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Flamel Technologies today announced that the U.S. Food and Drug Administration (FDA) has approved the company’s New Drug Application (NDA) for Bloxiverz (neostigmine methylsulfate)
Neostigmine
Flamel Technologies Announces FDA Approval of Bloxiverz
06/03/2013 — Flamel Technologies today announced that the U.S. Food and Drug Administration (FDA) has approved the company’s New Drug Application (NDA) for Bloxiverz (neostigmine methylsulfate), a drug used intravenously in the operating room for the reversal of the effects of non-depolarizing neuromuscular blocking agents after surgery. Flamel expects to launch Bloxiverz in July 2013 in 0.5 and 1.0 mg/mL strengths
Chemistry
Neostigmine, N,N,N-trimethyl-meta-(dimethylcarbomoyloxy)-phenylammonium methylsulfonate, which can be viewed as a simplified analog of physostigmine, is made by reacting 3-dimethylaminophenol with N-dimethylcarbamoyl chloride, which forms the dimethylcarbamate, and its subsequent alkylation using dimethylsulfate forming the desired compound. 
- J.A. Aeschlimann, U.S. Patent 1,905,990 (1933).
Neostigmine shows notable UV/VIS absorption at 261nm, 267nm, and 225nm.
Neostigmine’s 1H NMR Spectroscopy reveals shifts at: 7.8, 7.7, 7.4, 7.4, 3.8, and 3.1 parts per million. The higher shifts are due to the aromatic hydrogens. The lower shifts at 3.8ppm and 3.1ppm are due to the electronic withdrawing nature of the tertiary and quarterary nitrogen, respectively.
by WORLD DRUG TRACKER
DR ANTHONY CRASTO
All Yоu Nееd Tо Knоwn Abоut Hepatitis C
Thе mоѕt fearsome оf аll types оf hepatitis іѕ thе hepatitis C. Thіѕ disease, hepatitis C hаѕ bееn considered bу mаnу specialists tо bе аn epidemic. It іѕ аlѕо knоwn аѕ а silent illness, bесаuѕе уоu саn gеt hepatitis C fоr mаnу years аnd nоt еvеn knоw that. Studies hаvе аlѕо shown thаt аlmоѕt а thіrd оf chronic hepatits C patients will, аt ѕоmе point, suffer frоm symptoms thаt mау threaten thеіr lives.
Hepatitis C саn bе developed bу infection wіth thе hepatitis C virus, whісh аt fіrѕt wаѕ related tо intravenous drugs оr blood transfusions. Mаnу years аftеr thе hepatitis C affected people, іtѕ extent wаѕ knоw fоr а fact. Thаt happened whеn thе fіrѕt blood test fоr detecting thе hepatitis C virus wаѕ available. Mаnу studies hаvе shown thаt іn thе fіrѕt years оf hepatitis C, mоrе thаn а thіrd оf thе patients developed cirrhosis аnd…
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Turmeric- Nature’s Ibuprofen, But WAY Better
Turmeric (a plant often used as a spice that can be found in any grocery store) is likely the most common herbal supplement I recommend to my patients. Non steroidal anti inflammatory drugs (such as ibuprofen, advil, motrin, aleve, aspirin) are some of the most commonly used drugs, both by physicians and over the counter. However, their serious side effects are well known and feared by physicians. They are one of the leading causes of stomach and intestinal ulcers and can cause kidney failure. They are usually safe is short courses but for people with chronic pain it becomes a real problem.
Turmeric however has been used in traditional Indian (Ayurvedic) and Chinese medicine for hundreds (possibly thousands) of years for its pain relieving and anti-inflammatory qualities. A study was done in 2011 in the journal Inflammation that looked at the anti-inflammatory capability of turmeric vs ginger vs indomethacin (a…
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The New Jersey drug giant Merck announced this morning that its investigational cancer drug Pembrolizumab, lambrolizumab (MK-3475) had received the breakthrough blessing in recognition of the dramatic clinical benefits observed in an open-label, phase 1 trial involving people with advanced melanoma.
STRUCTURAL FORMULA
Heavy chain
QVQLVQSGVE VKKPGASVKV SCKASGYTFT NYYMYWVRQA PGQGLEWMGG 50
INPSNGGTNF NEKFKNRVTL TTDSSTTTAY MELKSLQFDD TAVYYCARRD 100
YRFDMGFDYW GQGTTVTVSS ASTKGPSVFP LAPCSRSTSE STAALGCLVK 150
DYFPEPVTVS WNSGALTSGV HTFPAVLQSS GLYSLSSVVT VPSSSLGTKT 200
YTCNVDHKPS NTKVDKRVES KYGPPCPPCP APEFLGGPSV FLFPPKPKDT 250
LMISRTPEVT CVVVDVSQED PEVQFNWYVD GVEVHNAKTK PREEQFNSTY 300
RVVSVLTVLH QDWLNGKEYK CKVSNKGLPS SIEKTISKAK GQPREPQVYT 350
LPPSQEEMTK NQVSLTCLVK GFYPSDIAVE WESNGQPENN YKTTPPVLDS 400
DGSFFLYSRL TVDKSRWQEG NVFSCSVMHE ALHNHYTQKS LSLSLGK 447
Light chain
EIVLTQSPAT LSLSPGERAT LSCRASKGVS TSGYSYLHWY QQKPGQAPRL 50′
LIYLASYLES GVPARFSGSG SGTDFTLTIS SLEPEDFAVY YCQHSRDLPL 100′
TFGGGTKVEI KRTVAAPSVF IFPPSDEQLK SGTASVVCLL NNFYPREAKV 150′
QWKVDNALQS GNSQESVTEQ DSKDSTYSLS STLTLSKADY EKHKVYACEV 200′
THQGLSSPVT KSFNRGEC 218′
Disulfide bridges
22-96 22”-96” 23′-92′ 23”’-92”’ 134-218′ 134”-218”’ 138′-198′ 138”’-198”’
147-203 147”-203” 226-226” 229-229” 261-321 261”-321” 367-425 367”-425”
Glycosylation sites (N)
Asn-297 Asn-297”
lambrolizumab, or MK-3475
| C6504H10004N1716O2036S46 (peptide) | |
| Mol. mass | 146.3 kDa (peptide) |
Pembrolizumab, Lambrolizumab (also known as MK-3475) is a drug in development by Merck that targets the PD-1 receptor. The drug is intended for use in treating metastatic melanoma.
http://www.ama-assn.org/resources/doc/usan/lambrolizumab.pdf structureof lambrolizumab, or MK-3475
https://download.ama-assn.org/resources/doc/usan/x-pub/pembrolizumab.pdf
Statement on a Nonproprietary Name Adopted by the USAN Council. November 27, 2013.
see above link for change in name
may 2, 2013,
An experimental drug from Merck that unleashes the body’s immune system significantly shrank tumors in 38 percent of patients with advanced melanoma, putting the company squarely in the race to bring to market one of what many experts view as the most promising class of drugs in years.
The drugs are attracting attention here at the annual meeting of the American Society of Clinical Oncology, even though they are still in the early stage of testing. Data from drugs developed by Bristol-Myers Squibb and by Roche had already been released.
The drugs work by disabling a brake that prevents the immune system from attacking cancer cells. The brake is a protein on immune system cells called programmed death 1 receptor, or PD-1.
Merck’s study, which was presented here Sunday and also published in the New England Journal of Medicine, involved 135 patients. While tumors shrank in 38 percent of the patients over all, the rate was 52 percent for patients who got the highest dose of the drug, which is called lambrolizumab, or MK-3475.
Hamid, O; Robert, C; Daud, A; Hodi, F. S.; Hwu, W. J.; Kefford, R; Wolchok, J. D.; Hersey, P; Joseph, R. W.; Weber, J. S.; Dronca, R; Gangadhar, T. C.; Patnaik, A; Zarour, H; Joshua, A. M.; Gergich, K; Elassaiss-Schaap, J; Algazi, A; Mateus, C; Boasberg, P; Tumeh, P. C.; Chmielowski, B; Ebbinghaus, S. W.; Li, X. N.; Kang, S. P.; Ribas, A (2013). “Safety and tumor responses with lambrolizumab (anti-PD-1) in melanoma”. New England Journal of Medicine 369 (2): 134–44. doi:10.1056/NEJMoa1305133. PMID 23724846
Property-based lead optimization software for chemists
Property-based lead optimization software for chemists
- Draw your compound and indicate a substituent(s) for modification
- Define the desired property profile (based on PhysChem, ADME/Tox parameters)
- Review the list of automatically selected substituent
- Generate analogs at the click of a button
Full property profiles on-the-fly; tools to review, sort and filter results; and the capability to include in-house models. Software that helps you do it ALL in one intuitive, user-friendly interface!
Watch the Movie
click here-http://www.acdlabs.com/comm/leadop/
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ASLAN’s Pan-HER Inhibitor Shows Positive Data In Gastric Cancer PhII Study
AsianScientist (Jun. 3, 2013) – ASLAN Pharmaceuticals Pte Ltd announced this week results of a Phase II clinical trial with ASLAN001, a small-molecule pan-HER inhibitor, in gastric cancer, a major public-health problem in Asia.
ASLAN001 was invented by Array BioPharma Inc and licensed to ASLAN in 2011. ASLAN001 (ARRY-543) is a novel, selective and oral HER2/EGFR inhibitor, and has previously shown clinical activity in both HER2 positive and EGFR positive tumors in US studies. READ ALL AT
Pharmathene Will Proceed With Anthrax Vaccine Test
May 31, 2013 — PharmAthene Inc. said Thursday that the Food and Drug Administration will allow it to proceed with new clinical trials of its experimental anthrax vaccine SparVax.
http://www.pharmalive.com/pharmathene-will-proceed-with-anthrax-vaccine-test
DR ANTHONY MELVIN CRASTO
ORGANIC SPECTROSCOPY
New Drug Approvals 