• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
LI Chengye, HUANG Wenlong, QIAN Hai. Advances in the research of long-acting strategy of insulin and GLP-1 analogs[J]. Journal of China Pharmaceutical University, 2018, 49(6): 660-670. DOI: 10.11665/j.issn.1000-5048.20180604
Citation: LI Chengye, HUANG Wenlong, QIAN Hai. Advances in the research of long-acting strategy of insulin and GLP-1 analogs[J]. Journal of China Pharmaceutical University, 2018, 49(6): 660-670. DOI: 10.11665/j.issn.1000-5048.20180604

Advances in the research of long-acting strategy of insulin and GLP-1 analogs

More Information
  • Insulin as well as glucagon-like peptide 1(GLP-1)and its analogs are commonly used in treating type II diabetes. Both insulin and GLP-1 are endogenous peptides, and have advantages such as high efficiency and selectivity. However, there are some disadvantages to using regular insulin with slow effect, short-time effect and risk of hypoglycemia. Due to the elimination of kidneys and the metabolism of enzymes, the half-life of GLP-1 is so short that neither of them can stabilize glucose. Therefore, it is of great significance to study the long-acting strategy of insulin and GLP-1. Based on the long-acting strategy and pharmacological assessment of peptide drugs, this paper reviewed the latest progress of the related drugs that already on the market and under research to provide references for the design of novel long-acting insulin and GLP-1 analogs.
  • [1]
    Cho NH,Shaw JE,Karuranga S,et al.IDF diabetes atlas:global estimates of diabetes prevalence for 2017 and projections for 2045[J].Diabetes Res Clin Pract,2018,138:271-281.
    [2]
    Donnelly D.The structure and function of the glucagon-like peptide-1 receptor and its ligands[J].Br J Pharmacol,2012,166(1):27-41.
    [3]
    Pham H,Hui H,Morvaridi S,et al.A bitter pill for type 2 diabetes? The activation of bitter taste receptor TAS2R38 can stimulate GLP-1 release from enteroendocrine L-cells[J].Biochem Biophys Res Commun,2016,475(3):295-300.
    [4]
    Kolterman OG,Kim DD,Shen L,et al.Pharmacokinetics,pharmacodynamics,and safety of exenatide in patients with type 2 diabetes mellitus[J].Am J Health Syst Pharm,2005,62(2):173-181.
    [5]
    Lepore M,Pampanelli S,Fanelli C,et al.Pharmacokinetics and pharmacodynamics of subcutaneous injection of long-acting human insulin analog glargine,NPH insulin,and ultralente human insulin and continuous subcutaneous infusion of insulin lispro[J].Diabetes,2000,49(12):2142-2148.
    [6]
    Rosenstock J,Park G,Zimmerman J,et al.Basal insulin glargine(HOE 901)versus NPH insulin in patients with type 1 diabetes on multiple daily insulin regimens.U.S.insulin glargine(HOE 901)type 1 diabetes unvestigator group[J].Diabetes Care,2000,23(8):1137-1142.
    [7]
    Ratner RE,Rosenstock J,Boka G,et al.Dose-dependent effects of the once-daily GLP-1 receptor agonist lixisenatide in patients with type 2 diabetes inadequately controlled with metformin:a randomized,double-blind,placebo-controlled trial[J].Diabet Med,2010,27(9):1024-1032.
    [8]
    Havelund S,Plum A,Ribel U,et al.The mechanism of protraction of insulin detemir,a long-acting,acylated analog of human insulin[J].Pharm Res,2004,21(8):1498-1504.
    [9]
    Plank J,Bodenlenz M,Sinner F,et al.A double-blind,randomized,dose-response study investigating the pharmacodynamic and pharmacokinetic properties of the long-acting insulin analog detemir[J].Diabetes Care,2005,28(5):1107-1112.
    [10]
    Jonassen I,Havelund S,Hoeg-Jensen T,et al.Design of the novel protraction mechanism of insulin degludec,an ultra-long-acting basal insulin[J].Pharm Res,2012,29(8):2104-2114.
    [11]
    Heise T,Hovelmann U,Nosek L,et al.Comparison of the pharmacokinetic and pharmacodynamic profiles of insulin degludec and insulin glargine[J].Expert Opin Drug Metab Toxicol,2015,11(8):1193-1201.
    [12]
    Heise T,Meneghini LF.Insulin stacking versus therapeutic accumulation:understanding the differences[J].Endocr Pract,2014,20(1):75-83.
    [13]
    Heller S,Mathieu C,Kapur R,et al.A meta-analysis of rate ratios for nocturnal confirmed hypoglycaemia with insulin degludec vs.insulin glargine using different definitions for hypoglycaemia[J].Diabet Med,2016,33(4):478-487.
    [14]
    Mathieu C,Hollander P,Miranda-Palma B,et al.Efficacy and safety of insulin degludec in a flexible dosing regimen vs insulin glargine in patients with type 1 diabetes(BEGIN:Flex T1):a 26-week randomized,treat-to-target trial with a 26-week extension[J].J Clin Endocrinol Metab,2013,98(3):1154-1162.
    [15]
    Lund A,Knop FK,Vilsboll T.Glucagon-like peptide-1 receptor agonists for the treatment of type 2 diabetes:differences and similarities[J].Eur J Intern Med,2014,25(5):407-414.
    [16]
    Blonde L,Russell-Jones D.The safety and efficacy of liraglutide with or without oral antidiabetic drug therapy in type 2 diabetes:an overview of the LEAD 1-5 studies[J].Diabetes Obes Metab,2009,11(Suppl 3):26-34.
    [17]
    Gotfredsen CF, Molck AM, Thorup I, et al. The human GLP-1 analogs liraglutide and semaglutide:absence of histopathological effects on the pancreas in nonhuman primates[J].Diabetes,2014,63(7):2486-2497.
    [18]
    Marso SP,Bain SC,Consoli A,et al.Semaglutide and cardiovascular outcomes in patients with type 2 diabetes[J].N Engl J Med,2016,375(19):1834-1844.
    [19]
    Pratley RE,Aroda VR,Lingvay I,et al.Semaglutide versus dulaglutide once weekly in patients with type 2 diabetes(SUSTAIN 7):a randomised,open-label,phase 3b trial[J].Lancet Diabetes Endocrinol,2018,6(4):275-286.
    [20]
    Jackson VM,Breen DM,Fortin JP,et al.Latest approaches for the treatment of obesity[J].Expert Opin Drug Discov,2015,10(8):825-839.
    [21]
    Granhall C,Sondergaard FL,Thomsen M,et al.Pharmacokinetics,safety and tolerability of oral semaglutide in subjects with renal impairment[J].Clin Pharmacokinet,2018.https://doi.org/10.1007/s40262-018-0649-2.
    [22]
    Han J, Sun L, Chu Y, et al. Design,synthesis,and biological activity of novel dicoumarol glucagon-like peptide 1 conjugates[J].J Med Chem,2013,56(24):9955-9968.
    [23]
    Roopenian DC,Akilesh S.FcRn:the neonatal Fc receptor comes of age[J].Nat Rev Immunol,2007,7(9):715-725.
    [24]
    Wronkowitz N,Hartmann T,Gorgens SW,et al.(LAPS)Insulin115:a novel ultra-long-acting basal insulin with a unique action profile[J].Diabetes Obes Metab,2017,19(12):1722-1731.
    [25]
    Choi IY.A long-acting Exendin-4 analog conjugate to the human Fc fragment reveals low immunogenic potential[EB/OL].http://www.hanmipharm.com/ehanmi/img/rnd/2014_01.pdf.
    [26]
    Watkins C.Overview of HM11260C(Efpeglenatide)[EB/OL].http://www.hanmi.co.kr/hanmi/img/rnd/2015_EASD_(HM11260C).pdf.
    [27]
    Hanmi Pharmaceutical Co.,Ltd.Hanmi′s LAPS-Exendin4 progresses to multi-national phase IIb clinical studies[EB/OL].http://www.marketwired.com/press-release/hanmi-pharmaceutical-announces-multinational-phase-iib-clinical-studies-on-laps-exendin4-kse-128940-1841437.htm.
    [28]
    Grunberger G,Chang A,Garcia SG,et al.Monotherapy with the once-weekly GLP-1 analogue dulaglutide for 12 weeks in patients with type 2 diabetes:dose-dependent effects on glycaemic control in a randomized,double-blind,placebo-controlled study[J].Diabet Med,2012,29(10):1260-1267.
    [29]
    Rosenstock J,Reusch J,Bush M,et al.Potential of albiglutide,a long-acting GLP-1 receptor agonist,in type 2 diabetes:a randomized controlled trial exploring weekly,biweekly,and monthly dosing[J].Diabetes Care,2009,32(10):1880-1886.
    [30]
    Pratley RE,Nauck MA,Barnett AH,et al.Once-weekly albiglutide versus once-daily liraglutide in patients with type 2 diabetes inadequately controlled on oral drugs(HARMONY 7):a randomised,open-label,multicentre,non-inferiority phase 3 study[J].Lancet Diabetes Endocrinol,2014,2(4):289-297.
    [31]
    O′connor-Semmes RL, Lin J, Hodge RJ, et al. GSK2374697,a novel albumin-binding domain antibody(AlbudAb),extends systemic exposure of exendin-4:first study in humans - PK/PD and safety[J].Clin Pharmacol Ther,2014,96(6):704-712.
    [32]
    Munoz-Garach A,Molina-Vega M,Tinahones FJ.How can a good idea fail? basal insulin peglispro [LY2605541] for the treatment of type 2 diabetes[J].Diabetes Ther,2017,8(1):9-22.
    [33]
    Sinha VP,Choi SL,Soon DK,et al.Single-dose pharmacokinetics and glucodynamics of the novel,long-acting basal insulin LY2605541 in healthy subjects[J].J Clin Pharmacol,2014,54(7):792-799.
    [34]
    Garg S,Dreyer M,Jinnouchi H,et al.A randomized clinical trial comparing basal insulin peglispro and insulin glargine,in combination with prandial insulin lispro,in patients with type 1 diabetes:IMAGINE 1[J].Diabetes Obes Metab,2016,18(Suppl 2):25-33.
    [35]
    Rong Y,Yang ZY.Progress in research and development of glucagon-like peptide 1 analogues as new drugs[J].Chin J Biologicals(中国生物制品学杂志),2011,24(7):866-868,872.
    [36]
    Cai Y,Wei L,Ma L,et al.Long-acting preparations of exenatide[J].Drug Des Devel Ther,2013,7:963-970.
    [37]
    Schellenberger V,Wang CW,Geething NC,et al.A recombinant polypeptide extends the in vivo half-life of peptides and proteins in a tunable manner[J].Nat Biotechnol,2009,27(12):1186-1190.
    [38]
    De LPA,Riddle M,Morrow LA,et al.Pharmacokinetics and pharmacodynamics of high-dose human regular U-500 insulin versus human regular U-100 insulin in healthy obese subjects[J].Diabetes Care,2011,34(12):2496-2501.
    [39]
    Sindelka G,Heinemann L,Berger M,et al.Effect of insulin concentration,subcutaneous fat thickness and skin temperature on subcutaneous insulin absorption in healthy subjects[J].Diabetologia,1994,37(4):377-380.
    [40]
    Becker RH, Nowotny I, Teichert L, et al. Low within- and between-day variability in exposure to new insulin glargine 300 U/mL[J].Diabetes Obes Metab,2015,17(3):261-267.
    [41]
    Becker RH,Dahmen R,Bergmann K,et al.New insulin glargine 300 Units/mL provides a more even activity profile and prolonged glycemic control at steady state compared with insulin glargine 100 Units/mL[J].Diabetes Care,2015,38(4):637-643.
    [42]
    Li X,Li L,Wang X,et al.Application of model-based methods to characterize exenatide-loaded double-walled microspheres: in vivo release,pharmacokinetic/pharmacodynamic model,and in vitro and in vivo correlation[J].J Pharm Sci,2012,101(10):3946-3961.
    [43]
    Norwood P,Liutkus JF,Haber H,et al.Safety of exenatide once weekly in patients with type 2 diabetes mellitus treated with a thiazolidinedione alone or in combination with metformin for 2 years[J].Clin Ther,2012,34(10):2082-2090.
    [44]
    Nikou KN,Stivaktakis N,Avgoustakis K,et al.A HER-2/neu peptide admixed with PLA microspheres induces a Th1-biased immune response in mice[J].Biochim Biophys Acta,2005,1725(2):182-189.
    [45]
    Mooradian AD, Bernbaum M, Albert SG. Narrative review:a rational approach to starting insulin therapy[J].Ann Intern Med,2006,145(2):125-134.
    [46]
    Jehle PM,Micheler C,Jehle DR,et al.Inadequate suspension of neutral protamine Hagendorn(NPH)insulin in pens[J].Lancet,1999,354(9190):1604-1607.
    [47]
    Narayan RJ.Transdermal delivery of insulin via microneedles[J].J Biomed Nanotechnol,2014,10(9):2244-2260.
    [48]
    Kumareswaran K, Evans ML, Hovorka R. Closed-loop insulin delivery:towards improved diabetes care[J].Discov Med,2012,13(69):159-170.
    [49]
    Roze S,Smith-Palmer J,Valentine W,et al.Cost-effectiveness of continuous subcutaneous insulin infusion versus multiple daily injections of insulin in type 1 diabetes:a systematic review[J].Diabet Med,2015,32(11):1415-1424.
    [50]
    Bergenstal RM,Garg S,Weinzimer SA,et al.Safety of a hybrid closed-loop insulin delivery system in patients with type 1 diabetes[J].JAMA,2016,316(13):1407-1408.
    [51]
    Oleck J,Kassam S,Goldman JD.Commentary:why was inhaled insulin a failure in the market [J]?Diabetes Spectr,2016,29(3):180-184.
    [52]
    Al-Tabakha MM.Future prospect of insulin inhalation for diabetic patients:the case of Afrezza versus Exubera[J].J Control Release,2015,215:25-38.
    [53]
    Henry RR,Rosenstock J,Denham DS,et al.Clinical impact of ITCA 650,a novel drug-device GLP-1 receptor agonist,in uncontrolled type 2 diabetes and very high baseline HbA1c:the FREEDOM-1 HBL(high baseline)study[J].Diabetes Care,2018,41(3):613-619.
    [54]
    Henry RR,Rosenstock J,Logan DK,et al.Randomized trial of continuous subcutaneous delivery of exenatide by ITCA 650 versus twice-daily exenatide injections in metformin-treated type 2 diabetes[J].Diabetes Care,2013,36(9):2559-2565.
    [55]
    Vora J.Combining incretin-based therapies with insulin:realizing the potential in type 2 diabetes[J].Diabetes Care,2013,36(Suppl 2):S226-S232.
    [56]
    Hughes E.IDegLira:redefining insulin optimisation using a single injection in patients with type 2 diabetes[J].Primary Care Diabetes,2016,10(3):202-209.
    [57]
    Rodbard HW,Buse JB,Woo V,et al.Benefits of combination of insulin degludec and liraglutide are independent of baseline glycated haemoglobin level and duration of type 2 diabetes[J].Diabetes Obes Metab,2016,18(1):40-48.
    [58]
    Wu W,Zhou S.Responsive materials for self-regulated insulin delivery[J].Macromol Biosci,2013,13(11):1464-1477.
    [59]
    Li D, Fu M, Qian H, et al. Phenylboronic acid-based glucose-responsive materials:synthesis and applications in insulin delivery[J].J China Pharm Univ(中国药科大学学报),2017,48(3):259-267.
  • Related Articles

    [1]XIA Ying, GUO Hongli, HU Yahui, CHEN Feng. Therapeutic drug monitoring for monoclonal antibody:progress in the application of LC-MS/MS technique[J]. Journal of China Pharmaceutical University, 2021, 52(1): 122-128. DOI: 10.11665/j.issn.1000-5048.20210117
    [2]JI Shunli, SONG Fanfan, ZHENG Yang, DING Li. Simultaneous determination of amoxicillin and clavulanic acid by LC-MS/MS in human plasma and its application to a bioequivalence study[J]. Journal of China Pharmaceutical University, 2019, 50(6): 699-706. DOI: 10.11665/j.issn.1000-5048.20190610
    [3]LIANG Feng, LI Duo, WANG Rongbin, SHU Chang, DING Li. Pharmacokinetics and absolute bioavailability of isoschaftoside in rat by LC-MS/MS[J]. Journal of China Pharmaceutical University, 2019, 50(1): 75-80. DOI: 10.11665/j.issn.1000-5048.20190110
    [4]LIU Chaoyi, ZHANG Ge, HANG Taijun, WANG Lei, ZHANG Xiaofei, SONG Min. Identification of related substances in rivaroxaban by LC-MS[J]. Journal of China Pharmaceutical University, 2015, 46(4): 450-457. DOI: 10.11665/j.issn.1000-5048.20150411
    [5]LI Jingjing, TAN Jingfu, YANG Jie, WANG Qiang. Pharmacokinetic study of corosolic acid in normal rats and diabetic rats by LC-MS[J]. Journal of China Pharmaceutical University, 2014, 45(1): 84-87. DOI: 10.11665/j.issn.1000-5048.20140115
    [6]YANG Youtian, MAO Baiyang, CHENG Lifei, SU Mengxiang, DI Bin. Identification of the related substances in telmisartan/amlodipine double layer tablets by LC-MS/MS[J]. Journal of China Pharmaceutical University, 2014, 45(1): 65-69. DOI: 10.11665/j.issn.1000-5048.20140111
    [7]MU Yanan, YANG Jin. Determination of epothilone B in human blood by LC-MS/MS and its application in phase I pharmacokinetics study[J]. Journal of China Pharmaceutical University, 2013, 44(1): 89-92. DOI: 10.11665/j.issn.1000-5048.20130115
    [8]SI Qian, CHEN Yuan-cheng, HUANG Li-hua, CHENG Yu, HE Hua, LIU Xiao-quan. Determination of nebivolol in human plasma by LC-MS/MS and study of its pharmacokinetics on the Chinese[J]. Journal of China Pharmaceutical University, 2011, 42(2): 136-140.
    [9]Determination of Ranolazine and Its Pharmacokinetics in Dog by LC-MS[J]. Journal of China Pharmaceutical University, 2004, (2): 59-62.
    [10]Determination of Clarithromycin in Human Plasma by LC-MS Method[J]. Journal of China Pharmaceutical University, 2004, (1): 52-55.

Catalog

    Article views (1423) PDF downloads (1882) Cited by()

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return