(12) United States Patent (10) Patent No.: US 9,526,728 B2 Klein Et Al
Total Page:16
File Type:pdf, Size:1020Kb

Load more
Recommended publications
-
WHO Drug Information Vol. 12, No. 3, 1998
WHO DRUG INFORMATION VOLUME 12 NUMBER 3 • 1998 RECOMMENDED INN LIST 40 INTERNATIONAL NONPROPRIETARY NAMES FOR PHARMACEUTICAL SUBSTANCES WORLD HEALTH ORGANIZATION • GENEVA Volume 12, Number 3, 1998 World Health Organization, Geneva WHO Drug Information Contents Seratrodast and hepatic dysfunction 146 Meloxicam safety similar to other NSAIDs 147 Proxibarbal withdrawn from the market 147 General Policy Issues Cholestin an unapproved drug 147 Vigabatrin and visual defects 147 Starting materials for pharmaceutical products: safety concerns 129 Glycerol contaminated with diethylene glycol 129 ATC/DDD Classification (final) 148 Pharmaceutical excipients: certificates of analysis and vendor qualification 130 ATC/DDD Classification Quality assurance and supply of starting (temporary) 150 materials 132 Implementation of vendor certification 134 Control and safe trade in starting materials Essential Drugs for pharmaceuticals: recommendations 134 WHO Model Formulary: Immunosuppressives, antineoplastics and drugs used in palliative care Reports on Individual Drugs Immunosuppresive drugs 153 Tamoxifen in the prevention and treatment Azathioprine 153 of breast cancer 136 Ciclosporin 154 Selective serotonin re-uptake inhibitors and Cytotoxic drugs 154 withdrawal reactions 136 Asparaginase 157 Triclabendazole and fascioliasis 138 Bleomycin 157 Calcium folinate 157 Chlormethine 158 Current Topics Cisplatin 158 Reverse transcriptase activity in vaccines 140 Cyclophosphamide 158 Consumer protection and herbal remedies 141 Cytarabine 159 Indiscriminate antibiotic -
IP Vol.2 No.2 Jul-Dec 2014.Pmd
International Physiology63 Short Communication Vol. 2 No. 2, July - December 2014 Role of Polyol Pathway in Pathophysiology of Diabetic Peripheral Neuropathy: An Updated Overview Kumar Senthil P.*, Adhikari Prabha**, Jeganathan*** Abstract The aim of this short communication article was to enlighten the role of polyol pathway in pathophysiology of diabetic peripheral neuropathy (DPN) through an evidence-informed overview of current literature. Findings from experimental models of DPN suggest that altered glutathione redox state, with exaggerated NA(+)-K(+)-ATPase activity, increased malondialdehyde content, decreased red blood cell 2,3-diphosphoglycerate concentration, reduced cyclic adenosine monophosphate, reduced myo- inositol and excessive sorbitol in peripheral nerves were indicative of polyol metabolic pathwayin producing pathophysiological changes of DPN, and treatments using aldose reductase inhibitors were found to reverse those changes. Keywords: Polyol pathway; Myo-inositol; Sorbitol; Neurophysiology; Endocrinology. The aim of this short communication oxidized (GSSG) glutathione levels in crude article was to enlighten the role of polyol homogenates of rat sciatic nerve. The study pathway in pathophysiology of diabetic concluded that altered glutathione redox peripheral neuropathy (DPN) through an state played no detectable role in the evidence-informed overview of current pathogenesis of this defect in diabetic literature. peripheral nerve. Calcutt et al[1] measured motor nerve Finegold et al[3] studied the effect of conduction velocity (MNCV), Na(+)-K(+)- polyol pathway blockade with sorbinil, a ATPase activity, polyol-pathway specific inhibitor of aldose reductase, on metabolites, and myo-inositol in sciatic nerve myo-inositol content in acutely nerves from control mice, galactose-fed streptozotocin-diabetic ratswhich (20% wt/wt diet) mice, and galactose-fed completely prevented the fall in nerve myo- mice given the aldose reductase inhibitor inositol. -
The Antidiabetic Drug Lobeglitazone Has the Potential to Inhibit PTP1B T Activity ⁎ Ruth F
Bioorganic Chemistry 100 (2020) 103927 Contents lists available at ScienceDirect Bioorganic Chemistry journal homepage: www.elsevier.com/locate/bioorg The antidiabetic drug lobeglitazone has the potential to inhibit PTP1B T activity ⁎ Ruth F. Rochaa, Tiago Rodriguesc, Angela C.O. Menegattia,b, , Gonçalo J.L. Bernardesc,d, Hernán Terenzia a Centro de Biologia Molecular Estrutural, Departamento de Bioquímica, Universidade Federal de Santa Catarina, Campus Trindade, 88040-900 Florianópolis, SC, Brazil b Universidade Federal do Piauí, CPCE, 64900-000 Bom Jesus, PI, Brazil c Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, Avenida Professor Egas Moniz, 1649-028 Lisbon, Portugal d Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge, UK ARTICLE INFO ABSTRACT Keywords: Protein tyrosine phosphatase 1B (PTP1B) is considered a potential therapeutic target for the treatment of type 2 Thiazolidinediones diabetes mellitus (T2DM), since this enzyme plays a significant role to down-regulate insulin and leptin sig- Lobeglitazone nalling and its over expression has been implicated in the development of insulin resistance, T2DM and obesity. PPAR-γ Some thiazolidinediones (TZD) derivatives have been reported as promising PTP1B inhibitors with anti hy- PTP1B perglycemic effects. Recently, lobeglitazone, a new TZD, was described as an antidiabetic drug that targetsthe Non-competitive inhibitors PPAR-γ (peroxisome γ proliferator-activated receptor) pathway, but no information on its effects on PTP1B have been reported to date. We investigated the effects of lobeglitazone on PTP1B activity in vitro. Surprisingly, lobeglitazone led to moderate inhibition on PTP1B (IC50 42.8 ± 3.8 µM) activity and to a non-competitive reversible mechanism of action. -
Dualism of Peroxisome Proliferator-Activated Receptor Α/Γ: a Potent Clincher in Insulin Resistance
AEGAEUM JOURNAL ISSN NO: 0776-3808 Dualism of Peroxisome Proliferator-Activated Receptor α/γ: A Potent Clincher in Insulin Resistance Mr. Ravikumar R. Thakar1 and Dr. Nilesh J. Patel1* 1Faculty of Pharmacy, Shree S. K. Patel College of Pharmaceutical Education & Research, Ganpat University, Gujarat, India. [email protected] Abstract: Diabetes mellitus is clinical syndrome which is signalised by augmenting level of sugar in blood stream, which produced through lacking of insulin level and defective insulin activity or both. As per worldwide epidemiology data suggested that the numbers of people with T2DM living in developing countries is increasing with 80% of people with T2DM. Peroxisome proliferator-activated receptors are a family of ligand-activated transcription factors; modulate the expression of many genes. PPARs have three isoforms namely PPARα, PPARβ/δ and PPARγ that play a central role in regulating glucose, lipid and cholesterol metabolism where imbalance can lead to obesity, T2DM and CV ailments. It have pathogenic role in diabetes. PPARα is regulates the metabolism of lipids, carbohydrates, and amino acids, activated by ligands such as polyunsaturated fatty acids, and drugs used as Lipid lowering agents. PPAR β/δ could envision as a therapeutic option for the correction of diabetes and a variety of inflammatory conditions. PPARγ is well categorized, an element of the PPARs, also pharmacological effective as an insulin resistance lowering agents, are used as a remedy for insulin resistance integrated with type- 2 diabetes mellitus. There are mechanistic role of PPARα, PPARβ/δ and PPARγ in diabetes mellitus and insulin resistance. From mechanistic way, it revealed that dual PPAR-α/γ agonist play important role in regulating both lipids as well as glycemic levels with essential safety issues. -
Diabetes Mellitus Typ 2 Medikamentöse Therapie
Übersicht AMT Diabetes mellitus Typ 2 Medikamentöse Therapie L. Cornelius Bollheimer, Christiane Girlich, Ulrike Woenckhaus und Roland Büttner, Regensburg Arzneimitteltherapie 2007;25:175–86. Literatur NIDDM subjects. A study of two ethnic groups. Diabetes Care 1993;16: 621–9. 1. Deutsche Diabetes Gesellschaft. Evidenzbasierte Leitlinie: Epidemiologie 24. Akbar DH. Effect of metformin and sulfonylurea on C-reactive protein und Verlauf des Diabetes mellitus in Deutschland. http://www.deutsche- level in well-controlled type 2 diabetics with metabolic syndrome. En- diabetes-gesellschaft.de/redaktion/mitteilungen/leitlinien/EBL_Update_ docrine 2003;20:215–8. Epidemiologie_05_2004_neues_Layout.pdf. Internetdokument. 2004. 25. Krentz AJ, Bailey CJ. Oral antidiabetic agents: current role in type 2 dia- 2. Seufert J. Kardiovaskuläre Endpunktstudien in der Therapie des Typ-2- betes mellitus. Drugs 2005;65:385–411. Diabetes-mellitus. Dtsch Ärzteblatt 2006;103:A934–42. 26. Parhofer KG, Laubach E, Geiss HC, Otto C. Effect of glucose control on 3. Deutsche Diabetes Gesellschaft. Praxis-Leitlinien der Deutschen Diabe- lipid levels in patients with type 2 diabetes. Dtsch Med Wochenschr tes Gesellschaft. Diabetologie und Stoffwechsel 2006;1:S2. 2002;127:958–62. 4. Häring HU, Matthaei S. Behandlung des Diabetes mellitus Typ 2. Diabe- 27. DeFronzo RA, Barzilai N, Simonson DC. Mechanism of metformin ac- tologie und Stoffwechsel 2006;1:S205–10. tion in obese and lean noninsulin-dependent diabetic subjects. J Clin 5. Brueckel J, Kerner W. Definition, Klassifikation und Diagnostik des Dia- Endocrinol Metab 1991;73:1294–301. betes mellitus. Diabetologie und Stoffwechsel 2006;1:S177–80. 28. Cryer DR, Nicholas SP, Henry DH, Mills DJ, et al. Comparative outcomes 6. -
Corporate Presentation June 2019 Disclaimer
Corporate Presentation June 2019 Disclaimer Some of the statements contained in this presentation constitute forward-looking statements. Statements that are not historical facts are forward-looking statements. Forward-looking statements generally can be identified by the use of forward-looking terminology such as “may”, “will”, “expect”, “intend”, “estimate”, “anticipate”, “believe”, “continue” or similar terminology. These statements are based on the Company’s current strategy, plans, objectives, assumptions, estimates and projections. Investors should therefore not place undue reliance on those statements. The Company makes no representation, warranty or prediction that the results anticipated by such forward- looking statements will be achieved, and such forward-looking statements represent, in each case, only one of many possible scenarios and should not be viewed as the most likely or standard scenario. Forward-looking statements speak only as of the date that they are made and the Company does not undertake to update any forward-looking statements in light of new information or future events. Forward-looking statements involve inherent risks and uncertainties. The Company cautions that a number of important factors could cause actual results to differ materially from those contained in any forward-looking statement. 2 Well Diversified Mid-to-Late Stage Metabolic Pipeline for Large Market Opportunities Global partnerships secured for late stage clinical program in type 2 diabetes • Imeglimin: First in class oral drug candidate targeting -
Lobeglitazone
2013 International Conference on Diabetes and Metabolism Lobeglitazone, A Novel PPAR-γ agonist with balanced efficacy and safety Kim, Sin Gon. MD, PhD. Professor, Division of Endocrinology and Metabolism Department of Internal Medicine, Korea University College of Medicine. Disclosure of Financial Relationships This symposium is sponsored by Chong Kun Dang Pharmaceutical Corp. I have received lecture and consultation fees from Chong Kun Dang. Pros & Cons of PPAR-γ agonist Pros Cons • Good glucose lowering • Adverse effects • Durability (ADOPT) (edema, weight gain, • Insulin sensitizing CHF, fracture or rare effects (especially in MS, macular edema etc) NAFLD, PCOS etc) • Possible safety issues • Prevention of new- (risk of MI? – Rosi or onset diabetes (DREAM, bladder cancer? - Pio) ACT-NOW) • LessSo, hypoglycemiathere is a need to develop PPAR-γ • Few GI troubles agonist• Outcome with data balanced efficacy and safety (PROactive) Insulin Sensitizers : Several Issues Rosi, Peak sale ($3.3 billion) DREAM Dr. Nissen Dr. Nissen ADOPT META analysis BARI-2D (5,8) Rosi, lipid profiles RECORD 1994 1997 1999 2000 2002 2004 2005 2006 2007 2008 2009 2010 2011 2012 2013 2014 Tro out d/t FDA, All diabetes hepatotoxicity drug CV safety Rosi (5) FDA, Black box Rosi, Rosi , CV safety warning - REMS in USA = no evidence - Europe out Pio (7) PIO, bladder cancer CKD 501 Lobeglitazone 2000.6-2004.6 2004.11-2007.1 2007.3-2008.10 2009.11-2011.04 Discovery& Preclinical study Phase I Phase II Phase III Developmental Strategy Efficacy • PPAR activity Discovery & Preclinical study • In vitro & vivo efficacy • Potent efficacy 2000.06 - 2004.06 Phase I 2004.11 - 2007.01 • In vitro screening • Repeated dose toxicity • Metabolites • Geno toxicity • Phase II CYP 450 • Reproductive toxicity 2007.03 - 2008.10 • DDI • Carcinogenic toxicity ADME Phase III Safety 2009.11 - 2011.04 CV Safety / (Bladder) Cancer / Liver Toxicity / Bone loss Lobeglitazone (Duvie) 1. -
Exendin-4 Peptide Analogues As Dual Glp-1/Gip Receptor Agonists
(19) TZZ¥ZZ_Z_T (11) EP 3 080 150 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07K 14/575 (2006.01) C07K 14/605 (2006.01) 01.08.2018 Bulletin 2018/31 (86) International application number: (21) Application number: 14828149.6 PCT/EP2014/077336 (22) Date of filing: 11.12.2014 (87) International publication number: WO 2015/086728 (18.06.2015 Gazette 2015/24) (54) EXENDIN-4 PEPTIDE ANALOGUES AS DUAL GLP-1/GIP RECEPTOR AGONISTS EXENDIN-4-PEPTIDANALOGA ALS DUALE GLP-1/GIP-REZEPTORAGONISTEN ANALOGUES PEPTIDIQUES D’EXENDINE-4 EN TANT QU’AGONISTES DU RÉCEPTEUR GIP/GLP-1 DOUBLE (84) Designated Contracting States: (74) Representative: Weickmann & Weickmann AL AT BE BG CH CY CZ DE DK EE ES FI FR GB PartmbB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO Postfach 860 820 PL PT RO RS SE SI SK SM TR 81635 München (DE) (30) Priority: 13.12.2013 EP 13306712 (56) References cited: WO-A1-2012/167744 WO-A2-2009/035540 (43) Date of publication of application: US-A1- 2011 166 062 US-A1- 2012 196 802 19.10.2016 Bulletin 2016/42 • JOHN L. KRSTENANSKY ET AL: "Importance of (73) Proprietor: SANOFI the 10-13 region of glucagon for its receptor 75008 Paris (FR) interactionsand activation of adenylate cyclase", BIOCHEMISTRY, vol. 25, no. 13, 1 July 1986 (72) Inventors: (1986-07-01), pages 3833-3839, XP055117918, • KADEREIT, Dieter ISSN: 0006-2960, DOI: 10.1021/bi00361a014 65926 Frankfurt am Main (DE) • VICTOR A. -
Comparative Effectiveness, Safety, and Indications of Insulin Analogues in Premixed Formulations for Adults with Type 2 Diabetes
Comparative Effectiveness Review Number 14 Comparative Effectiveness, Safety, and Indications of Insulin Analogues in Premixed Formulations for Adults With Type 2 Diabetes This report is based on research conducted by the Johns Hopkins Evidence-based Practice Center (EPC) under contract to the Agency for Healthcare Research and Quality (AHRQ), Rockville, MD (Contract No. 290-02-0018). The findings and conclusions in this document are those of the authors, who are responsible for its contents; the findings and conclusions do not necessarily represent the views of AHRQ. Therefore, no statement in this report should be construed as an official position of the Agency for Healthcare Research and Quality or of the U.S. Department of Health and Human Services. This report is intended as a reference and not as a substitute for clinical judgment. Anyone who makes decisions concerning the provision of clinical care should consider this report in the same way as any medical reference and in conjunction with all other pertinent information. This report may be used, in whole or in part, as the basis for development of clinical practice guidelines and other quality enhancement tools, or as a basis for reimbursement and coverage policies. AHRQ or U.S. Department of Health and Human Services endorsement of such derivative products may not be stated or implied. Comparative Effectiveness Review Number 14 Comparative Effectiveness, Safety, and Indications of Insulin Analogues in Premixed Formulations for Adults With Type 2 Diabetes Prepared for: Agency for Healthcare Research and Quality U.S. Department of Health and Human Services 540 Gaither Road Rockville, MD 20850 www.ahrq.gov Contract No. -
Renato Wilberto Zilli Eficácia Em Longo Prazo Das
RENATO WILBERTO ZILLI EFICÁCIA EM LONGO PRAZO DAS GLIFLOZINAS VERSUS GLIPTINAS NO TRATAMENTO DO DIABETES MELLITUS TIPO 2 APÓS FALÊNCIA DA METFORMINA COMO MONOTERAPIA: REVISÃO SISTEMÁTICA E METANÁLISE EM REDE Tese apresentada ao Programa de Ciências Médicas da Faculdade de Medicina da Universidade de São Paulo para obtenção do título de Doutor em Ciências. Área de Concentração: Processos Imunes e Infecciosos Orientador: Prof. Dr. Fabiano Pinheiro da Silva (Versão corrigida. Resolução CoPGr 6018/11, de 13 de outubro de 2011. A versão original está disponível na Biblioteca da FMUSP) São Paulo 2017 Dados Internacionais de Catalogação na Publicação (CIP) Preparada pela Biblioteca da Faculdade de Medicina da Universidade de São Paulo ©reprodução autorizada pelo autor Zilli, Renato Wilberto Eficácia em longo prazo das gliflozinas versus gliptinas no tratamento do diabetes mellitus tipo 2 após falência da metformina como monoterapia : revisão sistemática e metanálise em rede / Renato Wilberto Zilli ‐‐ São Paulo, 2017. Tese(doutorado)--Faculdade de Medicina da Universidade de São Paulo. Programa de Ciências Médicas. Área de concentração: Processos Imunes e Infecciosos. Orientador: Fabiano Pinheiro da Silva. Descritores: 1.Diabetes mellitus tipo 2 2.Metanálise 3.Terapia combinada 4.Falha de tratamento 5.Metformina 6.Inibidores da dipeptidil peptidase IV 7.Transportador 2 de glucose‐sódio/inibidores 8.Empagliflozina 9.Dapagliflozina 10.Saxagliptina USP/FM/DBD ‐302/17 Esta tese de doutorado está de acordo com as seguintes normas, em vigor no momento desta publicação: Referências: adaptado de International Committee of Medical Journals Editors (Vancouver). Guia de apresentação e dissertações, teses e monografias. Elaborado por Anneliese Cordeiro da Cunha, Maria Julia de A.L. -
Classification Decisions Taken by the Harmonized System Committee from the 47Th to 60Th Sessions (2011
CLASSIFICATION DECISIONS TAKEN BY THE HARMONIZED SYSTEM COMMITTEE FROM THE 47TH TO 60TH SESSIONS (2011 - 2018) WORLD CUSTOMS ORGANIZATION Rue du Marché 30 B-1210 Brussels Belgium November 2011 Copyright © 2011 World Customs Organization. All rights reserved. Requests and inquiries concerning translation, reproduction and adaptation rights should be addressed to [email protected]. D/2011/0448/25 The following list contains the classification decisions (other than those subject to a reservation) taken by the Harmonized System Committee ( 47th Session – March 2011) on specific products, together with their related Harmonized System code numbers and, in certain cases, the classification rationale. Advice Parties seeking to import or export merchandise covered by a decision are advised to verify the implementation of the decision by the importing or exporting country, as the case may be. HS codes Classification No Product description Classification considered rationale 1. Preparation, in the form of a powder, consisting of 92 % sugar, 6 % 2106.90 GRIs 1 and 6 black currant powder, anticaking agent, citric acid and black currant flavouring, put up for retail sale in 32-gram sachets, intended to be consumed as a beverage after mixing with hot water. 2. Vanutide cridificar (INN List 100). 3002.20 3. Certain INN products. Chapters 28, 29 (See “INN List 101” at the end of this publication.) and 30 4. Certain INN products. Chapters 13, 29 (See “INN List 102” at the end of this publication.) and 30 5. Certain INN products. Chapters 28, 29, (See “INN List 103” at the end of this publication.) 30, 35 and 39 6. Re-classification of INN products. -
Review of Nisha Amalaki –An Ayurvedic Formulation of Turmeric and Indian Goose Berry in Diabetes
wjpmr, 2017,3(9), 101-105 SJIF Impact Factor: 4.103 Review Article Bedarkar. WORLD JOURNAL OF PHARMACEUTICAL World Journal of Pharmaceutical and Medical Research AND MEDICAL RESEARCH ISSN 2455-3301 www.wjpmr.com WJPMR REVIEW OF NISHA AMALAKI –AN AYURVEDIC FORMULATION OF TURMERIC AND INDIAN GOOSE BERRY IN DIABETES Dr. Prashant Bedarkar* Assistant Prof. Dept. of Rasashastra and B.K., IPGT & R. A., Jamnagar, Gujarat, India. *Corresponding Author: Dr. Prashant Bedarkar Assistant Prof. Dept. of Rasashastra and B.K., IPGT & R. A., Jamnagar, Gujarat, India. Article Received on 01/08/2017 Article Revised on 22/08/2017 Article Accepted on 12/09/2017 ABSTRACT Introduction- Nishamalaki or Nisha Amalaki representing various combination formulations of Turmeric (Nisha, Haridra, Curcuma longa L.) and Indian gooseberry (Amalaki, Emblica officinalis Gaertn.) is recommended in Ayurvedic classics, proven efficacious and widely practiced in the management i.e. treatment of Diabetes along with management and prevention of complications of Madhumeha (Diabetes). Aims and objectives-Inspite of many pharmacological, clinical researches of Nishamalaki on Glucose metabolism and Glycemic control, their review is not available, hence present study was conducted. Material and methods- Evidence based online published researches of Nishamalaki on Glucose metabolism and Glycemic control and its efficacy in the management of complications of Diabetes from available databases and search engines were referred for review through. Summary of published researches was systematically arranged, analyzed and presented. Observations and results-Review of online Published original research studies reveals total were found to be 13 in number, comprising of 3 in vitro studies and animal experimental pharmacological researches each and 7 clinical researches.