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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Benzoxaboroles: A New Potential Drug for African Sleeping Sickness
Life cycle of the Trypanosoma brucei parasites, source: CDC
Human African trypanosomiasis, caused by the kinetoplastid parasite Trypanosoma brucei, affects thousands of people across sub-Saharan Africa, and is fatal if left untreated. Treatment options for this disease, particularly stage 2 disease, which occurs after parasites have infected brain tissue, are limited due to inadequate efficacy, toxicity, and the complexity of treatment regimens.
We have discovered and optimized a series of benzoxaborole- 6-carboxamides to provide trypanocidal compounds that are orally active in murine models of human African trypanosomiasis. A key feature of this series is the presence of a boron atom in the heterocyclic core structure, which is essential to the observed trypanocidal activity. We also report the in vivo pharmacokinetic properties of lead compounds from the series and selection of SCYX-7158 as a preclinical candidate.
Human African trypanosomiasis (HAT), more commonly known as African sleeping sickness, is caused by two subspecies of the kinetoplastid parasite Trypanosoma brucei, Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense, which are introduced into the victim through the bite of the tse-tse fly. Endemic across sub-Saharan Africa, tens of thousands of people are infected each year, with millions at risk of contracting the disease. If not treated early in the progression of the disease, the T. brucei parasites migrate across the blood–brain barrier and reside in brain tissue, ultimately causing neuronal death leading to a multitude of neurological symptoms including hallucinations, sleep disorders, coma and, ultimately, death.
Current treatment options for HAT are inadequate due to lack of efficacy, particularly once the parasites have migrated to the brain (stage 2 HAT), toxicity and the complexity of treatment regimens. The most commonly used treatment for stage 2 HAT, melarsoprol is highly toxic, with an estimated 5–10% drug-related mortality. A more recent drug, eflornithine, while effective against T.b. gambiense, is not effective against T.b. rhodesiense, and must be administered in a complex intravenous regime that is impractical in disease-endemic areas.
Consequently, there is an urgent need for new drugs to treat HAT and, in particular, a need for a safe, orally active drug that is effective against all known strains of T. brucei and is effective in stage 2 HAT
http://www.drugdiscoveryonline.com/doc/benzoxaboroles-african-trypanosomiasis-drug-0001
Importance Of Preclinical Imaging In Drug Discovery
The process of discovering and bringing a drug to market consists of several stages, beginning with identification and validation of a drug target and continuing through lead identification by high-throughput screening, lead optimization, and profiling in relevant disease models. When a promising compound is found, a decision must be made on whether to take the drug into development. This long and expensive undertaking typically requires nearly $800 million and takes about 12 years before an approved drug is brought to market .
Shortening the drug discovery and development process is critical to managing this cost and can be achieved by improving the characterization of compounds and their effects in early phases of testing. Imaging has the potential to dramatically increase the efficiency of lead candidate selection by providing earlier and more highly predictive data, compared with traditional methods. Imaging is also well suited to facilitating translation between preclinical testing and clinical evaluation of drugs. Imaging methods are also more easily applied than traditional methods in the newer, more realistic models of human disease that are becoming increasingly prevalent, such as models of invasive disease in the tissue of origin as well as transgenic mouse models.
http://www.drugdiscoveryonline.com/doc/importance-of-preclinical-imaging-in-drug-discovery-0001
New Method of ‘Starving’ Cancer Cells, Leaving Healthy Cells Unharmed
Chris Proud, Professor of Cellular Regulation in Biological Sciences at the University of Southampton says that they have discovered a cellular component, eEF2K, which plays a critical role in allowing cancer cells to survive nutrient starvation, whilst normal, healthy cells do not usually require eEF2K in order to survive. Therefore, they believe that “by blocking the function of eEF2K, one should be able to kill cancer cells, without harming normal, healthy cells in the process.”
The findings were recently published in the journal Cell
Traditional chemotherapy and radiotherapy cause damage to healthy cells, he says, and other more targeted treatments are usually only effective for individual types of cancer. Contrastingly, this new development does not damage healthy cells and could also be used to treat a wide variety of different cancers. Professor Proud and the team are now working with other labs, including pharmaceutical companies, to develop and test…
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Six new drugs in clinical development stage: Dr Reddy’s
Hyderabad: Country’s second largest drug maker Dr Reddy’s Laboratories has said it is working on six new drugs in different areas, including metabolic disorders and cardiovascular diseases, psoriasis and migraine.
According to a filing with US Securities Exchange Commission, the drug maker said as of March 31, 2013, DRL had 21 active products in the proprietary products pipeline, of which six are in clinical development stage.
including metabolic disorders and cardiovascular diseases, psoriasis and migraine.
read all at
Sihuan Pharma Receives OK from CFDA for Trials of Novel PPI Drug
http://www.telegraphindia.com/pressrelease/prnw/prna_086_1306033.html
Sihuan Pharma Receives OK from CFDA for Trials of Novel PPI Drug
HONG KONG, July 18, 2013 Sihuan Pharmaceutical Holdings Group Ltd. (“Sihuan Pharmaceutical” or the “Company”), a leading pharmaceutical company with the largest cardio-cerebral vascular (“CCV”) drug franchise in China’s prescription market, today announced that Anaprazole Sodium, a Category 1.1 new drug received the Approval for Clinical Studies from the State Food and Drug Administration (“SFDA”) of the People’s Republic of China. Anaprazole Sodium is the fifth Category 1 innovative drug in respect of which the Company has received approval for Clinical Studies, applications for patents have been made in China, the United States, Japan and Europe.
Anaprazole Sodium is a new generation of proton pump inhibitors (“PPIs”) which treats ulcers quickly and efficiently by inhibiting gastric acid secretion and eradicating Helicobacter pylori. Preclinical studies have shown that the new drug covalently binds to proton pump, thus providing substantially stronger and longer inhibitory effects when compared to other PPI drugs, traditional H2-receptor antagonists and antacids currently available in the market. Therefore, it can effectively treat various gastric acid diseases
The clinical benefit of high-dose toremifene for metastatic breast cancer
http://www.ncbi.nlm.nih.gov/pubmed/23863727
Source
Dept. of Surgery, Saga University Faculty of Medicine.
Abstract
Introduction: Toremifene(TOR)is a selective estrogen receptor modulator(SERM). A high dose of 120 mg TOR(HD-TOR) has been used for recurrent breast cancer in Japan, but there is still insufficient evidence regarding the efficacy of HD-TOR. Patients and methods: HD-TOR was administered for recurrent or metastatic breast cancer between January 2003 and May 2012. The primary end point of the study was the tumor response rate. Bone metastasis cases were excluded from the efficacy analysis, but were included in the safety population. Results: A total of 21 patients registered in the study and the 2 patients with bone metastasis only were excluded from the efficacy analysis. The median follow-up period was 8. 3 months. None of the patients in the study had a CR, 4 had a PR(21. 1%), 9 had SD(47. 4%), and 6 had PD(31. 6%). Eight of the 9 SD cases had a long-term SD. The ORR was 21. 1% and the CB rate was 63. 2%. The median TTP of CB cases was 18. 3 months. None of the patients discontinued treatment because of a grade 3 or grade 4 adverse effects. Conclusion: In summary, the current study showed that HD-TOR may lead to a CB for recurrent breast cancer in first- or second-line treatment rather than thirdline. In particular, HD-TOR may give a benefit in highly endocrine-sensitive cases.
toremifene
Toremifene citrate is an oral selective estrogen receptor modulator (SERM) which helps oppose the actions of estrogen in the body. Licensed in the United States under the brand name Fareston, toremifene citrate is FDA-approved for use in advanced (metastatic)breast cancer. It is also being evaluated for prevention of prostate cancer under the brand name Acapodene.[1]
In 2007 the pharmaceutical company GTx, Inc was conducting two different phase 3clinical trials; First, a pivotal Phase clinical trial for the treatment of serious side effects ofandrogen deprivation therapy (ADT) (especially vertebral/spine fractures and hot flashes, lipid profile, and gynecomastia) for advanced prostate cancer, and second, a pivotal Phase III clinical trial for the prevention of prostate cancer in high risk men with high gradeprostatic intraepithelial neoplasia, or PIN. Results of these trials are expected by first quarter of 2008[2]
An NDA for the first application (relief of prostate cancer ADT side effects) was submitted in Feb 2009,[3] and in Oct 2009 the FDA said they would need more clinical data, e.g. another phase III trial.[4]
- Price N, Sartor O, Hutson T, Mariani S. Role of 5a-reductase inhibitors and selective estrogen receptor modulators as potential chemopreventive agents for prostate cancer.Clin Prostate Cancer 2005;3:211-4. PMID 15882476
- “GTx’s Phase III Clinical Development of ACAPODENE on Course Following Planned Safety Review” (Press release). GTx Inc. 2007-07-12. Retrieved 2006-07-14.
- “GTx Announces Toremifene 80 mg NDA Accepted for Review by FDA” (Press release).
- “GTx and Ipsen End Prostate Cancer Collaboration due to Costs of FDA-Requested Phase III Study”. 2 Mar 2011.
New Drug Approvals 