DOCSLIB.ORG

COPD Presented by America’S Biopharmaceutical Research Companies

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
COPD Presented by America’S Biopharmaceutical Research Companies 2012 REPO Medicines in Development COPD R PRESENTED BY AMERICA’S BIOPHARMACEUTICAL T RESEARCH COMPANIES More Than 50 Medicines in Pipeline for Third Leading Cause of Death in the United States COPD Prevalence in the COPD affects United States more than 13 million (in millions) American adults; 13.1 more than 120,000 die from the disease each year 10.5 9.8 Today, more than 13 million American adults are America’s biopharmaceutical researchers are suffering from chronic obstructive pulmonary dis- exploring various new ways to attack this devas- ease (COPD), leading to limitations in their ability tating disease. Examples of new approaches to to work, exercise and perform normal social activ- treating COPD include: ity. COPD, a chronic lower respiratory disease • An adult stem cell therapy that targets a that includes chronic bronchitis and emphysema, protein in the blood that is often elevated 7.1 is characterized by obstruction of airflow to the in COPD. lungs that interferes with normal breathing. • A monoclonal antibody that acts on America’s biopharmaceutical research compa- IL-1 receptors involved in inflammatory nies have 54 medicines for treating COPD in the conditions. later stages of the pipeline, meaning they are either in clinical trials or awaiting FDA review. • A medicine that targets the underlying inflammation in COPD. Each year, more than 120,000 Americans die from the disease. In addition to robbing The quest for new medicines is intense and millions of patients of their ability to breathe financially risky. Each new medicine costs, normally, COPD costs the nation approximately on average, more than $1 billion and takes $49.9 billion, including direct healthcare costs 10 to 15 years to develop. But new scientific and other indirect costs, according to the advances are increasing our knowledge, and National Institutes of Health. researchers are using every cutting-edge tool While smoking is the main risk factor for COPD, at their disposal to find new treatments and and nearly 90 percent of COPD deaths are potential cures. 1980 1990 2000 2008 caused by smoking, other causes include air pollution, second-hand smoke, occupational Source: U.S. Centers for Disease dusts and chemicals, hereditary and childhood Control and Prevention respiratory infections. Medicines in Development for COPD CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) Product Name Sponsor Indication Development Status* aclidinium Almirall chronic obstructive pulmonary application submitted inhalation Barcelona, Spain disease (COPD) (800) 678-1605 Forest Laboratories New York, NY aclidinium/formoterol Almirall COPD Phase III inhalation Barcelona, Spain (800) 678-1605 Forest Laboratories New York, NY AM211 Panmira Pharmaceuticals COPD Phase I San Diego, CA (858) 875-4810 AZD1981 AstraZeneca COPD Phase II (CRTh2 receptor antagonist) Wilmington, DE (800) 236-9933 AZD 2115 AstraZeneca COPD Phase I (MABA) Wilmington, DE (800) 236-9933 AZD2423 AstraZeneca COPD Phase II (CCR2b antagonist) Wilmington, DE (800) 236-9933 AZD3199 AstraZeneca COPD Phase II (iLABA) Wilmington, DE (800) 236-9933 AZD5069 AstraZeneca COPD Phase II (CXCR2) Wilmington, DE (800) 236-9933 AZD5423 AstraZeneca COPD Phase II (inhaled SEGRA) Wilmington, DE (800) 236-9933 AZD8683 AstraZeneca COPD Phase I (muscarinic antagonist) Wilmington, DE (800) 236-9933 BCT197 Novartis Pharmaceuticals COPD Phase II East Hanover, NJ (888) 669-6682 BI-137882 Boehringer Ingelheim COPD Phase I Pharmaceuticals (800) 243-0127 Ridgefield, CT BIO-11006 BioMarck Pharmaceuticals COPD Phase II Durham, NC www.biomarck.com Dulera® Merck COPD application submitted mometasone/formoterol Whitehouse Station, NJ (800) 672-6372 * For more information about a specific medicine in this report, please call the telephone number listed. 2 Medicines in Development COPD 2012 Medicines in Development for COPD CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) Product Name Sponsor Indication Development Status* EP-101 Elevation Pharmaceuticals COPD Phase II (LAMA) San Diego, CA (858) 436-1616 EP-102 Elevation Pharmaceuticals COPD Phase II (LAMA/LABA) San Diego, CA (858) 436-1616 EPI-12323 EpiGenesis Pharmaceuticals COPD Phase II Cranbury, NJ (609) 409-6080 formoterol/fluticasone Dey Pharma COPD Phase II fixed-dose combination Basking Ridge, NJ (908) 542-1999 (inhalation) GSK256066 GlaxoSmithKline COPD Phase II (inhaled PDE4 inhibitor) Rsch. Triangle Park, NC (888) 825-5249 GSK573719 GlaxoSmithKline COPD Phase III (muscarinic acetylcholine Rsch. Triangle Park, NC (888) 825-5249 antagonist) GSK573719/vilanterol GlaxoSmithKline COPD Phase III (muscarinic acetylcholine Rsch. Triangle Park, NC (888) 825-5249 antagonist/long-acting Theravance (877) 275-8479 beta2 agonist) South San Francisco, CA GSK610677 GlaxoSmithKline COPD Phase I (inhaled p38 kinase inhibitor) Rsch. Triangle Park, NC (888) 825-5249 GSK961081 GlaxoSmithKline COPD Phase II (muscarinic antagonist/ Rsch. Triangle Park, NC (888) 825-5249 beta2 agonist) Theravance (877) 275-8479 South San Francisco, CA GSK1325756 GlaxoSmithKline COPD Phase I (chemokine receptor Rsch. Triangle Park, NC (888) 825-5249 antagonist-2) GSK2245840 GlaxoSmithKline COPD Phase I (SIRT1 activator) Rsch. Triangle Park, NC (888) 825-5249 Ilaris® Novartis Pharmaceuticals COPD Phase I/II completed canakinumab East Hanover, NJ (888) 669-6682 LAS 100977 Almirall COPD Phase II (LABA) Barcelona, Spain (800) 678-1605 Forest Laboratories New York, NY levosalbutamol/ipratropium Sunovion Pharmaceuticals COPD Phase II inhalation solution Marlborough, MA (508) 481-6700 Medicines in Development COPD 2012 3 Medicines in Development for COPD CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) Product Name Sponsor Indication Development Status* losmapimod GlaxoSmithKline COPD Phase II (oral p38 kinase inhibitor) Rsch. Triangle Park, NC (888) 825-5249 MEDI-2338 MedImmune COPD Phase I (anti-IL-18 mAb) Gaithersburg, MD (301) 398-0000 MEDI-8968 MedImmune COPD Phase I (anti-IL-1R) Gaithersburg, MD (301) 398-0000 MK-7123 Ligand Pharmaceuticals COPD Phase II (navarixin) La Jolla, CA (858) 550-7500 Merck (800) 672-6372 Whitehouse Station, NJ MN-166 MediciNova COPD Phase I completed (ibudilast) San Diego, CA (858) 373-1500 MN-221 MediciNova COPD Phase I (bedoradrine) San Diego, CA (858) 373-1500 NVA237 Novartis Pharmaceuticals COPD Phase III (glycopyrrolate inhalation) East Hanover, NJ (888) 669-6682 O-desulfated heparin ParinGenix COPD Phase II intravenous Tucson, AZ (617) 480-5068 olodaterol Boehringer Ingelheim COPD Phase III Pharmaceuticals (800) 243-0127 Ridgefield, CT olodaterol/tiotropium bromide Boehringer Ingelheim COPD Phase II Pharmaceuticals (800) 243-0127 Ridgefield, CT paclitaxel-loaded stent Broncus Technologies emphysema Phase III Mountain View, CA (650) 428-1600 PF-03715455 Pfizer COPD Phase I New York, NY (860) 732-5156 PH-797804 Pfizer COPD Phase II New York, NY (860) 732-5156 Prochymal® Osiris Therapeutics COPD Phase II remestemcel-L Columbia, MD (443) 545-1800 4 Medicines in Development COPD 2012 Medicines in Development for COPD CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) Product Name Sponsor Indication Development Status* PT001 Pearl Therapeutics COPD Phase II (glycopyrrolate inhalation Redwood City, CA (650) 305-2600 aerosol) PT003 Pearl Therapeutics COPD Phase II (glycopyrrolate/formoterol Redwood City, CA (650) 305-2600 inhalation aerosol) PT005 Pearl Therapeutics COPD Phase II (formoterol inhalation aerosol) Redwood City, CA (650) 305-2600 PUR118 Pulmatrix COPD Phase I Lexington, MA (781) 357-2333 QMF149 Novartis Pharmaceuticals COPD Phase II (indacaterol/mometasone) East Hanover, NJ (888) 669-6682 QVA149 Novartis Pharmaceuticals COPD Phase III (glycopyrrolate/indacaterol East Hanover, NJ (888) 669-6682 inhalation) Relovair™ GlaxoSmithKline COPD Phase III vilanterol/fluticasone furoate Rsch. Triangle Park, NC (888) 825-5249 Theravance (877) 275-8479 South San Francisco, CA RV568 RespiVert COPD Phase II London, England (800) 526-7736 Janssen Research & Development Raritan, NJ TD-4208 Theravance COPD Phase II (LAMA) South San Francisco, CA (877) 275-8479 tetomilast Otsuka America Pharmaceutical COPD Phase II Rockville, MD (800) 562-3974 vilanterol GlaxoSmithKline COPD Phase III (long-acting beta2 agonist) Rsch. Triangle Park, NC (888) 825-5249 Veldona® Amarillo Biosciences COPD (chronic coughing) Phase II interferon-alpha Amarillo, TX www.amarbio.com Medicines in Development COPD 2012 5 Glossary application submitted—Application for emphysema—An enlargement of the tiny air Phase III—Extensive clinical trials to demon- marketing has been submitted to the Food and sacs of the lungs (alveoli) and the destruction strate safety and efficacy in humans. Drug Administration (FDA). of their walls, which causes structural and permanent reduction of airflow. chronic obstructive pulmonary disease (COPD)—A group of lung diseases, icluding Phase I—Safety testing and pharmacological chronic bronchitis and emphysema, in which profiling in humans. there is a persistent disruption of airflow out of the lungs and eventual hypoxemia (low level of Phase II—Effectiveness and safety testing in oxygen in the blood). humans. The content of this report has been obtained through public, government and industry sources, and the Adis “R&D Insight” database based on the latest information. Report current as of January 12, 2012. The information in this report may not be comprehensive. For more specific information about a particular product, contact the individual company directly or go to www.clinicaltrials.gov. The entire series of Medicines
Load more

Recommended publications
  • Chapter Introduction
    VU Research Portal Trypanosoma brucei phosphodiesterase B1 as a drug target for Human African Trypanosomiasis Jansen, C.J.W. 2015 document version Publisher's PDF, also known as Version of record Link to publication in VU Research Portal citation for published version (APA) Jansen, C. J. W. (2015). Trypanosoma brucei phosphodiesterase B1 as a drug target for Human African Trypanosomiasis. General rights Copyright and moral rights for the publications made accessible in the public portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognise and abide by the legal requirements associated with these rights. • Users may download and print one copy of any publication from the public portal for the purpose of private study or research. • You may not further distribute the material or use it for any profit-making activity or commercial gain • You may freely distribute the URL identifying the publication in the public portal ? Take down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. E-mail address: [email protected] Download date: 05. Oct. 2021 An introduction into phosphodiesterases and their potential role as drug targets for neglected diseases Chapter 1 4 CHAPTER 1 1.1 Human African Trypanosomiasis Human African Trypanomiasis (HAT), also known as African sleeping sickness, is a deadly infectious disease caused by the kinetoplastid Trypanosoma
    [Show full text]
  • Annual Report 2016
    Annexes to the annual report of the European Medicines Agency 2016 Annex 1 – Members of the Management Board ............................................................... 2 Annex 2 - Members of the Committee for Medicinal Products for Human Use ...................... 4 Annex 3 – Members of the Pharmacovigilance Risk Assessment Committee ........................ 6 Annex 4 – Members of the Committee for Medicinal Products for Veterinary Use ................. 8 Annex 5 – Members of the Committee on Orphan Medicinal Products .............................. 10 Annex 6 – Members of the Committee on Herbal Medicinal Products ................................ 12 Annex 7 – Committee for Advanced Therapies .............................................................. 14 Annex 8 – Members of the Paediatric Committee .......................................................... 16 Annex 9 – Working parties and working groups ............................................................ 18 Annex 10 – CHMP opinions: initial evaluations and extensions of therapeutic indication ..... 24 Annex 10a – Guidelines and concept papers adopted by CHMP in 2016 ............................ 25 Annex 11 – CVMP opinions in 2016 on medicinal products for veterinary use .................... 33 Annex 11a – 2016 CVMP opinions on extensions of indication for medicinal products for veterinary use .......................................................................................................... 39 Annex 11b – Guidelines and concept papers adopted by CVMP in 2016 ...........................
    [Show full text]
  • Effect of Ibudilast: a Novel Antiasthmatic Agent, on Airway Hypersensitivity in Bronchial Asthma
    Journal of Asthma, 29(4), 245-252 (1992) Effect of Ibudilast: A Novel Antiasthmatic Agent, on Airway Hypersensitivity in Bronchial Asthma Akira Kawasaki, M.D., Kiyoshi Hoshino, M.D., Rokuo Osaki, M.D., Yutaka Mizushima, M.D., and Saburo Yano, M.D. First Department of Internal Medicine Toyania Medical and Pharmaceutical University 2630 Sugitani Toyama, Japan 930-01 ABSTRACT Ibudilast, a unique agent with vasodilating and anti- allergic actions, was studied in 13 asthmatics for its ef- fect on airway hypersensitivity to histamine inhalation. For personal use only. The PC20 values improved significantly from 355.6 to 620.5 &mi at 3 months and further to 731.4 pghl at 6 months following the initial treatment with ibudilast (20 mg twice daily orally). In addition, the severity of the at- tacks decreased significantly. Improvements in the PC2,, and asthmatic symptoms also were observed in the disodium c:hrornoglycate group, but these were equal to or lesser than those in the ibudilast group. No improve- ment was observed in the untreated control group. These J Asthma Downloaded from informahealthcare.com by Yeshiva University on 09/15/14 results suggest that ibudilast would be an effective agent for improving nonspecific airway hypersensitivity in asthmatics. INTRODUCTION and ibudilast have been developed in rapid succession in Japan and used for the treat- After the introduction of disodium cromo- ment of bronchial asthma. Among them, glycate (DSCG) (11, many so-called “anti- ibudilast seems to be especially unique, for allergic agents” such as tranilast (21, ketotifen vasodilating and antiallergic effects (7 3). (3), azelastine (4), amoxanox (51, repirinast (6), Therefore, this agent is used clinically for the 245 Copyright 0 1992 by Marcel Dekker, Inc.
    [Show full text]
  • Patent Application Publication ( 10 ) Pub . No . : US 2019 / 0192440 A1
    US 20190192440A1 (19 ) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2019 /0192440 A1 LI (43 ) Pub . Date : Jun . 27 , 2019 ( 54 ) ORAL DRUG DOSAGE FORM COMPRISING Publication Classification DRUG IN THE FORM OF NANOPARTICLES (51 ) Int . CI. A61K 9 / 20 (2006 .01 ) ( 71 ) Applicant: Triastek , Inc. , Nanjing ( CN ) A61K 9 /00 ( 2006 . 01) A61K 31/ 192 ( 2006 .01 ) (72 ) Inventor : Xiaoling LI , Dublin , CA (US ) A61K 9 / 24 ( 2006 .01 ) ( 52 ) U . S . CI. ( 21 ) Appl. No. : 16 /289 ,499 CPC . .. .. A61K 9 /2031 (2013 . 01 ) ; A61K 9 /0065 ( 22 ) Filed : Feb . 28 , 2019 (2013 .01 ) ; A61K 9 / 209 ( 2013 .01 ) ; A61K 9 /2027 ( 2013 .01 ) ; A61K 31/ 192 ( 2013. 01 ) ; Related U . S . Application Data A61K 9 /2072 ( 2013 .01 ) (63 ) Continuation of application No. 16 /028 ,305 , filed on Jul. 5 , 2018 , now Pat . No . 10 , 258 ,575 , which is a (57 ) ABSTRACT continuation of application No . 15 / 173 ,596 , filed on The present disclosure provides a stable solid pharmaceuti Jun . 3 , 2016 . cal dosage form for oral administration . The dosage form (60 ) Provisional application No . 62 /313 ,092 , filed on Mar. includes a substrate that forms at least one compartment and 24 , 2016 , provisional application No . 62 / 296 , 087 , a drug content loaded into the compartment. The dosage filed on Feb . 17 , 2016 , provisional application No . form is so designed that the active pharmaceutical ingredient 62 / 170, 645 , filed on Jun . 3 , 2015 . of the drug content is released in a controlled manner. Patent Application Publication Jun . 27 , 2019 Sheet 1 of 20 US 2019 /0192440 A1 FIG .
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9.254.262 B2 Casado Et Al
    USOO925.4262B2 (12) United States Patent (10) Patent No.: US 9.254.262 B2 Casado et al. (45) Date of Patent: *Feb. 9, 2016 (54) DOSAGE AND FORMULATION 5,290,815 A 3, 1994 Johnson et al. 5.435.301 A 7/1995 Herold et al. (71) Applicant: Almirall, S.A., Barcelona (ES) 5,569,4475,507,281 A 10,4/1996 1996 LeeKuhnel et al. et al. 5575280 A 11/1996 Guote et al. (72) Inventors: Rosa Lamarca Casado, Barcelona (ES); 5,610,163 A 3, 1997 SA et al. Gonzalo De Miquel Serra, Barcelona 5,617.845 A 4/1997 Posset al. (ES) 5,654,314 A 8, 1997 Banholzer et al. 5,676,930 A 10/1997 Jager et al. (73) Assignee: Almirall, S.A., Barcelona (ES) 5,885,8345,685,294 A 1 3/19991/1997 GupteEpstein et al. 5,962,505 A 10, 1999 Bob tal. (*) Notice: Subject to any disclaimer, the term of this 5,964,416 A 10, 1999 E. a patent is extended or adjusted under 35 6,150,415. A 1 1/2000 Hammocket al. U.S.C. 154(b) by 0 days. 6,299,861 B1 10/2001 Banholzer et al. 6,299,863 B1 10/2001 Aberg et al. This patent is Subject to a terminal dis 6,402,055 B1 6/2002 Jaeger et al. claimer. 6.410,563 B1 6/2002 Deschenes et al. 6,423.298 B2 7/2002 McNamara et al. 6,433,027 B1 8/2002 Bozung et al. (21) Appl. No.: 13/672,893 6,455,524 B1 9/2002 Bozung et al.
    [Show full text]
  • 1 Elevated Intracellular Camp Concentration Mediates Growth
    Elevated intracellular cAMP concentration mediates growth suppression in glioma cells Dewi Safitri1,2, Matthew Harris1, Harriet Potter1, Ho Yan Yeung1, Ian Winfield1, Liliya Kopanitsa3, Fredrik Svensson3,4, Taufiq Rahman1, Matthew T Harper1, David Bailey3, Graham Ladds1, *. 1 Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge CB2 1PD, United Kingdom 2 Pharmacology and Clinical Pharmacy Research Group, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia 3 IOTA Pharmaceuticals Ltd, Cambridge University Biomedical Innovation Hub, Clifford Allbutt Building, Hills Road, Cambridge CB2 0AH, United Kingdom 4 Computational Medicinal Chemistry, Alzheimer’s Research UK UCL Drug Discovery Institute, The Cruciform Building, Gower Street, London, WC1E 6BT *Corresponding author: Dr Graham Ladds, Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge, CB2 1PD Tel; +44 (0) 1223 334020. Email: [email protected]. ABSTRACT Supressed levels of intracellular cAMP have been associated with malignancy. Thus, elevating cAMP through activation of adenylyl cyclase (AC) or by inhibition of phosphodiesterase (PDE) may be therapeutically beneficial. Here, we demonstrate that elevated cAMP levels suppress growth in C6 cells (a model of glioma) through treatment with forskolin, an AC activator, or a range of small molecule PDE inhibitors 1 with differing selectivity profiles. Forskolin suppressed cell growth in a PKA-dependent manner by inducing a G2/M phase cell cycle arrest. In contrast, trequinsin (a non- selective PDE2/3/7 inhibitor), not only inhibited cell growth via PKA, but also stimulated (independent of PKA) caspase-3/-7 and induced an aneuploidy phenotype. Interestingly, a cocktail of individual PDE 2,3,7 inhibitors suppressed cell growth in a manner analogous to forskolin but not trequinsin.
    [Show full text]
  • Ibudilast for Alcohol Use Disorder: Study Protocol for a Phase II Randomized Clinical Trial Elizabeth M
    Burnette et al. Trials (2020) 21:779 https://doi.org/10.1186/s13063-020-04670-y STUDY PROTOCOL Open Access Ibudilast for alcohol use disorder: study protocol for a phase II randomized clinical trial Elizabeth M. Burnette1,2* , Wave-Ananda Baskerville1, Erica N. Grodin1 and Lara A. Ray1,2,3 Abstract Background: Alcohol use disorder (AUD) is a chronic and relapsing condition for which current pharmacological treatments are only modestly effective. The development of efficacious medications for AUD remains a high research priority with recent emphasis on identifying novel molecular targets for AUD treatment and to efficiently screen new compounds aimed at those targets. Ibudilast, a phosphodiesterase inhibitor, has been advanced as a novel addiction pharmacotherapy that targets neurotrophin signaling and neuroimmune function. Methods: This study will conduct a 12-week, double-blind, placebo controlled randomized clinical trial of ibudilast (50 mg BID) for AUD treatment. We will randomize 132 treatment-seeking men and women with current AUD. We will collect a number of alcohol consumption outcomes. Primary among these is percent heavy drinking days (PHDD); secondary drinking outcomes include drinks per day, drinks per drinking day, percent days abstinent, percent subjects with no heavy drinking days, and percent subjects abstinent, as well as measures of alcohol craving and negative mood. Additionally, participants will have the option to opt-in to a neuroimaging session in which we examine the effects of ibudilast on neural activation to psychosocial stress and alcohol cues. Finally, we will also collect plasma levels of proinflammatory markers, as well as subjective and biological (salivary cortisol) markers of stress response.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2003/0068365A1 Suvanprakorn Et Al
    US 2003.0068365A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0068365A1 Suvanprakorn et al. (43) Pub. Date: Apr. 10, 2003 (54) COMPOSITIONS AND METHODS FOR Related U.S. Application Data ADMINISTRATION OF ACTIVE AGENTS USING LIPOSOME BEADS (60) Provisional application No. 60/327,643, filed on Oct. 5, 2001. (76) Inventors: Pichit Suvanprakorn, Bangkok (TH); Tanusin Ploysangam, Bangkok (TH); Publication Classification Lerson Tanasugarn, Bangkok (TH); Suwalee Chandrkrachang, Bangkok (51) Int. Cl." .......................... A61K 9/127; A61K 35/78 (TH); Nardo Zaias, Miami Beach, FL (52) U.S. Cl. ............................................ 424/450; 424/725 (US) (57) ABSTRACT Correspondence Address: Law Office of Eric G. Masamori Compositions and methods for administration of active 6520 Ridgewood Drive agents encapsulated within liposome beads to enable a wider Castro Valley, CA 94.552 (US) range of delivery vehicles, to provide longer product shelf life, to allow multiple active agents within the composition, (21) Appl. No.: 10/264,205 to allow the controlled use of the active agents, to provide protected and designable release features and to provide (22) Filed: Oct. 3, 2002 Visual inspection for damage and inconsistency. US 2003/0068365A1 Apr. 10, 2003 COMPOSITIONS AND METHODS FOR toxic degradation of the products, leakage of the drug from ADMINISTRATION OF ACTIVE AGENTS USING the liposome and the modifications of the Size and morphol LPOSOME BEADS ogy of the phospholipid liposome vesicles through aggre gation and fusion. Liposome vesicles are known to be CROSS REFERENCE TO OTHER thermodynamically relatively unstable at room temperature APPLICATIONS and can Spontaneously fuse into larger, leSS Stable altered liposome forms.
    [Show full text]
  • Stembook 2018.Pdf
    The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © 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. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [Show full text]
  • Aminophylline Suppresses Stress-Induced Visceral Hypersensitivity and Defecation in Irritable Bowel Syndrome
    www.nature.com/scientificreports OPEN Aminophylline suppresses stress- induced visceral hypersensitivity and defecation in irritable bowel Received: 05 July 2016 Accepted: 05 December 2016 syndrome Published: 05 January 2017 Teita Asano1, Ken-ichiro Tanaka2, Arisa Tada3, Hikaru Shimamura3, Rikako Tanaka3, Hiroki Maruoka3, Mitsuko Takenaga1 & Tohru Mizushima4 Pharmacological therapy for irritable bowel syndrome (IBS) has not been established. In order to find candidate drugs for IBS with diarrhea (IBS-D), we screened a compound library of drugs clinically used for their ability to prevent stress-induced defecation and visceral hypersensitivity in rats. We selected the bronchodilator aminophylline from this library. Using a specific inhibitor for each subtype of adenosine receptors (ARs) and phosphodiesterases (PDEs), we found that both A2BARs and PDE4 are probably mediated the inhibitory effect of aminophylline on wrap restraint stress (WRS)-induced defecation. Aminophylline suppressed maternal separation- and acetic acid administration-induced visceral hypersensitivity to colorectal distension (CRD), which was mediated by both A2AARs and A2BARs. We propose that aminophylline is a candidate drug for IBS-D because of its efficacy in both of stress-induced defecation and visceral hypersensitivity, as we observed here, and because it is clinically safe. Irritable bowel syndrome (IBS) is characterized by chronic, recurrent abdominal pain and altered bowel habits (diarrhea or constipation) and is defined by symptom criteria and the absence of detectable organic disease1. The prevalence of IBS in the general population is remarkably high (approximately 11% of the world’s population), with the young displaying greater susceptibility1. Thus, although IBS is not life-threatening, it creates a large bur- den on global healthcare and causes a serious reduction in the quality of life2.
    [Show full text]
  • Elevated Intracellular Camp Concentration Mediates Growth Suppression in Glioma Cells
    bioRxiv preprint doi: https://doi.org/10.1101/718601; this version posted July 30, 2019. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. Elevated intracellular cAMP concentration mediates growth suppression in glioma cells Dewi Safitri1,2, Harriet Potter1, Matthew Harris1, Ian Winfield1, Liliya Kopanitsa3, Ho Yan Yeung1, Fredrik Svensson3,4, Taufiq Rahman1, Matthew T Harper1, David Bailey3, Graham Ladds1,5,*. 1 Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge CB2 1PD, United Kingdom 2 Pharmacology and Clinical Pharmacy Research Group, School of Pharmacy, Bandung Institute of Technology, Bandung 40534, Indonesia 3 IOTA Pharmaceuticals Ltd, Cambridge University Biomedical Innovation Hub, Clifford Allbutt Building, Hills Road, Cambridge CB2 0AH, United Kingdom 4 Computational Medicinal Chemistry, Alzheimer’s Research UK UCL Drug Discovery Institute, The Cruciform Building, Gower Street, London, WC1E 6BT 5 Lead Contact *Dr Graham Ladds, Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge, CB2 1PD Tel; +44 (0) 1223 334020. Email: [email protected]. SUMMARY Supressed levels of intracellular cAMP have been associated with malignancy. Thus, elevating cAMP through activation of adenylyl cyclase (AC) or by inhibition of phosphodiesterase (PDE) may be therapeutically beneficial. Here, we demonstrate that elevated cAMP levels suppress growth in C6 cells (a model of glioma) through treatment with forskolin, an AC activator, or a range of small molecule PDE inhibitors with differing selectivity profiles. Forskolin suppressed cell growth in a protein kinase A (PKA)-dependent manner by inducing a G2/M phase cell cycle arrest.
    [Show full text]
  • Ibudilast : a Review of Its Pharmacology, Efficacy and Safety in Respiratory and Neurological Disease
    Expert Opinion on Pharmacotherapy in press (EOOP-2009-0238.R1) Ibudilast : a review of its pharmacology, efficacy and safety in respiratory and neurological disease Rolan P MBBS MD FRACP Professor of Clinical Pharmacology* Discipline of Pharmacology, University of Adelaide, Adelaide 5005 Ph: +61-8-83034102 Fax: +61-8-82240685 Email: [email protected] Hutchinson MR BSc(Hons) PhD NHMRC CJ Martin Research Fellow Discipline of Pharmacology, University of Adelaide, Adelaide 5005 Ph: +61-8-83036086 Fax: +61-8-82240685 Johnson KW PhD Vice President, Research & Development, Avigen Inc. 1301 Harbor Bay Pkwy, Alameda, CA 94502, USA Ph: +1-510-748-7106 Fax: +1-510-748-4838 * Author for correspondence 1 Expert Opinion on Pharmacotherapy in press (EOOP-2009-0238.R1) Abstract Ibudilast is a relatively non-selective phosphodiesterase inhibitor which has been marketed for almost 20 years in Japan for treating asthma. More recently it has been found to have anti-inflammatory activity in both the peripheral immune system and in the central nervous system via glial cell attenuation. This CNS-directed anti-inflammatory activity is of potential use in the treatment of multiple sclerosis, neuropathic pain, and in the improved efficacy and safety of opioids by decreasing opioid tolerance, withdrawal and reinforcement. Its suitable pharmacokinetics and generally good tolerability make it a promising potential treatment for these conditions. Keywords (in alphabetical order) glia ibudilast multiple sclerosis neuropathic pain priming 2 Expert Opinion on Pharmacotherapy in press (EOOP-2009-0238.R1) 1. Introduction Ibudilast has been marketed for almost 2 decades in Japan for the treatment of asthma and post-stroke dizziness, presumably because of the bronchodilator and vasodilator effects of phosphodiesterase (PDE) inhibition attributed to the drug.
    [Show full text]