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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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GRAVIOLA TREE “10000 TIMES STRONGER KILLER OF CANCER THAN CHEMO” – FACTS ANALYSIS
“10000 times stronger killer of Cancer than Chemo”.. do share it.. can save many lives, fill up hopes and build confidence in the patients…
The Sour Sop or the fruit from the graviola tree is a miraculous natural cancer cell killer 10,000 times stronger than Chemo. Why are we not aware of this?
read all at
http://www.hoaxorfact.com/Health/graviola-tree-10000-times-stronger-killer-of-cancer-than-chemo.html
Dulaglutide Shows Superiority in Phase 3 Trials
DULAGLUTIDE
STRUCTURAL FORMULA
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′
http://www.ama-assn.org/resources/doc/usan/dulaglutide.pdf
7-37-Glucagon-like peptide I [8-glycine,22-glutamic acid,36-glycine] (synthetic
human) fusion protein with peptide (synthetic 16-amino acid linker) fusion protein with
immunoglobulin G4 (synthetic human Fc fragment), dimer
Eli Lilly and Co. announced detailed safety and efficacy results from three Phase 3 AWARD trials for dulaglutide, an investigational, long-acting glucagon-like peptide 1 (GLP-1) receptor agonist being studied as a once-weekly treatment for type 2 diabetes
Astellas’ Xtandi approved in EU for prostate cancer
enzalutamide
XTANDI
Regulators in European have given the green light to Astellas Pharma and Medivation’s oral prostate cancer drug Xtandi.
Specifically, the European Commission has approved Xtandi (enzalutamide) capsules for the treatment of men with metastatic castration-resistant prostate cancer whose disease has progressed on or after docetaxel therapy. The thumbs-up comes a couple of months after the European Medicines Agency’s Committee for Human Medicinal Productsissued a positive recommendation on the treatment….. READ ALL AT
http://www.pharmatimes.com/Article/13-06-24/Astellas_Xtandi_approved_in_EU_for_prostate_cancer.aspx
Enzalutamide (marketed as Xtandi and formerly known as MDV3100) is an androgen receptor antagonist drug developed by the pharmaceutical company Medivation for the treatment of metastatic castration-resistant prostate cancer. Medivation has reported up to an 89% decrease in prostate specific antigen serum levels after a month of taking the medicine. Early preclinical studies also suggest that enzalutamide inhibits breast cancer cell growth. In August of 2012, the U.S. Food and Drug Administrationapproved enzalutamide for the treatment of castration-resistant prostate cancer.
Enzalutamide was discovered by Charles Sawyers who is now at Memorial Sloan–Kettering Cancer Center and Michael Jung at UCLA.
A model of the interaction between the prostate cancer drug enzalutamide and the androgen receptor
FDA Approves Pediatric Indication for Astellas’ Mycamine (micafungin sodium) for Injection
micafungin sodium
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C56-H70-N9-O23-S.Na1292.265Fujisawa (Originator), Merck & Co. (Codevelopment)
Antifungal Agents, ANTIINFECTIVE THERAPY, 1,3-beta-Glucan Synthase Inhibitors, EchinocandinsLaunched-2002
{5-[(1S,2S)-2-[(3S,6S,9S,11R,15S,18S,20R,21R,24S,25S,26S)-3-[(1R)-2-carbamoyl-1-hydroxyethyl]-11,20,21,25-tetrahydroxy-15-[(1R)-1-hydroxyethyl]-26-methyl-2,5,8,14,17,23-hexaoxo-18-[(4-{5-[4-(pentyloxy)phenyl]-1,2-oxazol-3-yl}benzene)amido]-1,4,7,13,16,22-hexaazatricyclo[22.3.0.09,13]heptacosan-6-yl]-1,2-dihydroxyethyl]-2-hydroxyphenyl}oxidanesulfonic acid
June 24, 2013 , Astellas Pharma US, Inc. (“Astellas”), a U.S. subsidiary of Tokyo-based Astellas Pharma Inc. (Tokyo: 4503), announced that the U.S. Food and Drug Administration (FDA) has approved its Supplemental New Drug Application (sNDA) for the use of MYCAMINE® (micafungin sodium) for injection by intravenous infusion for the treatment of pediatric patients four months and older with candidemia, acute disseminated candidiasis, Candida peritonitis and abscesses, esophageal candidiasis, and prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplants (HSCT).
Micafungin (trade name Mycamine) is an echinocandin antifungal drug developed by Astellas Pharma. It inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls. Micafungin is administered intravenously. It received final approval from the U.S. Food and Drug Administration on March 16, 2005, and gained approval in the European Union on April 25, 2008.
Micafungin is indicated for the treatment of candidemia, acute disseminated candidiasis, Candida peritonitis, abscesses and esophageal candidiasis. Since January 23, 2008, micafungin has been approved for the prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplantation (HSCT).
Micafungin works by way of concentration-dependent inhibition of 1,3-beta-D-glucan synthase resulting in reduced formation of 1,3-beta-D-glucan, which is an essential polysaccharide comprising one-third of the majority of Candida spp. cell walls. This decreased glucan production leads to osmotic instability and thus cellular lysis
- Micafungin sodium, FK-463, Mycamine, Funguard,208538-73-2
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The synthesis of FK-463 can be performed as follows: The enzymatic deacylation of FR-901379 with Streptomyces anulatas No. 4811, S. anulatas No. 8703, Streptomyces strain No. 6907 or A. utahensis IFO13244 gives the deacylated lipopeptide FR-179642 (1), which is then reacylated with 1-[4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoyl]benzotriazole 3-oxide (VI) by means of dimethylaminopyridine (DMAP) in DMF. The acylating compound (VI) can be obtained as follows: The cyclization of 4-pentyloxyphenylacetylene (I) with 4-(hydroxyiminomethyl)benzoic acid methyl ester (II) by means of triethylamine in hot THF gives 4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoic acid methyl ester (III), which is hydrolyzed with NaOH in hot THF/water yielding the corresponding free acid (IV). Finally, this compound is condensed with 1-hydroxybenzotriazole (V) by means of 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide (EDMCA) in dichloromethane.Fromtling, R.A.; Castr, Drugs Fut 1998, 23, 12, 1273The synthesis of FK-463 can be performed as follows: The enzymatic deacylation of FR-901379 with Streptomyces anulatas No. 4811, S. anulatas No. 8703, Streptomyces strain No. 6907 or A. utahensis IFO13244 gives the deacylated lipopeptide FR-179642 (1), which is then reacylated with 1-[4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoyl]benzotriazole 3-oxide (VI) by means of dimethylaminopyridine (DMAP) in DMF. The acylating compound (VI) can be obtained as follows: The cyclization of 4-pentyloxyphenylacetylene (I) with 4-(hydroxyiminomethyl)benzoic acid methyl ester (II) by means of triethylamine in hot THF gives 4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoic acid methyl ester (III), which is hydrolyzed with NaOH in hot THF/water yielding the corresponding free acid (IV). Finally, this compound is condensed with 1-hydroxybenzotriazole (V) by means of 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide (EDMCD) in dichloromethane.
- 38th Intersci Conf Antimicrob Agents Chemother (Sept 24 1998, San Diego)1998,:Abst F-145
Novartis First-Generation Lung Cancer Drug Tweaked To Reduce Potential Side Effects
Sponge molecules isolated and synthesized for drug trials
By scouring the oceans for disease-fighting molecules, researchers have identified two new anticancer compounds. Isolated from a sea sponge, the compounds represent a new class of the natural products called polyketides, many of which have biological activity. Because it’s not possible to extract sufficient amounts of the molecules from the sponges, the researchers also devised chemical syntheses that allowed them to make enough material to initiate clinical trials on one of the substances,
Cancer Fighters From The Sea
Natural Products: Sponge molecules isolated and synthesized for drug trials.
read all at
Supervision of Chinese-Made Drug Substances by Philippe André
Why source drug substances from China?
Large markets, economies of scale and cheaper labor;An industrial ecosystem supplying raw materials and equipment;Developed infrastructure and industry friendly policies;About 5,000 manufacturers;
Thousands of chemists and students across China looking for novel synthesis routes for generic drug substances and intermediates.
read all at
http://www.allfordrugs.com/2013/06/21/supervision-of-chinese-made-drug-substances-by-philippe-andre/
Vivus has presented data on its already-approved but not-yet-marketed erectile dysfunction drug Stendra which shows that the treatment is effective for sexual activity within 15 minutes.
Stendra (avanafil) was given the green light by the US Food and Drug Administration over a year ago, but there has been no launch yet as Vivus has been seeking a partner. The latest data should be attractive to potential suitors and could help Stendra take on other phosphodiesterase type 5 (PDE5) inhibitors, notably Pfizer’s Viagra (sildenafil) but also Eli Lilly’s Cialis (tadalafil) and Bayer’s Levitra (vardenafil).
read all at
http://www.pharmatimes.com/Article/13-06-20/Vivus_ED_drug_gets_to_work_in_less_than_15_mins.aspx
Avanafil can be synthesized from a benzylamine derivative and a pyrimidine derivative:Yamada, K.; Matsuki, K.; Omori, K.; Kikkawa, K.; 2004, U.S. Patent 6,797,709
- A cutting that phenanthrene by a methylthio urea ( a ) and ethoxy methylene malonate ( 2 ) cyclization of 3 , chloride, phosphorus oxychloride get 4 , 4 with benzyl amine 5 occurred SNAr the reaction product after oxidation with mCPBA 6 . In pyrimidine, if the 2 – and 4 – positions are active simultaneously the same leaving group in the case, SNAr reaction occurs preferentially at 4 – position, but does not guarantee the 2 – side reaction does not occur. Here is an activity of the poor leaving group sulfide spans 2 – bit, and a good leaving group active chlorine occupy four – position, thus ensuring a high regioselectivity of the reaction. 4 – position after completion of the reaction, then the 2 – position of the group activation, where sulfide sulfoxide better than the leaving group. Amino alcohols 7 and 6 recurrence SNAr reaction 8 , 8 after alkaline hydrolysis and acid alpha amidation get that phenanthrene.
HPV Vaccine Halves Infection Rate in Teen Girls
A vaccine against a cervical cancer virus has cut infections in teen girls by half, according to a study released.
read all at
A vaccine against a cervical cancer virus has cut infections in teen girls by half, according to a study released. The study confirms research done before the HPV vaccine came on the market in 2006. But this is the first evidence of how well it works now that it is in general use.
Amgen In Focus
Amgen In Focus
Seeking Alpha
According to Amgen, they have 45 drugs in development from Phase 1 to Phase 3. Conversely, Gilead has 32 drugs in development and Pfizer has 64. Meanwhile, Gilead only has 8 drugs in Phase 3, Pfizer has 25, and Amgen has 14. 7 of those Phase 3 …
http://seekingalpha.com/article/1510002-amgen-in-focus?source=google_news
Amgen has the second deepest pipeline of drugs of the three large cap biotechs. According to Amgen, they have 45 drugs in development from Phase 1 to Phase 3. Conversely, Gilead has 32 drugs in development and Pfizer has 64. Meanwhile, Gilead only has 8 drugs in Phase 3, Pfizer has 25, and Amgen has 14. 7 of those Phase 3 drugs are focused on cancer treatments for Amgen, more than either Pfizer or Gilead. Keep in mind that 12.4 million people learn they have cancer each year, while 7.6 million people lose that battle each year. The CDC predicts that the global number of cancer related deaths will increase by 80% by 2030. It doesn’t take a rocket scientist to know that cancer treating drugs presents the largest opportunity for any drug maker considering those statistics. Amgen has the inside track versus Gilead and Pfizer as far as quantity of drugs in late stage development.
Modality
New Drug Approvals 