DOCSLIB.ORG

Metabolic Disease

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Metabolic Disease Metabolic Disease Metabolic diseases is defined by a constellation of interconnected physiological, biochemical, clinical, and metabolic factors that directly increases the risk of cardiovascular disease, type 2 diabetes mellitus, and all cause mortality. Associated conditions include hyperuricemia, fatty liver (especially in concurrent obesity) progressing to nonalcoholic fatty liver disease, polycystic ovarian syndrome (in women), erectile dysfunction (in men), and acanthosis nigricans. Metabolic disease modeling is an essential component of biomedical research and a mandatory prerequisite for the treatment of human disease. Somatic genome editing using CRISPR/Cas9 might be used to establish novel metabolic disease models. www.MedChemExpress.com 1 Metabolic Disease Inhibitors & Modulators (-)-(S)-Equol (-)-Fucose Cat. No.: HY-100583 (6-Desoxygalactose; L-(-)-Fucose; L-Galactomethylose) Cat. No.: HY-N1480 Bioactivity: (-)-(S)-Equol is a high affinity ligand for estrogen receptor Bioactivity: (-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure β with a Ki of 0.73 nM. determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions. Purity: 99.82% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 100 mg (-)-PX20606 trans isomer (24R)-MC 976 ((-)-PX-102 trans isomer; (-)-PX-104) Cat. No.: HY-100443B Cat. No.: HY-15267A Bioactivity: (-)-PX20606 trans isomer is a FXR agonist with EC50s of 18 Bioactivity: (24R)-MC 976 is a Vitamin D3 derivative. and 29 nM for FXR in FRET and M1H assay, respectively. Purity: 98.39% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 1 mg, 2 mg (24S)-MC 976 (R)-(+)-Etomoxir sodium salt Cat. No.: HY-15267B ((+)-Etomoxir sodium salt) Cat. No.: HY-50202A Bioactivity: (24S)-MC 976 is a Vitamin D3 derivative. Bioactivity: (R)-(+)-Etomoxir sodium salt is the R-form of Etomoxir sodium salt. Etomoxir is a potent inhibitor of carnitine palmitoyltransferase-I ( CPT-1). Purity: >98% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg (R)-(-)-Phenylephrine (R,S)-Ivosidenib (Phenylephrine) Cat. No.: HY-B0769 ((R,S)-AG-120) Cat. No.: HY-18767A Bioactivity: (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist Bioactivity: (R,S)-Ivosidenib is a inhibitor of Isocitrate Dehydrogenase primarily used as a decongestant. (IDH1). Purity: >98% Purity: 99.40% Clinical Data: Launched Clinical Data: No Development Reported Size: 200 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg (S)-2-Hydroxy-3-phenylpropanoic acid (S)-2-Hydroxysuccinic acid Cat. No.: HY-30220 Cat. No.: HY-Y1069 Bioactivity: (S)-2-Hydroxy-3-phenylpropanoic acid, a product of Bioactivity: (S)-2-Hydroxysuccinic acid is a dicarboxylic acid in naturally phenylalanine catabolism, is a NAPDH oxidase inhibitor. occurring form, contributes to the pleasantly sour taste of fruits and is used as a food additive. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 g 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] (±)-Carnitine chloride (±)-SLV319 (DL-Carnitine chloride) Cat. No.: HY-B1453 ((±)-Ibipinabant; (±)-BMS6462) Cat. No.: HY-14791A Bioactivity: (±)-Carnitine chloride exists in two isomers, known as D and Bioactivity: (±)-SLV319 is the racemate of SLV319. SLV319 is a potent and L. L-carnitine plays an essential role in the β-oxidation of selective cannabinoid-1 ( CB-1) receptor antagonist with an fatty acids and also shows antioxidant, and anti-inflammatory IC50 of 22 nM. activities. Purity: 98.0% Purity: 99.49% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 g 5 mg, 10 mg, 50 mg, 100 mg 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine 1,5-Anhydrosorbitol (1,2-DSPE) Cat. No.: HY-112530 Cat. No.: HY-113075 Bioactivity: 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine (DSPE) is a Bioactivity: 1,5-Anhydrosorbitol is a short-term marker for glycemic phosphoethanolamine (PE) lipid that can be used in the control. synthesis of liposomes. Purity: 97.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg 1-Deoxynojirimycin 1-Methyl-L-histidine (Duvoglustat) Cat. No.: HY-14860 Cat. No.: HY-W017006 Bioactivity: 1-Deoxynojirimycin (DNJ, Duvoglustat) is a potent Bioactivity: 1-Methyl-L-histidine is an objective indicator of meat α-glucosidase inhibitor, suppresses postprandial blood ingestion and exogenous 3-methylhistidine (3MH) intake. glucose, thereby possibly preventing diabetes mellitus. Purity: 98.0% Purity: 98.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 10 mg, 25 mg 1-Methyluric acid 10Z-Nonadecenoic acid Cat. No.: HY-W010031 Cat. No.: HY-113450 Bioactivity: 1-Methyluric acid acts on the urinary bladder mucosa and Bioactivity: 10Z-Nonadecenoic acid is a kind of long-chain fatty acid with increases the blood glucose, insulin, triglyceride, and anti-tumor activity. cholesterol levels. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 11-oxo-mogroside V 18-Hydroxycorticosterone Cat. No.: HY-N0501 Cat. No.: HY-W013179 Bioactivity: 11-oxo-mogroside V is a natural sweetener, isolated from the Bioactivity: 18-Hydroxycorticosterone is a corticosteroid and a derivative fruits of Momordica grosvenori, exhibits strong antioxidant of corticosterone, which can lead to serious electrolyte activity. It exhibits significant inhibitory effects on imbalances. - reactive oxygen species ( O2 , H2O2 and *OH) w… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: www.MedChemExpress.com 3 1alpha, 24, 25-Trihydroxy VD2 1alpha, 25-Dihydroxy VD2-D6 Cat. No.: HY-15156 Cat. No.: HY-15327 Bioactivity: 1alpha, 24, 25-Trihydroxy VD2 is a vitamin D analog. Bioactivity: 1alpha, 25-Dihydroxy VD2-D6 is a deuterated form of vitamin D. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg 2'-Deoxyinosine 2-Hydroxy-2-methylbutanoic acid Cat. No.: HY-W008638 Cat. No.: HY-W015874 Bioactivity: 2’-deoxyadenosine inhibits the growth of human colon-carcinoma Bioactivity: 2-Hydroxy-2-methylbutanoic acid, an unusual metabolite, is cell lines and is found to be associated with purine associated with 2-hydroxyglutaric aciduria and maple syrup nucleoside phosphorylase (PNP) deficiency. urine disease. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 1 g 2-Methoxyestrone 2-Methylsuccinic acid Cat. No.: HY-113252 Cat. No.: HY-W010381 Bioactivity: 2-Methoxyestrone is a methoxylated catechol estrogen and Bioactivity: 2-Methylsuccinic acid is a normal metabolite in human fluids metabolite of estrone, with a pKa of 10.81. and the main biochemical measurable features in ethylmalonic encephalopathy. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 1 g 2-Phenylethanamine 2-Phenylpropionic acid Cat. No.: HY-W010483 Cat. No.: HY-W015608 Bioactivity: 2-Phenylethanamine is believed to function as a neuromodulator Bioactivity: 2-Phenylpropionic acid is an intermediate in or neurotransmitter. alpha-Methylstyrene metabolism. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 g Size: 10mM x 1mL in DMSO, 1 g 2-γ-Linolenoyl-1,3-dilinoleoyl-sn-glycerol 21-Hydroxypregnenolone Cat. No.: HY-U00264 Cat. No.: HY-113020 Bioactivity: 2-γ-Linolenoyl-1,3-dilinoleoyl-sn-glycerol is a triglyceride. Bioactivity: 21-Hydroxypregnenolone is an essential intermediate in corticosterone synthesis. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] 24, 25-Dihydroxy VD2 24, 25-Dihydroxy VD3 (24,25-Dihydroxy vitamin D2) Cat. No.: HY-76801 Cat. No.: HY-76915 Bioactivity: 24, 25-Dihydroxy VD2 is a hydroxylated metabolite of Vitamin Bioactivity: 24, 25-Dihydroxy VD3 is a compound which is closely related to D2; a synthetic analog of Vitamin D. 1,25-dihydroxyvitamin D3, the active form of vitamin D3, but like vitamin D3 itself and 25-hydroxyvitamin D3 is inactive as a hormone both in vitro and in vivo. Purity: 99.79% Purity: 98.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 10 mg Size: 1 mg, 5 mg 25-Hydroxy VD2-D6 3,5-Dihydroxybenzoic acid Cat. No.: HY-15328 Cat. No.: HY-W015560 Bioactivity: 25-Hydroxy VD2-D6 is a labelled metabolite of Vitamin D2. Bioactivity: 3,5-Dihydroxybenzoic acid a potential biomarker for the consumption of many food products, including beer, nuts, peanut, and pulses. Purity: >98% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 5 g 3-(3-Methoxyphenyl)propionic acid 3-Amino-2-methylpropanoic acid Cat. No.: HY-W016482 Cat. No.: HY-W012974 Bioactivity: 3-(3-Methoxyphenyl)propionic acid is an organic acid, Bioactivity: 3-Amino-2-methylpropanoic acid could induce browning of white naturally occurring human metabolite and excreted in human fat and hepatic β-oxidation and is inversely correlated with urine. cardiometabolic risk factors.
Load more

Recommended publications
  • Compositions Comprising Drospirenone Molecularly
    (19) & (11) EP 1 748 756 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 9/00 (2006.01) A61K 9/107 (2006.01) 29.04.2009 Bulletin 2009/18 A61K 9/48 (2006.01) A61K 9/16 (2006.01) A61K 9/20 (2006.01) A61K 9/14 (2006.01) (2006.01) (2006.01) (21) Application number: 05708751.2 A61K 9/70 A61K 31/565 (22) Date of filing: 10.03.2005 (86) International application number: PCT/IB2005/000665 (87) International publication number: WO 2005/087194 (22.09.2005 Gazette 2005/38) (54) COMPOSITIONS COMPRISING DROSPIRENONE MOLECULARLY DISPERSED ZUSAMMENSETZUNGEN AUS DROSPIRENON IN MOLEKULARER DISPERSION DES COMPOSITIONS CONTENANT DROSPIRENONE A DISPERSION MOLECULAIRE (84) Designated Contracting States: (72) Inventors: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR • FUNKE, Adrian HU IE IS IT LI LT LU MC NL PL PT RO SE SI SK TR D-14055 Berlin (DE) Designated Extension States: • WAGNER, Torsten AL BA HR MK YU 13127 Berlin (DE) (30) Priority: 10.03.2004 EP 04075713 (74) Representative: Wagner, Kim 10.03.2004 US 551355 P Plougmann & Vingtoft a/s Sundkrogsgade 9 (43) Date of publication of application: P.O. Box 831 07.02.2007 Bulletin 2007/06 2100 Copenhagen Ø (DK) (60) Divisional application: (56) References cited: 08011577.7 / 1 980 242 EP-A- 1 260 225 EP-A- 1 380 301 WO-A-01/52857 WO-A-20/04022065 (73) Proprietor: Bayer Schering Pharma WO-A-20/04041289 US-A- 5 569 652 Aktiengesellschaft US-A- 5 656 622 US-A- 5 789 442 13353 Berlin (DE) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations.
    [Show full text]
  • )&F1y3x PHARMACEUTICAL APPENDIX to THE
    )&f1y3X PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE )&f1y3X PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 3 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. Product CAS No. Product CAS No. ABAMECTIN 65195-55-3 ACTODIGIN 36983-69-4 ABANOQUIL 90402-40-7 ADAFENOXATE 82168-26-1 ABCIXIMAB 143653-53-6 ADAMEXINE 54785-02-3 ABECARNIL 111841-85-1 ADAPALENE 106685-40-9 ABITESARTAN 137882-98-5 ADAPROLOL 101479-70-3 ABLUKAST 96566-25-5 ADATANSERIN 127266-56-2 ABUNIDAZOLE 91017-58-2 ADEFOVIR 106941-25-7 ACADESINE 2627-69-2 ADELMIDROL 1675-66-7 ACAMPROSATE 77337-76-9 ADEMETIONINE 17176-17-9 ACAPRAZINE 55485-20-6 ADENOSINE PHOSPHATE 61-19-8 ACARBOSE 56180-94-0 ADIBENDAN 100510-33-6 ACEBROCHOL 514-50-1 ADICILLIN 525-94-0 ACEBURIC ACID 26976-72-7 ADIMOLOL 78459-19-5 ACEBUTOLOL 37517-30-9 ADINAZOLAM 37115-32-5 ACECAINIDE 32795-44-1 ADIPHENINE 64-95-9 ACECARBROMAL 77-66-7 ADIPIODONE 606-17-7 ACECLIDINE 827-61-2 ADITEREN 56066-19-4 ACECLOFENAC 89796-99-6 ADITOPRIM 56066-63-8 ACEDAPSONE 77-46-3 ADOSOPINE 88124-26-9 ACEDIASULFONE SODIUM 127-60-6 ADOZELESIN 110314-48-2 ACEDOBEN 556-08-1 ADRAFINIL 63547-13-7 ACEFLURANOL 80595-73-9 ADRENALONE
    [Show full text]
  • FIELD Study Revealed Fenofibrate Reduced Need for Laser Treatment for Diabetic Retinopathy by Anthony C
    Supplement to Supported by an unrestricted educational grant from Abbott Laboratories March/April 2008 FIELD Study Revealed Fenofibrate Reduced Need for Laser Treatment for Diabetic Retinopathy By Anthony C. Keech, MBBS, Msc Epid, FRANZCS, FRACP; and Paul Mitchell, MBBS(Hons), MD, PhD, FRANZCO, FRACS, FRCOphth, FAFPHM This agent’s mechanism of benefit in diabetic retinopathy appears to go beyond its effects on lipid concentration or blood pressure, and this potential mechanism of action operates even when glycemic control and blood pressure levels are within goal. ABSTRACT icant relative reduction was seen of almost one-third in PURPOSE the rate of first laser application for retinopathy after The FIELD (Fenofibrate Intervention and Event an average treatment duration of 5 years with fenofi- Lowering in Diabetes) study sought to investigate brate 200 mg/day. whether long-term lipid-lowering therapy with fenofi- In this report, we detail the effects of fenofibrate brate would reduce macro- and microvascular compli- administration on ophthalmic microvascular compli- cations among patients with type 2 diabetes. We previ- cations and attempt to clarify some of the underlying ously reported that in type 2 diabetes patients with pathologies being addressed among patients undergo- adequate glycemic and blood pressure control, a signif- ing laser treatment. Jointly sponsored by The Dulaney Foundation and Retina Today MARCH/APRIL 2008 I SUPPLEMENT TO RETINA TODAY I 1 FIELD Study Revealed Fenofibrate Reduced Need for Laser Treatment for Diabetic Retinopathy Jointly sponsored by The Dulaney Foundation and Retina Today. Release date: April 2008. Expiration date: April 2009. This continuing medical education activity is supported by an unrestricted educational grant from Abbott Laboratories.
    [Show full text]
  • G Genito Urinary System and Sex Hormones
    WHO/EMP/RHT/TSN/2018.2 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. Learning clinical pharmacology with the use of INNs and their stems. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.2). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data. CIP data are available at http://apps.who.int/iris. Sales, rights and licensing. To purchase WHO publications, see http://apps.who.int/bookorders. To submit requests for commercial use and queries on rights and licensing, see http://www.who.int/about/licensing.
    [Show full text]
  • 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.
    [Show full text]
  • Disease Progression and Pharmacological Intervention in a Nutrient‑Defcient Rat Model of Nonalcoholic Steatohepatitis
    Digestive Diseases and Sciences https://doi.org/10.1007/s10620-018-5395-7 ORIGINAL ARTICLE Disease Progression and Pharmacological Intervention in a Nutrient‑Defcient Rat Model of Nonalcoholic Steatohepatitis Kirstine S. Tølbøl1,3,4 · Birgit Stierstorfer2 · Jörg F. Rippmann2 · Sanne S. Veidal1 · Kristofer T. G. Rigbolt1 · Tanja Schönberger2 · Matthew P. Gillum4 · Henrik H. Hansen1 · Niels Vrang1 · Jacob Jelsing1 · Michael Feigh1 · Andre Broermann2 Received: 14 June 2018 / Accepted: 22 November 2018 © The Author(s) 2018 Abstract Background There is a marked need for improved animal models of nonalcoholic steatohepatitis (NASH) to facilitate the development of more efcacious drug therapies for the disease. Methods Here, we investigated the development of fbrotic NASH in male Wistar rats fed a choline-defcient L-amino acid- defned (CDAA) diet with or without cholesterol supplementation for subsequent assessment of drug treatment efcacy in NASH biopsy-confrmed rats. The metabolic profle and liver histopathology were evaluated after 4, 8, and 12 weeks of dieting. Subsequently, rats with biopsy-confrmed NASH were selected for pharmacological intervention with vehicle, elafbranor (30 mg/kg/day) or obeticholic acid (OCA, 30 mg/kg/day) for 5 weeks. Results The CDAA diet led to marked hepatomegaly and fbrosis already after 4 weeks of feeding, with further progression of collagen deposition and fbrogenesis-associated gene expression during the 12-week feeding period. Cholesterol supple- mentation enhanced the stimulatory efect of CDAA on gene transcripts associated with fbrogenesis without signifcantly increasing collagen deposition. Pharmacological intervention with elafbranor, but not OCA, signifcantly reduced stea- tohepatitis scores, and fbrosis-associated gene expression, however, was unable to prevent progression in fbrosis scores.
    [Show full text]
  • Albiglutide Needs Greater Accuracy from Remaining Shots on Goal
    November 18, 2011 Albiglutide needs greater accuracy from remaining shots on goal Evaluate Vantage Victoza is looking increasingly bullet-proof. Novo Nordisk’s once-daily GLP-1 agonist proved superior to GlaxoSmithKline’s once-weekly version, albiglutide, in reducing blood glucose while also showing significant weight loss advantages in type II diabetics. This follows a similar win for Victoza against Amylin Pharmaceuticals’ once-weekly challenger in Bydureon (Amylin scores own goal in Bydureon vs Victoza head-to- head study, March 3, 2011). Albiglutide still has a number of shots on goal – data this week from the Harmony 7 trial was the first from eight phase III studies all nearing completion – with a head-to-head against Merck & Co’s DPP-IV inhibitor Januvia probably the most significant in terms of determining albiglutide’s future role and potential in the diabetes market. Although expectations have never been that high, Glaxo’s product had an opportunity to capitalise on the setbacks to Byetta, Bydureon and Roche’s once-weekly taspoglutide – this first trial read out suggests that opportunity will be limited at best or missed altogether. Playing catch up Glaxo’s decision almost three years ago to embark on an extensive phase III programme for albiglutide, branded Syncria at the time, was seen as a bit of a gamble (Glaxo makes brave decision with phase III trials for Syncria, February 17, 2009). Safety concerns about Amylin’s twice-daily Byetta, the only approved GLP-1 agonist at the time, and the fact albiglutide had a lot of ground to make up on Bydureon and taspoglutide, suggested an uphill struggle for Glaxo’s product which was licensed from Human Genome Sciences in 2004.
    [Show full text]
  • Profile Profile Uses and Administration Adverse Effects And
    Etacrynic Acid/Ezetimibe 1379 unchanged and partly in the form of metabolites. It is Efortil; Etilefril; Chile: Elfortilt; Fin.: Elfortil; Fr.: Effortil; Ger.: over 10 years, may be given ezetimibe for the same indica­ extensively bound to plasma proteins. Bioflutin; Effortil; Etil; Pholdyston; Thomasin; Gr.: Effortil; tions and at the same doses as in adults (see above). ' Efortil; Ita/. : Elfortil; Jpn: Effortil; Mex.: Effortil; Quimtatil; Pol.: Effortil; Port.: Effortil; S.Afr.: Effortilt; Spain: Efortil; Swed.: Hyperlipidaemias. Ezetimibe inhibits the absorption of �:.�!?.�.��.!��-��--·········································································· Effortil; Switz. : Effortil; Thai.: Buracard; Circula; Circuman; dietary cholesterol' and, although there is a compensatory Proprietary Preparations (details are given in Volume B) Venez. : Elfortilt; Effrine; Efxine; Hyposia; Hyprosiat; Effontil. increase in cholesterol synthesis in the liver.' overall Single-ingredient Preparations. Austral.: Edecrin; Canad.: Multi-ingredient Preparations. Austria: Agilan; Amphodynt; plasma LDL-cholesterol concentrations are reduced.2 Ezeti­ Edecrin; Hung.: Uregyt; Ita!. : Reomax; Rus.: Uregyt (Ypei"HT); Effortil camp; Hypodynt; Influbenet; Ger.: Dibydergot plus; mibe may be used alone' in the management of hyperlipi­ Ukr.: Uregyt (YperHT); USA: Edecrin. Effortil plust; Switz.: Dibydergot plust; Elfortil plust. daentias (p. 1248.1) but use with lipid regulating drugs Phannacopoeial Preparations that act by reducing cholesterol synthesis may
    [Show full text]
  • 07-101 Phrma NM Heart
    200R9ep ort M EDICINES IN D EVELOPMENT FOR Heart Disease and Stroke PRESENTED BY AMERICA ’ S PHARMACEUTICAL RESEARCH COMPANIES More Than 300 Medicines in Testing for Two Leading Causes of Death in Americans harmaceutical and biotechnology researchers are MEDICINES IN DEVELOPMENT FOR HEART DISEASE AND STROKE * working on 312 medicines for two of the three Pleading causes of death in Americans—heart disease Acute Coronary Syndrome 21 and stroke—keeping up the momentum of drug discovery Adjunctive Therapies 5 Angina 2 that has helped cut deaths from these diseases by more Arrhythmia/Atrial Fibrillation 20 than a quarter between 1999 and 2005. All of the medicines Atherosclerosis 18 are either in clinical trials or awaiting approval by the Coronary Artery Disease 11 Heart Attack 16 Food and Drug Administration. Heart Failure 33 Hypertension 36 According to the National Center for Health Statistics, Imaging Agents 10 heart disease has topped the list of killer diseases every Ischemic Disorders 18 Lipid Disorders 26 year but one since 1900. (The exception was 1918, Peripheral Vascular Disease 27 when an influenza epidemic killed more than 450,000 Pulmonary Vascular Disease 16 Stroke Americans.) In 2002, cancer surpassed heart disease as 22 Thrombosis 40 the top killer of Americans under age 85, who account Other 39 for 98.4 percent of the U.S. population. Stroke is the *S ome medicines are listed in more than one category. third leading cause of death. Thanks in large part to new drug treatments, death rates cost of these diseases to American society is more than from heart disease and stroke are falling.
    [Show full text]
  • A61p1/16 (2006.01) A61p3/00 (2006.01) Km, Ml, Mr, Ne, Sn, Td, Tg)
    ( (51) International Patent Classification: TR), OAPI (BF, BJ, CF, CG, Cl, CM, GA, GN, GQ, GW, A61P1/16 (2006.01) A61P3/00 (2006.01) KM, ML, MR, NE, SN, TD, TG). A61K 31/192 (2006.01) C07C 321/28 (2006.01) Declarations under Rule 4.17: (21) International Application Number: — as to the applicant's entitlement to claim the priority of the PCT/IB2020/000808 earlier application (Rule 4.17(iii)) (22) International Filing Date: Published: 25 September 2020 (25.09.2020) — with international search report (Art. 21(3)) (25) Filing Language: English — before the expiration of the time limit for amending the claims and to be republished in the event of receipt of (26) Publication Language: English amendments (Rule 48.2(h)) (30) Priority Data: 62/906,288 26 September 2019 (26.09.2019) US (71) Applicant: ABIONYX PHARMA SA [FR/FR] ; 33-43 Av¬ enue Georges Pompidou, Batiment D, 31130 Bahna (FR). (72) Inventor: DASSEUX, Jean-Louis, Henri; 7 Allees Charles Malpel, Bat. B, 31300 Toulouse (FR). (74) Agent: HOFFMANN EITLE PATENT- UND RECHTSANWALTE PARTMBB, ASSOCIATION NO. 151; Arabellastrasse 30, 81925 Munich (DE). (81) Designated States (unless otherwise indicated, for every kind of national protection available) : AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, IT, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, WS, ZA, ZM, ZW.
    [Show full text]
  • Joint Assessment Report Was Discussed by the Phvwp at Its Meeting in July 2007 and Finalised in September 2007
    ASSESSMENT REPORT on the benefit:risk of fibrates EXECUTIVE SUMMARY 1. BACKGROUND In the light of the established role of statins in the primary and secondary prevention of cardiovascular disease (CVD) and safety concerns arising from the use of fibrates, the CHMP Pharmacovigilance Working Party (PhVWP) agreed to undertake a benefit:risk assessment of this class of medicines. The objective was to establish the current place of fibrates in the treatment of cardiovascular and dyslipidaemic diseases, and in diabetes mellitus; also to provide recommendations regarding amendments of the Summary of Product Characteristics (SPC), as necessary. Fibrates exert their effects mainly by activating the peroxisome proliferator-activated receptor-alpha (PPAR-alpha). Unique in this class, bezafibrate is an agonist for all three PPAR isoforms alpha, gamma, and delta. Fibrates have been shown to reduce plasma triglycerides by 30% to 50% and raise the level of high density lipoprotein cholesterol (HDL- C) by 2% to 20%. Their effect on low density lipoprotein cholesterol (LDL-C) is variable, ranging from no effect to a small decrease of the order of 10%. Today there are four licensed fibrates: bezafibrate, fenofibrate, gemfibrozil and ciprofibrate. Their currently approved indications are quite broad and in many cases still use the old Fredrickson classification for dyslipidaemias. 2. METHODOLOGY In February 2006 a List of Questions was agreed by the PhVWP for the Marketing Authorisation Holders (MAHs) of medicinal products containing one of the four currently licensed fibrates (Annex 1). Other clofibrate-containing medicinal products (e.g. etofibrate, etofyllinclofibrate) were excluded from this class review, since these are available only in a few member states via national marketing authorizations.
    [Show full text]
  • Combination Use of Insulin and Incretins in Type 2 Diabetes
    Canadian Agency for Agence canadienne Drugs and Technologies des médicaments et des in Health technologies de la santé CADTH Optimal Use Report Volume 3, Issue 1C Combination Use of Insulin and July 2013 Incretins in Type 2 Diabetes Supporting Informed Decisions This report is prepared by the Canadian Agency for Drugs and Technologies in Health (CADTH). The report contains a comprehensive review of the existing public literature, studies, materials, and other information and documentation (collectively the “source documentation”) available to CADTH at the time of report preparation. The information in this report is intended to help Canadian health care decision-makers, health care professionals, health systems leaders, and policy-makers make well-informed decisions and thereby improve the quality of health care services. The information in this report should not be used as a substitute for the application of clinical judgment in respect of the care of a particular patient or other professional judgment in any decision-making process, nor is it intended to replace professional medical advice. While CADTH has taken care in the preparation of this document to ensure that its contents are accurate, complete, and up to date as of the date of publication, CADTH does not make any guarantee to that effect. CADTH is not responsible for the quality, currency, propriety, accuracy, or reasonableness of any statements, information, or conclusions contained in the source documentation. CADTH is not responsible for any errors or omissions or injury, loss, or damage arising from or relating to the use (or misuse) of any information, statements, or conclusions contained in or implied by the information in this document or in any of the source documentation.
    [Show full text]