DOCSLIB.ORG

Dipeptidyl Peptidase DPP

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Dipeptidyl Peptidase DPP Dipeptidyl Peptidase DPP Dipeptidyl Peptidase (DPP) is an antigenic enzyme expressed on the surface of most cell types and is associated with immune regulation,signal transduction and apoptosis. DPP is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides. The substrates of DPP are proline-containing peptides and include growth factors, chemokines, neuropeptides, and vasoactive peptides. DPP plays a major role in glucose metabolism. DPP is responsible for the degradation of incretins such as GLP-1. Furthermore, DPP appears to work as a suppressor in the development of cancer and tumours. DPP plays an important role in tumor biology, and is useful as a marker for various cancers, with its levels either on the cell surface or in the serum increased in some neoplasms and decreased in others. www.MedChemExpress.com 1 Dipeptidyl Peptidase Inhibitors & Modulators Alogliptin Alogliptin Benzoate (SYR-322 (free base)) Cat. No.: HY-A0023A (SYR 322) Cat. No.: HY-A0023 Bioactivity: Alogliptin (SYR-322 free base) is a potent, selective Bioactivity: Alogliptin benzoate(SYR 322) is a potent, selective inhibitor inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater of DPP-4 with IC50 of <10 nM, exhibits greater than than 10,000-fold selectivity over DPP-8 and DPP-9. IC50 value: 10,000-fold selectivity over DPP-8 and DPP-9. IC50 value: <10 nM Target: DPP4 Alogliptin is an orally administered, <10 nM Target: DPP4 Alogliptin is an orally administered, anti-diabetic drug in the DPP-4 inhibitor class. A randomized… anti-diabetic drug in the DPP-4 inhibitor class. A randomized… Purity: >98% Purity: 99.93% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg Anagliptin AZD7986 (SK-0403) Cat. No.: HY-14877 (INS 1007) Cat. No.: HY-101056 Bioactivity: Anagliptin is a highly selective, potent inhibitor of Bioactivity: AZD7986 is a Dipeptidyl peptidase 1 ( DPP1) inhibitor with dipeptidyl peptidase 4 (DPP-4), with an IC of 3.8 nM, and 50 pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, less selective at DPP-8/9 ( IC50, 68, 60 nM, respectively). dog and rabbit, respectively. Purity: 97.96% Purity: 99.07% Clinical Data: Launched Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg DBPR108 Diprotin A TFA Cat. No.: HY-12528 (Ile-Pro-Pro (TFA)) Cat. No.: HY-111174A Bioactivity: DBPR108 is a potent, selective, and orally bioavailable Bioactivity: Diprotin A (TFA) is an inhibitor of dipeptidyl peptidase IV dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no (DPP-IV). inhibition on DDP8 and DPP9. Purity: 99.90% Purity: 98.80% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg DPP-4 inhibitor 1 DPP-IV-IN-1 Cat. No.: HY-114408 Cat. No.: HY-U00346 Bioactivity: DPP-4 inhibitor 1 (compound 5) is a potent and long acting Bioactivity: DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV Dipeptidyl peptidase-4 (DPP-4) inhibitor for t treatment of (DPP-IV), a highly specific serine protease, with an IC50 of [1] T2DM, with a K D of 0.177 nM . 4.6 nM. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 1 mg, 5 mg, 10 mg, 20 mg DPP-IV-IN-2 Dutogliptin Cat. No.: HY-108319 Cat. No.: HY-10286 Bioactivity: DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV ( Bioactivity: Dutogliptin is an orally available, potent, and selective DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively. dipeptidyl peptidase-4 ( DPP4) inhibitor. Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 50 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Gemigliptin Gosogliptin (LC15-0444) Cat. No.: HY-14892 (PF-00734200; PF-734200) Cat. No.: HY-10287 Bioactivity: Gemigliptin is a highly selective dipeptidyl peptidase 4 Bioactivity: Gosogliptin is a potent and selective inhibitor of dipeptidyl (DPP4) inhibitor with a KD of 7.25 nM. peptidase-IV ( DPP-IV). Purity: 98.31% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg, 100 mg Linagliptin Omarigliptin (BI 1356) Cat. No.: HY-10284 (MK-3102) Cat. No.: HY-15981 Bioactivity: Linagliptin is a highly potent, selective DPP-4 inhibitor Bioactivity: Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all with IC50 of 1 nM. proteases tested (IC50 > 67 μM). Purity: 99.80% Purity: 99.91% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 250 mg, 1 g 2 mg, 5 mg, 10 mg, 50 mg, 100 mg Prodipine hydrochloride Retagliptin Phosphate Cat. No.: HY-101605 (SP 2086) Cat. No.: HY-112668 Bioactivity: Prodipine, a diphenyl-phosphonate derivative. The IC50s of Bioactivity: Retagliptin Phosphate is pharmaceutical composition of DPP-4 Prodipine for purified and plasma Dipeptidyl peptidase IV ( DPP inhibitor for treating type-2 diabetes. IV) from the rabbit are 4.5 μM and 30 μM, respectively. Purity: >98% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg Saikogenin A Saxagliptin Cat. No.: HY-N6584 (BMS-477118) Cat. No.: HY-10285 Bioactivity: Saikogenin A, extracted from a Chinese herbal plant called Bioactivity: Saxagliptin is an orally active dipeptidyl peptidase-4 (DPP4) Tsai-Fu, is a dipeptidyl peptidase-IV ( DPP-IV) inhibitor. inhibitor that helps control blood sugar levels. Purity: 98.31% Purity: 98.03% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg Saxagliptin hydrate Sitagliptin (BMS-477118 hydrate) Cat. No.: HY-10285A (MK0431) Cat. No.: HY-13749 Bioactivity: Saxagliptin H2O(BMS477118 H2O) is a selective and reversible Bioactivity: Sitagliptin is a potent inhibitor of DPP4 with IC50 of 19 nM DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM. in Caco-2 cell extracts. Purity: >98% Purity: 99.72% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 100 mg, 200 mg www.MedChemExpress.com 3 Sitagliptin phosphate Sitagliptin phosphate monohydrate (MK0431 phosphate) Cat. No.: HY-13749A (MK-0431 phosphate monohydrate) Cat. No.: HY-13749B Bioactivity: Sitagliptin phosphate is a potent inhibitor of DPP4 with IC50 Bioactivity: Sitagliptin phosphate monohydrate is a potent inhibitor of DPP4 with IC of 19 nM in Caco-2 cell extracts. of 19 nM in Caco-2 cell extracts. 50 Purity: >98% Purity: 99.78% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 200 mg Size: 10mM x 1mL in Water, 100 mg, 200 mg Talabostat Talabostat mesylate (PT100; Val-boroPro) Cat. No.: HY-13233 (PT100 (mesylate); Val-boroPro (mesylate)) Cat. No.: HY-13233A Bioactivity: Talabostat (PT100, Val-boroPro) is a potent, nonselective and Bioactivity: Talabostat mesylate (PT100 mesylate; Val-boroPro mesylate) is orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a potent, nonselective and orally available dipeptidyl a Ki of 0.18 nM. peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Purity: >98% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg Teneligliptin Teneligliptin hydrobromide (MP-513) Cat. No.: HY-14806 (MP-513 (hydrobromide)) Cat. No.: HY-14806A Bioactivity: Teneligliptin (MP-513) is a potent chemotype Bioactivity: Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. in vitro, with IC50s of approximately 1 nM. Purity: 99.82% Purity: 99.99% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg, 250 mg 10 mg, 50 mg, 100 mg, 250 mg Trelagliptin Trelagliptin succinate (SYR-472) Cat. No.: HY-15408 (SYR-472 succinate) Cat. No.: HY-15408A Bioactivity: Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 Bioactivity: Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). type 2 diabetes (T2D). Purity: 99.89% Purity: 99.89% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg UAMC00039 dihydrochloride Vildagliptin Cat.
Load more

Recommended publications
  • Renato Wilberto Zilli Eficácia Em Longo Prazo Das
    RENATO WILBERTO ZILLI EFICÁCIA EM LONGO PRAZO DAS GLIFLOZINAS VERSUS GLIPTINAS NO TRATAMENTO DO DIABETES MELLITUS TIPO 2 APÓS FALÊNCIA DA METFORMINA COMO MONOTERAPIA: REVISÃO SISTEMÁTICA E METANÁLISE EM REDE Tese apresentada ao Programa de Ciências Médicas da Faculdade de Medicina da Universidade de São Paulo para obtenção do título de Doutor em Ciências. Área de Concentração: Processos Imunes e Infecciosos Orientador: Prof. Dr. Fabiano Pinheiro da Silva (Versão corrigida. Resolução CoPGr 6018/11, de 13 de outubro de 2011. A versão original está disponível na Biblioteca da FMUSP) São Paulo 2017 Dados Internacionais de Catalogação na Publicação (CIP) Preparada pela Biblioteca da Faculdade de Medicina da Universidade de São Paulo ©reprodução autorizada pelo autor Zilli, Renato Wilberto Eficácia em longo prazo das gliflozinas versus gliptinas no tratamento do diabetes mellitus tipo 2 após falência da metformina como monoterapia : revisão sistemática e metanálise em rede / Renato Wilberto Zilli ‐‐ São Paulo, 2017. Tese(doutorado)--Faculdade de Medicina da Universidade de São Paulo. Programa de Ciências Médicas. Área de concentração: Processos Imunes e Infecciosos. Orientador: Fabiano Pinheiro da Silva. Descritores: 1.Diabetes mellitus tipo 2 2.Metanálise 3.Terapia combinada 4.Falha de tratamento 5.Metformina 6.Inibidores da dipeptidil peptidase IV 7.Transportador 2 de glucose‐sódio/inibidores 8.Empagliflozina 9.Dapagliflozina 10.Saxagliptina USP/FM/DBD ‐302/17 Esta tese de doutorado está de acordo com as seguintes normas, em vigor no momento desta publicação: Referências: adaptado de International Committee of Medical Journals Editors (Vancouver). Guia de apresentação e dissertações, teses e monografias. Elaborado por Anneliese Cordeiro da Cunha, Maria Julia de A.L.
    [Show full text]
  • Risk of Any Hypoglycemia with New Antihyperglycemic Agents in Patients with Type 2 Diabetes: a Systematic Review and Meta-Analysis
    Risk of Any Hypoglycemia with New Antihyperglycemic Agents in Patients with Type 2 Diabetes: A Systematic Review and Meta-Analysis by Sanaz Kamalinia A thesis submitted in conformity with the requirements for the degree of Master of Science Institute of Medical Sciences University of Toronto © Copyright by Sanaz Kamalinia (2019) Risk of Any Hypoglycemia with New Antihyperglycemic Agents in Patients with Type 2 Diabetes: A Systematic Review and Meta- Analysis Sanaz Kamalinia Master of Science Institute of Medical Sciences University of Toronto 2019 Abstract Background : Evaluation of hypoglycemia risk relative to placebo with new antihyperglycemic agents (AHA) including the dipeptidyl peptidase-4 inhibitors (DPP4i), glucagon-like peptide-1 receptor agonists (GLP1RA) and sodium-glucose co-transporter- 2 inhibitors (SGLT2i) remains inconclusive. Objective: This systematic review and meta-analysis aimed to assess risk of any and severe hypoglycemia with new AHA relative to placebo by excluding studies with background sulfonylureas and insulin. Methods: Randomized, placebo-controlled studies, 12 weeks or greater in duration were considered for inclusion. Studies allowing background use of any other AHA, apart from metformin, were excluded. This study is registered with PROSPERO (CRD42018095458). Results: 141 studies included in the meta-analysis demonstrate that relative to placebo, risk of any and severe hypoglycemia did not significantly differ for any new AHA. ii Acknowledgments First and foremost, I wish to express my sincere gratitude to my program advisor committee members. To my supervisor Dr Tobe, thank you for accepting me as your student and presenting me with this challenge. I thoroughly enjoyed it. Especially given your positive words of encouragement and insightful guidance for every step of this journey.
    [Show full text]
  • Dipeptidyl Peptidase IV (DPP4) Inhibitors As Potential
    Supporting Materials Drug repurposing: Dipeptidyl peptidase IV (DPP4) inhibitors as potential agents to treat SARS-CoV-2 (2019-nCov) infection Praveen P. N. Rao 1*, Amy Trinh Pham 1, Arash Shakeri 1, Amna El Shatshat 1, Yusheng Zhao 1, Rahul C. Karuturi 1 and Ahmed A. Hefny 1 School of Pharmacy, University of Waterloo, Health Sciences Campus, 200 University Ave West, Waterloo, Ontario N2L 3G1, Canada *Corresponding author Praveen P. N. Rao, School of Pharmacy, Health Sciences Campus, University of Waterloo, Waterloo, Ontario, Canada N2L 3G1, phone: 519-888-4567; ext: 21317; email: [email protected] Contents 1. Figure S1: Binding modes of DPP4 inhibitors anagliptin (A), alogliptin (B), trelagliptin (C) and sitagliptin (D) in the SARS-CoV-2 Mpro protomer 2. Figure S2: Binding modes of DPP4 inhibitors teneligliptin (A) and gosogliptin (B) in the SARS-CoV-2 Mpro protomer 3. Figure S3: Electrostatic surface potential map of SARS-CoV-2 Mpro protomer (A) and (B) dimer 4. Figure S4: Binding modes of DPP4 inhibitors gemigliptin, linagliptin and evogliptin in the MERS-CoV 3CLpro dimer 5. Figure S5: Pharmacophore model to design SARS-CoV-2 Mpro dimer inhibitors based on the docked poses of DPP4 inhibitors - gemigliptin, linagliptin and evogliptin 6. Figure S6: 2D Interaction map of linagliptin in the active sites of the serine protease DPP4 and cysteine protease SARS-CoV-2 Mpro 7. Table S1: Physicochemical properties of DPP4 inhibitors and the SARS-CoV-2 Mpro dimer inhibitor 1 1 Figure S1. Binding modes of DPP4 inhibitors anagliptin (A), alogliptin (B), trelagliptin (C) and sitagliptin (D) in the SARS-CoV-2 Mpro protomer (PDB ID: 6Y2F).
    [Show full text]
  • Dipeptidyl Peptidase-4 Inhibitors and the Risk of Heart Failure: a Systematic Review and Meta-Analysis
    CMAJ OPEN Research Dipeptidyl peptidase-4 inhibitors and the risk of heart failure: a systematic review and meta-analysis Subodh Verma MD PhD, Ronald M. Goldenberg MD, Deepak L. Bhatt MD MPH, Michael E. Farkouh MD MSc, Adrian Quan MPhil, Hwee Teoh PhD, Kim A. Connelly MBBS PhD, Lawrence A. Leiter MD, Jan O. Friedrich MD DPhil Abstract Background: Given recent discrepant results from randomized controlled trials (RCTs), we examined the totality of RCT evidence assessing the association between dipeptidyl peptidase-4 (DPP-4) inhibitors and heart failure. Methods: MEDLINE, Embase and ClinicalTrials.gov were searched without language restrictions to August 2016 for RCTs compar- ing DPP-4 inhibitors to placebo or no therapy for a period of 24 weeks or more. We included all heart failure outcomes when listed either as a serious adverse event or adverse event. Pooled analyses used random-effects. Results: We identified 100 RCTs (n = 79 867) — 3 large cardiovascular-safety RCTs (SAVOR-TIMI 53[saxagliptin]/n = 16 492, EXAMINE[alogliptin]/n = 5380, and TECOS[sitagliptin]/n = 14 735), and 97 smaller RCTs with a primary outcome that was usually change in glycated hemoglobin. Virtually all RCTs were high-quality, multicentre, placebo-controlled trials. A total of 96% (1192/1244) of heart failure events were prespecified, blindly adjudicated and required hospital admission. Pooled results suggested a 13% increase in heart failure (relative risk [RR] 1.13, 95% confidence interval [CI] 1.01–1.26, I2 = 0%; 32 RCTs, n = 54 640, 1244 events). When including only the 3 large RCTs, the increase was similar, but not significant (RR 1.14, 95% CI 0.97–1.32; 3 RCTs, n = 36 543, 1169 adjudicated events; number needed to harm 246) owing to heterogeneity (I2 = 42%), which lead to wider CIs, because SAVOR- TIMI 53 showed increased heart failure (RR 1.26, 95% CI 1.06–1.49) and TECOS showed no effect (RR 1.00, 95% CI 0.83–1.19).
    [Show full text]
  • 2011/064352 Al
    (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 , , ,, , 3 June 2011 (03.06.2011) 201 1/064352 Al (51) International Patent Classification: (74) Agents: HAMMANN, Heinz et al; Boehringer Ingel A61K 31/155 (2006.01) A61K 31/519 (2006.01) heim GmbH, Corporate Patents, Binger Str. 173, 55216 A61K 31/44 (2006.01) A61K 45/06 (2006.01) Ingelheim am Rhein (DE). (21) International Application Number: (81) Designated States (unless otherwise indicated, for every PCT/EP20 10/068349 kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, (22) International Filing Date: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, 26 November 2010 (26.1 1.2010) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (25) Filing Language: English HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, (26) Publication Language: English ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (30) Priority Data: NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, 09177418.2 27 November 2009 (27.1 1.2009) EP SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, 10166714.5 2 1 June 2010 (21 .06.2010) EP TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (71) Applicant (for all designated States except US): (84) Designated States (unless otherwise indicated, for every BOEHRINGER INGELHEIM INTERNATIONAL kind of regional protection available): ARIPO (BW, GH, GMBH [DE/DE]; Binger Str.
    [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]
  • 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
    [Show full text]
  • Current Progress in Pharmacogenetics of Second-Line Antidiabetic Medications: Towards Precision Medicine for Type 2 Diabetes
    Journal of Clinical Medicine Review Current Progress in Pharmacogenetics of Second-Line Antidiabetic Medications: Towards Precision Medicine for Type 2 Diabetes Chan Uk Heo and Chang-Ik Choi * College of Pharmacy, Dongguk University-Seoul, Goyang 10326, Korea; [email protected] * Correspondence: [email protected]; Tel.: +82-31-961-5230 Received: 4 March 2019; Accepted: 18 March 2019; Published: 21 March 2019 Abstract: Precision medicine is a scientific and medical practice for personalized therapy based on patients’ individual genetic, environmental, and lifestyle characteristics. Pharmacogenetics and pharmacogenomics are also rapidly developing and expanding as a key element of precision medicine, in which the association between individual genetic variabilities and drug disposition and therapeutic responses are investigated. Type 2 diabetes (T2D) is a chronic metabolic disorder characterized by hyperglycemia mainly associated with insulin resistance, with the risk of clinically important cardiovascular, neurological, and renal complications. The latest consensus report from the American Diabetes Association and European Association for the Study of Diabetes (ADA-EASD) on the management of T2D recommends preferential use of glucagon-like peptide-1 (GLP-1) receptor agonists, sodium-glucose cotransporter-2 (SGLT2) inhibitors, and some dipeptidyl peptidase-4 (DPP-4) inhibitors after initial metformin monotherapy for diabetic patients with established atherosclerotic cardiovascular or chronic kidney disease, and with risk of hypoglycemia
    [Show full text]
  • Extended Commentary from the American Diabetes Association
    MEETING REPORT Extended commentary from the American Diabetes Association 2015 meeting Dr Mike Gwilt1 and Dr Caroline Day2 take a closer look at the 75th Annual Scientific Sessions of the American Diabetes Association, Boston, MA, June 4–9, 2015 Introduction ........................................... 1 Table 1 Awards at ADA 2015 Cardiovascular safety............................. 1 Award Recipient PDE5 inhibitors and myocardial National Scientific & Health Care Achievement Awards infarction ................................................ 2 Banting Medal for Scientific Achievement Award Philipp E Scherer, Texas, USA Outstanding Scientific Achievement Award Pere Puigserver, Massachusetts, USA PCSK9 inhibitors..................................... 2 Albert Renold Award Richard N Bergman, California, USA DPP4 inhibitors....................................... 2 Outstanding Achievement in Clinical Diabetes GLP-1 receptor agonists ........................ 2 Research Award David M Nathan, Massachusetts, USA Outstanding Physician in Clinical Diabetes Novel insulins ......................................... 3 Research Award Lori Lafel, Massachusetts, USA Devices .................................................... 4 Outstanding Educator in Diabetes Award Linda M Delahanty, Massachusetts, USA SGLT2 inhibitors –the newest class ....... 5 Harold Rifkin Award for Distinguished International Service in the Care of Diabetes Karl Eric Morgensen, Denmark Novel antidiabetic mechanisms ............ 5 Kelly West Award for Outstanding Achievement Looking back…and
    [Show full text]
  • Towards Precision Medicine for Type 2 Diabetes
    Review Current Progress in Pharmacogenetics of Second-Line Antidiabetic Medications: Towards Precision Medicine for Type 2 Diabetes Chan Uk Heo and Chang-Ik Choi * College of Pharmacy, Dongguk University-Seoul, Goyang 10326, Korea; [email protected] * Correspondence: [email protected]; Tel.: +82-31-961-5230 Received: 4 March 2019; Accepted: 18 March 2019; Published: 21 March 2019 Abstract: Precision medicine is a scientific and medical practice for personalized therapy based on patients’ individual genetic, environmental, and lifestyle characteristics. Pharmacogenetics and pharmacogenomics are also rapidly developing and expanding as a key element of precision medicine, in which the association between individual genetic variabilities and drug disposition and therapeutic responses are investigated. Type 2 diabetes (T2D) is a chronic metabolic disorder characterized by hyperglycemia mainly associated with insulin resistance, with the risk of clinically important cardiovascular, neurological, and renal complications. The latest consensus report from the American Diabetes Association and European Association for the Study of Diabetes (ADA-EASD) on the management of T2D recommends preferential use of glucagon-like peptide-1 (GLP-1) receptor agonists, sodium-glucose cotransporter-2 (SGLT2) inhibitors, and some dipeptidyl peptidase-4 (DPP-4) inhibitors after initial metformin monotherapy for diabetic patients with established atherosclerotic cardiovascular or chronic kidney disease, and with risk of hypoglycemia or body weight-related problems. In this review article, we summarized current progress on pharmacogenetics of newer second-line antidiabetic medications in clinical practices and discussed their therapeutic implications for precision medicine in T2D management. Several biomarkers associated with drug responses have been identified from extensive clinical pharmacogenetic studies, and functional variations in these genes have been shown to significantly affect drug-related glycemic control, adverse reactions, and risk of diabetic complications.
    [Show full text]
  • Product List
    PRODUCT LIST Active Pharma Ingredients API Acid Reflux Disorders Product Pharmacopoeia CAS No. Technical Document A Acotiamide Hydrochloride - 773092-05-0 - Almagate EP 66827-12-1 - Aluminum Hydroxide BP, USP 21645-51-2 - C Cimetidine - 51481-61-9 - D Dexlansoprazole - 138530-94-6 - Dexlansoprazole - 313640-86-7 DMF Sesquihydrate Dexrabeprazole Sodium - 171440-18-9 ODMF, Tech Pack E Ecabet Sodium - 86408-72-2 DMF Esomeprazole - 119141-88-7 - Esomeprazole Magneisum - 217087-10-0 - Dihydrate Esomeprazole Magnesium - 161973-10-0 - Esomeprazole Magnesium USP 217087-09-7 CEP, DMF Trihydrate Esomeprazole Potassium IHS 161796-84-5 DMF Esomeprazole Sodium - 161796-78-7 - Esomeprazole Zinc/ 793668-08-3, - - Base/Strontium 119141-88-7 F Famotidine - 76824-35-6 - E Glycopyrrolate - 596-51-0 - H Hydrotelcite BP 12304-65-3 - I Ilaprazole IHS, IP 172152-36-2 DMF Ilaprazole Sodium - 172152-50-0 ODMF, Tech Pack Itopride - 122898-67-3 - Itopride Hydrochloride IHS 122892-31-3 - Patent Disclaimer: Products protected by valid patents are not offered for sale in countries, where the sale of such products constitutes a patent infringement. The buyers should make their independent evaluation of the patent scenario for their respective markets and will be responsible for all patent related liabilities. 2021-01-11 © ExSyn Corp | All rights reserved. | www.exsyncorp.com 1 API Acid Reflux Disorders Product Pharmacopoeia CAS No. Technical Document L Lafutidine - 118288-08-7 - Lansoprazole - 103577-45-3 - Lansoprazole Sodium - 226904-00-3 - M Magaldrate USP 74978-16-8
    [Show full text]
  • Supplementary Information Drug Repurposing: Dipeptidyl Peptidase IV
    Supplementary Information Drug repurposing: Dipeptidyl peptidase IV (DPP4) inhibitors as potential agents to treat SARS-CoV-2 (2019-nCov) infection Praveen P. N. Rao*, Amy Trinh Pham, Arash Shakeri, Amna El Shatshat, Yusheng Zhao, Rahul C. Karuturi & Ahmed A. Hefny School of Pharmacy, University of Waterloo, Health Sciences Campus, 200 University Ave West, Waterloo, Ontario N2L 3G1, Canada *Corresponding author Praveen P. N. Rao, School of Pharmacy, Health Sciences Campus, University of Waterloo, Waterloo, Ontario, Canada N2L 3G1, phone: 519-888-4567; ext: 21317; email: [email protected] Contents 1. Figure S1: Binding modes of DPP4 inhibitors anagliptin (A), alogliptin (B), trelagliptin (C) and sitagliptin (D) in the SARS-CoV-2 Mpro protomer 2. Figure S2: Binding modes of DPP4 inhibitors teneligliptin (A) and gosogliptin (B) in the SARS-CoV-2 Mpro protomer 3. Figure S3: Electrostatic surface potential map of SARS-CoV-2 Mpro protomer (A) and (B) dimer 4. Figure S4: Binding modes of DPP4 inhibitors gemigliptin, linagliptin and evogliptin in the MERS-CoV 3CLpro dimer 5. Figure S5: Top two binding modes (red and yellow stick representation) of the peptidomimetic inhibitor 1 in the DPP4 dimer 6. Figure S6: Pharmacophore model to design SARS-CoV-2 Mpro dimer inhibitors based on the docked poses of DPP4 inhibitors - gemigliptin, linagliptin and evogliptin 2 7. Figure S1. Binding modes of DPP4 inhibitors anagliptin (A), alogliptin (B), trelagliptin (C) and sitagliptin (D) in the SARS-CoV-2 Mpro protomer (PDB ID: 6Y2F). Hydrogen atoms are not shown to enhance clarity. 3 Figure S2. Binding modes of DPP4 inhibitors teneligliptin (A) and gosogliptin (B) in the SARS- CoV-2 Mpro protomer (PDB ID: 6Y2F).
    [Show full text]