NCT00730275

A Study to Assess the Pharmacokinetics, Safety and Tolerability of Sitagliptin in Adolescents (0431-081)

Completed Phase 1 Results posted Last updated 12 May 2017

What this trial tests

Phase 1 trial testing Sitagliptin phosphate in Type 2 Diabetes in 35 participants. Completed in 14 February 2011.

Timeline

18 July 2008

Primary endpoint
30 December 2010

14 February 2011

Quick facts

Lead sponsor	Merck Sharp & Dohme LLC
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	parallel
Masking	double
Primary purpose	treatment
Enrollment	35
Start date	18 July 2008
Primary completion	30 December 2010
Estimated completion	14 February 2011

Drugs / interventions tested

• Sitagliptin phosphate — full drug profile →
• Comparator: matching placebo — full drug profile →

Conditions studied

• Type 2 Diabetes — all drugs for Type 2 Diabetes →

Sponsor

Merck Sharp & Dohme LLC — full company profile →

Who can join

Adults 10 to 17, any sex, with Type 2 Diabetes. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Number of Participants Who Experienced at Least One Adverse Event Primary · Pre-study through 10 to 14 days following administration of study drug

Group	Value	95% CI
Sitagliptin 50 mg	3
Sitagliptin 100 mg	1
Sitagliptin 200 mg	1
Placebo	2

Area Under the Concentration-time Curve (AUC) From Time 0 to Infinity Following a Single Dose of Sitagliptin Primary · Pre-dose through 72 hours post-dose

Serum samples were used to determine the AUC from time 0 to infinity for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.

Group	Value	95% CI
Sitagliptin 50 mg	3438	2881 – 4103
Sitagliptin 100 mg	5869	4918 – 7003
Sitagliptin 200 mg	12965	10749 – 15638

Maximum Concentration (Cmax) Following a Single Dose of Sitagliptin Secondary · Pre-dose through 72 hours post-dose

Serum samples were used to determine the Cmax for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.

Group	Value	95% CI
Sitagliptin 50 mg	366	288 – 464
Sitagliptin 100 mg	666	526 – 845
Sitagliptin 200 mg	1876	1458 – 2413

Time of Occurence of Maximum Concentration (Tmax) Following a Single Dose of Sitagliptin Secondary · Pre-dose through 72 hours post-dose

Serum samples were used to determine the Tmax for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.

Group	Value	95% CI
Sitagliptin 50 mg	3.0	1.5 – 5.0
Sitagliptin 100 mg	3.0	2.0 – 4.5
Sitagliptin 200 mg	2.5	1.0 – 3.1

Apparent Terminal Half-life (Apparent t1/2) Following a Single Dose of Sitagliptin Secondary · Pre-dose through 72 hours post-dose

Serum samples were used to determine the apparent t1/2 for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.

Group	Value	95% CI
Sitagliptin 50 mg	12.1	± 1.7
Sitagliptin 100 mg	11.2	± 2.1
Sitagliptin 200 mg	11.7	± 1.8

Plasma Dipeptidyl Peptidase-4 (DPP-4) Activity Following a Single Dose of Sitagliptin or Placebo Secondary · Pre-dose through 24 hours post-dose

Plasma DPP-4 activity was analyzed using the 24-hour weighted average inhibition (WAI) and percent inhibition at 24 hours post-dose. WAI was defined as the AUC of inhibition divided by the length of the post-dose time interval. Positive values of WAI represent a decrease in DPP-4 activity.

24-hour WAI of DPP-4 activity

Group	Value	95% CI
Sitagliptin 50 mg	73.98	70.59 – 76.99
Sitagliptin 100 mg	80.53	77.98 – 82.78
Sitagliptin 200 mg	87.96	86.29 – 89.43
Placebo	6.76	-6.21 – 18.14

DDP-4 activity at 24 hours post-dose

Group	Value	95% CI
Sitagliptin 50 mg	53.98	46.74 – 60.24
Sitagliptin 100 mg	62.78	56.92 – 67.84
Sitagliptin 200 mg	75.76	71.70 – 79.24
Placebo	3.57	-12.60 – 17.43

Adverse events — posted to ClinicalTrials.gov

Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Sitagliptin 50 mg

Serious: 0/9 (0%)

Deaths: —

Sitagliptin 100 mg

Serious: 0/9 (0%)

Deaths: —

Sitagliptin 200 mg

Serious: 0/8 (0%)

Deaths: —

Placebo

Serious: 0/9 (0%)

Deaths: —

Other adverse events (14 terms — click to expand)

Reaction	System	Sitagliptin 50 mg	Sitagliptin 100 mg	Sitagliptin 200 mg	Placebo
Anaemia	Blood and lymphatic system disorders	—	—	—	—
Abdominal pain	Gastrointestinal disorders	—	—	—	—
Abdominal pain upper	Gastrointestinal disorders	—	—	—	—
Diarrhoea	Gastrointestinal disorders	—	—	—	—
Vomiting	Gastrointestinal disorders	—	—	—	—
Infusion site pain	General disorders	—	—	—	—
Infusion site swelling	General disorders	—	—	—	—
Pyrexia	General disorders	—	—	—	—
Hypoglycaemia	Metabolism and nutrition disorders	—	—	—	—
Headache	Nervous system disorders	—	—	—	—
Dysmenorrhoea	Reproductive system and breast disorders	—	—	—	—
Nasal congestion	Respiratory, thoracic and mediastinal disorders	—	—	—	—
Oropharyngeal pain	Respiratory, thoracic and mediastinal disorders	—	—	—	—
Phlebitis	Vascular disorders	—	—	—	—

Data from ClinicalTrials.gov NCT00730275 adverse events section.

Sponsor's own description

This study will assess the safety, tolerability and pharmacokinetics of sitagliptin in 10 to 17 year old diabetic patients.

Publications & conference data

2 peer-reviewed publications reference this trial (live from Europe PMC):

1. Diabetic kidney disease in children and adolescents: an update.
   Lopez LN, Wang W, Loomba L, Afkarian M, et al · · 2022 · cited 14× · PMID 34913986 · DOI 10.1007/s00467-021-05347-7
2. A randomized clinical trial to evaluate the single-dose pharmacokinetics, pharmacodynamics, and safety of sitagliptin in pediatric patients with type 2 diabetes.
   Fraser IP, Neufeld ND, Fox LA, Kipnes MS, et al · · 2019 · cited 10× · PMID 30346099 · DOI 10.1111/pedi.12790