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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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NICE has given a provisional green light for Bayer’s blood thinner Xarelto for help patients with thrombotic events
NICE has given a provisional green light for Bayer’s blood thinner Xarelto for help patients with thrombotic events
NICE IS
National Institute for Health and Care Excellence
Developing a series of national clinical guidelines to secure consistent, high quality, evidence based care for patients using the National Health Service in
April 22, 2013
READ MORE AT PHARMATIMES
http://www.pharmatimes.com/Article/13-04-22/Xarelto_gains_NICE_thumbs_up_for_DVT_licence.aspx
RIVAROXABAN
Rivaroxaban (BAY 59-7939) is an oral anticoagulant invented and manufactured by Bayer; in a number of countries it is marketed as Xarelto. In the United States, it is marketed by Janssen Pharmaceutica. It is the first available orally active direct factor Xa inhibitor. Rivaroxaban is well absorbed from the gut and maximum inhibition of factor Xa occurs four hours after a dose. The effects lasts 8–12 hours, but factor Xa activity does not return to normal within 24 hours so once-daily dosing is possible. There is no specific way to reverse the anticoagulant effect of rivaroxaban in the event of a major bleeding event, unlike warfarin
In September 2008, Health Canada granted marketing authorization for rivaroxaban as one 10 mg tablet taken once daily for the prevention of venous thromboembolism (VTE) in patients who have undergone elective total hip replacement or total knee replacement surgery.
In September 2008, the European Commission granted marketing authorization of rivaroxaban for the prevention of venous thromboembolism in adult patients undergoing elective hip and knee replacement surgery. In December 2011 rivaroxaban has been approved by the European Commission for use in two new indications: prevention of stroke and systemic embolism in adult patients with non-valvular atrial fibrillation (AF) with one or more risk factors and treatment of deep vein thrombosis (DVT) and prevention of recurrent DVT and pulmonary embolism (PE) following an acute DVT in adults.
On July 1, 2011, the U.S. Food and Drug Administration (FDA) approved rivaroxaban for prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE), in adults undergoing hip and knee replacement surgery. On November 4, 2011, the U.S. FDA approved rivaroxaban for stroke prophylaxis in patients with non-valvular atrial fibrillation. On November 2, 2012, the U.S. Food and Drug Administration (FDA) approved rivaroxaban for the treatment of patients with deep vein thrombosis (DVT) and pulmonary embolism (PE) and for long-term treatment to prevent recurrence.
Cipla launches first Biosimilar of Etanercept in India under brand name ‘ETACEPT’
Etanercept
is made from the combination of two naturally occurring soluble human 75-kilodalton TNF receptors linked to an Fc portion of an IgG1. The effect is an artificially engineered dimeric fusion protein.
| Wed, Apr 17 2013 |
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Cipla, the fifth largest pharma company in India with consolidated net sales of Rs.6,800 crore plus, has launched the first biosimilar of Etanercept in India; under the brand name ‘ETACEPT’ for the treatment of rheumatic disorders. Formed through a partnership alliance, ETACEPT is manufactured by a China-based company Shanghai CP Guojian Pharmaceutical Co. Ltd., which will be marketed by Cipla in India. The introduction of Etacept now signals Cipla’s entry into the Biologic segment offering an option to the patients suffering from rheumatic disorders at a lower cost. Etacept is available as a lyophilized powder to be given by subcutaneous injection. It is available with stockists across the country at Rs.6,150 and the recommended dose for adults is 25mg twice weekly by subcutaneous injection. READ MORE AT PHARMABIZ http://www.pharmabiz.com/NewsDetails.aspx?aid=74842&sid=2
Etanercept (trade name Enbrel) is a biopharmaceutical that treats autoimmune diseases by interfering with tumor necrosis factor (TNF; a soluble inflammatory cytokine) by acting as a TNF inhibitor. It has U.S. F.D.A. approval to treat rheumatoid, juvenile rheumatoid andpsoriatic arthritis, plaque psoriasis and ankylosing spondylitis. TNF-alpha is the “master regulator” of the inflammatory (immune) response in many organ systems. Autoimmune diseases are caused by an overactive immune response. Etanercept has the potential to treat these diseases by inhibiting TNF-alpha. Etanercept is a fusion protein produced by recombinant DNA. It fuses the TNF receptor to the constant end of the IgG1 antibody. First, the developers isolated the DNA sequence that codes the human gene for soluble TNF receptor 2, which is a receptor that binds to tumor necrosis factor-alpha. Second, they isolated the DNA sequence that codes the human gene for the Fc end of immunoglobulin G1 (IgG1). Third, they linked the DNA for TNF receptor 2 to the DNA for IgG1 Fc. Finally, they expressed the linked DNA to produce a protein that links the protein for TNF receptor 2 to the protein for IgG1 Fc. The prototypic fusion protein was first synthesized and shown to be highly active and unusually stable as a modality for blockade of TNF in vivo in the early 1990s by Bruce A. Beutler, an academic researcher then at the University of Texas Southwestern Medical Center at Dallas, and his colleagues.[2][3][4] These investigators also patented the protein, selling all rights to its use to Immunex, a biotechnology company that was acquired by Amgen in 2002. It is a large molecule, with a molecular weight of 150 kDa., that binds to TNFα and decreases its role in disorders involving excess inflammation in humans and other animals, including autoimmune diseases such as ankylosing spondylitis, juvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, rheumatoid arthritis, and, potentially, in a variety of other disorders mediated by excess TNFα. In North America, etanercept is co-marketed by Amgen and Pfizer under the trade name Enbrel in two separate formulations, one in powder form, the other as a pre-mixed liquid. Wyeth is the sole marketer of Enbrel outside North America excluding Japan whereTakeda Pharmaceuticals markets the drug. Etanercept is an example of a protein-based drug created using the tools of biotechnologyand conceived through an understanding afforded by modern cell biology. |
FDA OKs Sun Pharma for Generic Januvia, Glumetza
Sun Pharma announces tentative USFDA approvals for generic Januvia® and generic Glumetza®
SUNPHARMA, BSE: 524715) announced that the US FDA has granted its subsidiary, two tentative approvals for its Abbreviated New Drug Applications (ANDA) for generic version of Januvia®, Sitagliptin Tablets and generic version of Glumetza®, Metformin HCl Extended-release tablets.
read more at pharmalive
http://www.pharmalive.com/fda-oks-sun-pharma-for-generic-januvia-glumetza
Ceregene announces top-line data from CERE-120 Phase 2b clinical study for Parkinson’s disease
Ceregene, Inc. today announced the top-line data from its double-blind, randomized, controlled Phase 2b clinical study of CERE-120 (AAV-neurturin), a gene therapy product designed to deliver the neurotrophic factor neurturin, for Parkinson’s disease……………read more at
Alcon announces FDA approval of Simbrinza(TM) Suspension
20/04/2013
Alcon, the global leader in eye care and a division of Novartis, announces US FDA approval for Simbrinza(TM) Suspension, indicated for the reduction of elevated intraocular pressure (IOP) in patients with primary open-angle glaucoma or ocular hypertension.
Elevated IOP is the only modifiable risk factor for glaucoma. Glaucoma is a group of eye diseases that lead to progressive damage of the optic nerve[5] and can result in gradual, irreversible loss of vision, and eventually blindness, if left untreated. Glaucoma affects more than 2.2 million Americans and is the second-leading cause of preventable blindness worldwide, according to Novartis AG.
Simbrinza is a fixed-dose combination medication that offers a wide range of treatment possibilities due to its strong efficacy and ability to decrease elevated IOP by 21- 35%. In addition, it is the only available, fixed-dose combination therapy for glaucoma in the US without a beta blocker.
read all at
COMPANIES – India’s Orchid links up with new antibiotics firm Allecra
Indian drugmaker Orchid Pharma has bought a stake in a newly-formed European firm, Allecra Therapeutics, which has been set up to develop novel antibiotics…………………READ MORE AT PHARMATIMES
Links
www.allecra.com
www.orchidpharma.com
The Chennai-based pharmaceuticals major, Orchid Chemicals & Pharmaceuticals Ltd, With exports spanning more than 75 countries, it is the largest manufacturer-exporter of cephalosporin bulk actives in India and is ranked amongst the top 5 cephalosporin-producers globally.
Orchid is a first-generation enterprise founded in 1992 by K Raghavendra Rao, who is also the firm’s managing director.——- READ MORE
http://www.rediff.com/money/2004/apr/07spec.htm
HOMEOPATHY- BOTHROPS for thrombosis
Bothrops
Yellow pit viper / Fer de lance
Bothrops lanceolatus / Lachesis lanceolatus
The homeopathic remedy bothrops is prepared using the freshly obtained venom of bothrops lanceolatus and it is mainly used to cure thrombosis (intravascular coagulation of blood in any part of the circulatory system) and hemorrhages.
Belonging to a genus of venomous pit vipers that are found in Central and South America, Bothrops contains a heat-sensitive pit on both sides of its head. The generic name bothrops has its origin in the Greek words bothrops denoting ‘pit’ and ‘ops’ meaning ‘eye’ or ‘face’ – a reference to the heat-sensitive organs on its head. Compared to any other group of venomous snakes, members of this genus are liable for more number of snake-bite deaths in the Americas. As of date, 32 species of snakes in this genus have been identified.
It may be noted that the yellow pit viper is a highly poisonous snake and its bite may prove to be fatal for humans. This species is distinguished by its gray or brown color and a series of black-edged diamonds, which usually have a paler shade along the border. Anyone suffering a yellow pit viper bite on a limb experiences rapid swelling of the part, so much so that it becomes enormous in size. At the same time, the limb is infected along with the formation of gangrene.
The yellow pit viper is a very violent and extremely poisonous snake that is indigenous to the island of Martinique. The highly poisonous snake, which belongs to the family of Crotalidae, is commonly known as the Martinique lance head or fer-de-lance.
Usually, a large, semi-arborial and heavy-bodied Martinique lance head adult is about 150 cm to 200 cm, however, there have been instances when snakes as long as 300 cm too have been sighted. The color of this species body ranges from gray to brown to yellowish tan and usually has marked darker patterns on the back as well as laterally. The top of the lance head’s head generally has a darker color. The color of the belly region of the snake varies from a paler yellowish-gray to grayish-brown. In the case of some snakes, the belly region is also freckled with small, relatively darker grayish marks.
The yellow pit viper or bothrops lanceolatus is mainly found in humid tropical forests as well as tropical soggy forest in the highlands. Sometimes, this species is also found inhabiting the stony hillsides. Previously, this species was found in a number of other Caribbean islands, but now it is only found on Martinique island, on land ranging from the sea level to about 1,300 m height.
Although the yellow pit viper is generally a nocturnal species and primarily land-dwelling, some members of this species have also been found living at a height of 20 meters above the ground. As mentioned before, the yellow pit viper or bothrops lanceolatus is a very aggressive snake and has the ability to attack swiftly when it is taken aback or endangered. This species is known to be ovoviviparous (producing eggs and hatching them inside the body), but the size of the litter has not yet been reported. This species of snakes mainly feeds of birds, lizards, small mammals that are available to it and also frogs.
The venom of bothrops lanceolauts is basically hemotoxic (a poison that results in hemolytic reactions), usually with cytotoxic (a substance poisonous to living cells) aspects. Envenomation or the injection of this snake’s venom is likely to cause regular internal bleeding and at the same time, damage the local tissues. Several deaths of humans owing to bites by bothrops lanceolauts (B. lanceolauts) have been kept in details.
Parts used
The homeopathic remedy bothrops is prepared from the freshly obtained venom of the poisonous snake bothrops lanceolauts or the yellow pit viper found in the South and Central America. Although this homeopathic medication is prepared from deadly snake venom, it does not retain any of the toxic or poisonous attributes of the substance it is made from and is absolutely safe for human use.
Uses
Unlike most other homeopathic medications, bothrops has limited therapeutic uses. This homeopathic remedy is primarily used to treat thrombosis or hemorrhaging. In addition, bothrops may also be given to patients who have suffered strokes on the left side along with paralysis on the right side and enduring incapability to be eloquent or memorize the right words. Generally, individuals needing this homeopathic medication are somewhat slow or tired and they also experience trembling due to nervousness.
There are no specific factors that are known to make people bitten by the yellow pit viper feel better or improve their symptoms. On the other hand, they feel worse or their symptoms deteriorate when they are walking, on their right side or taking a deep breath. In addition, their condition worsens after midnight and also at sunrise.
Source
The yellow pit viper or bothrops lanceolatus, whose venom forms the basis of the homeopathic remedy bothrops, is found on the Martinique Island in the Caribbean. Earlier, this species was also found on several other islands of the Caribbean. This species is an Ophidian belonging to the Crotalidae family. Bothrops lanceolatus is a highly aggressive snake and its venom is extremely poisonous.
HOMEOPATHY-REVIEW
Samuel Hahnemann, the founder of homeopathy
Homeopathy uses very dilute substances to stimulate the body’s healing power. Its basic principle is treat ‘like with like’. This involves treating a patient’s symptoms with minute amounts of a substance that would cause similar symptoms in a healthy person. This practice contrasts with conventional allopathic medicine, in which treating ‘like with opposite’ prevails; that is, a disease is treated with a substance that opposes it.
The first person to practise the healing principle of treating ‘like with like’ was Greek physician Hippocrates (c.460-377BCE). His method went against the thinking of the time, which held that the gods were the main force behind a disease, and that a cure could be found by treating with a substance that had an opposite effect in a healthy person.
German doctor Samuel Hahnemann (1755-1843) was the modern-day founder of homeopathy. He proved the principle of ‘like curing like’ with his experiments with quinine, known to be an effective treatment for malaria. He found he developed malarial symptoms after taking doses of quinine (he was otherwise in good health). These effects lasted hours after each dose.
He tested other substances in the same way, in a process known as ‘proving’. He ‘proved’ more than 100 homeopathic remedies in his lifetime, publishing his findings in ‘The Organon of Rational Medicine’ in 1811. He believed that the remedies worked by activating a person’s ‘vital force’, that is, the body’s own healing potential. Having conducted tests on many volunteers, he came to realise the importance of taking into account the personality traits of each person receiving the treatment. He found that particular ‘types’ of people manifested different symptoms to the same disease and so required treatment with different remedies in accordance with their ‘type’.
American doctor James Tyler Kent (1849-1943) furthered Hahnemann’s work on the different ‘types’ of people and the matching of a remedy to their emotional and physical characteristics. These ‘types’ became known as ‘constitutional types’.
Homeopathic remedies
Remedies can be made from many different substances. The most common sources are flowers, plants, roots, trees, poisons, minerals and metals. Certain insects are also used. Hahnemann used the smallest possible amount of a substance to trigger a healing effect. This was to minimise side effects. He realised that the more a substance was diluted, the better the results, provided it was also vigorously shaken (in a process known as succussion) at each stage of dilution. Counterintuitive though it seems, the less of the original substance that remained in the remedy, the greater its potency and effectiveness. The process of diluting a remedy to render it effective is called potentisation. First an alcohol/water extract is made from the substance. This is the mother tincture. The extract is diluted to the required potency.
Old homeopathic belladonna remedy.
The main potencies are denoted by x, c and m: x means the remedy has been diluted one part mother tincture in 9 drops of water; c means one part of mother tincture in 99 drops of water; and m means one part of mother tincture in 999 drops of water. A 1c potency is one part in 99 parts of water. A 2c potency is created by taking one part of the previous dilution (i.e., the 1c potency) and diluting it in 99 parts of water. The most common potencies used are 6c, 12c and 30c.
Once the required potency is reached, a few drops of the substance are applied to lactose (milk sugar) tablets. The tablets must be kept dry and away from direct sunlight. For the purposes of self-treatment as detailed here, it is suggested that the 30c potencies are used, as these are commonly available. To obtain the best results, consult a homeopath. They may prescribe higher potencies depending on the initial consultation and the presenting problem. This is particularly the case if the ailment has a strong emotional or mental aspect.
1857 painting by Alexander Beydeman showing historical figures and personifications of homeopathy observing the brutality of medicine of the 19th century
Homeopathic pills, homeopathic remedy oscillococcinum
Historical context
Hippocrates, in about 400 BC, perhaps originated homeopathy when he prescribed a small dose of mandrake root – which in larger doses produced mania – to treat mania itself; in the 16th century the pioneer of pharmacology Paracelsus declared that small doses of “what makes a man ill also cures him.” Samuel Hahnemann (1755–1843) gave homeopathy its name and expanded its principles in the late 18th century. At that time, mainstream medicine used methods like bloodletting and purging, and administered complex mixtures, such as Venice treacle, which was made from 64 substances including opium, myrrh, and viper’s flesh. These treatments often worsened symptoms and sometimes proved fatal. Hahnemann rejected these practices – which had been extolled for centuries as irrational and inadvisable; instead, he advocated the use of single drugs at lower doses and promoted an immaterial, vitalistic view of how living organisms function, believing that diseases have spiritual, as well as physical causes.
Homeopathic remedy Rhus toxicodendron, derived from poison ivy.
Lilly’s diabetes drug dulaglutide shines again in Phase III
STRUCTURAL FORMULA OF DULAGLUTIDE
Monomer
HGEGTFTSDV SSYLEEQAAK EFIAWLVKGG GGGGGSGGGG SGGGGSAESK 50
YGPPCPPCPA PEAAGGPSVF LFPPKPKDTL MISRTPEVTC VVVDVSQEDP 100
EVQFNWYVDG VEVHNAKTKP REEQFNSTYR VVSVLTVLHQ DWLNGKEYKC 150
KVSNKGLPSS IEKTISKAKG QPREPQVYTL PPSQEEMTKN QVSLTCLVKG 200
FYPSDIAVEW ESNGQPENNY KTTPPVLDSD GSFFLYSRLT VDKSRWQEGN 250
VFSCSVMHEA LHNHYTQKSL SLSLG 275
Disulfide bridges location
55-55′ 58-58′ 90-150 90′-150′ 196-254 196′-254′
MOLECULAR FORMULA C2646H4044N704O836S18
MOLECULAR WEIGHT 59.67 kDa
MANUFACTURER Eli Lilly and Company
CODE DESIGNATION LY2189265
CAS REGISTRY NUMBER 923950-08-7
http://www.ama-assn.org/resources/doc/usan/dulaglutide.pdf FOR ALL DATA
Dulaglutide
APRIL 17, 2013
Eli Lilly has presented more promising late-stage data on its investigational long-acting diabetes drug dulaglutide.
The US major has presented top-line results from two Phase III studies from the five-trial AWARD programme. The first showed that dulaglutide demonstrated statistically superior reduction in HbA1c (blood sugar) levels compared to Sanofi’s Lantus (insulin glargine) at 52 weeks in patients with type 2 diabetes who were on metformin and glimeperide (AWARD-2). The second trial demonstrated that the drug, a once-weekly glucagon-like peptide 1 (GLP-1) receptor agonist, in combination with Lilly’s own Humalog (insulin lispro) was more effective than a Lantus/Humalog combo.
In October, Lilly posted impressive data from three other AWARD trials which showed that dulaglutide controlled HbA1c levels better than Byetta (exenatide), a drug Lilly helped develop before ending a collaboration with Amylin (since bought by Bristol-Myers Squibb and AstraZeneca), metformin and Merck & Co’s Januvia (sitagliptin).
Lilly stated that it expects to submit dulaglutide to regulatory authorities this year and present detailed data from the AWARD studies at scientific meetings in 2013 and 2014.
Links
DRUG SPOTLIGHT- EXENATIDE, BYETTA
EXENATIDE
ACETATE CAS NO 141732-76-5
Exenatide, derived from a compound found in the saliva of the Gila monster, a large lizard native to the southwestern US, is a functional analog of Glucagon-Like Peptide-1 (GLP-1), a naturally occuring peptide.
Exenatide (INN, marketed as Byetta, Bydureon) is a glucagon-like peptide-1 agonist(GLP-1 agonist) medication approved in April 2005 for the treatment of diabetes mellitus type 2. It belongs to the group of incretin mimetics and is manufactured by Amylin Pharmaceuticals. Exenatide in its Byetta form is administered as a subcutaneous injection (under the skin) of the abdomen, thigh, or arm, any time within the 60 minutes before the first and last meal of the day. A once-weekly injection has been approved as of January 27, 2012 under the trademark Bydureon
Exenatide is a synthetic version of exendin-4, a hormone found in the saliva of the Gila monster that was first isolated by Dr. John Eng in 1992 while working at the Veterans Administration Medical Center in the Bronx, New York. It displays biological properties similar to human glucagon-like peptide-1 (GLP-1), a regulator of glucose metabolism andinsulin secretion. According to the package insert, exenatide enhances glucose-dependent insulin secretion by the pancreatic beta-cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying, although the mechanism of action is still under study.
Exenatide is a 39-amino-acid peptide, an insulin secretagogue, with glucoregulatory effects. Exenatide was approved by the FDA on April 28, 2005 for patients whose diabetes was not well-controlled on other oral medication. The medication is injected subcutaneously twice per day using a filled pen-like device. The abdomen is a common injection site, after the area is cleaned with an alcohol pad. A new pen must first be tested to see if the medicine is flowing.
GILA MONSTER
| Indication | Indicated as adjunctive therapy to improve glycemic control in patients with Type 2 diabetes mellitus who are taking metformin, a sulfonylurea, or a combination of both, but have not achieved adequate glycemic control. |
| Pharmacodynamics | Exenatide is an incretin mimetic, which has glucoregulatory effects. While it is has blood-sugar lowering actions alone, it can also be combined with other medications such as pioglitazone, metformin, sulfonylureas, and/or insulin to improve glucose control. The approved use of exenatide is with either sulfonylureas, metformin and thiazolinediones. The medication is injected twice per day using a pre-filled pen device. Typical human responses to exenatide plus eating include improvements in the initial rapid release of endogenous insulin, suppression of glucagon release by the pancreas, regulation of gastric empyting and reduced appetite; all behaviors more typical of individuals without blood sugar control problems. Exenatide is self-regulating in that in lowers blood sugar when levels are elevated but does not continue to lower blood sugar when levels return to normal, unlike with sulfonylureas or insulins. |
| Mechanism of action | Exenatide is a functional analog of the human incretin Glucagon-Like Peptide-1 (GLP-1). Incretins enhance glucose-dependent insulin secretion and exhibit other antihyperglycemic actions following their release into the circulation from the gut. The GLP-1 system increases insulin secretion only in the presence of elevated plasma glucose levels, avoiding inappropriately high insulin levels during fasting. The drug also moderates peak serum glucagon levels during hyperglycemic periods following meals, but does not interfere with glucagon release in response to hypoglycemia. Secondary effects of drug administration reduces the rate of gastric emptying and decreases food intake, mitigating the potential severity of hyperglycemic events after meal |
| Following subcutaneous administration to patients with type 2 diabetes, exenatide reaches median peak plasma concentrations in 2.1 hours. |
New Drug Approvals 