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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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New late-stage data on Boehringer Ingelheim’s lung cancer drug nintedanib and its benefit to overall survival in some patients has caused a stir at the American Society of Clinical Oncology meeting in Chicago.
nintedanib
The German drugmaker presented results from the LUME-Lung 1 Phase III trial looking at the addition of nintedanib, to docetaxel as a second-line treatment in patients with advanced non-small cell lung cancer (NSCLC) compared to chemotherapy alone.
New late-stage data on Boehringer Ingelheim’s lung cancer drug nintedanib and its benefit to overall survival in some patients has caused a stir at the American Society of Clinical Oncology meeting inChicago.
read all at
http://www.pharmatimes.com/Article/13-06-04/Boehringer_NSCLC_drug_impresses_at_ASCO.aspx
Nintedanib (also known as BIBF 1120 and Vargatef) is a small molecule inhibitor of vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptor (PDGFR) being developed by Boehringer Ingelheim for use as an anti-vascular anti-cancer agent.
Tesaro and the European Network of Gynecological Oncological Trial Groups Forge Partnership to Develop Niraparib for Ovarian Cancer
Niraparib; MK 4827
MOLECULAR FORMULA C19H20N4O
MOLECULAR WEIGHT 320.4
SPONSOR Merck Sharp & Dohme Corp.
CAS REGISTRY NUMBER 1038915-60-4
THERAPEUTIC CLAIM Antineoplastic
CHEMICAL NAMES
1. 2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-
2. 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide
TESARO and the European Network of Gynecological Oncological Trial Groups (ENGOT) Forge Partnership to Develop Niraparib for Ovarian Cancer
June 3, 2013 — TESARO, Inc. an oncology-focused biopharmaceutical company, and the European Network of Gynecological Oncological Trial Groups (ENGOT), a network of national and regional clinical trial organizations, today announced a partnership for the Phase 3 clinical development of niraparib, an orally active, potent poly (ADP-ribose) polymerase (PARP) inhibitor. READ ALL AT http://www.pharmalive.com/tesaro-and-the-european-network-of-gynecological-oncological-trial-groups-forge-partnership-to
http://www.ama-assn.org/resources/doc/usan/niraparib.pdf
http://clinicaltrials.gov/show/NCT01847274
MK-4827:
MK-4827 is a potent, Selective, PARP 1/2 inhibitor with IC50 of 3.8 and 2.1 nM for PARP1 and 2, respectively. MK-4827 possesses potential Antineoplastic Activity. In a Whole Cell assay, MK -4827 prevented PARP activity with an EC50 of 4 nM, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. MK-4827 induces selective synthetic lethality in homologous recombination (HR) repair deficient tumors with BRCA1 / 2 loss and tumor cell lines with non-BRCA-related HR defects, supporting clinical utility in sporadic tumors. MK-4827 reveals good pharmacokinetic properties and is currently in phase I clin. trials. The phase I clinical trials for MK-4827 is ongoing in the treatment of solid tumors.
BY WORLD DRUG TRACKER
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…
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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.
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