Showing posts with label PATENTS. Show all posts
Showing posts with label PATENTS. Show all posts

Friday, 26 July 2013

Why Vertex Earnings Prospects Are So Bright

Why Vertex Earnings Prospects Are So Bright
Motley Fool
With few drugs targeting cystic fibrosis and almost half of patients suffering from the particular mutation that the study targeted, Vertex could well have identified a blockbuster in the space. Moreover, with an ongoing phase 3 trial of another ...

Vertex Pharmaceuticals has a couple of approved drugs, including its Kalydeco cystic fibrosis drug and its Incivek treatment for hepatitis C. But it also has some promising prospects in the development stage. With the company having reported some positive study results during the quarter, Vertex saw its shares soar as more investors got aboard the biotech's bandwagon. Let's take an early look at what's been happening with Vertex Pharmaceuticals over the past quarter and what we're likely to see in its quarterly report

Wednesday, 24 July 2013

Isis Phase II drug APOIIIRx slashes triglycerides by 64%

Isis Pharmaceuticals is "very encouraged" by a second set of mid-stage data for its heart drugAPOIIIRx, which shows that it can substantially slash levels of dangerous fats in the blood. 

In a 26-patient Phase II trial, patients with severely high levels of triglycerides taking Isis' drug alongside fibrates experienced 64% drop in triglycerides, and a 70% drop in apolipoprotein C-III (apoC-III), a component of 'bad' low-density lipoprotein
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Tuesday, 23 July 2013

Phase III prostate cancer trial for 'homing' injection shows improvements

Prostate cancer

Phase III prostate cancer trial for 'homing' injection shows improvements
A new treatment for advanced prostate cancer that homes-in on tumours to deliver a high-energy burst of radiation to cancer cells has shown significant benefits in a large scale clinical trial.
The trial of 921 patients showed that treatment with the radioactive Radium-223 gave men with late-stage prostate cancer an average extra of 15 weeks of life.

Monday, 22 July 2013

Anticancer agent – elacytarabin

Cytarabine is a cytosine derivative that is a common component of chemotherapy regimens for blood cancers such as acute myeloid leukaemia (AML), and because it can cross the blood–brain barrier, it is useful in the treatment of central nervous system lymphomas. However, the response is variable, and resistance commonly develops via multiple mechanisms. Its activity is dependent on the intracellular concentrations of the active phosphorylated form, and one of the main mechanisms of resistance involves the deficiency of the transporter molecule hENT1 that carries it into the cells. As a result, Clavis Pharma developed a lipophilic ester derivative, elacytarabine, whose cellular uptake is not hENT1-dependent.1
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Cancer drug tested in pet dogs is now bound for human trials

Thanks to a new $2 million investment, a drug that spurs cancer cells to self-destruct while sparing healthy cells is on the road to human clinical trials. The compound, known as PAC-1, has so far proven safe and has promising anti-cancer effects in cell culture, in mouse models of cancer and in pet dogs with spontaneously occurring lymphomas and osteosarcomas.

If PAC-1 (pack one) makes it through the U.S. Food and Drug Administration’s Investigational New Drug review, the first human (Phase I) clinical trial of the drug will begin in mid-2014. The investor, who wishes to remain anonymous, has an option to invest another $2 million to take the drug into human trials. The clinical work will be conducted at the University of Illinois Cancer Center in Chicago.

Photo by
L. Brian Stauffer

University of Illinois chemistry professor Paul Hergenrother, left, and veterinary clinical medicine professor Tim Fan led a study of an anti-cancer compound in pet dogs that is now headed for human clinical trials.
PAC-1 (first procaspase activating compound) is a synthesized chemical compound that selectively induces apoptosis, or cell suicide, in cancerous cells. PAC-1 has shown good results in mouse models and is being further evaluated for use in humans. In 2010 a published study showed PAC-1 to be safe to research dogs, and a second study published later that same year reported that a PAC-1 derivative (called S-PAC-1) was well tolerated in a small Phase I Clinical Trial of pet dogs with lymphoma. Even at low doses of S-PAC-1, tumors regressed in 1/6 dogs, and the disease was stabilized (no additional tumor growth) in 3/6 dogs

Friday, 19 July 2013

Alkermes Adds Multiple Sclerosis Pill To Expanding Pipeline

Alkermes Adds Multiple Sclerosis Pill To Expanding PipelineTheStreet.comThe company expects to seek permission from FDA to begin human testing of its MMF prodrugs for multiple sclerosis in 2014, with a phase I study slated to begin mid-year. Composition of matter patents have been filed, which if granted, would give the ...

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Santarus Completes Patient Enrollment in CONTRIBUTE Study with UCERIS (budesonide) as Add-on Treatment to 5-ASA Drugs

Santarus Completes Patient Enrollment in CONTRIBUTE Study with UCERIS ...MarketWatchA Biologics License Application for RUCONEST for the treatment of acute angioedema attacks in patients with hereditary angioedema is under review by the U.S. Food and Drug Administration with a response expected in April 2014. Santarus is also ...

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SAN DIEGO, Jul 18, 2013 (BUSINESS WIRE) -- Santarus, Inc. /quotes/zigman/91852/quotes/nls/snts SNTS -0.61% today announced the completion of enrollment in the CONTRIBUTE clinical study designed to evaluate the incremental benefit of adding UCERIS(R) (budesonide) extended release 9 mg tablets to oral aminosalicylate (5-ASA) therapy for the induction of clinical remission in adult patients with active, mild to moderate ulcerative colitis. UCERIS is currently approved in the U.S. for the induction of remission in patients with active, mild to moderate ulcerative colitis.

Wednesday, 17 July 2013

Sanofi starts dengue vaccine production for 2015 launch

Sanofi starts dengue vaccine production for 2015 launch

Sanofi starts dengue vaccine production for 2015 launch

Sanofi Pasteur is poised to produce the first validation batches of their dengue vaccine at the company’s state-of-the-art production centre near Lyon, France.
According to Antoine Quin, manager at the site in Neuville-sur-Saone, the plant has a design capacity of 100 million doses of the vaccine, tetravalent CYD-TDV, annually. Starting around 2015, Sanofi Pasteur expects to manufacture one billion doses over the following decade.
Investing 300 million euros in building and staffing the plant was a substantial gamble for Sanofi, said Guillaume Leroy, dengue vaccine head. The Lyon facility got the green light in 2009, when only Phase II data was available. Although promising, this was far from definitive........................
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more on dengue
Learn about prevention of dengue fever, a disease transmitted by mosquitoes.

Dengue Fever Prevention

Neither vaccine nor drugs for preventing infection are available. The bite of one infected mosquito can result in infection. The risk of being bitten is highest during the early morning, several hours after daybreak, and in the late afternoon before sunset. However, mosquitoes may feed at any time during the day. Aedes mosquitoes typically live indoors and are often found in dark, cool places such as in closets, under beds, behind curtains, and in bathrooms. Travelers should be advised to use insecticides to get rid of mosquitoes in these areas and to select accommodations with well-screened windows or air conditioning when possible. Additionally, travelers should take measures to avoid being bitten by mosquitoes. Long-term travelers and expatriates can take extra precautions to reduce mosquito-breeding sites around their accommodations by emptying and cleaning or covering any standing water (such as in water storage tanks and flowerpot trays).

Dengue fever facts

  • Dengue fever is a disease caused by a family of viruses that are transmitted by mosquitoes.
  • Symptoms such as headache, fever, exhaustion, severe joint and muscle pain, swollen glands (lymphadenopathy), and rash. The presence (the "dengue triad") of fever, rash, and headache (and other pains) is particularly characteristic of dengue fever.
  • Dengue is prevalent throughout the tropics and subtropics. Outbreaks have occurred recently in the Caribbean, including Puerto Rico, the U.S. Virgin Islands, Cuba, and in Paraguay in South America, and Costa Rica in Central America.
  • Because dengue fever is caused by a virus, there is no specific medicine or antibiotic to treat it. For typical dengue fever, the treatment is purely concerned with relief of the symptoms (symptomatic).
  • The acute phase of the illness with fever and myalgias lasts about one to two weeks.
  • Dengue hemorrhagic fever (DHF) is a specific syndrome that tends to affect children under 10 years of age. It causes abdominal pain, hemorrhage (bleeding), and circulatory collapse (shock).
  • The prevention of dengue fever requires control or eradication of the mosquitoes carrying the virus that causes dengue.
  • There is currently no vaccine available for dengue fever.

What is dengue fever?

Dengue (pronounced DENG-gay) can affect anyone but tends to be more severe in people with compromised immune systems. Because it is caused by one of four serotypes of virus, it is possible to get dengue fever multiple times. However, an attack of dengue produces immunity for a lifetime to that particular serotype to which the patient was exposed.Dengue fever is a disease caused by a family of viruses that are transmitted by mosquitoes. It is an acute illness of sudden onset that usually follows a benign course with symptoms such as headache,fever, exhaustion, severe muscle and joint painswollen glands(lymphadenopathy), and rash. The presence (the "dengue triad") of fever,rash, and headache (and other pains) is particularly characteristic of dengue. Other signs of dengue fever include bleeding gums, severe pain behind the eyes, and red palms and soles.
Dengue goes by other names, including "breakbone" or "dandy fever." Victims of dengue often have contortions due to the intense joint andmuscle pain, hence the name breakbone fever. Slaves in the West Indies who contracted dengue were said to have dandy fever because of their postures and gait.
Dengue hemorrhagic fever is a more severe form of the viral illness. Symptoms include headache, fever, rash, and evidence of hemorrhage in the body. Petechiae (small red or purple splotches or blisters under the skin), bleeding in the nose or gumsblack stools, or easy bruising are all possible signs of hemorrhage. This form of dengue fever can be life-threatening and can progress to the most severe form of the illness, dengue shock syndrome.

Tuesday, 16 July 2013

Top Selling Schizophrenia Drug Abilify (Aripiprazole)


Abilify-Aripirazole-Atypical Antipsychotics-Otsuka-BMS
Aripiprazole (brand names: Abilify, Aripiprex, OPC-14597,) is an atypical antipsychotic drug with the chemical name 7-[4-(2,3-dichlorophenyl)-1-piperazinyl]-butyloxy]-3,4-dihydro-2(1H)-quinolinone. It was first discovered by the Otsuka Pharmaceutical Company, Ltd., based in Japan, and in collaboration with Bristol-Myers Squibb began to market the drug in the United States following the approval by the Food and Drug Administration for schizophrenia in November 2002. According to IMS Health, Abilify was the fourth top-selling drug in the United States in 2011, with sales of $5.2 billion.
Chemical Structure of Aripiprazole (brand names: Abilify)
Chemical Strutcure of Aripirazole-Abilify-Antipsychotics-Otsuka-BMS-阿立哌唑-安律凡-大冢制药-エビリファイ
Chemical Synthesis of Aripiprazole(active ingredient for Abilify)
Chemical Synthesis of Abilify-Aripirazole-Atypical Antipsychotics-Otsuka-BMS-阿立哌唑-アリピプラゾール
Experimental Procedures for the preparation of Aripiprazole (Abilify)
US 5,006,528 discloses process for the preparation of Aripiprazole in two steps. The first step comprises synthesis of 7-(4-bromobutoxy)-3,4-dihydrocarbostyril (7-BBQ) by alkylating the hydroxy group of 7-hydroxy-3,4-dihydrocarbostyril (7-HQ) with 1 ,4-dibromobutane using potassium carbonate in water at reflux temperature for 3 hours to obtain 7-BBQ in 68% yield. The resulting 7-BBQ is further reacted with 1- (2,3-dichlorophenyl)-piperazine to obtain Aripiprazole.
Preparation of 7-(4-bromobutoxy)-3,4-dihydro-2(1H)quinolinone (7-(4-bromobutoxy)-3,4-dihydrocarbostyril; 7-BBQ)
7-Hydroxy-3,4-dihydro-2(1H)-quinolinone (aka 7-Hydroxy-3,4-dihydrocarbostyril, 60gm) and potassium carbonate (76.3 gm) were taken in acetonitrile (1200ml) at room temperature. To this tetra butyl ammonium iodide (13.7 gm) and 1 ,4-dibromobutane (238.5gm) were added and heated at 40- 45°C for 24 hours. Reaction mass was cooled upto room temperature and was filtered off. The resulting filtrate was distilled off under vacuum. The resultant mass was cooled to 25-30°C and cyclohexane (300 ml) was added under stirring. The resulting solid was filtered off and was dried. The resulting solid was taken in water and was stirred for few minutes. The solid was filtered and dried under vacuum at 55-60°C for 20 hours to obtain title compound. mp 110.5-111 °C; 1H NMR (DMSO-d6) ä 1.81 (2H, m, -CH2-), 1.95 (2H, m, -CH2-), 2.41 (2H, t, J ) 7 Hz, -CH2CO-), 2.78 (2H, t, J) 7 Hz, -CH2-C-CO-), 3.60 (2H, t, J ) 6 Hz, -CH2Br), 3.93 (2H,t, J ) 6 Hz, O-CH2-), 6.43 (1H, d, J ) 2.5 Hz), 6.49 (1H, dd, J) 2.5, 8 Hz), 7.04 (1H, d, J ) 8 Hz), 9.98 (1H, s, NHCO). Anal. (C13H16NO2Br) C, H, N.
Yield: 73-75%; Purity: 93-95%
Preparation of Aripiprazole (7-{4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one)
7-(4-Bromobutoxy)-l ,2,3,4-tetrahydroquinolin-2-one (50 gm) was taken in acetonitrile (500 ml) at 25-30°C. To this potassium carbonate (67.2 gm) and l-(2,3- dichlorophenyl) piperazine hydrochloride (44.9gm) were added under stirring. The reaction mixture was refluxed at 80-85°C for 8 hours. The reaction mass was cooled to room temperature, filtered and the resulting solid was washed with acetonitrile. To the resulting solid, water was added and was stirred. The solid was filtered off, washed with water and dried under vacuum at 75-80°C for 15 hrs. The resulting crude aripiprazole was crystallized from isopropyl alcohol and water to obtain title compound. Yield: 75-80%; Dimer Impurity: <0.1%. 1H NMR: DMSO-d6 d 9.96 [1H, s, NH]; 7.29 [2H, m, Ar]; 7.13 [1H, q, Ar]; 7.04 [1H, d, Ar]; 6.49 [1H, dd, Ar]; 6.45 [1H, d, Ar]; 3.92 [2H, t, -CH2-O-]; 2.97 [4H, bb,2(-CH2-)]; 2.78 [2H, t, -CH2-N2-)]; 2.39 [4H, m, 2(-CH2-)]; 1.73 [2H, m, - CH2-]; 1.58 [2H, m, -CH2-]. IR:cm-1 3193; 2939; 2804; 1680; 1627; 1579; 1520; 1449; 1375; 1270; 1245; 1192; 1169; 1045; 965; 649; 869; 780; 712; 588.
Preparation of aripiprazole anhydrous Type I using isopropyl alcohol and water
Crude aripiprazole (30 g) was taken in isopropyl alcohol (600 ml) and was heated to 80-85°C. Water (90 ml) was added at the same temperature. Activated carbon was added and the mixture was stirred for 30 minutes at the same temperature. The resulting hot solution was filtered and the bed was washed with hot isopropyl alcohol. The resulting filtrate was cooled to 25-30°C for 4 hours. The resulting solid was filtered, washed with isopropyl alcohol and dried under suction for 1 hour. The resulting wet solid was dried in preheated oven maintained at 100-105°C for 6 hours to obtain title compound.
Yield: 87-89% HPLC Purity: 99.89
Anhydrous crystal D: Below detectable limit (BDL) at limit of detection 1%.
Hydrate A: Below detectable limit (BDL) at limit of detection 1 %.
Particle size distribution: d10=15.83 m, d50=60.12 m, d90=144.99 m
Preparation of aripiprazole anhydrous Type I using ethanol and water
Crude aripiprazole (15 g) was taken in ethanol (300 ml) and water (45 ml) and was heated to 80-85°C for 1-2 hours. The resulting mixture was cooled to 25-30°C within 4 hours and stirred for 3 hours. The resulting solid was filtered and dried under suction for 1 hour. The resulting wet solid was dried in preheated oven maintained at 100-105°C for 3 hours to obtain title compound. Yield: 90% HPLC Purity: 99.9%
Anhydrous crystal D: Below detectable limit (BDL) at limit of detection 1%.
Hydrate A: Below detectable limit (BDL) at limit of detection 1%.
Particle size distribution: d10=22.01 m, d50=105.10 m, d90=232.97 m
References For the Process of Aripiprazole (Abilify,)
Yasuo Oshiro, Seiji Sato, Nobuyuki Kurahashi, Tatsuyoshi Tanaka, Tetsuro Kikuchi, Katsura Tottori, Yasufumi Uwahodo, and Takao Nishi; Novel Antipsychotic Agents with Dopamine Autoreceptor Agonist Properties: Synthesis and Pharmacology of 7-[4-(4-Phenyl-1-piperazinyl)butoxy]- 3,4-dihydro-2(1H)-quinolinone DerivativesJ. Med. Chem. 1998, 41, 658-667
Yasuo Oshiro, Seiji Sato, Nobuyuki Kurahashi; Carbostyril derivatives, Otsuka Pharmaceutical Co., Ltd; US patent 5006528;Issue date: Apr 9, 1991
BANDO, Takuji, YANO, Katsuhiko, FUKANA, Makoto, AOKI, Satoshi ;Method for producing fine particles of aripiprazole anhydride crystals b; OTSUKA PHARMACEUTICAL CO., LTD., WO 2013002420 A1
CN 201210235157
GUPTA, Vijay Shankar, KUMAR, Pramod, VIR, Dharam ;Process for producing aripiprazole in anhydrous type i crystals;JUBILANT LIFE SCIENCES LIMITED;WO 2012131451 A1
SRIVASTAVA JAYANT GUPTA Vijay Shankar;Improved process for the preparation of 7.(4-bromobutoxy) 3,4-dihydrocarbostyril, a precursor of aripiprazole;wo2011030213 A1
No Generic Abilify in the US until April 2015
On May 7, 2012, The U.S. Court of Appeals for the Federal Circuit ruled in favor of Otsuka Pharmaceutical Co., Ltd. in its patent litigation against several companies including Israel-based Teva and Weston, Ontario-based Apotex seeking FDA approval to market generic copies of Abilify®. (see the pdf file for the decision upholding the Otsuka patent here). The Federal Circuit affirmed a decision of the U.S. District Court for the District of New Jersey holding that the asserted claims of U.S. Patent No. 5,006,528 (pdf file here) covering aripiprazole, the active ingredient in Abilify®, are valid, thus maintaining patent and regulatory protection for Abilify® in the U.S. until at least April 20, 2015. The case is Otsuka Pharma Co. v. Sandoz Inc., 2011-1126 and 2011-1127, U.S. Court of Appeals for the Federal Circuit (Washington). The lower court case is Otsuka Pharmaceutical Co. v. Sandoz Inc., 07cv1000, U.S. District Court for the District of New Jersey (Trenton).
Chemical Name for Aripiprazole(active ingredient for Abilify): 7-{4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one
CAS number 129722-12-9
Aripiprazole  brand names: AbilifyAripiprex) is a partial dopamine agonist of the second generation class of atypical antipsychotics with additional antidepressant properties that is primarily used in the treatment ofschizophreniabipolar disordermajor depressive disorder, and irritability associated with autism.[1] It was approved by the U.S.Food and Drug Administration (FDA) for schizophrenia on November 15, 2002 and the European Medicines Agency on 4 June 2004; for acute manic and mixed episodes associated with bipolar disorder on October 1, 2004; as an adjunct for major depressive disorder on November 20, 2007;[2] and to treat irritability in children with autism on 20 November 2009.[3] Aripiprazole was developed by Otsuka in Japan, and in the United StatesOtsuka America markets it jointly with Bristol-Myers Squibb.
Aripiprazole can be synthesized beginning with a dichloroaniline and bis(2-chloroethyl)amine:
  1.  U.S. Patent 5,006,528
Aripiprazole synth.png

Monday, 15 July 2013

Research in HIV therapies -A review- The global community has made significant strides forward in its mission to eradicate the HIV epidemic

HIV therapies 
Over the last 30 years, the face of human immunodeficiency virus (HIV) has changed from one largely associated with homosexuality, drug addicts, prejudice, fear and rejection without much hope of a future, to one involving innocent children born of mothers living with HIV for whom it is hoped the disease will be curable and even eradicated. 
According to the World Health Organization (WHO) and UNAIDS, 34 million people were living with HIV worldwide in 2011. Sub-Saharan Africa was, and still is, the most severely affected area. Approximately 5 per cent of adults in this region live with HIV, representing almost 70 per cent of the global HIV-infected population. On a positive note, the number of newly infected people has declined by approximately 25 per cent over the past ten years and, importantly, over the past two years, half of the reductions in HIV infections has been in children.
Treatment and prevention
The approach to, and success of, HIV treatment and prevention has.....................cont
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 article by
Wendy McNeely
Adis International (Springer Healthcare), using data derived from Adis R&D Insight and Clinical Trials Insight. For further information on Adis services, please contact Daniela Ranzani on +39 02 423 4562 or email her

Friday, 12 July 2013

Vical's Allovectin Phase III Trial Results: Consider The Possibilities

Cohen: We saw that happen last year when JNJ prematurely unblinded the pre- chemo Phase III study for the prostate cancer drug Zytiga. The trial achieved ...

Allovectin-7 is a substance that is being studied as a gene therapy agent in the treatment of cancer, such as malignant melanoma. It is a plasmid/lipid complex containing the DNA sequences encoding HLA-B7 and ß2 microglobulin - two components of major histocompatibility complex (MHC, class I). It increases the ability of the immune system to recognize cancer cells and kill them.
In 1999, FDA granted Allovectin-7 orphan drug designation for the treatment of invasive and metastatic melanoma.

  • Allovectin-7 entry in the public domain NCI Dictionary of Cancer Terms

Thursday, 4 July 2013

Chocolate as medicine: a quest over the centuries

The rehabilitation of chocolate has occurred only in recent times. The pages of scientific magazines have been positively recaptured and chocolate’s reputation is being restored to the value that Carl Linnaeus credited to this food, when he named the generous plant Theobroma cacao, the food of the gods
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Monday, 1 July 2013

Verona Pharma Plc Peer-Reviewed Paper Suggests RPL554 With Glycopyrrolate, Or Other Muscarinic Receptor Antagonists, Produces Synergistic Bronchodilation


Verona Pharma Plc ("Verona Pharma" Or The "Company") Peer-Reviewed ...

Wall Street Journal
Verona Pharma is developing first-in-class drugs to treat respiratory disease, such as COPD, asthma and chronic, severe cough. The Company has three drug programmes, two of which are in Phase II. The lead programme, RPL554, is an innovative dual ...

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RPL-554 (LS-193,855) is a drug which acts as a long-acting inhibitor of the phosphodiesterase enzymes PDE-3 and PDE-4, producing both bronchodilator and antiinflammatory effects.[1] It is being developed by Verona Pharma as a potential treatment for asthma and hay fever, and is currently in clinical trials.[2][3]
  1.  Boswell-Smith V, Spina D, Oxford AW, Comer MB, Seeds EA, Page CP. The Pharmacology of Two Novel Long-Acting Phosphodiesterase 3/4 Inhibitors, RPL554 (9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl) -3,4,6,7-tetrahydro-2H-pyrimido(6,1-a)isoquinolin-4-one) and RPL565 (6,7-Dihydro-2-(2,6-diisopropylphenoxy)-9,10-dimethoxy-4H-pyrimido(6,1-a)isoquinolin-4-one). Journal of Pharmacology and Experimental Therapeutics 2006; 318(2):840-848.
  2.  Verona Pharma Plc - Lead Drug RPL554
  3.  Asthma and hay fever drug tested. BBC News, Wednesday 10 September 2008

Friday, 28 June 2013