DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Zalicus Granted Composition-of-Matter Patent for Z944
Z944 R1=F, R2=Cl
http://courses.washington.edu/phcol512/data/Tringham.pdf
disclaimer-The above link was available on the web freely, email me immediately amcrasto@gmail.com or call India +91 9323115463
Research Article
EPILEPSY
T-Type Calcium Channel Blockers That Attenuate Thalamic Burst Firing and Suppress Absence Seizures
- Elizabeth Tringham, et AL
Sci Transl Med 15 February 2012 4:121ra19. DOI:10.1126/scitranslmed.3003120
…T-type calcium channel blockers, termed Z941 and Z944, were identified
Key Patent Provides Broad Coverage for Z944 through April 2029
CAMBRIDGE, Mass.Feb 20, 2013 – Zalicus Inc. , a biopharmaceutical company that discovers and develops novel treatments for patients suffering from pain, today announced that it has been granted a patent by the U.S. Patent and Trademark office (USPTO) covering its product candidate Z944. United States patent number 8,377,968 entitled “N-Piperidinyl Acetamide Derivatives as Calcium Channel Blockers” provides broad coverage for Z944 including compositions of matter and certain therapeutic methods of use through April 2029. Z944 is a novel, oral, T-type calcium channel blocker which has demonstrated efficacy in a number of preclinical inflammatory pain models and other disease models. Z944 completed Phase 1 single and multiple ascending dose clinical studies in late 2012 and the Company plans to continue further clinical development with Z944 during 2013.
“This key patent provides the foundation of a solid and enforceable intellectual property estate for Z944, with issued claims through April 2029,” commented Mark H.N. Corrigan, MD, President and CEO of Zalicus. “Based on our preclinical and early-stage clinical work, we are excited to further explore the potential of Z944 as a novel, oral, non-opioid pain treatment.”
Absence seizures — which are a common type of seizure in children with genetic generalized epilepsy — could now be treated by a potential new class of drugs with enhanced selectivity and efficacy over the drugs that are currently used in the clinic.
The molecular mechanisms underlying absence seizures are unclear; nevertheless, current literature indicates that the low-voltage-activated Cav3.1 and Cav3.2 T-type calcium channels have a crucial role. T-type calcium channels are also thought to be the site of action of the first-line drug ethosuximide; however, as it is nonspecific, ethosuximide causes side effects such as drowsiness, and not all patients respond to treatment. Therefore, the authors sought to identify a more specific and potent T-type calcium channel blocker.
A rational drug design approach produced two candidates — Z941 and Z944 — that had suitable properties for further development. They both had nanomolar affinities for Cav3.2 channels and significantly improved potencies compared to ethosuximide and valproate (another drug used for treating absence seizures). Importantly, Z944 has a higher affinity for the inactivated state of T-type channels (the state that is predominant during seizure activity) than for the closed state, and a higher affinity for neuronal T-type channels than for the cardiovascular-related channels.
ONO Pharmaceutcal files for approval of Additional Indication for Onoact® 50 injection, Short-Acting Selective β1 Blocker in Japan
disease. AF/AFL with LV dysfunction accompanying by persistent elevated heart rate would lead to further deterioration of cardiac performance. Swift rate control is inevitable to be restored from this detrimental condition, however, no drug on market can provide both the features of fast-acting and easy titratability for tachyarrhythmia (AF/AFL) with LV dysfunction.
Onoact® 50 for injection is the short-acting selective β1 blocker which reduces heart rate by selectively blocking β1 receptors located chiefly in the heart and this fast-acting drug can be easily titrated.
We expect that Onoact® 50 for injection can contribute to promptly reducing heart rate without causing deterioration of cardiac performance in treatment of tachyarrhythmia (AF/AFL) with LV dysfunction.
This short-acting selective β1 blocker drug is discovered and developed by ONO and has been widely used by many patients since its launch. The drug has firstly received approval for emergency treatment of intra-operative tachyarrhythmia (atrial fibrillation and flutter, and sinus tachycardia) in July 2002. Then, it had also been approved for additional indication of emergency treatment of post-operative tachyarrhythmia (atrial fibrillation and flutter, and sinus tachycardia) with monitoring of circulatory dynamics in October 2006.
| Identifiers | |
|---|---|
| CAS number | 133242-30-5 |
| Chemical data | |
| Formula | C25H39N3O8 |
| Mol. mass | 509.59 g/mol |
Landiolol (INN) is a drug which acts as a highly cardioselective, ultra short-acting beta blocker. It is used as an anti-arrhythmic agent.
- Yoshiya I (December 1998). “[Landiolol hydrochloride, a new sympathetic beta blocker]” (in Japanese). Masui 47 Suppl: S126–32. PMID 9921175.
- Ogata J, Okamoto T, Minami K (2003). “Landiolol for the treatment of tachyarrhythmia associated with atrial fibrillation”. Can J Anaesth 50 (7): 753. doi:10.1007/BF03018726. PMID 12944459
FDA Approves Natrelle 410 Breast Implant
Silicone gel-filled breast implants
Image/FDA
Feb. 20, 2013
The U.S. Food and Drug Administration (FDA) approved Allergan’s new silicone gel-filled breast implant today, making it the fourth FDA-approved silicone gel-filled breast implant product available in the U.S, according to an FDA news release Feb. 20.
The product, the Natrelle 410 Highly Cohesive Anatomically Shaped Silicone-Gel Filled Breast Implant, can be used increase breast size (augmentation) in women at least 22 years old and to rebuild breast tissue (reconstruction) in women of any age.
According to the FDA, the approval is based on seven years of data from 941 women. Most complications and outcomes reflect those found in previous breast implant studies including tightening of the area around the implant (capsular contracture), re-operation, implant removal, an uneven appearance (asymmetry), and infection.
It’s important to remember that breast implants are not lifetime devices. Women should fully understand the risks associated with breast implants before considering augmentation or reconstruction surgery, and they should recognize that long-term monitoring is essential,” said Jeffrey Shuren, M.D., director of the FDA’s Center for Devices and Radiological Health.
“The data we reviewed showed a reasonable assurance of safety and effectiveness,” said Shuren.
The FDA requires that Allergan conduct a series of post-approval studies to assess long-term safety and effectiveness outcomes and the risks of rare disease.
Edison commences EPI-743 Vatiquinone Phase 2 study in cobalamin C deficient patients
19 February 2013
EPI-743 Vatiquinone is a new drug that is based on vitamin E. Tests have shown that it can help improve the function of cells with mitochondrial problems. It may be able to treat people with genetic disorders that affect metabolism and mitochondria
Edison Pharmaceuticals and Bambino Gesu Children’s Hospital have announced the commencement of EPI-743 Phase 2 cobalamin C deficiency syndrome trial.
EPI-743 is an orally bioavailable small molecule and a member of the para-benzoquinone class of drugs.
The trial’s principal investigator, Bambino Gesu Children’s Hospital, division of metabolism Professor Carlo Dionisi-Vici said, “Given the central role of glutathione in cellular redox balance and antioxidant defense systems, we are eager to explore whether a therapeutic that increases glutathione such as EPI-743 will provide clinical benefit.”
Improvement in visual function is the primary endpoint of the placebo-controlled study while secondary outcome measurements assess neurologic and neuromuscular function, glutathione biomarkers, quality of life, in addition to safety parameters.
The investigation is aimed at assessing the efficacy of EPI-743 in disorders of intermediary metabolism that also result in redox disturbances.
EPI-743 is an orally absorbed small molecule that readily crosses into the central nervous system. It works by targeting the enzyme NADPH quinone oxidoreductase 1 (NQO1). Its mode of action is to synchronize energy generation in mitochondria with the need to counter cellular redox stress
Neurim Pharmaceuticals Announces Positive Phase 2 Clinical Trial Results of Piromelatine for the Treatment of Insomnia
Chemical structures of Neu-P11 (a) and Neu-P5 (b).
structure from- http://www.sciencedirect.com/science/article/pii/S0731708512005304#gr1
ZURICH, Feb. 18, 2013 Neurim Pharmaceuticals announced today positive results from a phase II clinical study evaluating the efficacy and safety of Piromelatine (Neu-P11), a novel investigational multimodal sleep medicine developed for the treatment of patients with primary and co-morbid insomnia. The new results are from a recent double-blind, randomized, placebo controlled, parallel group, non-confirmatory, sleep-laboratory study. The study evaluated piromelatine compared to placebo in 120 adult primary insomnia patients ages 18 years and older.
Piromelatine 20/50mg treatment for 4 weeks resulted in statistically significant and clinically meaningful improvements relative to placebo in key polysomnographic (PSG) parameters including Wake After Sleep Onset (WASO) (p=0.02 for both doses) and in particular WASO for the first 6 hours of sleep (WASO-6h) (p=0.0008 and p=0.04 for the 50 mg and 20 mg groups, respectively). Piromelatine 50 mg also improved Sleep Efficiency (SEF) (p=0.02), Total Sleep Time (TST) (p=0.02), Total Time Awake (TTA) (p=0.01) and time in NREM sleep (p=0.028) indicating beneficial effects on sleep maintenance. Subjective improvements relative to placebo in quality of sleep and total sleep time measured by the Pittsburg Sleep Quality Questionnaire (PSQI) were also observed, confirming the PSG findings. Piromelatine enhanced NREM sleep EEG delta power and significantly reduced beta power (p<0.05). The decrease in EEG beta activity, a marker of cortical arousal, is a physiological surrogate marker of the efficacy of Piromelatine in sleep maintenance. Piromelatine was generally safe and well tolerated, had no detrimental effects on next-day psychomotor performance (as assessed by the Digit Symbol Substitution Test (DSST)) for any dose group and no deleterious effects on sleep structure and architecture.
“Piromelatine demonstrates a good potential for the treatment of primary insomnia characterized by sleep maintenance disturbances as well as insomnia with psychiatric or medical co-morbidities,” said Prof. Nava Zisapel, CSO of Neurim. The study results will be presented at the 27th Annual Meeting of the Associated Professional Sleep Societies (APSS) -Sleep 2013 meeting in Baltimore.
PIROMELATINE (NEU-P11)
Piromelatine is a novel compound under development for the treatment of insomnia associated with pain.
Piromelatine is a melatonin agonist, serotonin 5-HT-1A and 5-HT-1D agonist. The compound binds to the MT1, 2 and 3 receptors which govern the body’s sleep-wake cycle and circadian rhythm. The sleep promoting, analgesic, anti-diabetic, antihypertensive, anti-neurodegenerative, anxiolytic and antidepressant effects of Piromelatine have been demonstrated in a series of relevant animal models.
Piromelatine is a multi-facet drug addressing a wide range of potential indications including, but not limited to, insomnia, IBS, neuropathy and fibromyalgia.
Neurim has recently completed a phase-II clinical trial to assess the efficacy and safety of Piromelatine in patients with primary insomnia.
FDA approves UCLA IND application to commence embryonic stem cell-based trial
12 feb 2013
The USFDA has approved the investigator investigational new drug (IND) application of University of California, Los Angeles (UCLA), the clinical partner of Advanced Cell Technology (ACT), to commence a clinical trial using the human embryonic stem cells (hESCs)-derived cells to treat severe myopia.
Embryonic stem cell-based trial was designed to assess the hESC-derived ACT’s retinal pigment epithelial (RPE) cells in patients with severe myopia (nearsightedness).
ACT chairman and CEO Gary Rabin said, “We are pleased to be on track to broaden the scope of our RPE program with the initiation of the new Investigator IND.”
Human embryonic stem cells (hESCs) are pluripotent cells derived from the inner cell mass of the blastocyst. They have the ability to renew themselves and to differentiate into a variety of different cell types that are found in the body. Unlike somatic or ‘adult’ stem cells, hESCs proliferate indefinitely. This, together with their ability to differentiate into most adult cell types, has resulted in the preferred use of these cells for research and therapeutic applications, as they represent a potentially indefinite source of therapeutic cells. Any cell therapy derived from hESCs would be allogeneic by nature. Some current studies involve the potential therapeutic application of hESCs for spinal cord injury, age-related macular degeneration (AMD), cardiovascular diseases, and diabetes. Among the start up cell therapy companies, Geron and Advanced Cell Technologies have pioneered clinical trials using cells differentiated from hESCs.
Mafenide Acetate Topical Solution 5% Approved: February 12, 2013 – Par Pharmaceutical, Inc. Sulfamylon
Mafenide acetate, USP is a synthetic antimicrobial agent designated chemically as a-amino-p- toluenesulfonamide monoacetate. It has the following structural formula:
 |
C7H10N2O2S • C2H4O2
M.W. 246.29Mafenide acetate, USP is a white, crystalline powder which is freely soluble in water.
SULFAMYLON® (mafenide acetate) For 5% Topical Solution is provided in packets containing 50 g of sterile mafenide acetate to be reconstituted in 1000 mL of Sterile Water for irrigation, USP or 0.9% Sodium Chloride Irrigation, USP. After mixing, the solution contains 5% w/v of mafenide acetate. The solution is an antimicrobial preparation suitable for topical administration. The solution Is not for Injection. The reconstituted solution may be held up to 28 days after preparation if stored in unopened containers. ONCE A CONTAINER IS OPENED, ANY UNUSED PORTION SHOULD BE DISCARDED AFTER 48 HOURS. Store the reconstituted solution at 20° to 25°C (68° to 77°F). Limited storage periods at 15° to 30°C (59° to 86°F) are acceptable.
- Mafenide Acetate Topical Solution 5%
Approved: February 12, 2013 – Par Pharmaceutical, Inc.
Generic for: Sulfamylon
FDA grants fresh approval for Novartis’ Zortress, Everolimus
dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
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.
18 feb 2013
The US Food and Drug Administration has approved Novartis’ Zortress for preventing organ rejection in adults receiving a liver transplant.
The Swiss major noted that Zortress (everolimus) is the first mammalian target of rapamycin (mTOR) inhibitor given the green light for use following liver transplantation and the first immunosuppressant approved by the FDA in over a decade for that use. The treatment is already on the market for preventing organ rejection in kidney transplant patients.
The approval was based on the largest liver transplant study to date, conducted in 719 liver transplant patients, Novartis says. The data showed that Zortress plus reduced-exposure tacrolimus (a well-established immunosuppresant) led to comparable efficacy and higher renal function compared to standard tacrolimus at 12 months.
Novartis Pharma chief David Epstein noted that this second indication for Zortress in just three years in the USA follows the recent European approval (in the fourth quarter of 2012) of the drug for liver transplants. It is marketed there as Certican and is also approved in Europe in kidney and heart transplantation.
Everolimus is also sold as Afinitor and Volubia in various oncology indications and is licensed to Abbott Laboratories (and sublicensed to Boston Scientific) for use in drug-eluting stents.
http://www.nature.com/nrd/journal/v8/n7/full/nrd2924.html
take a tour
Eritrea, africa
Eritrea – Wikipedia, the free encyclopedia
Eritrea (/ˌɛrɨˈtreɪ.ə/ or /ˌɛrɨˈtriːə/; Tigrinya: ኤርትራ ʾErtrā ; Arabic: إرتريا … Its name Eritrea is based on the Greek name for the Red Sea (Ἐρυθρὰ …
Isaias AfwerkiIsaias Afwerki (sometimes spelled Afewerki; Tigrinya: ኢሳይያስ …
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History of EritreaHistory of Eritrea. Coat of Arms of Eritrea. Pre-colonial. Kingdom …
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asmara
asmara
Massawa Old City
Eritrea – Island of the Red Seo of Eritrea –
keren
“Asara” traditional sesami oil press – Eritrea (Saied Ibrahim Yehdego)
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Nanyang Technological University, Singapore, prepares for trial of glaucoma drug
If glaucoma is left untreated, it can lead to blindness.–Courtesy of NIH
LipoLat, a controlled-release glaucoma therapeutic, is a suspension of nanocapsules each trapping a payload of drug. Designed as an injection into the conjunctiva (the outer layer of the eye), LipoLat gradually released the drug and was as effective as eye drops for as long as three months in preclinical trials. According to the researchers, this is now ready to move into human studies.
12th feb 2013
preclinical trials
http://media.ntu.edu.sg/NewsReleases/Pages/newsdetail.aspx?news=15fdbb3e-6724-4bc9-a699-a486c25f510e
For glaucoma patients, taking daily medication will soon become a thing of the past. With Nanyang Technological University’s (NTU) newest solution, a simple, quick and painless injection four times a year would be enough. The solution contains an anti-glaucoma drug wrapped in nano-sized capsules, and is delivered by an injection into the outer layer in the front of the eye (conjunctiva) by the doctor.
The nanocarrier will then slowly release the drug over several weeks. LipoLat, as it is known, is now ready for clinical trials. Extensive pre-clinical studies have shown that this single injection is as effective at treating glaucoma as taking daily eye drops for up to three months.
The newly launched Ocular Therapeutic Engineering Centre will work on this research. Housed at NTU’s School of Materials Science and Engineering, the center builds upon the School’s successful research collaboration with the Singapore Eye Research Institute. The center’s director Professor Subbu Venkatraman, who is also the school chair, said the center will build on the strong research collaboration between clinical scientists and NTU technologists, to develop new drug delivery systems for the eye.
“I hope to showcase this as a good example of how close interactions between medical practitioners and technology providers can lead to rapid translation of ideas to the clinic, such as LipoLat,” said Prof Venkatraman. “We are confident that the products co-developed at the centre will lead on to further discoveries and innovations in ocular therapy.” Working closely with Prof Venkatraman as the co-director of the center is Dr Tina Wong, an adjunct associate professor at the School of Materials Science and Engineering and a senior consultant at the Singapore National Eye Centre. She is also head of the Ocular Therapeutics and Drug Delivery Research Group at the Singapore Eye Research Institute
.
Extensive pre-clinical studies have shown that a single injection of the solution developed by Nanyang Technological University is effective in treating glaucoma
The solution developed by the university contains an anti-glaucoma drug wrapped in nano-sized capsules
The solution developed by the university contains an anti-glaucoma drug wrapped in nano-sized capsules
Working closely with Prof Venkatraman (picture) as the Co-Director of the centre is Dr Tina Wong (picture)
Celgene gains SFDA China, approval for marketing Revlimid (lenalidomide) to treat multiple myeloma
(RS)-3-(4-amino-1-oxo 1,3-dihydro-2H-isoindol- 2-yl)piperidine-2,6-dione
Lenalidomide
REVLIMID® is an oral immunomodulatory drug marketed in the United States and many international markets, in combination with dexamethasone, for treatment of patients with multiple myeloma who have received at least one prior therapy. It is also marketed in the United States and certain international markets for the treatment of transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes, or MDS, associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalitie.Revlimid Worldwide annual sales in 2011 was $3.2bLenalidomide (Revlimid) is a derivative of thalidomideintroduced in 2004.It was initially intended as a treatment for multiple myeloma, for which thalidomide is an accepted therapeutic treatment. Lenalidomide has also shown efficacy in the class of hematological disorders known as myelodysplastic syndromes (MDS). Lenalidomide has significantly improved overall survival in myeloma (which generally carries a poor prognosis), although toxicity remains an issue for users. [1]It costs $163,381 per year for the average patient.[2]
Mechanism of action
Lenalidomide has been used to successfully treat both inflammatory disorders and cancers in the past 10 years. There are multiple mechanisms of action, and they can be simplified by organizing them as mechanisms of action in vitro and in vivo.[3] In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the microenvironment support for tumor cells, and immunomodulatory role. In vivo, lenalidomide induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity. Lenalidomide has a broad range of activities that can be exploited to treat many hematologic and solid cancers.
- McCarthy; Philip L. McCarthy, Kouros Owzar, Craig C. Hofmeister, et al. (May 10, 2012). “Lenalidomide after Stem-Cell Transplantation for Multiple Myeloma”. N Engl J Med 366 (19): 1770–1781. doi:10.1056/NEJMoa1114083. PMID 22571201.
- Badros, Ashraf Z. Badros (May 10, 2012). “Lenalidomide in Myeloma — A High-Maintenance Friend”. N Engl J Med 366 (19): 1836–1838. doi:10.1056/NEJMe1202819. PMID 22571206.
- Vallet S, Palumbo A, Raje N, Boccadoro M, Anderson KC (July 2008). “Thalidomide and lenalidomide: Mechanism-based potential drug combinations”. Leukemia & Lymphoma 49 (7): 1238–45. doi:10.1080/10428190802005191. PMID 18452080.
New Drug Approvals 