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WADA Technical Letter – TL07 ANDARINE
WADA Technical Letter – TL07 Document Number: TL07 Version Number: 3.0 Written by: WADA Science Approved by: WADA Executive Committee Reviewed by: WADA Laboratory Expert Group Date: 21 December 2020 Effective Date: 1 January 2021 ANDARINE - FLUTAMIDE 1.0 Introduction WADA wishes to draw the attention of the Laboratories to the following observations and instructions on the analysis and reporting of SARM S4 (Andarine) Metabolites O-dephenylandarine and O- dephenylandarine glucuronide. The andarine Metabolites O-dephenylandarine and of O-dephenylandarine glucuronide may also be present in a Sample as a Metabolite of the anti-androgen Flutamide (Drogenil®, Eulexin®, Euflex®, Flutamin®, Flugere®), used primarily in the treatment of prostate cancer [1]. Since flutamide is not a Prohibited Substance in sports, the Laboratories shall not report an Adverse Analytical Finding (AAF) for andarine based on the monitoring of O-dephenylandarine [2]. Figure 1. Proposed metabolic pathway of flutamide and andarine (adapted from Perrenoud et al. [1]). 2.0 Analysis and Reporting Requirements Report the result as an AAF for andarine only when the presence of andarine (parent compound), and/or its glucuronic acid conjugate, and/or its deacetylated and/or hydroxylated Metabolites, and/or its bishydroxylated product [2] are confirmed in the Sample (regardless of the presence of flutamide and/or its Metabolite 2-hydroxyflutamide); [Comment: Laboratories shall not report an AAF for andarine based only on the presence of O- dephenylandarine.] 3.0 References [1] Perrenoud L. et al. Risk of false positive results to SARM S4 in case of therapeutic use of antineoplastic/antiandrogen drug containing flutamide: a case study. -
The Role of Histidine-Rich Proteins in the Biomineralization of Hemozoin Lisa Pasierb
Duquesne University Duquesne Scholarship Collection Electronic Theses and Dissertations Fall 2005 The Role of Histidine-Rich Proteins in the Biomineralization of Hemozoin Lisa Pasierb Follow this and additional works at: https://dsc.duq.edu/etd Recommended Citation Pasierb, L. (2005). The Role of Histidine-Rich Proteins in the Biomineralization of Hemozoin (Doctoral dissertation, Duquesne University). Retrieved from https://dsc.duq.edu/etd/1021 This Immediate Access is brought to you for free and open access by Duquesne Scholarship Collection. It has been accepted for inclusion in Electronic Theses and Dissertations by an authorized administrator of Duquesne Scholarship Collection. For more information, please contact [email protected]. The Role of Histidine-Rich Proteins in the Biomineralization of Hemozoin A Dissertation presented to the Bayer School of Natural and Environmental Sciences of Duquesne University As partial fulfillment of the requirements for the degree of Doctor of Philosophy By Lisa Pasierb August 26, 2005 Dr. David Seybert, thesis director Dr. David W. Wright, advisor In memory of Anna Pasierb April 24, 1924 – May 31, 2005 ii Acknowledgements First and foremost, I would like to express my sincerest gratitude to my advisor, Dr. David W. Wright. His exuberating energy and conviction attracted me to his research group, while his unwavering faith in me taught me more than he could ever know. Secondly, of course, I would like to extend my appreciation to Glenn Spreitzer and James Ziegler, the other two original members of the Wright group, whom initially tried to exert male dominance, but eventually became very faithful friends and colleagues. Finally, to all the other members of the Wright group over the years, thanks for all of your help, suggestions, and camaraderie. -
WO 2017/145013 Al 31 August 2017 (31.08.2017) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/145013 Al 31 August 2017 (31.08.2017) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C07D 498/04 (2006.01) A61K 31/5365 (2006.01) kind of national protection available): AE, AG, AL, AM, C07D 519/00 (2006.01) A61P 25/00 (2006.01) 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, (21) Number: International Application DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, PCT/IB20 17/050844 HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (22) International Filing Date: KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, 15 February 2017 (15.02.2017) MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (25) Filing Language: English RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, (26) Publication Language: English TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: 62/298,657 23 February 2016 (23.02.2016) US (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, New York, New York 10017 (US). -
(12) Patent Application Publication (10) Pub. No.: US 2013/0253056A1 Nemas Et Al
US 20130253 056A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0253056A1 Nemas et al. (43) Pub. Date: Sep. 26, 2013 (54) CONTINUOUS ADMINISTRATION OF (60) Provisional application No. 61/179,511, filed on May LEVODOPA AND/OR DOPA 19, 2009. DECARBOXYLASE INHIBITORS AND COMPOSITIONS FOR SAME Publication Classification (71) Applicant: NEURODERM, LTD., Ness-Ziona (IL) (51) Int. Cl. A63L/216 (2006.01) (72) Inventors: Mara Nemas, Gedera (IL); Oron (52) U.S. Cl. Yacoby-Zeevi, Moshav Bitsaron (IL) CPC .................................... A6 IK3I/216 (2013.01) USPC .......................................................... 514/538 (73) Assignee: Neuroderm, Ltd., Ness-Ziona (IL) (57) ABSTRACT (21) Appl. No.: 13/796,232 Disclosed herein are for example, liquid aqueous composi (22) Filed: Mar 12, 2013 tions that include for example an ester or salt of levodopa, or an ester or salt of carbidopa, and methods for treating neuro Related U.S. Application Data logical or movement diseases or disorders such as restless leg (63) Continuation-in-part of application No. 12/961,534, syndrome, Parkinson's disease, secondary parkinsonism, filed on Dec. 7, 2010, which is a continuation of appli Huntington's disease, Parkinson's like syndrome, PSP. MSA, cation No. 12/836,130, filed on Jul. 14, 2010, now Pat. ALS, Shy-Drager syndrome, dystonia, and conditions result No. 7,863.336, which is a continuation of application ing from brain injury including carbon monoxide or manga No. 12/781,357, filed on May 17, 2010, now Pat. No. nese intoxication, using Substantially continuous administra 8,193,243. tion of levodopa and/or carbidopa or ester and/or salt thereof. -
Screening of a Composite Library of Clinically Used Drugs and Well
HHS Public Access Author manuscript Author ManuscriptAuthor Manuscript Author Pharmacol Manuscript Author Res. Author Manuscript Author manuscript; available in PMC 2017 November 01. Published in final edited form as: Pharmacol Res. 2016 November ; 113(Pt A): 18–37. doi:10.1016/j.phrs.2016.08.016. Screening of a composite library of clinically used drugs and well-characterized pharmacological compounds for cystathionine β-synthase inhibition identifies benserazide as a drug potentially suitable for repurposing for the experimental therapy of colon cancer Nadiya Druzhynaa, Bartosz Szczesnya, Gabor Olaha, Katalin Módisa,b, Antonia Asimakopoulouc,d, Athanasia Pavlidoue, Petra Szoleczkya, Domokos Geröa, Kazunori Yanagia, Gabor Töröa, Isabel López-Garcíaa, Vassilios Myrianthopoulose, Emmanuel Mikrose, John R. Zatarainb, Celia Chaob, Andreas Papapetropoulosd,e, Mark R. Hellmichb,f, and Csaba Szaboa,f,* aDepartment of Anesthesiology, The University of Texas Medical Branch, Galveston, TX, USA bDepartment of Surgery, The University of Texas Medical Branch, Galveston, TX, USA cLaboratory of Molecular Pharmacology, Department of Pharmacy, University of Patras, Greece dCenter of Clinical, Experimental Surgery & Translational Research, Biomedical Research Foundation of the Academy of Athens, Greece eNational and Kapodistrian University of Athens, School of Pharmacy, Athens, Greece fCBS Therapeutics Inc., Galveston, TX, USA Abstract Cystathionine-β-synthase (CBS) has been recently identified as a drug target for several forms of cancer. Currently no -
New Developments in Prokinetic Therapy for Gastric Motility Disorders
REVIEW published: 24 August 2021 doi: 10.3389/fphar.2021.711500 New Developments in Prokinetic Therapy for Gastric Motility Disorders Michael Camilleri* and Jessica Atieh Clinical Enteric Neuroscience Translational and Epidemiological Research (CENTER), Division of Gastroenterology and Hepatology, Mayo Clinic, Rochester, MN, United States Prokinetic agents amplify and coordinate the gastrointestinal muscular contractions to facilitate the transit of intra-luminal content. Following the institution of dietary recommendations, prokinetics are the first medications whose goal is to improve gastric emptying and relieve symptoms of gastroparesis. The recommended use of metoclopramide, the only currently approved medication for gastroparesis in the United States, is for a duration of less than 3 months, due to the risk of reversible or irreversible extrapyramidal tremors. Domperidone, a dopamine D2 receptor antagonist, is available for prescription through the FDA’s program for Expanded Access to Investigational Drugs. Macrolides are used off label and are associated with tachyphylaxis and variable duration of efficacy. Aprepitant relieves some symptoms of gastroparesis. There are newer agents in the pipeline targeting diverse gastric (fundic, antral and pyloric) motor functions, including novel serotonergic 5-HT4 agonists, dopaminergic D2/3 antagonists, neurokinin NK1 antagonists, and ghrelin agonist. Novel Edited by: targets with potential to improve gastric motor functions include the pylorus, macrophage/ Jan Tack, inflammatory function, oxidative -
Drug-Related Deaths in Scotland in 2019
Drug-related deaths in Scotland in 2019 Published on 15 December 2020 Statistics of drug-related deaths in 2019 and earlier years, broken down by age, sex, selected drugs reported, underlying cause of death and NHS Board and Council areas. Drug-related deaths in Scotland, 2019 Summary Drug-related deaths Drug-related deaths, 1996 to 2019 continue to increase 1,264 The number of drug-related The dashed line shows the 5-year moving average and the shaded area deaths has increased almost shows the likely range of variation every year. In 2019 there around the 5-year moving average. were 1,264, which is the largest number ever recorded and more than 527 double the number recorded a decade ago. 244 1996 2013 2019 Largest increase was in Drug-related death rates by age group, 2000 to 2019 35-54 year olds 15-24 25-34 35-44 45-54 55-64 Most of the increase in drug related death rates* has 0.6 occurred in the 35-44 year old and 45-54 year old age 0.4 groups. 0.2 0.0 * Deaths per 1,000 people 2000 2019 2000 2019 2000 2019 2000 2019 2000 2019 Death rates vary Drug-related death rates by health board, 2015 to 2019 geographically Greater Glasgow & Clyde 0.27 Tayside 0.21 Greater Glasgow & Clyde Ayrshire & Arran 0.20 had the highest rate* at 0.27 Scotland 0.18 per 1,000 population, Lanarkshire 0.18 Forth Valley 0.17 followed by Tayside and Fife 0.16 Ayrshire & Arran with rates Lothian 0.15 of 0.21 and 0.20 per 1,000 Dumfries & Galloway 0.14 Grampian 0.14 population respectively. -
18 December 2020 – to Date)
(18 December 2020 – to date) MEDICINES AND RELATED SUBSTANCES ACT 101 OF 1965 (Gazette No. 1171, Notice No. 1002 dated 7 July 1965. Commencement date: 1 April 1966 [Proc. No. 94, Gazette No. 1413] SCHEDULES Government Notice 935 in Government Gazette 31387 dated 5 September 2008. Commencement date: 5 September 2008. As amended by: Government Notice R1230 in Government Gazette 32838 dated 31 December 2009. Commencement date: 31 December 2009. Government Notice R227 in Government Gazette 35149 dated 15 March 2012. Commencement date: 15 March 2012. Government Notice R674 in Government Gazette 36827 dated 13 September 2013. Commencement date: 13 September 2013. Government Notice R690 in Government Gazette 36850 dated 20 September 2013. Commencement date: 20 September 2013. Government Notice R104 in Government Gazette 37318 dated 11 February 2014. Commencement date: 11 February 2014. Government Notice R352 in Government Gazette 37622 dated 8 May 2014. Commencement date: 8 May 2014. Government Notice R234 in Government Gazette 38586 dated 20 March 2015. Commencement date: 20 March 2015. Government Notice 254 in Government Gazette 39815 dated 15 March 2016. Commencement date: 15 March 2016. Government Notice 620 in Government Gazette 40041 dated 3 June 2016. Commencement date: 3 June 2016. Prepared by: Page 2 of 199 Government Notice 748 in Government Gazette 41009 dated 28 July 2017. Commencement date: 28 July 2017. Government Notice 1261 in Government Gazette 41256 dated 17 November 2017. Commencement date: 17 November 2017. Government Notice R1098 in Government Gazette 41971 dated 12 October 2018. Commencement date: 12 October 2018. Government Notice R1262 in Government Gazette 42052 dated 23 November 2018. -
Supplement Ii to the Japanese Pharmacopoeia Fifteenth Edition
SUPPLEMENT II TO THE JAPANESE PHARMACOPOEIA FIFTEENTH EDITION Official From October 1, 2009 English Version THE MINISTRY OF HEALTH, LABOUR AND WELFARE Notice: This English Version of the Japanese Pharmacopoeia is published for the conven- ience of users unfamiliar with the Japanese language. When and if any discrepancy arises between the Japanese original and its English translation, the former is authentic. The Ministry of Health, Labour and Welfare Ministerial Notification No. 425 Pursuant to Paragraph 1, Article 41 of the Pharmaceutical Affairs Law (Law No. 145, 1960), we hereby revise a part of the Japanese Pharmacopoeia (Ministerial Notification No. 285, 2006) as follows*, and the revised Japanese Pharmacopoeia shall come into ef- fect on October 1, 2009. However, in the case of drugs which are listed in the Japanese Pharmacopoeia (hereinafter referred to as “previous Pharmacopoeia”) [limited to those listed in the Japanese Pharmacopoeia whose standards are changed in accordance with this notification (hereinafter referred to as “new Pharmacopoeia”)] and drugs which have been approved as of October 1, 2009 as prescribed under Paragraph 1, Article 14 of the same law [including drugs the Minister of Health, Labour and Welfare specifies (the Ministry of Health and Welfare Ministerial Notification No. 104, 1994) as those ex- empted from marketing approval pursuant to Paragraph 1, Article 14 of the Pharmaceu- tical Affairs Law (hereinafter referred to as “drugs exempted from approval”)], the Name and Standards established in the previous Pharmacopoeia (limited to part of the Name and Standards for the drugs concerned) may be accepted to conform to the Name and Standards established in the new Pharmacopoeia before and on March 31, 2011. -
Gait Analysis in Advanced Parkinson's Disease – Effect of Levodopa And
ORIGINAL ARTICLE Gait Analysis in Advanced Parkinson’s Disease – Effect of Levodopa and Tolcapone Din-E Shan, Shwn-Jen Lee, Ling-Yi Chao, and Shyh-Ing Yeh ABSTRACT: Objective: To determine the therapeutic effect of levodopa/benserazide and tolcapone on gait in patients with advanced Parkinson’s disease. Methods: Instrumental gait analysis was performed in 38 out of 40 patients with wearing-off phenomenon during a randomized, double-blind, placebo- controlled trial of tolcapone. R e s u l t s : Gait analysis disclosed a significant improvement by levodopa/benserazide in walking speed, stride length and the range of motion of hip, knee and ankle joints. At the end of the study, both the UPDRS motor scores during off-period and the percentage of off time improved significantly using tolcapone. However, gait analysis could not confirm this improvement. With respect to levodopa/benserazide effect, the reduction in rigidity correlated with improved angular excursion of the ankle, whereas the decreased bradykinesia correlated with improved stride length and angular excursion of the hip and knee joints. Conclusion: The results of our gait analysis confirmed that in parkinsonian patients with fluctuating motor symptoms levodopa/benserazide, but not tolcapone, produced a substantial improvement. RÉSUMÉ: Analyse de la démarche chez les patients en phase avancée de la maladie de Parkinson – Effet de la lévodopa et du tolcapone. Objectif: Le but de cette étude était de déterminer l’effet thérapeutique de la lévodopa/bensérazide et du tolcapone sur la démarche, chez les patients en phase avancée de la maladie de Parkinson. Méthodes: Une analyse instrumentale de la démarche a été réalisée chez 38 de 40 patients ayant un phénomène de détérioration de fin de dose pendant un essai randomisé, en double insu, contrôlé par placebo, du tolcapone. -
Dalbavancin • Oritavancin • Tedizolid • Ceftolozane/Tazobactam • Ceftazidime/Avibactam • Fecal Transplant
What’s New in Infectious Diseases? Bruce L. Gilliam, M.D. Institute of Human Virology University of Maryland School of Medicine Baltimore, MD Topics New Antibacterial Therapeutics Emerging Pathogens HIV Hepatitis C Disclosures Research Studies Pfizer – Staph aureus Vaccine Trial TaiMed Biologics - Ibaluzimab Advisory Board Viiv Healthcare New Antibacterial Therapeutics • Dalbavancin • Oritavancin • Tedizolid • Ceftolozane/tazobactam • Ceftazidime/avibactam • Fecal Transplant Incidence of Staph aureus hospitalizations in U.S.A., 2001–2009 BMC Infect Dis 2014, 14:296 Dalbavancin (Dalvance) • Derived from Teicoplanin • ½ life – Effective: 8.5 days – Terminal: 346 hrs (14 days) • Bactericidal • Similar spectrum to Vancomycin, active against: – Staphylococci • MSSA, MRSA, CoNS – Streptococci • resistant pneumococci • anaerobic strep – Enterococci • VRE with van B, C but not A – Corynebacterium Dalbavancin Once Weekly Non- Inferior to Vanco/Linezolid N Engl J Med 2014;370:2169-79. Single-Dose (1.5 g) Non-Inferior to Weekly Dalbavancin for Treatment of Acute Bacterial Skin and Skin Structure Infection 100 90 80 70 60 50 Single Dose 40 Once Weekly 30 20 10 0 Overall Clinical Success Rate Success Rate Success Rate Response Day 14 Day 28 Day 14 MRSA Clin Infect Dis. 2015 Nov 26. pii: civ982. [Epub ahead of print] VA Experience with Dalbavancin • Background – Levels in bone > MIC for 14 days • 8 patients treated for osteomyelitis with IV Dalbavancin – Former IV drug users not eligible for home IV or unwilling to do home IV • Treated for up to 8 weeks • No adverse events • All with resolution of osteomyelitis • Cost savings vs. placement in facility Oritavancin (Orbactiv) • Derived from Vancomycin • ½ life – Terminal 245-393 hrs (10-16 days) • Bactericidal • Similar spectrum to Vancomycin, active against: – Staphylococci • MSSA, MRSA, CoNS – Streptococci • resistant pneumococci • anaerobic strep – Enterococci • VRE with van A, B, C – Corynebacterium Single Dose Oritavancin vs. -
International Journal of Medicine and Pharmaceutical Research
Wayal Sunil Anil et al, IJMPR, 2019, 7(6): 180-183 CODEN (USA): IJCPNH | ISSN: 2321-2624 International Journal of Medicine and Pharmaceutical Research Journal Home Page: www.pharmaresearchlibrary.com/ijmpr R E S E A R C H A R T I C L E Formulation and In-vitro Evaluation of Alosetron Oral Thin Films Wayal Sunil Anil1, G.S. Valluri2, Gampa Vijay Kumar3 Department of Pharmacy, KGR Institute of Technology and Management, Rampally, Kesara, Medchal, Telangana, India. A B S T R A C T Alosetron, is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome. In present study oral thin films of Alosetron were developed to have a faster on set of action. The oralthin films were developed by using polymers Guar gum, Pullulan and PVP K30.Oral thin films were prepared by employing solvent casting method. Propylene glycol was selected as permeation enhancer and plasticizer. Drug excipient compatibility studies were carried out by using FTIR, and it was observed that there were no interactions. Formulations were prepared with the varying concentrations polymers ranging from F1-F9, and all the formulations were evaluated for various physical parameters Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, Drug content, Moisture uptake, Moisture content and all the results were found to be were found to be within the pharmacopeial limits, in-vitro drug release studies by using USP dissolution Apparatus Type II. Among all the 9 formulations F4 formulation which contain Pullulan 10mg and shown 97.06% cumulative drug release within 30 min.