DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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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/
…..
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.
Incivo (Telaprevir) Receives European Commission Approval for Twice Daily Dosing for Treatment of Genotype-1 Chronic Hepatitis C Virus (HCV)
TELAPREVIR
may 31, 2013
Incivo (Telaprevir) Receives European Commission Approval for Twice Daily Dosing for Treatment of Genotype-1 Chronic Hepatitis C Virus (HCV)
Janssen Infectious Diseases-Diagnostics BVBA (Janssen) announced today that the European Commission (EC) has approved a new twice daily (BID) dosing of INCIVO(R) (telaprevir), a direct acting antiviral (DAA) protease inhibitor, in combination with pegylated-interferon and ribavirin (PR) for naive and previous treatment experienced patients. The newly approved dosing regimen for INCIVO(R) is now 1,125 mg twice daily in combination with PR, which aligns a morning and evening dose to the already twice daily dosing schedule for ribavirin versus 750 mg every 8 hours in combination with PR.
Telaprevir (VX-950), marketed under the brand names Incivek and Incivo, is a pharmaceutical drug for the treatment of hepatitis C co-developed by Vertex Pharmaceuticals and Johnson & Johnson. It is a member of a class of antiviral drugsknown as protease inhibitors. Specifically, telaprevir inhibits the hepatitis C viral enzymeNS3.4A serine protease. Telaprevir is only indicated for use against hepatitis c genotype1 viral infections and hasn´t been proven to have an effect on or being safe when used for other genotypes of the virus. The standard therapy of pegylated interferon and ribavirin is less effective on genotype 1 and telaprevir offers a welcome addition to the treatment of this genotype.
PROCESS FOR MANUFACTURE OF TELMISARTAN PATENT US2013137878 (A1)30 MAY 2013
A process for preparing telmisartan by reacting 2-n-propyl-4-methyl-6-(1′-methylbenzimidazol-2′-yl)benzimidazole with a compound of formula (IV) wherein Z is a leaving group, to obtain the compound 2-cyano-4′-[2”-n-propyl-4”-methyl-6”-(1”’-methylbenzimidazol-2”’-yl)benzimidazol-1”-ylmethyl]biphenyl, and subsequently hydrolyzing the nitrile function to obtain the acid function.
Lucentis rival one step away from NHS approval
Bayer’s Eylea (aflibercept),
lucentis, novartis
http://www.pharmatimes.com/Article/13-05-31/Lucentis_rival_one_step_away_from_NHS_approval.aspx
http://www.bioportfolio.com/news/article/1484477/Lucentis-rival-one-step-away-from-NHS-approval.html
Aflibercept is a fusion protein approved in the United States for the treatment of wet macular degeneration and metastatic colorectal cancer.
It is an inhibitor of vascular endothelial growth factor.It is designed to bind to VEGF-A, VEGF-B, and placental growth factor (a.k.a PIGF, gene symbol PGF)
Aflibercept is being co-developed by Sanofi-Aventis and Regeneron Pharmaceuticals.
Ranibizumab (trade name Lucentis) is a monoclonal antibody fragment (Fab) derived from the same parent mouse antibody as bevacizumab (Avastin). It is much smaller than the parent molecule and has been affinity matured to provide stronger binding to VEGF-A. It is an anti-angiogenic that has been approved to treat the “wet” type of age-related macular degeneration (AMD, also ARMD), a common form of age-related vision loss.
Ranibizumab sells for $1,593 per dose, compared to bevacizumab, which can be prepared for macular degeneration treatment in doses that cost $42. Clinical trials have shown both to be equally effective; however there were some reports of infection after dividing bevacizumab into smaller doses.
Ranibizumab was developed by Genentech and is marketed in the United States by Genentech and elsewhere by Novartis,under the brand name Lucentis.
New Drug Approvals 