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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Pharmaceutical Industry In Global Market: Issues To Be Handled For Better Growth
In the global market, the position of the pharmaceutical industry is not parallel as compared to other information and technology based industries.
Among the Leading industries, the pharmaceutical industry lacks behind in the growth rate as far as innovative research, capital investment and
government regulations are concern. Most of the countries simply depends on bulk production of the generic drugs and not focused on core research. In
comparison with the growth rate of the electronic and IT industry stands first where as the pharmaceutical comes at the 9th position.
read all at
Vivus has presented data on its already-approved but not-yet-marketed erectile dysfunction drug Stendra which shows that the treatment is effective for sexual activity within 15 minutes.
Stendra (avanafil) was given the green light by the US Food and Drug Administration over a year ago, but there has been no launch yet as Vivus has been seeking a partner. The latest data should be attractive to potential suitors and could help Stendra take on other phosphodiesterase type 5 (PDE5) inhibitors, notably Pfizer’s Viagra (sildenafil) but also Eli Lilly’s Cialis (tadalafil) and Bayer’s Levitra (vardenafil).
read all at
http://www.pharmatimes.com/Article/13-06-20/Vivus_ED_drug_gets_to_work_in_less_than_15_mins.aspx
Avanafil can be synthesized from a benzylamine derivative and a pyrimidine derivative:Yamada, K.; Matsuki, K.; Omori, K.; Kikkawa, K.; 2004, U.S. Patent 6,797,709
- A cutting that phenanthrene by a methylthio urea ( a ) and ethoxy methylene malonate ( 2 ) cyclization of 3 , chloride, phosphorus oxychloride get 4 , 4 with benzyl amine 5 occurred SNAr the reaction product after oxidation with mCPBA 6 . In pyrimidine, if the 2 – and 4 – positions are active simultaneously the same leaving group in the case, SNAr reaction occurs preferentially at 4 – position, but does not guarantee the 2 – side reaction does not occur. Here is an activity of the poor leaving group sulfide spans 2 – bit, and a good leaving group active chlorine occupy four – position, thus ensuring a high regioselectivity of the reaction. 4 – position after completion of the reaction, then the 2 – position of the group activation, where sulfide sulfoxide better than the leaving group. Amino alcohols 7 and 6 recurrence SNAr reaction 8 , 8 after alkaline hydrolysis and acid alpha amidation get that phenanthrene.
Tocilizumab Impresses in Polyarticular Juvenile Arthritis
tocilizumab
Tocilizumab Impresses in Polyarticular Juvenile Arthritis
Medscape
MADRID, Spain — Children with polyarticular juvenile idiopathic arthritis treated with tocilizumab (Actemra, Genentech) achieved high response rates with sustained improvement in the phase 3 CHERISH trial.
The results prompted the US Food and Drug Administration toapprove tocilizumab for this indication. The drug is already approved for systemic juvenile idiopathic arthritis and for adults with moderate to severe rheumatoid arthritis.
read all at
http://www.medscape.com/viewarticle/806572
Tocilizumab (INN, or atlizumab, developed by Hoffmann–La Roche and Chugai and sold under the trade names Actemra and RoActemra) is an immunosuppressive drug, mainly for the treatment of rheumatoid arthritis (RA) and systemic juvenile idiopathic arthritis, a severe form of RA in children. It is a humanized monoclonal antibody against the interleukin-6 receptor (IL-6R). Interleukin 6 (IL-6) is a cytokine that plays an important role in immune response and is implicated in the pathogenesis of many diseases, such asautoimmune diseases, multiple myeloma and prostate cancer.
Let’s Set a Global Drug Quality Benchmark by Kiran M Shaw, Biocon
With Indian-made generics accounting for a US market share of over 25 per cent, it is not surprising that it is gaining significant mindshare of the Food and Drug Administration ( FDA). The spate of quality issues with leading Indian pharmaceutical companies in the past couple of years however should not be viewed in isolation. Big Pharma in the West, too, has been facing increasing flak from the FDA and other regulators over good manufacturing practice ( GMP) violations. High profile names like J& J, Genzyme (Sanofi), GSK, Sandoz, Watson, Teva and many others have encountered their share of quality problems and have been served with ‘warning letters’ from FDA
http://kiranmazumdarshaw.blogspot.in/2013/06/lets-set-global-drug-quality-benchmark.html
READ ALL AT THE LINK ABOVE
Adamas claims success with new and improved Parkinson’s drug
amantadine
Adamas claims success with new and improved Parkinson’s drug
Amantadine (trade name Symmetrel, by Endo Pharmaceuticals) is a drug that has US Food and Drug Administration approval for use both as an antiviral and an antiparkinsonian drug. It is the organic compound 1-adamantylamine or 1-aminoadamantane, meaning it consists of an adamantane backbone that has an amino group substituted at one of the four methyne positions. Rimantadine is a closely related derivative of adamantane with similar biological properties.
Apart from medical uses, this compound is useful as a building block, allowing the insertion of an adamantyl group.
According to the US Centers for Disease Control and Prevention, 100% of seasonal H3N2 and 2009 pandemic flu samples tested have shown resistance to adamantanes, and amantadine is no longer recommended for treatment of influenza in the United States. Additionally, its effectiveness as an antiparkinsonian drug is undetermined, with a 2003 Cochrane Review concluding that there was insufficient evidence in support or against its efficacy and safety.
Synthesis
Amantadine may be prepared by reacting adamantane with bromine or nitric acid to give the bromide or nitroester at position one. Reaction of either compound with acetonitrile affords the acetamide, which is hydrolyzed to give 1-adamantylamine:
Patent of Fresenius Kabi Oncology Ltd.Novel intermediates and process for the preparation of lapatinib and…….
LAPATINIB
Lapatinib (INN), used in the form of lapatinib ditosylate, (USAN) (Tykerb/Tyverb, GSK) is an orally active drug for breast cancer and other solid tumours. It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. It is used in combination therapy for HER2-positive breast cancer. It is used for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 (ErbB2).
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Beilstein J. Org. Chem. 2013, 9, 2265–2319.
http://www.beilstein-journals.org/bjoc/single/articleFullText.htm?publicId=1860-5397-9-265
GlaxoSmithKline’s lapatinib (3.38, Tykerb) is a novel dual kinase inhibitor used in the treatment of solid tumors such as those found in breast cancer and contains a quinazoline core structure. It consists of a 2,5-disubstituted furan ring, which is directly linked to the aminoquinazoline unit (Scheme 41). The quinazoline heterocycle was prepared starting from 5-iodoanthranilic acid (3.72) via initial condensation with formamidine acetate (3.73) followed by chlorination using oxalyl chloride or phosphorous oxychloride [101]. Performing a nucleophilic aromatic substitution on the chloride 3.74 with aniline 3.75 renders the extended core of lapatinib. This intermediate (3.76) was then coupled with 5-formyl-2-furanoboronic acid (3.77) using standard Suzuki cross-coupling conditions. Finally, a reductive amination of the pendant aldehyde of 3.78 with 2-(methylsulfonyl)ethylamine (3.79) furnishes the desired product lapatinib (Scheme 41).
![[1860-5397-9-265-i41]](http://www.beilstein-journals.org/bjoc/content/inline/1860-5397-9-265-i41.png?scale=2.0&max-width=1024&background=FFFFFF)
http://www.beilstein-journals.org/bjoc/single/articleFullText.htm?publicId=1860-5397-9-265
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Fresenius Kabi Oncology Ltd.WO 2013080218
Lahiri, Saswata; Gupta, Nitin; Singh, Hemant Kumar; Handa, Vishal; Sanghani, Sunil
6 JUNE 2013, http://www.google.com/patents/WO2013080218A1?cl=en
Literature References: Reversible dual inhibitor of ErbB1 and ErbB2 tyrosine kinases. Prepn: M. C. Carter et al., WO 9935146(1999 to Glaxo); eidem, US 6727256 (2004 to SmithKline Beecham). Mechanism of action study: W. Xia et al., Oncogene 21, 6255 (2002); and crystal structure in complex with epidermal growth factor receptor (EGFR, ErbB1): E. R. Wood et al., Cancer Res. 64, 6652 (2004). In vitro antitumor activity in combination with anti-ErbB2 antibodies: W. Xia et al., Oncogene 24, 6213 (2005). Biologic effects on tumor growth: N. L. Spector et al., J. Clin. Oncol. 23, 2502 (2005). Pharmacokinetics and clinical activity in metastatic carcinomas: H. A. Burris III et al., ibid. 5305. Review of clinical development: T. E. Kim, J. R. Murren, IDrugs6, 886-893 (2003); H. A. Burris III, Oncologist 9, Suppl. 3, 10-15 (2004).
Constituents And Factors Of Technology Transfer In Pharmaceutical Industry
Technology transfer is helpful to develop dosage forms in various ways as it provides efficiency in process, maintains quality of product, helps to achieve standardized process which facilitates cost effective production. It is the process by which an original innovator of technology makes its technology available to commercial partner that will exploit the technology.
Technology transfer is both integral and critical to drug discovery and development for new medicinal products. The cost of product development raises during pilot scale-up and initial production batch i.e. the critical path for success is dependent on completion of technology transfer to the production site at an affordable cost.
Technology transfer is defined as “The processes that are needed for successful progress from drug discovery to product development to clinical trials to full-scale commercialization.”
Forest Announces U.S. Availability of New Once-Daily NAMENDA XR
memantine
Forest Announces U.S. Availability of New Once-Daily NAMENDA XR
— Treatment for moderate to severe Alzheimer’s Disease is now available to patients in a convenient extended release formulation —
NYSE:FRX.NEW YORK–(BUSINESS WIRE)–Forest Laboratories, Inc. announced today that NAMENDA XR(TM) (memantine hydrochloride) once-daily formulation is now available in pharmacies throughout the United States. NAMENDA XR is approved by the U.S. Food and Drug Administration (FDA) for the treatment of moderate to severe dementia of the Alzheimer’s type.
http://www.pharmalive.com/once-daily-namenda-xr-launched-in-us
Memantine is the first in a novel class of Alzheimer’s disease medications acting on theglutamatergic system by blocking NMDA-type glutamate receptors. It was first synthesized by Eli Lilly and Company in 1968. Memantine is marketed under the brandsAxura and Akatinol by Merz, Namenda by Forest, Ebixa and Abixa by Lundbeck andMemox by Unipharm. Memantine has been shown to have a modest effect in moderate-to-severe Alzheimer’s disease and in dementia with Lewy bodies. Despite years of research, there is little evidence of effect in mild Alzheimer’s disease.
Amgen, Cytokinetics expand collaboration on Omecamtiv mecarbil , CK-1827452, is a cardiac specific myosin activator
Omecamtiv mecarbil
Omecamtiv mecarbil provides new hope for heart failure patients
A new drug which helps the heart pump more easily could improve the lives of thousands of people afflicted by debilitating heart failure, research suggests. Omecamtiv mecarbil is the first of a new class of drugs, called myosin activators, targeting proteins that make the heart contract. Rather than forcing the heart to beat more often, the drug causes heart muscles to contract for longer, increasing the volume of blood pumped out with each stroke. A British trial reported in The Lancet medical journal showed that omecamtiv mecarbil significantly improved the heart function of 45 heart failure patients.
Amgen, Cytokinetics expand collaboration
Thursday, June 13, 2013
Amgen and Cytokinetics, a clinical-stage biopharmaceutical company, have expanded their strategic collaboration to include Japan. In 2006, Cytokinetics and Amgen entered into a collaboration to discover, develop and commercialize novel small-molecule therapeutics that activate cardiac muscle contractility for potential applications in the treatment of heart failure. Omecamtiv mecarbil is the most advanced drug candidate in this collaboration.
– See more at:
http://www.centerwatch.com//news-online/article/4852/amgen-cytokinetics-expand-collaboration
Omecamtiv mecarbil , previously codenamed CK-1827452, is a cardiac specific myosin activator. It is clinically tested for its role in the treatment of left ventricular systolic heart failure. Systolic heart failure is characterised as a decreased cardiac output (<40% ejection fraction), due to decreased stroke volume, resulting in the inability to meet the metabolic demands of the body. The loss of contraction is caused by a reduced number of effective actin-myosin cross bridges in the left ventricular myocytes.
One possible underlying mechanism is altered signal transduction that interferes with excitation-contraction coupling. A decreased cardiac output causes peripheral hypotension and activation of the sympathetic nervous system. This in turn stimulates the cardiac myocytes excessively, eventually leading to left ventricular hypertrophy, characteristic of chronic heart failure. Some symptoms of systolic heart failure are fatigue, peripheral oedema, dyspnoea, exercise intolerance and breathlessness. Current inotropic drug therapies such as dobutamine, are palliative and not a cure. They also cause many adverse effects including arrhythmias related to increased myocardical oxygen consumption, desensitization of adrenergic receptors and altering intracellular calcium levels. Thus systolic heart failure is considered malignant, however the novel mechanism of Omecamtiv Mecarbil is a hopeful long-term resolution.
Heart failure is often caused after the heart has suffered significant damage, this is something that can occur during a heart attack. A failing heart cannot provide sufficient blood flow to the body. Natasha Steward works for the British Heart Foundation (BHF) as a senior cardiac nurse. She has stated that, “it does seem that using certain doses of Omecamtiv Mercabil can offer some improvement to a damaged heart.”
Stewart also commented that, “This is a very early stage for the drug, the study we have seen here only took place for a very short time and with a small number of patients. Before we can say this drug is safe for use and will be effective, clinical trials of a much greater scale will need to be conducted.”
The BHF runs the Mending Broken Hearts campaign which raises money in the hope of finding a cure for heart failure. The campaign hopes to raise over £50m to spend on research to help the quarter of a million people who suffer from heart failure in the UK.
Miglustat- to treat Type 1 Gaucher disease (GD1)
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| Miglustat | |
| (2R,3R,4R,5S)-1-butyl-2-(hydroxymethyl)piperidine-3,4,5-triol |
PATENT-US 5,525,616, US 5,472,969 TO Actelion Pharms Ltd
Miglustat is a drug developed by Actelion and is used primarily to treat Type 1 Gaucher disease (GD1). It is marketed under the trade name Zavesca. Miglustat (OGT 918, N-butyl-deoxynojirimycin) is an imino sugar (molecular weight: 219 daltons), a synthetic analogue of D-glucose and a white to off-white crystalline solid that has a bitter taste The primary pharmacological activity of miglustat is inhibition of the enzyme glucosylceramide synthase, catalyzing the first step in the biosynthesis of glycosphingolipids (GSL), i.e., the formation of glucosylceramide (GlcCer). Reduced formation of GlcCer will lead to decreased biosynthesis of more complex GSL. This therapeutic principle, called substrate reduction therapy (SRT), may be useful in disorders of intracellular (predominantly lysosomal) accumulation of GSL either due to their deficient breakdown or intracellular transport/trafficking. Miglustat exhibits a large volume of distribution and has the capacity to access deep organs such as the brain, bone and lung.
Miglustat is a synthetic derivative of a family of polyhydroxylated alkaloids or amino sugar extracted from plants and microorganisms. Its synthesis starts from D-glucose sugar in plants. The sugar then aminated and oxidized to amino fructose sugar, which then can form a cyclic aminohemiacetal called nojirimycin. Then the dehydration and reduction takes place successively before the formation of deoxynojirimycin, which is a precursor of miglustat. Since it is a synthetic derivative drug, alkylation ofdeoxynojirimycin can be synthesized in the laboratory with 1-butyl halide via amine alkylation.
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