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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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First in Class Once-Daily Dual Bronchodilator Ultibro® Breezhaler® (QVA149) Gains Positive CHMP Opinion for the Treatment of COPD
The developer: Novartis, Vectura
Peak projections: $2 billion-$5 billion
TOKYO, July 27, 2013 /CNW/ –
- QVA149 (indacaterol/glycopyrronium) is the first once-daily fixed-dose combination of both a LABA and a LAMA bronchodilator to gain positive CHMP opinion
- Pivotal Phase III IGNITE data showed QVA149 significantly improved lung function and patient-reported outcomes including breathlessness and rescue medication use, compared to current standard of care[1]
- QVA149 demonstrated significantly reduced rates of COPD exacerbations and improved health-related quality of life compared to open-label tiotropium 18 mcg and glycopyrronium 50 mcg[2],[3]
Sosei Group Corporation (“Sosei”; TSE Mothers Index: 4565) confirms the information released by Novartis that the European Medicines Agency’s Committee for Medicinal Products for Human Use (CHMP) has adopted a positive opinion for approval of once-daily Ultibro® Breezhaler®(indacaterol 85 mcg/glycopyrronium 43 mcg delivered dose, equivalent to 110 mcg/50 mcg metered dose per capsule), as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD). Ultibro Breezhaler was developed under the name of QVA149.
QVA149 is an investigational fixed dose combination of two bronchodilators, indacaterol, a long-acting beta2-adrenergic agonist (LABA) and glycopyrronium, a long-acting muscarinic antagonist (LAMA).http://www.newswire.ca/en/story/1203847/first-in-class-once-daily-dual-bronchodilator-ultibro-breezhaler-qva149-gains-positive-chmp-opinion-for-the-treatment-of-copd
QVA149 is an inhaled fixed dose combination product for the treatment of COPD, an irreversible and chronic obstruction of the airways. The product combinesNVA237, the long acting muscarinic antagonist (LAMA) licensed to Novartis by Sosei in 2005, together with Novartis’ long acting beta agonist (LABA), indacaterol, now approved in more than 80 countries, including EU, Japan and the USA.
Both NVA237 and indacaterol are once-daily bronchodilators but act on different receptors in the lung thereby offering the potential in combination to provide additional patient benefit.
Phase III studies (IGNITE: Indacaterol and GlycopyrroNium bromide clInical sTudiEs) for QVA149 is one of the largest international patient registration programs in COPD comprising 10 studies and including more than 7,000 subjects across 42 countries. Up to date, Novartis announced positive results of five Phase III studies: SHINE, BRIGHT, ENLIGHTEN, ILLUMINATE and SPARK. IGNITE data demonstrated the efficacy of QVA149 and showed a superior effect on lung function and patient-reported outcomes versus comparators.
>> More
QVA149 was filed for approval in Europe in October, and in Japan in November 2012. The US filing is expected at the end of 2014.
About COPD
COPD is a chronic obstruction of the airways which in the developed world is caused primarily by smoking. Symptoms include chronic bronchitis and/or emphysema which slowly progress and eventually lead to a largely irreversible loss of lung function. Worldwide, COPD is estimated to affect a total of 210 million people and is projected to become the third leading cause of death by 2020.
Market Overview
COPD is a large and fast expanding market which is estimated to be worth around $9 billion (2008) and is expected to reach $14 billion by 2014 as a result of better recognition of the disease and improved treatment options.
indacaterol
glycoprronium
US OK for Forest/Pierre Fabre antidepressant fetzima, levomilnacipran
levomilnacipran
The US Food and Drug Administration has approved Forest Laboratories and Pierre Fabre’s Fetzima for major depressive disorder.
Fetzima (levomilnacipran extended-release), a once-daily serotonin and norepinephrine reuptake inhibitor, has been given the green light based on Phase III studies of adults with MDD and statistically significant and clinically meaningful improvement in depressive symptoms across three doses (40, 80, and 120 mg).
read all at
http://www.pharmatimes.com/Article/13-07-26/US_OK_for_Forest_Pierre_Fabre_antidepressant.aspx
Levomilnacipran (F2695) is an antidepressant currently under development by Forest Laboratories for the treatment of depression in the United States and Canada.[1][2][3] As of 2009 it is in phase III clinical trials.[4] Levomilnacipran is an active enantiomer of milnacipran and therefore has similar effects and pharmacology, acting as a serotonin-norepinephrine reuptake inhibitor.[2][5] On 20 January 2011, Forest and Pierre Fabre Medicament announced that levomilnacipran was no better than placebo in a late-stage clinical trial. Two other late-stage trials will be finished in mid-2011.
References
- “Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD — Neurotransmitter.net”.
- “Pierre Fabre Medicament and Forest Laboratories to Collaborate on Development and Commercialization of F2695 for Depression – FierceBiotech”.
- “News: Forest Buys CNS Disease-Related Drug for $75M Upfront.”.
- “Search of: F2695 – List Results – ClinicalTrials.gov”.
- Deprez D, Chassard D, Baille P, Mignot A, Ung HL, Puozzo C (1998). “Which bioequivalence study for a racemic drug? Application to milnacipran”. European Journal of Drug Metabolism and Pharmacokinetics 23 (2): 166–71. PMID 9725476.
Vifor gets FDA approval for Injectafer
Switzerland’s Vifor Pharma is celebrating after getting the thumbs-up from US regulators for Injectafer for the treatment of iron deficiency anaemia.
The US Food and Drug Administration has approved the treatment, sold in Europe as Ferinject (ferric carboxymaltose) since getting the green light in 2007. Specifically, Injectafer will be available for the treatment of IDA in adults who have had an unsatisfactory response or are intolerant to oral iron.
The approval is based on two large trials conducted by Vifor’s US partner Luitpold Pharmaceuticals which studied more than 3,500 patients, of which 1,800 were treated with Injectafer.
read all at
http://www.pharmatimes.com/Article/13-07-26/Vifor_gets_FDA_approval_for_Injectafer.aspx
Ferric carboxymaltose
Chemical structure
The active substance of FERINJECT is a complex of polynuclear iron(III)-hydroxide with 4(R)-(poly-(1→4)-
O-α-D-glucopyranosyl)-oxy-2(R),3(S),5(R),6-tetrahydroxy-hexanoate. The relative molecular weight is
approximately 150,000 Da, corresponding to the empirical formula:
[FeOx(OH)y(H2O)z]n [{(C6H10O5)m (C6H12O7)}l]k, where n ≈ 103, m ≈ 8, l ≈ 11, and k ≈ 4.
CAS-Number
9007-72-1
http://www.tga.gov.au/pdf/auspar/auspar-ferric.pdf for structure
Mavoglurant (AFQ-056) is an experimental drug candidate for the treatment of fragile X syndrome
Mavoglurant (AFQ-056) is an experimental drug candidate for the treatment of fragile X syndrome.[1] It exerts its effect as an antagonist of the metabotropic glutamate receptor 5 (mGLU5).[2]
Mavoglurant is under development by Novartis and is currently in Phase II and Phase III clinical trials.[1][3] If successful, it would be the first drug to treat the underlying disorder instead of the symptoms of fragile X syndrome.[4]
- P. Cole (2012). “Mavoglurant”. Drugs of the Future 37 (1): 7–12. doi:10.1358/dof.2012.37.1.1772147.
- Levenga, J; Hayashi, S; De Vrij, FM; Koekkoek, SK; Van Der Linde, HC; Nieuwenhuizen, I; Song, C; Buijsen, RA et al. (2011). “AFQ056, a new mGluR5 antagonist for treatment of fragile X syndrome”. Neurobiology of disease 42 (3): 311–7. doi:10.1016/j.nbd.2011.01.022. PMID 21316452.
- Jacquemont, S.; Curie, A.; Des Portes, V.; Torrioli, M. G.; Berry-Kravis, E.; Hagerman, R. J.; Ramos, F. J.; Cornish, K. et al. (2011). “Epigenetic Modification of the FMR1 Gene in Fragile X Syndrome is Associated with Differential Response to the mGluR5 Antagonist AFQ056”. Science Translational Medicine 3 (64): 64ra1. doi:10.1126/scitranslmed.3001708. PMID 21209411.
- “AFQ056 drug improves symptoms in Fragile X patients: Study”. news-medical.net. January 9, 2011.
Fragile X syndrome (FXS), Martin–Bell syndrome, or Escalante’s syndrome (more commonly used in South American countries), is a genetic syndrome that is the most widespread single-gene cause of autism and inherited cause of mental retardation among boys. It results in a spectrum of intellectual disabilities ranging from mild to severe as well as physical characteristics such as an elongated face, large or protruding ears, and large testes (macroorchidism), and behavioral characteristics such as stereotypic movements (e.g. hand-flapping), and social anxiety.
Fragile X syndrome is associated with the expansion of the CGG trinucleotide repeat affecting the Fragile X mental retardation 1 (FMR1) gene on the X chromosome, resulting in a failure to express the fragile X mental retardation protein (FMRP), which is required for normal neural development. Depending on the length of the CGG repeat, an allele may be classified as normal (unaffected by the syndrome), a premutation (at risk of fragile X associated disorders), or full mutation (usually affected by the syndrome).[1] A definitive diagnosis of fragile X syndrome is made through genetic testing to determine the number of CGG repeats. Testing for premutation carriers can also be carried out to allow for genetic counseling. The first complete DNA sequence of the repeat expansion in someone with the full mutation was generated by scientists in 2012 using SMRT sequencing.
There is currently no drug treatment that has shown benefit specifically for fragile X syndrome. However, medications are commonly used to treat symptoms of attention deficit and hyperactivity, anxiety, and aggression. Supportive management is important in optimizing functioning in individuals with fragile X syndrome, and may involve speech therapy, occupational therapy, and individualized educational and behavioral programs.
orphan drug designation EMA
http://www.orpha.net/consor/cgi-bin/OC_Exp.php?lng=EN&Expert=317238
Mavoglurant regulatory update 12/03/2012
ماووگلوران (به انگلیسی: Mavoglurant) یک ترکیب شیمیایی با شناسه پابکم ۹۹۲۶۸۳۲ است.
جستارهای وابسته[ویرایش]
Curis phase 1 Cancer Trial for CUDC-427 Begins
CUDC-427, GDC-0917; RG-7459
Genentech Inc (Roche Holding AG)
Curis licenses GDC-0917 from Genentech
Curis Cancer Trial Begins
Curis Inc. has initiated patient dosing in a second Phase 1 dose-escalation study of CUDC-427 that is being conducted using a continuous, twice-daily oral dosing regimen in patients with advanced and refractory solid tumors or lymphoma.
FULL STORY
About CUDC-427 (GDC-0917)
CUDC-427 is an orally bioavailable small molecule that is designed to promote cancer cell death by antagonizing IAP proteins. IAP proteins are a family of functionally and structurally related proteins that promote cancer cell survival by inhibiting programmed cell death, also known as apoptosis, which is a normal process inherent in every cell. Using IAP proteins and other anti-apoptotic factors, cancer cells evade apoptosis in response to a variety of signals, including those provided by anti-cancer agents such as chemotherapy, or naturally occurring inflammatory and immune signals transmitted through members of the tumor necrosis factor, or TNF, family of factors. Evasion from apoptosis is a fundamental mechanism whereby human cancers develop resistance to standard anti-cancer treatments. IAP inhibitors such as CUDC-427 are designed to counteract the effects of IAP proteins, thus shifting the balance away from cancer cell survival and allowing apoptosis to proceed.
CUDC-427 was designed to mimic the endogenous IAP antagonist mitochondrial protein second mitochondria-derived activator of caspases/direct IAP-binding protein (Smac/DIABLO) that is released into the cytoplasm in response to pro-apoptotic stimuli. CUDC-427 has demonstrated single-agent and combination anti-tumor activity in mouse xenograft tumor models when administered orally on a daily schedule, and IND-enabling safety studies have shown it to be well tolerated when dosed daily by oral administration, potentially enabling sustained target inhibition.
In October 2010, an open-labeled, uncontrolled, dose-escalation, Phase I clinical trial of CUDC-427 (NCT01226277; IAM4914g) began in patients with refractory solid tumors or lymphoma. Genentech recently completed this Phase I clinical trial in which 42 people received daily oral doses of CUDC-427 for two weeks, followed by a one week rest period. This 21-day cycle is repeated until disease progression or study discontinuation for any other reason. The primary endpoints of the study include evaluating the safety and tolerability and the pharmacokinetics of CUDC-427 in people with solid tumors or lymphoma and determining the maximum-tolerated-dose and a potential recommended dose for further clinical studies. Secondary endpoints include a preliminary assessment of anti-tumor activity of CUDC-427 and evaluating pharmacodynamic markers. Genentech plans to present full study results at a medical conference in mid-2013. Please refer to http://www.clinicaltrials.gov for additional study details.
About Inhibitor of Apoptosis Proteins
Impairment of programmed cell death or apoptosis often contributes to the formation and progression of cancer, and evasion of apoptosis is one of the primary strategies by which cancer cells develop resistance to anticancer therapies. Inhibitor of apoptosis (IAP) proteins are a family of functionally and structurally related proteins which include X-linked IAP (XIAP), cellular IAPs (cIAP1 and cIAP2), and melanoma IAP (ML-IAP). They confer protection from death-inducing stimuli by exerting a range of biological activities that promote cancer cell survival and proliferation. Some even directly inhibit caspases, critical players in the execution of apoptosis.
Mutations, amplifications and chromosomal translocations of IAP genes are associated with various solid and hematologic cancer types, and increased IAP expression has been associated with an unfavorable prognosis and poor outcome for patients. As a consequence, IAP proteins are considered promising molecular targets for anticancer therapy.
Antibody Effective Against Norovirus
Antibody Effective Against Norovirus
Researchers have released data showing that a monoclonal antibody can neutralize human norovirus. Norovirus causes roughly 20 million cases of acute diarrhea and vomiting annually in the United States, alone. It is also responsible for roughly 800 deaths annually.
FULL STORY
What is Norovirus?
Norovirus is a stomach bug that sets in within 10 hours of transmission and usually lasts up to three days. It is completely different from the flu in that only your stomach is affected. While most people recover completely after three days, norovirus is more serious for young children, the elderly and people with other serious health conditions. Every year 70,000 people are hospitalized and 800 deaths are caused by the virus.
What are the symptoms?
The most common symptoms of norovirus include stomach pain, vomiting, diarrhea and nausea. Some people also experience a low-grade fever, headache and body ache. Because it is common to have continued vomiting and diarrhea during the three days of illness, dehydration is another concern for those affected.
How do you get it?
Norovirus is spread through direct contact with an infected person’s vomit or feces. Most commonly, unwashed hands can be attributed to spreading the virus through surfaces or food. The virus spreads quickly in enclosed spaces like cruise ships, nursing homes and schools.
What is the treatment?
Unfortunately, there are no medications to treat norovirus. Health care providers say the best thing to do is try to stay hydrated, rest and wait for the virus to run its course. People who are unable to keep fluids down may need to receive fluids intravenously.
How can you protect yourself?
Hand washing is the best defense against the norovirus, since no one is immune to the always-changing strains of the virus. However, new research has found hand sanitizers are not affective in killing the virus. Avoid direct contact with anyone who is infected and pay close attention to cleaning and preparing food. Also, anyone who is infected should not prepare food. Use disinfectants to wipe down all surfaces that have come in contact with someone who is infected. Also, launder infected clothes immediately on the longest wash cycle to help from spreading the virus.
CSIR, INDIA-WO PATENT–synthesis of amprenavir and saquinavir
amprenavir
saquinavir
A process for synthesis of syn azido epoxide and its use as intermediate in the synthesis of amprenavir and saquinavir
Published as ———WO-2013105118
Council of Scientific & Industrial Research
Inventors
Gadakh, Sunita, Khanderao; Rekula, Reddy, Santhosh; Sudalai, Arumugam
Publication date 18-JUL-2013
HIV protease inhibitor
Disclosed herein is a novel route of synthesis of syn azide epoxide of formu 5, which is used as a common intermdeiate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt- catalyzed hydrolyti kinetic resolution of racemic anti-(2SR, 3SR) – 3 -azido – 4 -phenyl – 1, 2- epoxybutane (azido-epoxide
| IN2012DE82 | 10-JAN-2012 [priority] |
Nanomagnets clean blood
Nanomagnets clean blood
Nanoparticles latch onto toxins in blood but are magnetically trapped before they can enter the body
http://www.rsc.org/chemistryworld/2013/07/nanomagnets-clean-blood
The group used their extracorporeal circuit to remove lead and the drug digoxin from the blood of rats. Target compounds in blood adhered to the nanoparticles as they collided within the circuit. The nanoparticles were then collected by magnetic separation with the toxin immobilised on the particle surface before blood could re-enter the body.
Actavis submits ANDAs for two more generic version of Bayer’s Safyral and Fresenius Kabi’s Diprivan (propofol) injection
Actavis submits ANDAs for two more generic version of
Bayer’s Safyral and
Fresenius Kabi’s Diprivan (propofol) injection
Actavis has filed for US approval for generic versions of a contraceptive and a sedative/anaesthetic.http://www.gabionline.net/Generics/News/Actavis-submits-ANDAs-for-two-more-generics
Biosimilars applications under review by EMA – 2013 Q2
The European Medicines Agency (EMA) is the body responsible for approval of biosimilars within the EU. A legal framework for approving biosimilars was established in 2003. Approval of biosimilars is based on an abbreviated registration process, which allows biosimilars manufacturers to provide a reduced package of information compared to originator drugs, provided they can prove ‘similarity’ to the originator or ‘reference drug’.
read all at
http://www.gabionline.net/Biosimilars/General/Biosimilars-applications-under-review-by-EMA-2013-Q2
DR ANTHONY MELVIN CRASTO
ORGANIC SPECTROSCOPY
New Drug Approvals 