients, with overall survival as a primary endpoint. Biomarker findings and other patient selection and treatment experience from the Phase 2b stage will be incorporated into the design of the Phase 3 stage. An announcement with additional Phase 3 details is anticipated later this year, following discussion with regulatory agencies.
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