Tinjauan atas Glucagon-like Peptide-1 Receptor Agonist

Penulis

  • Johan Indra Lukito Medical Department, PT. Kalbe Farma Tbk. Jakarta, Indonesia

DOI:

https://doi.org/10.55175/cdk.v47i6.628

Kata Kunci:

Diabetes, glucagon-like peptide-1 receptor agonist, incretin

Abstrak

GLP-1 receptor agonist secara struktur mirip hormon alami GLP-1 yang memiliki efek incretin, namun degradasinya dapat dicegah oleh DPP-4. Saat ini terdapat 8 jenis yang terdiri dari exenatide, exenatide ER, liraglutide, albiglutide, dulaglutide, lixisenatide, semaglutide injeksi, dan semaglitode oral. GLP-1 receptor agonist merupakan pilihan pengobatan DM tipe 2 baik sebagai tambahan maupun monoterapi.

 

The GLP-1 receptor agonist is structurally similar to the natural hormone GLP-1 which has an incretin effect but prevented from breakdown by DPP-4. There are currently 8 types of GLP-1: exenatide, exenatide ER, liraglutide, albiglutide, dulaglutide, lixisenatide, injection semaglutide, and oral semaglutide. GLP-1 receptor agonist is an option for the treatment of type 2 DM both as adjunctive and as monotherapy.

Unduhan

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Referensi

Tran KL, Park YI, Pandya S, Muliyil NJ, Jensen BD, Huynh K, et al. Overview of glucagon-like peptide-1 receptor agonists for the treatment of patients with type 2 diabetes. Am Health Drug Benefits 2017;10(4):178–88.

Centers for Disease Control and Prevention. National Diabetes Statistics Report: Estimates of diabetes and its burden in the United States [Internet]. 2014 [cited 2019 October 2]. Available from: https://www.fda.gov/news-events/press-announcements/fda-approves-first-oral-glp-1-treatment-type-2-diabetes www.cdc.gov/diabetes/pubs/statsreport14/national-diabetes-report-web.pdf.

American Diabetes Association. Standards of medical care in diabetes—2017. Diabetes Care. 2017;40(suppl 1):1-135.

American Diabetes Association. Economic costs of diabetes in the U.S. in 2012. Diabetes Care. 2013;36:1033-46.

Byrne MM, Sturis J, Sobel RJ, Polonsky KS. Elevated plasma glucose 2 h postchallenge predicts defects in beta-cell function. Am J Physiol. 1996;270(4 pt 1):572-9.

Bergstrom RW, Wahl PW, Leonetti DL, Fujimoto WY. Association of fasting glucose levels with a delayed secretion of insulin after oral glucose in subjects with glucose intolerance. J Clin Endocrinol Metab. 1990;71:1447-53.

Nauck M, Stöckmann F, Ebert R, Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia. 1986;29:46-52.

Vilsbøll T, Krarup T, Madsbad S, Holst JJ. Defective amplification of the late phase insulin response to glucose by GIP in obese type II diabetic patients. Diabetologia. 2002;45:1111-9

Exenatide injectable solution. Medscape [Internet]. 2019 [cited 2019 October 10]. Available from: https://reference.medscape.com/drug/byetta-exenatideinjectable-solution-342892

Exenatide injectable suspension. Medscape [Internet]. 2019 [cited 2019 October 10]. Available from: https://reference.medscape.com/drug/bydureon-bcisebydureon-exenatide-injectable-suspension-999717

Liraglutide injectable suspension. Medscape [Internet]. 2019 [cited 2019 October 10]. Available from: https://reference.medscape.com/drug/victoza-saxendaliraglutide-999449

Lixisenatide. Medscape [Internet]. 2019 [cited 2019 October 10]. Available from: https://reference.medscape.com/drug/adlyxin-lixisenatide-1000059

Albiglutide injectable suspension. Medscape [Internet]. 2019 [cited 2019 October 10]. Available from: https://reference.medscape.com/drug/tanzeumalbiglutide-999914

Dulaglutide injectable suspension. Medscape [Internet]. 2019 [cited 2019 October 10]. Available from: https://reference.medscape.com/drug/trulicitydulaglutide-999965

Semaglutide. Medscape [Internet]. 2019 [cited 2019 October 10]. Available from: https://reference.medscape.com/drug/ozempic-rybelsus-semaglutide-1000174#0

Chakraborti CK. A new promising antidiabetic agent. Indian J Pharm Sci. 2010;72(1):1–11. doi: 10.4103/0250-474X.62228

Coleman CI, Gryskiewicz KA. Exenatide: A novel incretin mimetic hormone for the treatment of type 2 diabetes. Formulary. 2005;40:86-90.

Jose B, Tahrani AA, Piya MK, Barnett AH. Exenatide once weekly: Clinical outcomes and patient satisfaction. Patient Prefer Adherence. 2010;4:313-24.

Buse JB, Bergenstal RM, Glass LC, Heilmann CR, Lewis MS, Kwan AYM, et al. Use of twice-daily exenatide in basal insulin-treated patients with type 2 diabetes: A randomized, controlled trial. Ann Intern Med. 2011;154:103-12.

Bydureon (exenatide extended-release) for injectable suspension [prescribing information]. Wilmington, DE: AstraZeneca Pharmaceuticals; 2015..

Buse JB, Drucker DJ, Taylor KL, Kim T, Walsh B, Hu H, et al; for the DURATION-1 Study Group. DURATION-1: Exenatide once weekly produces sustained glycemic control and weight loss over 52 weeks. Diabetes Care. 2010;33:1255-61.

Drucker DJ, Buse JB, Taylor K, et al; for the DURATION-1 Study Group.

Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: A randomised, open-label, non-inferiority study. Lancet. 2008;372:1240-50.

Wysham C, Bergenstal R, Malloy J, Yan P, Walsh B, Malone J, et al. DURATION-2: Efficacy and safety of switching from maximum daily sitagliptin or pioglitazone to once-weekly exenatide. Diabet Med. 2011;28:705-14.

Diamant M, Van Gaal L, Guerci B, Stranks S, Han J, Malloy J, et al. Exenatide once weekly versus insulin glargine for type 2 diabetes (DURATION-3): 3-year results of an open-label randomised trial. Lancet Diabetes Endocrinol. 2014;2:464-73. Erratum in: Lancet Diabetes Endocrinol. 2014;2:13.

Russell-Jones D, Cuddihy RM, Hanefeld M, Kumar A, Gonzalez JG, Chan M, et al; for the DURATION-4 Study Group. Efficacy and safety of exenatide once weekly versus metformin, pioglitazone, and sitagliptin used as monotherapy in drug-naïve patients with type 2 diabetes (DURATION-4): A 26-week double blind study. Diabetes Care. 2012;35:252-8.

Blevins T, Pullman J, Malloy J, Yan P, Taylor K, Schulteis C, et al. DURATION-5: Exenatide once weekly resulted in greater improvements in glycemic control compared with exenatide twice daily in patients with type 2 diabetes. J Clin Endocrinol Metab. 2011;96:1301-10.

Buse JB, Nauck M, Forst T, Sheu WHH, Shenouda SK, Heilmann CR, et al. Exenatide once weekly versus liraglutide once daily in patients with type 2 diabetes (DURATION-6): A randomised, open-label study. Lancet. 2013;381:117-24.

Harder H, Nielsen L, Tu DT, Astrup A. The effect of liraglutide, a long-acting glucagon-like peptide 1 derivative, on glycemic control, body composition, and 24-h energy expenditure in patients with type 2 diabetes. Diabetes Care. 2004;27:1915-21

Marre M, Shaw J, Brändle M, Bebakar WMW, Kamaruddin NA, Strand J, et al; for the LEAD-1 SU Study Group. Liraglutide, a once-daily human GLP-1 analogue, added to a sulphonylurea over 26 weeks produces greater improvements in glycaemic and weight control compared with adding rosiglitazone or placebo in subjects with type 2 diabetes (LEAD-1 SU). Diabet Med. 2009;26:268-78.

Nauck M, Frid A, Hermansen K, Shah NS, Tankova T, Mitha IH, et al; for the LEAD-2 Study Group. Efficacy and safety comparison of liraglutide, glimepiride, and placebo, all in combination with metformin, in type 2 diabetes: the LEAD (Liraglutide Effect and Action in Diabetes)-2 study. Diabetes Care. 2009;32:84-90.

Garber A, Henry R, Ratner R, et al; for the LEAD-3 (Mono) Study Group.

Liraglutide versus glimepiride monotherapy for type 2 diabetes (LEAD-3 Mono): a randomised, 52-week, phase III, double-blind, parallel-treatment trial. Lancet. 2009;373:473-81.

Zinman B, Gerich J, Buse JB, Lewin A, Schwartz S, Raskin P, et al; for the LEAD-4 Study Investigators. Efficacy and safety of the human glucagon-like peptide-1 analog liraglutide in combination with metformin and thiazolidinedione in patients with type 2 diabetes (LEAD-4 Met+TZD). Diabetes Care. 2009;32:1224-30.

Russell-Jones D, Vaag A, Schmitz O, Sethi BK, Lalic N, Antic S, et al; for the Liraglutide Effect and Action in Diabetes 5 (LEAD-5) met+SU Study Group. Liraglutide vs insulin glargine and placebo in combination with metformin and sulfonylurea therapy in type 2 diabetes mellitus (LEAD-5 met+SU): A randomised controlled trial. Diabetologia. 2009;52:2046-55.

Buse JB, Rosenstock J, Sesti G, Schmidt WE, Montanya E, Brett JH, et al; for the LEAD-6 Study Group. Liraglutide once a day versus exenatide twice a day for type 2 diabetes: A 26-week randomised, parallel-group, multinational, open label trial (LEAD-6). Lancet. 2009;374:39-47.

Montanya E, Sesti G. A review of efficacy and safety data regarding the use of liraglutide, a once-daily human glucagon-like peptide 1 analogue, in the treatment of type 2 diabetes mellitus. Clin Ther. 2009;31:2472-88.

Thompson PL, Davis TM. Cardiovascular effects of glucose-lowering therapies for type 2 diabetes: new drugs in perspective. Clin Ther. 2017;39:1012-25

Tanzeum (albiglutide) for injection [prescribing information]. Research Triangle Park, NC: GlaxoSmithKline; 2016.

Reusch J, Stewart MW, Perkins CM, Cirkel DT, Ye J, Perry CR, et al. Efficacy and safety of once weekly glucagon-like peptide 1 receptor agonist albiglutide (HARMONY 1 trial): 52- week primary endpoint results from a randomized, double-blind, placebo-controlled trial in patients with type 2 diabetes mellitus not controlled on pioglitazone, with or without metformin. Diabetes Obes Metab. 2014;16:1257-64.

Nauck MA, Stewart MW, Perkins C, Jones-Leone A, Yang F, Perry C, et al. Efficacy and safety of once weekly GLP-1 receptor agonist albiglutide (HARMONY 2): 52 week primary endpoint results from a randomised, placebo-controlled trial in patients with type 2 diabetes mellitus inadequately controlled with diet and exercise. Diabetologia. 2016;59:266-74.

Ahrén B, Johnson SL, Stewart M, Cirkel DT, Yang F, Perry C, et al; for the HARMONY 3 Study Group. HARMONY 3: 104-week randomized, double-blind, placebo- and active-controlled trial assessing the efficacy and safety of albiglutide compared with placebo, sitagliptin, and glimepiride in patients with type 2 diabetes taking metformin. Diabetes Care. 2014;37:2141-8.

Weissman PN, Carr MC, Ye J, Cirkel DT, Stewart M, Perry C, et al. HARMONY 4: Randomised clinical trial comparing once-weekly albiglutide and insulin glargine in patients with type 2 diabetes inadequately controlled with metformin with or without sulfonylurea. Diabetologia. 2014;57:2475-84.

Home PD, Shamanna P, Stewart M, Yang F, Miller M, Carr MC. Efficacy and tolerability of albiglutide versus placebo or pioglitazone over 1 year in people with type 2 diabetes currently taking metformin and glimepiride: HARMONY 5. Diabetes Obes Metab. 2015;17:179-87.

Rosenstock J, Fonseca VA, Gross JL, Ratner RE, Ahren B, Chow FCC, et al; for the HARMONY 6 Study Group. Advancing basal insulin replacement in type 2 diabetes inadequately controlled with insulin glargine plus oral agents: A comparison of adding albiglutide, a weekly GLP-1 receptor agonist, versus thrice-daily prandial insulin lispro. Diabetes Care. 2014;37:2317-25.

Pratley RE, Nauck MA, Barnett AH, Feinglos MN, Ovalle F, Harman-Boehm I, et al; for the HARMONY 7 Study Group. 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. Lancet Diabetes Endocrinol. 2014;2:289-97.

Leiter LA, Carr MC, Stewart M, Jones-Leone A, Scott R, Yang F, et al. Efficacy and safety of the once-weekly GLP-1 receptor agonist albiglutide versus sitagliptin in patients with type 2 diabetes and renal impairment: A randomized phase III study. Diabetes Care 2014;37(10):2723-30.

Trulicity (dulaglutide) injection [prescribing information]. Indianapolis, IN: Eli Lilly; February 2017.

Wysham C, Blevins T, Arakaki R, Colon G, Garcia P, Atisso C, et al. Efficacy and safety of dulaglutide added onto pioglitazone and metformin versus exenatide in type 2 diabetes in a randomized controlled trial (AWARD-1). Diabetes Care. 2014;37:2159-67.

Giorgino F, Benroubi M, Sun JH, Zimmermann AG, Pechtner V. Efficacy and safety of once-weekly dulaglutide versus insulin glargine in patients with type 2 diabetes on metformin and glimepiride (AWARD-2). Diabetes Care. 2015;38:2241-9.

Umpierrez G, Tofé Povedano S, Pérez Manghi F, Shurzinske L, Pechtner V. Efficacy and safety of dulaglutide monotherapy versus metformin in type 2 diabetes in a randomized controlled trial (AWARD-3). Diabetes Care. 2014;37:2168-76.

Blonde L, Jendle J, Gross J, Woo V, Jiang H, Fahrbach JL, et al. Once-weekly dulaglutide versus bedtime insulin glargine, both in combination with prandial insulin lispro, in patients with type 2 diabetes (AWARD-4): A randomised, open-label, phase 3, non-inferiority study. Lancet. 2015;385:2057-66.

Nauck M, Weinstock RS, Umpierrez GE, Guerci B, Skrivanek Z, Milicevic Z. Efficacy and safety of dulaglutide versus sitagliptin after 52 weeks in type 2 diabetes in a randomized controlled trial (AWARD-5). Diabetes Care. 2014;37:2149-58.

Dungan KM, Povedano ST, Forst T, Gonzalez JGG, Atisso C, Sealls W, et al. Lancet. 2014;384:1349-57.

Dungan KM, Weitgasser R, Perez Manghi F, Pintilei E, Fahrbach JL, Jiang HH, et al. A 24-week study to evaluate the efficacy and safety of once-weekly dulaglutide added on to glimepiride in type 2 diabetes (AWARD-8). Diabetes Obes Metab. 2016;18:475-82.

Adlyxin (lixisenatide) injection [prescribing information]. Bridgewater, NJ: sanofi-aventis US; 2016.

Seino Y, Yabe D, Takami A, Niemoeller E, Takagi H. Long-term safety of once-daily lixisenatide in Japanese patients with type 2 diabetes mellitus: GetGoal-Mono-Japan. J Diabetes Complications. 2015;29:1304-9.

Fonseca VA, Alvarado-Ruiz R, Raccah D, Boka G, Miossec P, Gerich JE, et al; for the EFC6018 GetGoal-Mono Study Investigators. Efficacy and safety of the oncedaily GLP-1 receptor agonist lixisenatide in monotherapy: A randomized, double-blind, placebo- controlled trial in patients with type 2 diabetes (GetGoal-Mono). Diabetes Care. 2012;35:1225-31.

Bolli GB, Munteanu M, Dotsenko S, Niemoeller E, Boka G, Wu Y, et al. Efficacy and safety of lixisenatide once daily vs. placebo in people with type 2 diabetes insufficiently controlled on metformin (GetGoal-F1). Diabet Med. 2014;31:176-84.

Onishi Y, Niemoeller E, Ikeda Y, Takagi H, Yabe D, Seino Y. Efficacy and safety of lixisenatide in Japanese patients with type 2 diabetes mellitus inadequately controlled by sulfonylurea with or without metformin: subanalysis of GetGoal-S. J Diabetes Investig. 2015;6:201-9.

Riddle MC, Aronson R, Home P, Marre M, Niemoeller E, Miossec P, et al. Adding once-daily lixisenatide for type 2 diabetes inadequately controlled by established basal insulin: A 24-week, randomized, placebo-controlled comparison (GetGoal-L). Diabetes Care. 2013; 36:2489-96.

Pinget M, Goldenberg R, Niemoeller E, Muehlen-Bartmer I, Guo H, Aronson R. Efficacy and safety of lixisenatide once daily versus placebo in type 2 diabetes insufficiently controlled on pioglitazone (GetGoal-P). Diabetes Obes Metab. 2013;15:1000-7.

Seino Y, Min KW, Niemoeller E, Takami A; for the EFC10887 GETGOAL-

L Asia Study Investigators. Randomized, double-blind, placebo controlled trial of the once-daily glp-1 receptor agonist lixisenatide in Asian patients with type 2 diabetes insufficiently controlled on basal insulin with or without a sulfonylurea (GetGoal-L-Asia). Diabetes Obes Metab. 2012;14:910-7.

Rosenstock J, Raccah D, Korányi L, Maffei L, Boka G, Miossec P, et al. Efficacy and safety of lixisenatide once daily versus exenatide twice daily in type 2 diabetes inadequately controlled on metformin: A 24-week, randomized, open-label, active-controlled study (GetGoal-X). Diabetes Care. 2013;36:2945-51.

Yu Pan C, Han P, Liu X, Yan S, Feng P, Zhou Z, et al. Lixisenatide treatment improves glycaemic control in Asian patients with type 2 diabetes mellitus inadequately controlled on metformin with or without sulfonylurea: A randomized, double-blind, placebo-controlled, 24-week trial (GetGoal-M-Asia). Diabetes Metab Res Rev. 2014;30:726-35.

Pfeffer MA, Claggett B, Diaz R, Dickstein K, Gerstein HC, Kober LV, et al; for the ELIXA Investigators. Lixisenatide in patients with type 2 diabetes and acute coronary syndrome. N Engl J Med. 2015;373:2247-57.

Novo Nordisk. Novo Nordisk files for regulatory approval of once-weekly semaglutide with the FDA for the treatment of type 2 diabetes. Press release [Internet]. 2016 December 5 [cited 2017 May 18]. Available from: http://press.novonordisk-us.com/2016-12-05-Novo-Nordisk- Files-for-Regulatory-Approval-of-Once-Weekly-Semaglutide-with-the-FDAfor- the-Treatment-of-Type-2-Diabetes.

Lau J, Bloch P, Schäffer L, Pettersson I, Spetzler J, Kofoid J, et al. Discovery of the once-weekly glucagon-like peptide-1 (GLP-1) analogue semaglutide. J Med Chem. 2015;58:7370-80.

Marso SP, Bain SC, Consoli A, Eliaschewitz FG, Jodar E, Leiter LA, et al; for the SUSTAIN-6 Investigators.

Semaglutide and cardiovascular outcomes in patients with type 2 diabetes. N Engl J Med. 2016;375:1834-44.

US Food and Drug Administration. FDA approves first oral GLP-1 treatment for type 2 diabetes [Internet]. 2019 [cited 2019 October 2]. Available from: https://www.fda.gov/news-events/press-announcements/fda-approves-first-oral-glp-1-treatment-type-2-diabetes

US Food and Drug Administration. HIGHLIGHTS OF PRESCRIBING INFORMATION: RYBELSUS [Internet]. 2019 [cited 2019 October 2]. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/213051s000lbl.pdf

Davies M, Jabbour S, Pieber TR, Rosenstock J, Hartof-Nielsen ML, Hansen OKH, et al. Robust dose-dependent glucose lowering and body weight (BW) reductions with the novel oral formulation of semaglutide in patients with early type 2 diabetes (T2D). Endocr Rev. 2016; 37(2 suppl):Abstract OR15-3.

Diterbitkan

2020-08-03

Cara Mengutip

Lukito, J. I. (2020). Tinjauan atas Glucagon-like Peptide-1 Receptor Agonist. Cermin Dunia Kedokteran, 47(6), 448–454. https://doi.org/10.55175/cdk.v47i6.628