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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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Sitasentan TBC 11251

March 3, 2015 4:53 am / Leave a comment

Sitasentan,TBC 11251

210421-64-0

N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide

Sitaxentan sodium (TBC-11251) is a medication for the treatment of pulmonary arterial hypertension (PAH).^[1] It was marketed as Thelin by Encysive Pharmaceuticals until Pfizer purchased Encysive in February 2008. In 2010, Pfizer voluntarily removed sitaxentan from the market due to concerns about liver toxicity.^[2]

Sitaxentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Sitaxentan blocks the binding of endothelin to its receptors, thereby negating endothelin’s deleterious effects.

Mechanism of action

Sitaxentan is a small molecule that blocks the action of endothelin (ET) on the endothelin-A (ET_A) receptor selectively (by a factor of 6000 compared to the ET_B).^[3] It is a sulfonamide class endothelin receptor antagonist (ERA) and is undergoing Food and Drug Administration (FDA) review for treating pulmonary hypertension. The rationale for benefit compared to bosentan, a nonselective ET blocker, is negligible inhibition of the beneficial effects of ET_B stimulation, such as nitric oxide production and clearance of ET from circulation. In clinical trials, the efficacy of sitaxentan has been much the same as bosentan, but the hepatotoxicity of sitaxentan outweighs its benefits. Dosing is once daily, as opposed to twice daily for bosentan.

Regulatory status

On December 10, 2010 Pfizer announced it would be withdrawing sitaxentan worldwide (both from marketing and from all clinical study use), citing that it is a cause of fatal liver damage.^[2]

Sitaxentan was approved for marketing in the European Union in 2006, in Canada in 2006^[4] and in Australia in 2007. By February 2008 it had been launched commercially in Germany, Austria, The Netherlands, the United Kingdom, Ireland, France, Spain and Italy.

In March 2006, the FDA recommended an approvable status to sitaxentan but said it would not yet approve the product. In July 2006, sitaxentan received a second approvable letter stating that efficacy outcome issues raised in the context of the STRIDE-2 study were still unresolved. In July 2007, Encysive commenced a formal dispute resolution process in a preliminary meeting with the FDA. In September 2007 the company announced that it was making preparations for another phase III clinical trial (intended to be named STRIDE-5) to overcome the FDA’s concerns.^[5] The takeover by Pfizer resulted in a reconfiguration and extension of these plans, to include combination therapy with sildenafil. The Sitaxentan Efficacy and Safety Trial With a Randomized Prospective Assessment of Adding Sildenafil (SR-PAAS) was an ongoing program of three clinical trials conducted in the United States (ClinicalTtrials.gov identifiers: NCT00795639, NCT00796666 and NCT00796510) with anticipated completion dates between June 2010 and January 2014.

N-(4-Chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonamide sodium salt, Sitaxsentan sodium salt, TBC-11251 sodium salt, Thelin

CAS Number 210421-74-2
Empirical Formula C₁₈H₁₄ClN₂NaO₆S₂
Molecular Weight 476.89

Adverse effects

Adverse effects observed with sitaxentan are class effects of endothelin receptor antagonists, and include :

liver enzyme abnormalities (increased ALT and AST)
headache
edema
constipation
nasal congestion
upper respiratory tract infection
dizziness
insomnia
flushing

Because sitaxentan inhibits metabolism of warfarin, a decreased dose of warfarin is needed when co-administered with sitaxentan. This is because warfarin acts to prevent blood from clotting, and if it remains unmetabolized, it can continue to thin the blood.

http://www.google.com/patents/WO2007149568A2?cl=en

As used herein “sitaxsentan” refers to N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2- methyl-4,5-(methylenedioxy)phenylacetyl]-thiophene-3-sulfonamide. Sitaxsentan is also known as TBCl 1251. Other chemical names for sitaxsentan include 4-chloro-3-methyl-5-(2- (2-(6-methylbenzo[d][l ,3]dioxol-5-yl)acetyl)-3-thienylsulfonamido)isoxazole and N-(4- chloro-3-methyl-5-isoxazolyl)-2-[3,4-(methylenedioxy)-6-methylphenylacetyl]-thiophene-3- sulfonamide.

The chemical name for sitaxsentan is N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2- methyl-4,5-(methylenedioxy)phenylacetyl]-thiophene-3-sulfonamide, and its structural formula is as follows:

Sitaxsentan

Sitaxsentan is a potent endothelin receptor antagonist that has oral bioavailability in several species, a long duration of action, and high specificity for ETA receptors.

EXAMPLE 1

Preparation of 4-chloro-3-methyl-5-(2-(2-(6-methylbenzo[d] [l,3|dioxol-5-yl)aeetyl)-3- thienylsulfonamido)isoxazole, or N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-methy 1-4,5- (methylenedioxy)phenylacetyl]-thiophene-3-sulfonamide, or N-(4-chIoro-3-methyl-5- isoxazolyl)-2-[3,4-(methylenedioxy)-6-methylphenylacetyl]-thiophene-3-sulfonamide.

A. Preparation of (4-chIoro-3-methyl-5-(2-(2-(6-methylbenzo[d] [l,3]dioxol-5-yl)acetyl)- 3-thienylsuIfonamido)isoxazole 1. Preparation of 5-chloromethyI-6-methylbenzo[d][l,3]dioxole

To a mixture of methylene chloride (130 L), concentrated HCl (130 L), and tetrabuylammonium bromide (1.61 Kg) was added 5-methylbenzo[d][l,3]dioxole (10 Kg) followed by the slow addition of formaldehyde (14 L, 37 wt% in water). The mixture was stirred overnight. The organic layer was separated, dried with magnesium sulfate and concentrated to an oil. Hexane (180 L) was added and the mixture heated to boiling. The hot hexane solution was decanted from a heavy oily residue and evaporated to give almost pure 5-chloromethyl-6-methylbenzo[d][l,3]dioxole as a white solid. Recrystallization from hexane (50 L) gave 5-chloromethyl-6-methylbenzo[d][l,3]dioxole (80% recovery after recrystallization). 2. Formation of (4-chloro-3-methyl-5-(2-(2-(2-methyIbenzo[d][l,3]dioxol-5-yl) acetyl)-3-thienylsulfonamido)isoxazole

A portion of a solution of 5-chloromemyl-6-methylbenzo[d][l,3]di-oxole (16.8 g, 0.09 mol) in tetrahydrofuran (THF)(120 mL) was added to a well stirred slurry of magnesium powder, (3.3 g, 0.136 g-atom, Alfa, or Johnson-Mathey, -20 +100 mesh) in THF (120 mL) at room temperature. The resulting reaction admixture was warmed up to about 40-45⁰C for about 2-3 min, causing the reaction to start. Once the heating activated the magnesium, and the reaction began, the mixture was cooled and maintained at a temperature below about 8 ⁰C. The magnesium can be activated with dibromoethane in place of heat.

A flask containing the reaction mixture was cooled and the remaining solution of 5- chloromethlybenzo[d][l,3]dioxole added dropwise during 1.5 hours while maintaining an internal temperature below 8 ⁰C. Temperature control is important: if the Grignard is generated and kept below 8 ⁰C₅ Wurtz coupling is suppressed. Longer times at higher temperatures promote the Wurtz coupling pathway. Wurtz coupling can be avoided by using high quality Mg and by keeping the temperature of the Grignard below about 8 ⁰C and stirring vigorously. The reaction works fine at -20 ⁰C, so any temperature below 8 ⁰C is acceptable at which the Grignard will form. The color of the reaction mixture turns greenish.

The reaction mixture was stirred for an additional 5 min at 0 ⁰C, while N²-methoxy- N²-methyl-3-(4-chloro-3-methyl-5-isoazolylsulfamoyl)-2-thiophenecarboxamide (6.6 g, 0.018 mol) in anhydrous THF (90 mL) was charged into the addition funnel. The reaction mixture was degassed two times then the solution of N²-methoxy-N²-methyl-3-(4-chloro-3- methyl-5-isoxazolylsulfamoyl)-2-thiophenecarboxamide was added at 0 ⁰C over 5 min. TLC of the reaction mixture (Silica, 12% MeOHZCH₂Cl₂) taken immediately after the addition shows no N²-methoxy-N²-methyl-3-(4-chloro-3-methyl-5-isoxazolysulfamoyl)-2-thio- phenecarboxamide. The reaction mixture was transferred into a flask containing IN HCl (400 mL, 0.4 mol

HCl, ice-bath stirred), and the mixture stirred for 2 to 4 min, transferred into a separatory funnel and diluted with ethyl acetate (300 mL). The layers were separated after shaking. The water layer was extracted with additional ethyl acetate (150 mL) and the combined organics washed with half-brine. Following separation, THF was removed by drying the organic layer over sodium sulfate and concentrating under reduced pressure at about 39 ⁰C to obtain the title compound. EXAMPLE 2

1.0 g Sitaxentan was dissolved in 10 ml ethyl acetate and 5 ml hexanes were added. The formed suspension was heated until a clear solution was obtained. Upon cooling light yellow plates were formed. After filtration and drying under vacuum 515 mg of sitaxentan polymorph A was obtained as light yellow plates in very high purity.

EXAMPLE 3

Preparation of 4-chloro-3-methyl-5-(2-(2-(6-methyIbenzo[dJ [l,3]dioxol-5-yl)acetyl)-3- thienylsulfonamido)isoxazole, Sodium Salt

The crystalline sitaxsentan from Example 2 is dissolved in ethyl acetate and washed with saturated NaHCO₃ (5 x 10 mL). The solution is washed with brine, dried over Na₂SO₄ and concentrated in vacuo to obtain a solid residue. 10 mL OfCH₂Cl₂ is added and the mixture is stirred under nitrogen for 5 to 10 minutes. Ether (15 mL) is added and the mixture stirred for about 10 min. The product is isolated by filtration, washed with a mixture of CH₂Cl₂ /ether (1 :2) (10 mL) then with ether (10 mL) and dried under reduced pressure to obtain 4-Chloro-3-methyl-5-(2-(2-(6-methyIbenzo[d][l ,3]dioxol-5-yl)acetyl)-3- thienylsulfonamido)isoxazole, sodium salt.

………………………..

J. Med. Chem., 1997, 40 (11), pp 1690–1697

DOI: 10.1021/jm9700068

http://pubs.acs.org/doi/suppl/10.1021/jm9700068/suppl_file/jm1690.pdf

15q.Yellowpowder;

1HNMR(CDCl3):88.88(brs,1H),7.59(s,2H),6.72(s,1H),6.69(s,111),5.94(s,2H),4.22(s,2H),2.22(s,311),2.21(s,3H);

IR(KBrpellet):3455,3233,

3109,2899,1674,1632,1505,1487,1395,1373cm-1;

HRMS:[M+H]*455.0137

………………………..

see

Current Opinion in Investigational Drugs (PharmaPress Ltd.) (2001), 2(4), 531-536.

…………….

Synthesis of Sitaxsentan sodium
Yingyong Huaxue (2007), 24, (11), 1310-1313. Publisher: (Kexue Chubanshe, ) CODEN:YIHUED ISSN:1000-0518.

………………………………………

http://www.google.co.in/patents/WO2007106494A2?cl=en

Table 1: Sitaxsentan Sodium Lyophilized Formulation

References

1Barst RJ, Langleben D, Frost A et al. (2004). “Sitaxsentan therapy for pulmonary arterial hypertension”. American Journal of Respiratory Critical Care Medicine 169 (4): 441–447. doi:10.1164/rccm.200307-957OC. PMID 14630619.

2
Citing liver damage, Pfizer withdraws Thelin, Associated Press, December 12, 2010
3
Girgis, RE; Frost, AE; Hill, NS; Horn, EM; Langleben, D; McLaughlin, VV; Oudiz, RJ; Robbins, IM et al. (2007). “Selective endothelinA receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease”. Annals of the rheumatic diseases 66 (11): 1467–72. doi:10.1136/ard.2007.069609. PMC 2111639. PMID 17472992.
4
“UPDATE 1-Encysive gets Canadian approval for hypertension drug”. Reuters. 30 May 2007. Retrieved 2007-07-08.
5

“Encysive Pharmaceuticals to Conduct Phase III Study With Thelin (Sitaxsentan Sodium) in Pulmonary Arterial Hypertension”. PrimeNewswire via COMTEX News Network. 29 September 2007. Retrieved 2007-12-12.

External links

http://www.drugs.com/nda/thelin_050714.html
Mucke HAM: Sitaxsentan for the Oral Treatment of Pulmonary Arterial Hypertension: Benefits from Endothelin Receptor Subtype Selectivity? Clinical Medicine: Therapeutics 2009:1 111–121.
ATS 2005. The International Conference of the American Thoracic Society. 20–25 May 2005. San Diego, CA.
Robyn J. Barst, MD; Stuart Rich, MD, FCCP; Allison Widlitz, MS, PA; Evelyn M. Horn, MD; Vallerie McLaughlin, MD and Joyce McFarlin, RN : Clinical Efficacy of Sitaxsentan, an Endothelin-A Receptor Antagonist, in Patients With Pulmonary Arterial Hypertension Chest. 2002;121:1860-1868.
American Heart Association. Primary or Unexplained Pulmonary Hypertension

US20010021714 *	Apr 4, 1996	Sep 13, 2001	Ming Fai Chan	Compounds such as n-(4-bromo-3-methyl-5-isoxazolyl)-2-n-benzylbenzo(b)thiophene-3-sufonamide administered as endothelin peptide receptor antagonists

Reference
1	*	WU C ET AL: “Discovery of TBC11251, a Potent, Long Acting, Orally Active Endothelin Receptor-A Selective Antagonist” JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 40, no. 11, 23 May 1997 (1997-05-23), pages 1690-1697, XP002164198 ISSN: 0022-2623

Patent	Submitted	Granted
ANTIHYPERTENSIVE THERAPY METHOD [US2007293552]	2007-12-20
Crystalline N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-methyl-4.5-(methylenedioxy)phenylacetyl]-thiophene-3-sulfonamide [US2008026061]	2008-01-31
Gnrh agonist combination drugs [US2005215528]	2005-09-29
THIENYL-, FURYL-, PYRROLYL- AND BIPHENYLSULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN [WO9631492]	1996-10-10
SULFONAMIDES FOR TREATMENT OF ENDOTHELIN-MEDIATED DISORDERS [WO9849162]	1998-11-05


Patent	Submitted	Granted
Respiratory Drug Condensation Aerosols and Methods of Making and Using Them [US2009258075]	2009-10-15
Method and Composition for Treating Alzheimer’s Disease and Dementias of Vascular Origin [US2010173872]	2010-07-08
Method and Composition for Treating Alzheimer’s Disease and Dementias of Vascular Origin [US2010184725]	2010-07-22
Formulations of sitaxsentan sodium [US2008076812]	2008-03-27
Methods and compositions for treatment of sleep apnea [US2008085313]	2008-04-10
Processes for the preparation of 4-chloro-3-methyl-5-(2-(2-(6-methylbenzo[d][1,3]dioxol-5-yl)acetyl)-3-thienylsulfonamido)isoxazole [US2008086010]	2008-04-10
Method and composition for treating alzheimer’s disease and dementias of vascular origin [US2004092427]	2004-05-13
Method for preventing or treating pulmonary inflammation by administering an endothelin antagonist [US2003004199]	2003-01-02
Methods and Compositions for Treatment of an Interstitial Lung Disease [US2009004268]	2009-01-01
Methods and compositions for treatment of diastolic heart failure [US2007232671]	2007-10-04

Patent	Submitted	Granted
Isoxazolyl endothelin antagonists [US6043265]	2000-03-28
Aminoguanidine hydrazone derivatives, process for producing the same and drugs thereof [US6350749]		2002-02-26
Method for preventing or treating pain by administering an endothelin antagonist [US6573285]	2002-06-27	2003-06-03
Method for preventing or treating erectile dysfunction by administering an endothelin antagonist [US6268388]		2001-07-31
Method and composition for potentiating the antipyretic action of a nonopioid analgesic [US7351692]	2003-12-25	2008-04-01
Method and Composition for Potentiating an Opiate Analgesic [US8114896]	2010-05-06	2012-02-14
SUBSTITUTED THIOPHENES [US7863308]	2008-10-16	2011-01-04
Respiratory drug condensation aerosols and methods of making and using them [US7550133]	2004-06-03	2009-06-23
SUBSTITUTED THIOPHENES [US2010280086]	2010-11-04
Method and Composition for Potentiating an Opiate Analgesic [US2010311665]	2010-12-09

Sitaxentan
Systematic (IUPAC) name

N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-2H-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide
Clinical data
AHFS/Drugs.com	International Drug Names
Licence data	EMA:Link
Legal status	AU: Prescription Only (S4) UK: POM
Routes	Oral
Pharmacokinetic data
Bioavailability	70 to 100%
Protein binding	>99%
Metabolism	Hepatic (CYP2C9– and CYP3A4-mediated)
Half-life	10 hours
Excretion	Renal (50 to 60%) Fecal (40 to 50%)
Identifiers
CAS number	184036-34-8 210421-64-0 (sodium salt)
ATC code	C02KX03
PubChem	CID 216235
IUPHAR ligand	3950
DrugBank	DB06268
ChemSpider	21106381
UNII	J9QH779MEM
KEGG	D07171
ChEMBL	CHEMBL282724
Synonyms	Sitaxsentan; TBC-11251
Chemical data
Formula	C₁₈H₁₅Cl N₂O₆S₂
Molecular mass	454.906 g/mol

Structures and observed activities of the ET_A receptor antagonists for the HipHop training set

COCK WILL TEACH YOU NMR

COCK SAYS MOM CAN TEACH YOU NMR

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE

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KISUMU, KENYA

Kisumu – Wikipedia, the free encyclopedia

en.wikipedia.org/wiki/Kisumu

Kisumu is a port city in Kisumu County, Kenya 1,131 m (3,711 ft), with a population of 409,928 (2009 census). It is the third largest city in Kenya, the principal city …

Kisumu County Kisumu County is one of the new devolved counties of Kenya. Its …	Kisumu International Airport Kisumu International Airport is an airport in Kisumu, Kenya (IATA …
More results from wikipedia.org »

Boat riding in Kisumu

Local inhabitants near Kisumu, 1911

Clockwise: Lake Victoria Panorama, Kisumu Panorama, sunset at Oginga Odinga street, Downtown, Kiboko Point, Nighttime in Kisumu and Jomo Kenyatta Stadium.
Kisumu
Coordinates: 0°6′S 34°45′E
Country	Kenya
County	Kisumu County

Kisumu panorama, viewed from Lake Victoria

Jomo Kenyatta Stadium

Kisumu Harbour. The green vegetation is water hyacinth

Nairobi University Kisumu Campus

Your visit to Kisumu is not complete if you do not visit this amazing beach, which happens to be a favourite spot fishing spot for the fishermen.

///////

Warner Chilcott Announces FDA Approval of New Ulcerative Colitis Product Delzicol

February 8, 2013 9:44 am / 1 Comment on Warner Chilcott Announces FDA Approval of New Ulcerative Colitis Product Delzicol

Mesalazine (INN, BAN), also known as mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammatory bowel disease, such as ulcerative colitis^[1] and mild-to-moderate Crohn’s disease.^[2] Mesalazine is a bowel-specific aminosalicylate drug that acts locally in the gut and has its predominant actions there, thereby having few systemic side effects.^[3]

As a derivative of salicylic acid, mesalazine is also thought to be an antioxidant that traps free radicals, which are potentially damaging byproducts of metabolism.^[3]

Mesalazine is considered the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.^[4]

About Delzicol

DUBLIN, Ireland, Feb. 5, 2013 — Warner Chilcott plc today announced that the United States Food and Drug Administration (FDA) has approved its new 400 mg mesalamine product indicated for the treatment of ulcerative colitis. The product will be marketed as Delzicol (mesalamine) 400 mg delayed-release capsules. The Company anticipates that it will commercially launch Delzicol in March 2013.Delzicol (mesalamine) delayed-release capsules are indicated for the treatment of mildly to moderately active ulcerative colitis and for the maintenance of remission of ulcerative colitis. For information on dosage and administration, contraindications, warnings and precautions, adverse reactions, and other important safety information, please see the prescribing information.

Warner Chilcott is a leading specialty pharmaceutical company currently focused on the women’s healthcare, gastroenterology, urology and dermatology segments of the branded pharmaceuticals market, primarily in North America. We are a fully integrated company with internal resources dedicated to the development, manufacture and promotion of our products.

Kruis, W.; Schreiber, I.; Theuer; Brandes; Schütz; Howaldt; Krakamp; Hämling et al. (2001). “Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses”. Gut 49 (6): 783–789. doi:10.1136/gut.49.6.783. PMC 1728533. PMID 11709512. edit
Sandborn WJ, Feagan BG, Lichtenstein GR (October 2007). “Medical management of mild to moderate Crohn’s disease: evidence-based treatment algorithms for induction and maintenance of remission”. Alimentary Pharmacology & Therapeutics 26 (7): 987–1003. doi:10.1111/j.1365-2036.2007.03455.x. PMID 17877506. Retrieved 2009-12-20.
“mesalazine”. PharmGKB.
Lippencott’s Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark

COCK WILL TEACH YOU NMR

COCK SAYS MOM CAN TEACH YOU NMR

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE

Join me on Linkedin

Join me on Facebook

FACEBOOK

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KISUMU, KENYA

Kisumu – Wikipedia, the free encyclopedia

en.wikipedia.org/wiki/Kisumu

Kisumu is a port city in Kisumu County, Kenya 1,131 m (3,711 ft), with a population of 409,928 (2009 census). It is the third largest city in Kenya, the principal city …

Kisumu County Kisumu County is one of the new devolved counties of Kenya. Its …	Kisumu International Airport Kisumu International Airport is an airport in Kisumu, Kenya (IATA …
More results from wikipedia.org »

Boat riding in Kisumu

Local inhabitants near Kisumu, 1911

Clockwise: Lake Victoria Panorama, Kisumu Panorama, sunset at Oginga Odinga street, Downtown, Kiboko Point, Nighttime in Kisumu and Jomo Kenyatta Stadium.
Kisumu
Coordinates: 0°6′S 34°45′E
Country	Kenya
County	Kisumu County

Kisumu panorama, viewed from Lake Victoria

Jomo Kenyatta Stadium

Kisumu Harbour. The green vegetation is water hyacinth

Nairobi University Kisumu Campus

Your visit to Kisumu is not complete if you do not visit this amazing beach, which happens to be a favourite spot fishing spot for the fishermen.

///////

BOTOX® (onabotulinumtoxinA) Receives U.S. Food and Drug Administration Approval for the Treatment of Overactive Bladder for Adults Who Have an Inadequate Response to or Are Intolerant of an Anticholinergic Medication

February 2, 2013 12:57 pm / Leave a comment

BOTOX^®(onabotulinumtoxinA) Receives U.S. Food and Drug Administration Approval for the Treatment of Overactive Bladder for Adults Who Have an Inadequate Response to or Are Intolerant of an Anticholinergic Medication

Allergan, Inc. (NYSE:AGN) announced today that the U.S. Food and Drug Administration (FDA) has approved BOTOX^® (onabotulinumtoxinA) for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency and frequency in adults who have had an inadequate response to or are intolerant of an anticholinergic medication. In two double-blind, randomized, multi-center, placebo-controlled 24-week clinical trials among adults with overactive bladder who had not been adequately managed with anticholinergic treatments, BOTOX^® reduced daily urinary incontinence (leakage) episodes as compared to placebo by 50 percent or more by week 12 (reduction of 2.5 episodes from baseline of 5.5 episodes in one study and reduction of 3 episodes from baseline of 5.5 episodes in the second study for those treated with BOTOX® vs. a reduction of 0.9 episodes from a baseline of 5.1 episodes in one study and a reduction of 1.1 episodes from a baseline of 5.7 episodes in the second study for those treated with placebo).¹

Allergan has a long-standing commitment to study the potential of BOTOX® to treat a number of different medical conditions

“Allergan has a long-standing commitment to study the potential of BOTOX® to treat a number of different medical conditions,” said Scott Whitcup, M.D., Allergan’s Executive Vice President, Research and Development, Chief Scientific Officer. “With today’s approval, BOTOX® is now approved for 26 different indications in more than 85 countries. Most importantly, today’s FDA approval is a milestone in the treatment of this burdensome condition and will provide a novel option for urologists and their OAB patients.”

While the exact cause is often unknown, OAB is a medical condition that results in an uncontrolled urge to urinate, frequent urination and, in many patients, uncontrollable leakage of urine. In the United States, an estimated 14.7 million adults experience symptoms of OAB with urinary incontinence (unexpected leakage of urine).² Anticholinergics, which are often prescribed as pills, are used by approximately 3.3 million Americans with OAB, with or without urinary incontinence, to manage their condition.³ It is estimated, however, that greater than 50 percent of these patients stop taking at least one oral medication within 12 months, likely due to an inadequate response to, or intolerance of, the medication.⁴

“Overactive bladder can be a difficult condition to treat as there have been limited options for patients when currently available medications have failed to provide them with adequate relief,” said Dr. Victor Nitti*, Vice Chairman, Department of Urology and Director of Female Pelvic Medicine and Reconstructive Surgery at NYU Langone Medical Center. “With the approval of BOTOX®, we have a new treatment option to offer these patients that has demonstrated efficacy in reducing urinary leakage and other symptoms of OAB with the effect lasting up to six months.”

The median duration for efficacy with BOTOX® at reducing urinary leakage and other symptoms of OAB in the two clinical studies was 135-168 days compared to 88-92 days with placebo based on qualification for retreatment. To qualify for retreatment, at least 12 weeks must have passed since the prior treatment, post-void residual urine volume must have been less than 200 mL and patients must have reported at least two urinary incontinence episodes over three days. BOTOX® treatment relieves OAB symptoms by temporarily calming muscle contractions by blocking the transmission of nerve impulses to the bladder muscle.

BOTOX Cosmetic (onabotulinum toxin A) For Injection, is a sterile, vacuum-dried purified botulinum toxin type A, produced from fermentation of Hall strain Clostridium botulinum type A grown in a medium containing casein hydrolysate, glucose, and yeast extract, intended for intramuscular use. It is purified from the culture solution bydialysis and a series of acid precipitations to a complex consisting of the neurotoxin, and several accessory proteins. The complex is dissolved in sterile sodium chloride solution containing Albumin Human and is sterile filtered (0.2 microns) prior to filling and vacuum-drying.

The primary release procedure for BOTOX Cosmetic uses a cell-based potency assay to determine the potency relative to a reference standard. The assay is specific to Allergan’s products BOTOX and BOTOX Cosmetic. One Unit of BOTOX Cosmetic corresponds to the calculated median intraperitoneal lethal dose (LD50) in mice. Due to specific details of this assay such as the vehicle, dilution scheme and laboratory protocols, Units of biological activity of BOTOX Cosmetic cannot be compared to nor converted into Units of any other botulinum toxin or any toxin assessed with any other specific assay method. The specific activity of BOTOX Cosmetic is approximately 20 Units/nanogram of neurotoxin protein complex.

Each vial of BOTOX Cosmetic contains either 50 Units of Clostridium botulinum type A neurotoxin complex, 0.25 mg of Albumin Human, and 0.45 mg of sodium chloride; or 100 Units of Clostridium botulinum type A neurotoxin complex, 0.5 mg of Albumin Human, and 0.9 mg of sodium chloride in a sterile, vacuum-dried form without a preservative.

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KISUMU, KENYA

Kisumu – Wikipedia, the free encyclopedia

en.wikipedia.org/wiki/Kisumu

Kisumu is a port city in Kisumu County, Kenya 1,131 m (3,711 ft), with a population of 409,928 (2009 census). It is the third largest city in Kenya, the principal city …

Kisumu County Kisumu County is one of the new devolved counties of Kenya. Its …	Kisumu International Airport Kisumu International Airport is an airport in Kisumu, Kenya (IATA …
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Boat riding in Kisumu

Local inhabitants near Kisumu, 1911

Clockwise: Lake Victoria Panorama, Kisumu Panorama, sunset at Oginga Odinga street, Downtown, Kiboko Point, Nighttime in Kisumu and Jomo Kenyatta Stadium.
Kisumu
Coordinates: 0°6′S 34°45′E
Country	Kenya
County	Kisumu County

Kisumu panorama, viewed from Lake Victoria

Jomo Kenyatta Stadium

Kisumu Harbour. The green vegetation is water hyacinth

Nairobi University Kisumu Campus

Your visit to Kisumu is not complete if you do not visit this amazing beach, which happens to be a favourite spot fishing spot for the fishermen.

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