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Use and Cardiovascular Safety of Transdermal and Other Granisetron Preparations in Cancer Management
Cancer Management and Research Dovepress open access to scientific and medical research Open Access Full Text Article REVIEW Use and cardiovascular safety of transdermal and other granisetron preparations in cancer management 1 Jay W Mason Abstract: 5-HT3 antagonists have been available as oral and intravenous preparations for Thomas E Moon2 decades. The availability more recently of transdermal granisetron and the anticipated availability of a subcutaneous granisetron preparation have provided helpful alternatives to patients, and 1School of Medicine, University of Utah, Salt Lake City, UT, these preparations have been shown to have less potential to prolong QT than other drugs in 2Tarizona eHealth Services, Inc, the class. Emeryville, CA, USA Keywords: chemotherapy-induced nausea, vomiting, granisetron, QT prolongation Introduction Problem of chemotherapy-induced nausea and vomiting For personal use only. Chemotherapy-induced nausea and vomiting (CINV) occurs in 10%–90% of patients, depending on the emetic risk of the chemotherapeutic agent.1,2 There is a consider- able cost involved, not only for the expense of hospitalization and the direct treatment of CINV, but also because of the loss of workdays and the consequences of delayed 3–7 chemotherapy administration. There is consistent evidence that 5-HT3 antagonist antiemetic therapy has improved this problem without increasing the cost.3–7 Unmet needs in CINV treatment Delayed nausea and vomiting occurring hours or days after chemotherapy, either as a result of reduced plasma concentrations -
In February 2013, Glaxosmithkline (GSK) Announced a Commitment To
In February 2013, GlaxoSmithKline (GSK) announced a commitment to further clinical transparency through the public disclosure of GSK Clinical Study Reports (CSRs) on the GSK Clinical Study Register. The following guiding principles have been applied to the disclosure: Information will be excluded in order to protect the privacy of patients and all named persons associated with the study Patient data listings will be completely removed* to protect patient privacy. Anonymized data from each patient may be made available subject to an approved research proposal. For further information please see the Patient Level Data section of the GSK Clinical Study Register. Aggregate data will be included; with any direct reference to individual patients excluded *Complete removal of patient data listings may mean that page numbers are no longer consecutively numbered CONFIDENTIAL HM2009/00361/00HM2009/00361/00 TheThe GlaxoSmithKline GlaxoSmithKline group group of companies of companies NKP106254 Division: Worldwide Development Retention Category: GRS019 Information Type: Clinical Pharmacology Study Report Title: Randomised, double-blind, placebo controlled, cross-over study comparing the effects of both single dose and repeated dosing treatment for 14 days of vestipitant or vestipitant + paroxetine combination in an enriched population of subjects with tinnitus & hearing loss. Phase: II Compound Number: GW597599 Effective Date: 10-DEC-2009 Description: Tinnitus associated with hearing loss is a high prevalent audiologic disorder with important unmet needs as far as therapy is concerned. The present study explored the possible beneficial effects on tinnitus loudness or annoyance of a combination drug treatment aimed to increase the local inhibitory activity of neural circuitries involved in sound perception and generation. -
Compositions for Treating Centrally Mediated
(19) TZZ Z_T (11) EP 2 722 045 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/4178 (2006.01) A61K 31/473 (2006.01) 06.07.2016 Bulletin 2016/27 A61K 31/496 (2006.01) A61K 31/573 (2006.01) A61K 45/06 (2006.01) A61K 9/00 (2006.01) (2006.01) (2006.01) (21) Application number: 14151683.1 A61K 9/20 A61K 9/48 A61P 1/08 (2006.01) (22) Date of filing: 18.11.2010 (54) Compositions for treating centrally mediated nausea and vomiting Zusammensetzungen zur Behandlung von zentral vermitteltem Unwohlsein und Erbrechen Compositions pour traiter les nausées et vomissements à médiation centrale (84) Designated Contracting States: (56) References cited: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB WO-A1-2008/049552 WO-A2-2007/096763 GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR • REDDY G KESAVA ET AL: "Novel neurokinin-1 antagonists as antiemetics for the treatment of (30) Priority: 18.11.2009 US 262470 P chemotherapy-induced emesis.", SUPPORTIVE 14.09.2010 US 382709 P CANCER THERAPY 1 APR 2006 LNKD- PUBMED:18632487, vol. 3, no. 3, 1 April 2006 (43) Date of publication of application: (2006-04-01), pages140-142, XP002626039, ISSN: 23.04.2014 Bulletin 2014/17 1543-2912 • DIEMUNSCH P ET AL: "Neurokinin-1 receptor (62) Document number(s) of the earlier application(s) in antagonists in the prevention of postoperative accordance with Art. -
( 12 ) United States Patent
US009974742B2 (12 ) United States Patent (10 ) Patent No. : US 9 , 974 , 742 B2 Ottoboni et al. (45 ) Date of Patent: * May 22, 2018 ( 54 ) EMULSION FORMULATIONS OF AN NK - 1 2013 /0236501 A1 * 9 /2013 Booth . .. .. .. A61K 9 /0019 424 / 400 RECEPTOR ANTAGONIST AND USES 2013 /0317016 AL 11 /2013 Hingorani et al. THEREOF 2016 / 0024092 Al 1 / 2016 Wan et al. 2016 / 0082013 Al 3 / 2016 Ottoboni et al . @(71 ) Applicant : Heron Therapeutics , Inc. , Redwood 2016 /0206622 A1 3 / 2016 Ottoboni et al . City , CA (US ) 2017 / 0112847 AL 4 /2017 Ottoboni et al. @(72 ) Inventors : Thomas B . Ottoboni, Belmont, CA (US ) ; Han Han , Mountain View , CA FOREIGN PATENT DOCUMENTS (US ) CN 102379 * 3 / 2012 CN 102379845 A 3 / 2012 @(73 ) Assignee : Heron Therapeutics, Inc. , San Diego , WO WO 2005 /016308 AL 2 / 2005 WO WO 2009 / 124756 AL 10 / 2009 CA (US ) WO WO 2011 / 158053 AL 12 / 2011 WO WO 2013 / 177501 A2 11 / 2013 @( * ) Notice : Subject to any disclaimer , the term of this WO WO 2014 /0209962 AL 12 /2014 patent is extended or adjusted under 35 WO WO 2014 /005606 AL 3 / 2016 U . S . C . 154 ( b ) by 0 days . days . WO WO 2016 /044784 Al 3 / 2016 This patent is subject to a terminal dis claimer . OTHER PUBLICATIONS (21 ) Appl. No. : 15 /012 , 532 Cassileth et al. in Arch . Intern Med . 1983 ; 143 ( 7 ) : 1347 - 1349 ( Abstract ) . * Dexamethasone Hydrogen Phosphate at web .archive . org/ web / ( 22 ) Filed : Feb . 1 , 2016 20141224130045 /http :/ /www . drugs . com / pro / dexamethasone -so dium -phosphate .html ( retrieved on the internet Mar. -
CDR Clinical Review Report for Akynzeo
CADTH COMMON DRUG REVIEW Clinical Review Report Netupitant/Palonosetron 300 mg/0.5 mg (Akynzeo) (Purdue Pharma) Indication: In combination with dexamethasone, once- per-cycle treatment for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic cancer chemotherapy, or with moderately emetogenic cancer chemotherapy that is uncontrolled by a 5-hydroxytryptamine-3 receptor antagonist alone. Service Line: CADTH Common Drug Review Version: Final Publication Date: June 2018 Report Length: 96 Pages Disclaimer: The information in this document 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. While patients and others may access this document, the document is made available for informational purposes only and no representations or warranties are made with respect to its fitness for any particular purpose. The information in this document should not be used as a substitute for professional medical advice or 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. The Canadian Agency for Drugs and Technologies in Health (CADTH) does not endorse any information, drugs, therapies, treatments, products, processes, or services. While care has been taken to ensure that the information prepared by CADTH in this document is accurate, complete, and up-to-date as at the applicable date the material was first published by CADTH, CADTH does not make any guarantees to that effect. CADTH does not guarantee and is not responsible for the quality, currency, propriety, accuracy, or reasonableness of any statements, information, or conclusions contained in any third-party materials used in preparing this document. -
Neurokinin Receptor NK Receptor
Neurokinin Receptor NK receptor There are three main classes of neurokinin receptors: NK1R (the substance P preferring receptor), NK2R, and NK3R. These tachykinin receptors belong to the class I (rhodopsin-like) G-protein coupled receptor (GPCR) family. The various tachykinins have different binding affinities to the neurokinin receptors: NK1R, NK2R, and NK3R. These neurokinin receptors are in the superfamily of transmembrane G-protein coupled receptors (GPCR) and contain seven transmembrane loops. Neurokinin-1 receptor interacts with the Gαq-protein and induces activation of phospholipase C followed by production of inositol triphosphate (IP3) leading to elevation of intracellular calcium as a second messenger. Further, cyclic AMP (cAMP) is stimulated by NK1R coupled to the Gαs-protein. The neurokinin receptors are expressed on many cell types and tissues. www.MedChemExpress.com 1 Neurokinin Receptor Antagonists, Agonists, Inhibitors, Modulators & Activators Aprepitant Befetupitant (MK-0869; MK-869; L-754030) Cat. No.: HY-10052 (Ro67-5930) Cat. No.: HY-19670 Aprepitant (MK-0869) is a selective and Befetupitant is a high-affinity, nonpeptide, high-affinity neurokinin 1 receptor antagonist competitive tachykinin 1 receptor (NK1R) with a Kd of 86 pM. antagonist. Purity: 99.67% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg Size: 1 mg, 5 mg Biotin-Substance P Casopitant mesylate Cat. No.: HY-P2546 (GW679769B) Cat. No.: HY-14405A Biotin-Substance P is the biotin tagged Substance Casopitant mesylate (GW679769B) is a potent, P. Substance P (Neurokinin P) is a neuropeptide, selective, brain permeable and orally active acting as a neurotransmitter and as a neurokinin 1 (NK1) receptor antagonist. -
(12) United States Patent (10) Patent No.: US 9.446,029 B2 Boscan Et Al
USOO9446O29B2 (12) United States Patent (10) Patent No.: US 9.446,029 B2 BOScan et al. (45) Date of Patent: Sep. 20, 2016 (54) USE OF NK-1 RECEPTOR ANTAGONISTS IN GB 2216529 10, 1989 MANAGEMENT OF VISCERAL PAIN WO 9102745 A1 3, 1991 WO 911226.6 A1 8, 1991 (75) Inventors: Pedro Boscan, Bellvue, CO (US); WO O11801.6 A1 3, 2001 David Twedt, Fort Collins, CO (US) OTHER PUBLICATIONS (73) Assignee: Colorado State University Research Glerum et al. (Veterinary Surgery, 30, 351-358, 2001).* Foundation, Fort Collins, CO (US) Devitt et al. (JAVMA, 227, 6, Sep. 15, 2005).* Papich (Veterinary Pharmacology and Therapeutics, Ninth Edition, (*) Notice: Subject to any disclaimer, the term of this 2009, p. 1247-1272, editors: Jim E. Riviere Mark G. Papich).* patent is extended or adjusted under 35 Bradesi et al. (Gastroenterology, 2006, 130, 1729-1742).* U.S.C. 154(b) by 452 days. Heard, D.J. et al. Effect of acepromazine on the anesthetic require ment of halothane in the dog, AJVR, 1986, pp. 2113-2115, vol. 47. (21) Appl. No.: 13/192.283 No. 10. Hellyer, P.W. et al. Effects of diazepam and flumazenil on minimum alveolar concentrations for dogs anesthetized with isoflurane or a (22) Filed: Jul. 27, 2011 combination of isoflurane and fentanyl, AJVR, 2001, pp. 555-560, (65) Prior Publication Data vol. 62, No. 4. Muir, W.W. III, et al. Effects of morphine, lidocaine, ketamine, and US 2012/002898O A1 Feb. 2, 2012 morphine-lidocaine-ketamine drug combination on minimum alveolar concentration in dogs anesthetized with isoflurane, AJVR, Related U.S. -
Use and Cardiovascular Safety of Transdermal and Other Granisetron Preparations in Cancer Management
Cancer Management and Research Dovepress open access to scientific and medical research Open Access Full Text Article REVIEW Use and cardiovascular safety of transdermal and other granisetron preparations in cancer management 1 Jay W Mason Abstract: 5-HT3 antagonists have been available as oral and intravenous preparations for Thomas E Moon2 decades. The availability more recently of transdermal granisetron and the anticipated availability of a subcutaneous granisetron preparation have provided helpful alternatives to patients, and 1School of Medicine, University of Utah, Salt Lake City, UT, these preparations have been shown to have less potential to prolong QT than other drugs in 2Tarizona eHealth Services, Inc, the class. Emeryville, CA, USA Keywords: chemotherapy-induced nausea, vomiting, granisetron, QT prolongation Introduction Problem of chemotherapy-induced nausea and vomiting For personal use only. Chemotherapy-induced nausea and vomiting (CINV) occurs in 10%–90% of patients, depending on the emetic risk of the chemotherapeutic agent.1,2 There is a consider- able cost involved, not only for the expense of hospitalization and the direct treatment of CINV, but also because of the loss of workdays and the consequences of delayed 3–7 chemotherapy administration. There is consistent evidence that 5-HT3 antagonist antiemetic therapy has improved this problem without increasing the cost.3–7 Unmet needs in CINV treatment Delayed nausea and vomiting occurring hours or days after chemotherapy, either as a result of reduced plasma concentrations -
Management of Chemotherapy-Induced Nausea and Vomiting
R E V I E W A R T I C L E Management of Chemotherapy-Induced Nausea and Vomiting POOJA D EWAN, SWATI SINGHAL* AND DEEPIKA HARIT From Department of Pediatrics, UCMS and GTB Hospital, Delhi 110 095; and *Department of Pediatrics, Maulana Azad Medical College, Delhi 110 001; India. Correspondence to: Dr Pooja Dewan, DII/65, Kaka Nagar, Dr Zakir Hussain Marg, New Delhi 110 003, India. [email protected] Context: Chemotherapy-induced nausea and vomiting (CINV) is a significant problem in the treatment of children with cancer. The last decade has seen a variety of newer antiemetics being evaluated for CINV; their efficacy and side-effects need to be assessed in children. This article attempts to highlight this revised management of CINV. Evidence acquisition: Online search; journals. Search period: 6 months. Results: Newer drugs (aprepitant, fosapritant and newer 5HT3 antagonists) have been found to be effective in CINV: both acute and delayed phases. Most of the available literature is, however, based on adult oncology patients, with a few trials on adolescent patients. Conclusion: Every child receiving treatment for cancer should be evaluated for possible CINV. Their treatment should take into account the emetogenic potential of the chemotherapeutic drugs. Newer antiemetic drugs have good efficacy and can be tried in pediatric patients, especially in children > 11 years of age. Keywords: Antiemetics, Cancer, Chemotherapy, Nausea, Vomiting. hemotherapy is a common modality tears, and anxiety, it is imperative to provide for treatment of cancer. Regardless prophylaxis and treatment for CINV. of the fact that chemotherapy improves CLASSIFICATION Csurvival; it has its own toxicity and side- effects, which have a negative impact on the quality Chemotherapy-induced nausea and vomiting of life of children with cancer. -
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. -
A Abacavir Abacavirum Abakaviiri Abagovomab Abagovomabum
A abacavir abacavirum abakaviiri abagovomab abagovomabum abagovomabi abamectin abamectinum abamektiini abametapir abametapirum abametapiiri abanoquil abanoquilum abanokiili abaperidone abaperidonum abaperidoni abarelix abarelixum abareliksi abatacept abataceptum abatasepti abciximab abciximabum absiksimabi abecarnil abecarnilum abekarniili abediterol abediterolum abediteroli abetimus abetimusum abetimuusi abexinostat abexinostatum abeksinostaatti abicipar pegol abiciparum pegolum abisipaaripegoli abiraterone abirateronum abirateroni abitesartan abitesartanum abitesartaani ablukast ablukastum ablukasti abrilumab abrilumabum abrilumabi abrineurin abrineurinum abrineuriini abunidazol abunidazolum abunidatsoli acadesine acadesinum akadesiini acamprosate acamprosatum akamprosaatti acarbose acarbosum akarboosi acebrochol acebrocholum asebrokoli aceburic acid acidum aceburicum asebuurihappo acebutolol acebutololum asebutololi acecainide acecainidum asekainidi acecarbromal acecarbromalum asekarbromaali aceclidine aceclidinum aseklidiini aceclofenac aceclofenacum aseklofenaakki acedapsone acedapsonum asedapsoni acediasulfone sodium acediasulfonum natricum asediasulfoninatrium acefluranol acefluranolum asefluranoli acefurtiamine acefurtiaminum asefurtiamiini acefylline clofibrol acefyllinum clofibrolum asefylliiniklofibroli acefylline piperazine acefyllinum piperazinum asefylliinipiperatsiini aceglatone aceglatonum aseglatoni aceglutamide aceglutamidum aseglutamidi acemannan acemannanum asemannaani acemetacin acemetacinum asemetasiini aceneuramic -
Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD
Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD This list was graciously provided by JR Becker ([email protected]). Some additions have been made by Shawn Thomas ([email protected]). Please send additions or corrections to [email protected] Information about recent drug approvals can be obtained from the FDA Center for Drug Evaluation and Research. For information about drugs already marketed in the US, see Neurotransmitter.net's Drug Reference for FDA Approved Psychiatric Drugs. A List of Drugs in Development for Neurodegenerative Diseases [PDF] compiled by Myoung-Ok Kwon and colleagues (2004) is available from the journal Neurodegenerative Diseases; 1(2-3):113–152. Please support the NIMH's GenRED (Genetics of Recurrent Early-onset Depression) study, the largest psychiatric genetics study ever attempted. Updated 12/03/07 Treatments for Depression and Anxiety Drug Name Pharmacologic Action Company Indication Developmen Links tal Phase Pristiq (DVS- Metabolite of Effexor Wyeth Depression, Approvable 233 SR, (venlafaxine) anxiety (but further desvenlafaxine needed ) Phase III trials suggest a 2008 approval date) Gepirone ER 5-HT1A partial agonist Fabre- Depression, Not [Fabre- Kramer anxiety Approvable Kramer's Drug Profile] Saredutant (SR NK2 antagonist Sanofi- Depression, Phase III [Effects of SR 48968) Aventis anxiety 48968 on rodents] Valdoxan 5-HT2C antagonist, 5-HT2B Servier, Depression, EU: [Receptor (agomelatine, antagonist, melatonin M1/M2 Novartis anxiety, Resubmissio activity] [Oct AGO 178) receptor agonist sleep n planned in 2005 press disorders ’07. US: release] Phase III Amibegron, SR beta-3-adrenoceptor agonist Sanofi- Depression, A [SR 58611 is 58611 Aventis anxiety supplement a selective al NDA is beta-3- possible in adrenoceptor 2007 agonist] Vilazodone 5-HT1A partial agonist, Clinical Data Depression Phase III [January serotonin reuptake inhibitor Online, Inc.