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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Drug to ‘cure’ cravings-compound found in the bark of an African bush may hold clues to the development of drugs for reversing a host of addictive behaviours from drug
(–)-18-Methoxycoronaridine (18-MC)
A compound found in the bark of an African bush may hold clues to the development of drugs for reversing a host of addictive behaviours from drug and alcohol abuse and even smoking and compulsive over-eating, scientists reported at the BIO convention in Chicago, US, in April 2013.
read all at
http://www.soci.org/Chemistry-and-Industry/CnI-Data/2013/5/Drug-to-cure-cravings
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(–)-18-Methoxycoronaridine (18-MC) is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont. In animal studies it has proved to be effective at reducing self-administration of morphine, cocaine, methamphetamine, nicotine and sucrose. 18-MC is a selective α3β4 nicotinic antagonist and, in contrast to ibogaine, has no affinity at the α4β2 subtype nor at NMDA-channels nor at the serotonin transporter, and has significantly reduced affinity for sodium channels and for the σ receptor, but retains modest affinity for the μ and κ opioid receptors. The sites of action in the brain include the medial habenula, interpeduncular nucleus, dorsolateral tegmentum and basolateral amygdala. It has also been shown to produce anorectic effects in obese rats, most likely due to the same actions on the reward system which underlie its anti-addictive effects against drug addiction.
18-MC has not yet been tested in humans. In 2002 the research team started trying to raise funds for human trials, but were unable to secure the estimated $5 million needed. Efforts to raise funds for future trials are still ongoing. In January 2010, Obiter Research, a chemical manufacturer in Champaign, Illinois, signed a patent license with Albany Medical College and the University of Vermont allowing them the right to synthesize and market 18-MC and other congeners.
A number of derivatives of 18-MC have also been developed, with several of them being superior to 18-MC itself, the methoxyethyl congener ME-18-MC being more potent than 18-MC but with similar efficacy, and the methylamino analogue 18-MAC being more effective than 18-MC but with around the same potency. These compounds were also found to act as selective α3β4 nicotinic acetylcholine antagonists, with little or no effect on NMDA receptors.
BY WORLD DRUG TRACKER
Impotence: When You Can’t Get It Up is Getting You Down
Probably nothing devastates a man more than having a failure in the bedroom. Impotence or erectile dysfunction affects nearly 33 million men in the United States. You are not alone. Help is available for nearly every man who has erectile dysfunction.
Diet
According to the Urology Channel’s “Erectile Dysfunction: Natural/Alternative Treatments,” erectile dysfunction can be treated by eating right, drinking plenty of water and avoiding sugar, dairy and caffeine. They recommend to eat whole, fresh, unrefined and unprocessed foods, including vegetables, whole grains, soy, beans, seeds, nuts, olive oil and cold-water fish such as salmon and tuna.
Taking your vitamins can also help; the Urology Channel suggests supplements such as flaxseed, and in particular vitamins C, E and the mineral zinc. These vitamins and supplements help bolster the vascular system, which is an important part of good sexual health.
Exercise
Since sexual health relies on the vascular system, a strong heart…
View original post 638 more words
Drug development can be a gas
Pharmaceutical and biotech industries are heavily dependent on gas mixtures to grow biological cultures
The pharmaceutical and biotech industries rely heavily on industrial gases for applications such as supercritical fluid chromatgraphy and lyophilisation. Gas supply systems theefore need to offer high purity and traceability through the supply chain
http://www.manufacturingchemist.com/technical/article_page/Drug_development_can_be_a_gas/87137
Novartis Japan Achieves Primary Endpoint In HER2 Positive Advanced Breast Cancer Phase III Afinitor Trials
Everolimus
Novartis announced it achieved its primary endpoint of significantly extending progression-free survival with Afinitor (everolimus) in Phase III trials of patients with HER2 positive advanced breast cancer.
read all at
Everolimus (RAD-001) is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an inhibitor of mammalian target of rapamycin (mTOR).
It is currently used as an immunosuppressant to prevent rejection of organ transplants and treatment of renal cell cancer and other tumours. Much research has also been conducted on everolimus and other mTOR inhibitors for use in a number of cancers.
It is marketed by Novartis under the tradenames Zortress (USA) and Certican (Europe and other countries) in transplantation medicine, and Afinitor in oncology.
GSK’s Votrient meets primary objective in Phase III ovarian cancer trial
pazopanib
GlaxoSmithKline’s (GSK) Votrient (pazopanib) has met the primary objective of a statistically significant improvement in the time to disease progression or death that is the progression-free survival (PFS) against placebo in Phase III ovarian cancer..
Pazopanib (trade name Votrient) is a potent and selective multi-targeted receptortyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis. It has been approved for renal cell carcinoma and soft tissue sarcoma by the U.S. Food and Drug Administration.Pazopanib may also be active in ovarian cancer Pazopanib also appears effective in the treatment of non-small cell lung carcinoma.
New Drug Target Identified For Treating Deadly Form Of Leukemia
A research team in Singapore has identified a promising drug target for the treatment of patients with terminal-stage chronic myeloid leukemia (CML).
AsianScientist (Jun. 4, 2013) – A research team in Singapore has identified ways to inhibit the function of a key protein linked to stem cell-like behavior in terminal-stage chronic myeloid leukemia (CML). The discovery makes it possible to develop drugs that may extend the survival of patients suffering from this deadly form of leukemia.read all this at
http://www.asianscientist.com/in-the-lab/new-drug-target-deadly-form-leukemia-2013/
New Rule on Importing Active Pharmaceutical Ingredients (API) to the EU
READ ALL AT
http://ec.europa.eu/health/files/documents/active_pharmaceutical_
by WORLD DRUG TRACKER
DR ANTHONY CRASTO
New Drug Ganetespib May Help Fight Certain Advanced Lung Cancers
ganetespib
STA 9090, cas no 888216-25-9
read all at
http://www.drugs.com/news/new-may-help-fight-certain-advanced-lung-cancers-44819.html
by
WORLD DRUG TRACKER
DR ANTHONY CRATO
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
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
