Comparison of DPP-4 Inhibitors

Nam Hoon Kim; Sin Gon Kim

doi:10.4093/jkd.2013.14.3.111

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Kim and Kim: Comparison of DPP-4 Inhibitors

Statement

J Korean Diabetes 2013;14(3):111-119.

Published online: 10 January 2013

DOI: https://doi.org/10.4093/jkd.2013.14.3.111

Comparison of DPP-4 Inhibitors

Nam Hoon Kim, Sin Gon Kim

Division of Endocrinology and Metabolism, Department of Internal Medicine, Korea University College of Medicine, Seoul, Korea

This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

During past several years, a novel class of antihyperglycemic agents, dipeptidyl peptidase-4 (DPP-4) inhibitors, has become one of the most important options in the management of type 2 diabetes. These agents have unique insulinotropic actions as well as other advantages such as lower hypoglycemia and a weight-neutral effect compared to traditional insulin secretagogues. To date, 6 different DPP-4 inhibitors have been introduced: sitagliptin, vildagliptin, saxagliptin, linagliptin, alogliptin and gemiglitin. This review provides a summary of the clinical data for each DPP-4 inhibitor, and discusses the similarities and differences between them.

Keywords: Dipeptidyl-peptidase IV inhibitors, Incretins, Diabetes mellitus

References

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Table 1.

Structure-activtiy relationship and pharmacodynamics of dipeptidyl peptidase (DPP)-4 inhibitors

Drug (ref.)	Structure	IC50 (nmol/L)	DPP-4 selectivity^a	Inhibition of plasma DPP-4 activity (%)	Increase in active GLP-1 levels	Half-life (hr)
Sitagliptin [8]	Piperazine	18	＞ 2600	≥ 80	2-fold	8–14
Vildagliptin [9,10]	Cyanopyrrolidine	3.5	100	≥ 80	3-fold	2–3
Saxagliptin [11]	Cyanopyrrolidine	0.5	100	≥ 70	1.5 to 2-fold	2.5
Linagliptin [12,13]	Xanthine-based	1	＞ 10000	≥ 70	2 to 3-fold	113–131
Alogliptin [14,15]	Pyrimidine	7	＞ 14000	＞ 75	2 to 2-fold	12.4–21.4
Gemigliptin [16]^b	Pyrimidopiperidine	6.3	＞ 3400	NA	2 to 3-fold	17–21

^a vs. DPP-8 or DPP-9.

^b also from unpublished data of LG Life Science. GLP-1, glucagon like peptide-1; NA, not available.

Table 2.

Dosage adjustments for kidney disease

Drug	Usual dose (daily)	Ccr ＞ 50 mL/min	Renal impairment Ccr 30–50 mL/min	Ccr ＜ 30 mL/min
Sitagliptin	100 mg	100 mg	50 mg	25 mg
Vildagliptin	100 mg	100 mg	50 mg	50 mg
Saxagliptin	5 mg	5 mg	2.5 mg	2.5 mg
Linagliptin	5 mg	5 mg	5 mg	5 mg
Alogliptin	25 mg	25 mg	12.5 mg	6.25 mg
Gemigliptin^a	50 mg	50 mg	50 mg	50 mg

^a KFDA approved based on pharmacokinetic/pharmacodynamic data but not clinical data.

Table 3.

Efficacy of dipeptidyl peptidase (DPP)-4 inhibtors as an initial monotherapy in drug-naïve type 2 diabetic patients

Drug	No. of patients	Study duration	Baseline HbA1c level	Study group	Control	Reduction of HbA1c	Reference no.
Sitagliptin	741	24 wk	8.0%	Sita 100 mg	Placebo	–0.79%	[20]
				Sita 200 mg		–0.94%
	1091	24 wk	8.8%	Sita 100 mg	Placebo	–0.83%	[21]
Vildagliptin	354	24 wk	8.4%	Vilda 50 mg qd	Placebo	–0.5%	[22]
				Vilda 50 mg bid		–0.7%
				Vilda 100 mg qd		–0.9%
	632	24 wk	8.4%	Vilda 50 mg qd	Placebo	–0.5%	[23]
				Vilda 50 mg bid		–0.5%
				Vilda 100 mg qd		–0.6%
Saxagliptin	401	24 wk	7.9%	Saxa 2.5 mg	Placebo	–0.52%	[24]
				Saxa 5 mg		–0.55%
				Saxa 10 mg		–0.63%
Linagliptin	503	24 wk	8.0%	Lina 5 mg	Placebo	–0.69%	[25]^a
Alogliptin	329	26 wk	7.9%	Alo 12.5 mg	Placebo	–0.58%	[26]
				Alo 25 mg		–0.61%
Gemigliptin	180	24 wk	8.2%	Gemi 50 mg	Placebo	–0.71%	[27]

^a Includes patients who were either drug-naïve or had previously received one oral antihyperglycemic drug (with washout).

Table 4.

Efficacy of dipeptidyl peptidase (DPP)-4 inhibtors as add-on therapy to metformin in type 2 diabetic patients

Drug	No. of patients	Study duration	Baseline HbA1c level	Study group	Control	Reduction of HbA1c	Reference no.
Sitagliptin	701	24 wk	8.0%	MET + Sita 100 mg	MET + Placebo	–0.65%	[28]
	273	18 wk	7.7%	MET + Sita 100 mg	MET + Placebo	–0.51%	[29]
Vildagliptin	544	24 wk	8.4%	MET + Vilda 50 mg	MET + Placebo	–0.7%	[30]
				MET + Vilda 100 mg		–1.1%
	370	24 wk	8.5%	MET + Vilda 100 mg	MET + Placebo	–0.83%	[31]
Saxagliptin	743	24 wk	8.0%	MET + Saxa 2.5 mg	MET + Placebo	–0.73%	[32]
				MET + Saxa 5 mg		–0.83%
				MET + Saxa 10 mg		–0.72%
Linagliptin	701	24 wk	8.1%	MET + Lina 5 mg	MET + Placebo	–0.64%	[33]
Alogliptin	527	26 wk	7.9%	MET + Alo 12.5 mg	MET + Placebo	–0.5%	[34]
				MET + Alo 25 mg		–0.5%

Table 5.

Comparison of dipeptidyl peptidase (DPP)-4 inhibitors with sulfonylureas in type 2 diabetic patients

Drug	No. of patients	Study duration	Baseline HbA1c level	Study group	Control	Reduction of HbA1c	Reference no.
Sitagliptin	1172	52 wk	7.5%	Sita 100 mg + MET	Glipizide 5 mg + MET	–0.67% vs. −0.67%	[35]
Vildagliptin	2789	52 wk	7.3%	MET + Vilda 100 mg	MET + glimepiride (∼6 mg)	–0.44% vs. −0.53%	[36]
	1007	52 wk	8.5%	MET + Vilda 100 mg	MET + gliclazide (∼320 mg)	–0.81% vs. −0.85%	[37]
Saxagliptin	858	52 wk	7.7%	MET + Saxa 5 mg	MET + glipizide (∼20 mg)	–0.74% vs. −0.80%	[38]
Linagliptin	1552	96 wk	7.7%	MET + Lina 5 mg	MET + glimepiride (∼4 mg)	–0.16% vs. −0.36%	[39]

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