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loteprednol etabonate…Patent expiry this week……of October 20, 2013
loteprednol etabonate
82034-46-6 cas
Drug Patent Expiry for the week of October 20, 2013
Tradename….LOTEMAX
Applicant………Pharmos
SUSPENSION/DROPS; OPHTHALMIC, o.5%
Generic Name………loteprednol etabonate
Patent No.US 5,540,930
http://www.google.co.in/patents/US5540930
The invention provides novel compositions of matter containing water-insoluble steroid drugs suitable for therapeutic use. The invention provides stable aqueous suspensions of water-insoluble steroid drugs of particle sizes of ≦15 μm which remain in such a state so as to allow for immediate suspension, when desired, even after extended periods of settling.
| Date | Supplement No. | Action | Documents |
|---|---|---|---|
| 1998-03-09 | 000 | Approval |
| Publication number | US5540930 A |
| Publication type | Grant |
| Application number | US 08/142,743 |
| Publication date | 30 Jul 1996 |
| Filing date | 25 Oct 1993 |
| Priority date | 25 Oct 1993 |
| Fee status | Paid |
| Also published as | CA2174550A1, CA2174550C, DE69430635D1, DE69430635T2, EP0730443A1, EP0730443A4, EP0730443B1, US5747061, WO1995011669A1, Less «8 More » |
| Publication number | 08142743, 142743, US 5540930 A, US 5540930A, US-A-5540930, US5540930 A, US5540930A |
| Inventors | Doron I. Friedman, Yaacov J. Guy |
| Original Assignee | Pharmos Corporation |
| Company | |||
|---|---|---|---|
| LOTEMAX NDA (020583) | BAUSCH AND LOMB | LOTEPREDNOL ETABONATE | |
| ALREX NDA (020803) | BAUSCH AND LOMB | LOTEPREDNOL ETABONATE | |
| LOTEMAX NDA (020841) | PHARMOS | LOTEPREDNOL ETABONATE…expired | |
| ZYLET NDA (050804) | BAUSCH AND LOMB | LOTEPREDNOL ETABONATE; TOBRAMYCIN | |
| LOTEMAX NDA (200738) | BAUSCH AND LOMB | LOTEPREDNOL ETABONATE | |
| LOTEMAX NDA (202872) | BAUSCH AND LOMB | LOTEPREDNOL ETABONATE |
Loteprednol (as the ester loteprednol etabonate) is a corticosteroid used in optometry and ophthalmology. Marketed by Bausch and Lomb as Lotemax in the U.S., ocular applications for this drug include the treatment of inflammation of the eye due to allergies (according to the prescription information sheet), as well as chronic forms of keratitis (e.g.: adenoviral and Thygeson’s keratitis), vernal keratoconjunctivitis, pingueculitis, and episcleritis. The drug has little or no effect on intraocular pressure.
Druzgala, P.; Hochhaus, G.; Bodor, N.; J. Steroid Biochem. Mol. Biol. 1991, 38, 149.
http://dx.doi.org/10.1016/0960-0760(91)90120-T
- Steward, R; et al. (November 1998). “Double-masked, placebo-controlled evaluation of loteprednol etabonate 0.5% for postoperative inflammation”. J Cataract Surg 24: 1480–1489.
- Pavesio, CE; Decory, HH (2008). “Treatment of ocular inflammatory conditions with loteprednol etabonate”. Br J Ophthalmol 92 (4): 455–459. doi:10.1136/bjo.2007.132621. PMID 18245274.
GSK and Genmab seek FDA approval for ofatumumab combination therapy for CLL first-line treatment
GlaxoSmithKline (GSK) and Genmab have submitted a supplemental Biologics License Application (sBLA) to the US Food and Drug Administration (FDA) seeking the use of Arzerra (ofatumumab) in combination with an alkylator-based therapy in patients with chronic lymphocytic leukaemia (CLL) who have not received prior treatment.
READ AT
GSK and Genmab seek FDA approval for ofatumumab combination therapy for CLL first-line treatment
Iroko Pharmaceuticals Receives FDA Approval for ZORVOLEX™
Philadelphia, Pennsylvania, October 18, 2013 – Iroko Pharmaceuticals, LLC, a global specialty pharmaceutical company dedicated to advancing the science of analgesia, today announced that the U.S. Food and Drug Administration (FDA) has approved ZORVOLEX™ (diclofenac) capsules, a nonsteroidal anti-inflammatory drug (NSAID), for the treatment of mild to moderate acute pain in adults[i]. ZORVOLEX was approved at dosage strengths that are 20 percent lower than currently available diclofenac products. FDA approval of ZORVOLEX was supported by data from a Phase 3 multi-center, randomized study in which patients treated with ZORVOLEX reported significant pain relief compared with patients receiving placebo
Antifungal drugs-Antibiotics
Antifungal drugs-Antibiotics
by Parasuraman S, Senior Lecturer at AIMST University, Malaysia on Oct 20, 2013
Health Canada approves Levemir® FlexTouch® prefilled insulin pen for the treatment of type 1 and type 2 diabetes
MISSISSAUGA, ON, Oct. 18, 2013 /CNW/ – Novo Nordisk today announced that Health Canada has approved Levemir® FlexTouch®, a disposable prefilled insulin pen containing Levemir® (insulin detemir). Levemir® FlexTouch® has been designed to improve ease of use for insulin administration and to help decrease barriers to good treatment adherence for Canadians living with type 1 and type 2 diabetes mellitus (diabetes).
The approval was also announced at the 2013 Vascular Conference in Montreal, Quebec.
Health Canada approves Levemir® FlexTouch® prefilled insulin pen for the treatment of type 1 and type 2 diabetes
http://www.pharmalive.com/health-canada-approves-levemir-flextouch
Actelion wins crucial FDA approval for next-gen lung disease drug Opsumit
MACITENTAN
N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N’-propylsulfamide, CAS NO 441798-33-0
Late on Friday the FDA came through with an approval for Actelion’s pulmonary arterial hypertension (PAH) drug Opsumit (macitentan), its next-gen successor to the franchise drug Tracleer.
Read more: Actelion wins crucial FDA approval for next-gen lung disease drug Opsumit – FierceBiotech http://www.fiercebiotech.com/story/actelion-wins-crucial-fda-approval-next-gen-lung-disease-drug-opsumit/2013-10-18#ixzz2i7tDhpZT
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Macitentan (Opsumit® )is a novel dual endothelin receptor antagonist that resulted from a tailored drug discovery process. Macitentan has a number of potentially key beneficial characteristics – i.e., increased in vivo preclinical efficacy vs. existing ERAs resulting from sustained receptor binding and tissue penetration properties. A clinical pharmacology program indicated a low propensity of macitentan for drug-drug interactions.
Macitentan is an investigational drug being studied for the treatment of pulmonary arterial hypertension. It acts as a dualendothelin receptor antagonist and is being developed by Actelion.[1] A Phase III clinical trial was successfully completed in 2012.[2]
on 22 October 2012 – Actelion (SIX: ATLN) announced that it has submitted a New Drug Application (NDA) to the US Food and Drug Administration (FDA) seeking approval for macitentan (Opsumit®) for the treatment of patients with pulmonary arterial hypertension
Actelion’s experimental lung drug macitentan prolonged overall survival by more than a third according to detailed study data, which the company hopes will convince investors it has a viable follow-up product to secure its commercial future.
Europe’s largest standalone biotech company wants the drug, which treats pulmonary arterial hypertension — a disease that causes high blood pressure in the arteries of the lungs — to replace blockbuster Tracleer.
Tracleer currently makes up 87 percent of sales but loses patent protection in 2015 and has also seen its market share eroded by Gilead’s Letairis.
Pharmacokinetics
Macitentan has an active metabolite, ACT-132577, which is an oxidative depropylation product. Both macitentan and ACT-132577 are mainly excreted in form of hydrolysis products via urine (about 2/3 of all metabolites) and faeces (1/3).[3]
Co-administration of ciclosporin has only a slight effect on the concentrations of macitentan and its active metabolite, whilerifampicin decreases the area under the curve (AUC) of the drug’s blood plasma concentration by 79%, and ketoconazoleapproximately doubles it. This corresponds to the finding that macitentan is mainly metabolised via the liver enzyme CYP3A4.[4]
- ^ Bolli, M. H.; Boss, C.; Binkert, C.; Buchmann, S.; Bur, D.; Hess, P.; Iglarz, M.; Meyer, S.; Rein, J.; Rey, M.; Treiber, A.; Clozel, M.; Fischli, W.; Weller, T. (2012). “The Discovery of N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist”. Journal of Medicinal Chemistry 55 (17): 7849–7861. doi:10.1021/jm3009103. PMID 22862294. edit
- ^ “Macitentan”. Actelion. Retrieved 22 August 2012.
- ^ Bruderer, S.; Hopfgartner, G. R.; Seiberling, M.; Wank, J.; Sidharta, P. N.; Treiber, A.; Dingemanse, J. (2012). “Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans”. Xenobiotica 42 (9): 901–910.doi:10.3109/00498254.2012.664665. PMID 22458347. edit
- ^ Bruderer, S.; Äänismaa, P. I.; Homery, M. C.; Häusler, S.; Landskroner, K.; Sidharta, P. N.; Treiber, A.; Dingemanse, J. (2011).“Effect of Cyclosporine and Rifampin on the Pharmacokinetics of Macitentan, a Tissue-Targeting Dual Endothelin Receptor Antagonist”. The AAPS Journal 14 (1): 68–78. doi:10.1208/s12248-011-9316-3. PMC 3282010. PMID 22189899. edit
External links
Actelion Ltd
Actelion Ltd is a biopharmaceutical company with its corporate headquarters in Allschwil/Basel, Switzerland. Actelion’s first drug Tracleer®, an orally available dual endothelin receptor antagonist, has been approved as a therapy for pulmonary arterial hypertension. Actelion markets Tracleer through its own subsidiaries in key markets worldwide, including the United States (based in South San Francisco), the European Union, Japan, Canada, Australia and Switzerland. Actelion, founded in late 1997, is a leading player in innovative science related to the endothelium – the single layer of cells separating every blood vessel from the blood stream. Actelion’s over 2,400 employees focus on the discovery, development and marketing of innovative drugs for significant unmet medical needs. Actelion shares are traded on the SIX Swiss Exchange (ticker symbol: ATLN) as part of the Swiss blue-chip index SMI (Swiss Market Index SMI®).
Characterization of the “hygroscopic” properties of active pharmaceutical ingredients
Characterization of the “hygroscopic” properties of active pharmaceutical ingredients.
Source
SSCI, Inc., West Lafayette, IN, USA. ann.newman@aptuit.com
http://www.ncbi.nlm.nih.gov/pubmed/17630643
Abstract
The amount of water vapor taken up by an active pharmaceutical ingredient (API) as a function of relative humidity is routinely evaluated to characterize and monitor its “hygroscopicity” throughout the drug development process. In this minireview we address the necessity of going beyond the measurement of water vapor sorption isotherms to establish the various mechanisms by which solids interact with water and the important role played by the crystalline or amorphous form of the solid. Practical approaches for choosing experimental conditions under which water vapor sorption should be measured, including the pre-treatment of samples and the time allowed to reach an equilibrium state are presented. With the assistance of a flowchart, we provide a basis for the systematic examination of samples to establish the likely mechanisms of sorption and the indicators pointing toward future problems with physical and chemical instabilities. Finally, we present strategies for managing materials that might be susceptible to the detrimental effects of water vapor sorption.
(Copyright) 2008 Wiley-Liss, Inc.
DR ANTHONY MELVIN CRASTO
ORGANIC SPECTROSCOPY
New Drug Approvals 