Teneligliptin: expectations for its pleiotropic action

Figures & data

Figure 1. Structure and classification of the DPP-4 inhibitors, showing the J-shaped structure and anchor-lock domain of teneligliptin.

Figure 2. Effect of teneligliptin on glycosylated hemoglobin (HbA_1c) levels in type 2 diabetic patients (n = 324) in Japan in a double-blind placebo-controlled trial. Values are least square means ± standard error.

Figure 3. Effect of teneligliptin on 1- or 2-h postprandial glucose levels and fasting plasma glucose at week 4 in type 2 diabetic patients in Japan in a placebo-controlled trial. Values are least square means ± standard error. Teneligliptin 20 mg group: n = 33; placebo group: n = 32.

Table 1. Indices of daily blood glucose fluctuations measured by continuous glucose monitoring in patients before or 1 – 3 days after the start of teneligliptin treatment.

	Before	1 – 3 days after	p value
24-h mean glucose level (mg/dl)	162.6 ± 16.7	144.7 ± 13.9	0.014
Day time (06:00 – 21:00) mean glucose level (mg/dl)	177.3 ± 14.4	154.8 ± 18.0	0.016
Night time (21:00 – 06:00) mean glucose level (mg/dl)	136.8 ± 25.2	127.6 ± 14.3	0.20
Standard deviation of 24-h glucose levels (mg/dl)	38.9 ± 12.1	27.6 ± 12.8	0.0078
Mean amplitude of glycemic excursions (mg/dl)	83.1 ± 31.5	64.5 ± 29.1	0.047
Proportion (%) of time of
Hyperglycemia (> 180 mg/dl)	33.5 ± 11.1	13.4 ± 14.3	0.0078
Hypoglycemia (< 70 mg/dl)	0	0

Table reproduced from [32] with permission from the Japan Endocrine Society © 2014.

Figure 4. A. Action of teneligliptin in a metabolic syndrome rat model. B. Vasoprotective effects of teneligliptin in a metabolic syndrome rat model.

Box 1. Drug summary.

Drug name (generic)	Teneligliptin
Phase (for indication under discussion)	Approved in Japan and Korea; currently undergoing Phase I trials in the USA and Phase II trials in Europe
Indication (specific to discussion)	Type 2 diabetes mellitus (T2DM)
Pharmacology description/mechanism of action	Prolylthiazolidine-based dipeptidyl peptidase (DPP)-4 inhibitor
Route of administration	Oral
Chemical structure	(3-[(2S,4S)- 4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine)
Pivotal trial(s)	[27-30]

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