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Tag Archives: medicinal chemistry
DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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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
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
Novo Nordisk Files for Regulatory Approval of Ideglira in the EU
May 31, 2013) – Novo Nordisk today announced the submission to the European Medicines Agency of the marketing authorisation application for the approval of IDegLira, the combination product of insulin degludec (Tresiba®), the once-daily new-generation basal insulin analogue, with an ultra-long duration of action, and liraglutide (Victoza®), the once-daily human GLP-1 analogue. IDegLira has been developed for the treatment of people with type 2 diabetes.
New Drug Approvals 