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CompletedNCT01112670Updated Jan 24, 2013Results posted

The Role of P-glycoprotein in Sitagliptin Clinical Pharmacology

A Phase 4 interventional study of Sitagliptin and atorvastatin in Healthy, sponsored by University of Colorado, Denver. Completed at 1 site in United States. Open to participants aged 21 Years to 60 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2013-01-24.

Sponsored by University of Colorado, Denver · Phase 4 and Interventional

Phase
Phase 4
Study type
Interventional
Enrollment
33
Allocation
Randomized
Ages
21 Years to 60 Years
Sex
All
01

Study summary

The purpose of this study is to determine the pharmacogenetics, pharmacokinetics, and drug-drug interactions of sitagliptin therapy.

02

Conditions studied

  • Healthy

Keywords

  • Healthy volunteers
03

In context

Lead sponsor

University of Colorado, Denver is the lead sponsor of 1,499 studies on the registry; 315 are open to participants now.

Of its 139 completed or terminated interventional studies of FDA-regulated products, 89 (64%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
21 Years to 60 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

Inclusion criteria

  • Healthy men and women between 21 to 60 years of age will be recruited to participate in this study.
  • Subjects will be eligible if metabolic, renal, hepatic, and hematological laboratory tests are within normal limits.

Exclusion criteria

Exclusion Criteria:

  • Subjects will be excluded from the study if they have a current or past history of cardiovascular, hepatic, endocrine (e.g., diabetes), renal, pancreatic, gastrointestinal, pulmonary, immunologic, hematologic, or neurologic disease.
05

Study design

Phase
Phase 4
Allocation
Randomized
Intervention model
Crossover assignment
Masking
None (open label)
Enrollment
33 participants (actual)

Study arms

  • Experimental
    ABCB1 Group 1

    ABCB1 CGC/CGC genetic make-up; sitagliptin 100 mg x 1 dose; atorvastatin 40 mg x 5 doses

    Drug: Sitagliptin · Drug: atorvastatin

  • Experimental
    ABCB1 Group 2

    ABCB1 CGC/TTT genetic make-up; sitagliptin 100 mg x 1 dose; atorvastatin 40 mg x 5 doses

    Drug: Sitagliptin · Drug: atorvastatin

  • Experimental
    ABCB1 Group 3

    ABCB1 TTT/TTT genetic make-up; sitagliptin 100 mg x 1 dose; atorvastatin 40 mg x 5 doses

    Drug: Sitagliptin · Drug: atorvastatin

Interventions

  • DrugSitagliptin

    sitagliptin 100 mg x 1 dose

    Also known as: Januvia

  • Drugatorvastatin

    atorvastatin 40 mg x 5 doses

    Also known as: Lipitor

06

What researchers measure

Primary outcomes

  1. Sitagliptin Monotherapy: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

  2. Sitagliptin Monotherapy: Sitagliptin Maximum Plasma Concentration (Cmax)

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

  3. Sitagliptin Monotherapy: Sitagliptin Renal Clearance (CLr)

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Secondary outcomes

  1. Sitagliptin + Atorvastatin: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

  2. Sitagliptin + Atorvastatin: Sitagliptin Maximum Plasma Concentration (Cmax)

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

  3. Sitagliptin + Atorvastatin: Sitagliptin Renal Clearance (CLr)

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

Other outcomes

  1. Relative Change in Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity

    AUC of sitagliptin when administered with atorvastatin divided by AUC of sitagliptin when administered alone

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

  2. Relative Change in Sitagliptin Maximum Plasma Concentration (Cmax)

    Cmax of sitagliptin when administered with atorvastatin divided by Cmax of sitagliptin when administered alone

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

  3. Relative Change in Sitagliptin Renal Clearance (CLr)

    CLr of sitagliptin when administered with atorvastatin divided by CLr of sitagliptin when administered alone

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours

  4. Atorvastatin Area Under the Plasma Concentration Time Curve (AUC) Over the Dosing Interval (0-24 Hours)

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

  5. Atorvastatin Maximum Plasma Concentration (Cmax)

    Time frame: 0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose

07

Results

Posted Jan 8, 2013
Limitations and caveats
Findings are only applicable to individuals with ABCB1 CGC/CGC, CGC/TTT, or TTT/TTT diplotypes.

Participant flow

Healthy volunteers were recruited from the Denver metro area between November 2009 and December 2010.

Sitagliptin to Sitagliptin+Atorvastatin
Participant flow — Sitagliptin to Sitagliptin+Atorvastatin
MilestoneABCB1 Group 1ABCB1 Group 1*ABCB1 Group 2ABCB1 Group 2*ABCB1 Group 3ABCB1 Group 3*
Started807060
Completed706050
Not completed101010
Sitagliptin+Atorvastatin to Sitagliptin
Participant flow — Sitagliptin+Atorvastatin to Sitagliptin
MilestoneABCB1 Group 1ABCB1 Group 1*ABCB1 Group 2ABCB1 Group 2*ABCB1 Group 3ABCB1 Group 3*
Started030405
Completed030405
Not completed000000

Outcome measures

PrimarySitagliptin Monotherapy: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ng*hr/ml
Sitagliptin Monotherapy: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
ng*hr/mlABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Sitagliptin Monotherapy: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity3638 ± 14393502 ± 11333129 ± 795
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.83
PrimarySitagliptin Monotherapy: Sitagliptin Maximum Plasma Concentration (Cmax)
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ng/ml
Sitagliptin Monotherapy: Sitagliptin Maximum Plasma Concentration (Cmax)
ng/mlABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Sitagliptin Monotherapy: Sitagliptin Maximum Plasma Concentration (Cmax)454 ± 180438 ± 152394 ± 160
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.67
SecondarySitagliptin + Atorvastatin: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ng*h/ml
Sitagliptin + Atorvastatin: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
ng*h/mlABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Sitagliptin + Atorvastatin: Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity3501 ± 16173430 ± 12793117 ± 1216
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.90
SecondarySitagliptin + Atorvastatin: Sitagliptin Maximum Plasma Concentration (Cmax)
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ng/ml
Sitagliptin + Atorvastatin: Sitagliptin Maximum Plasma Concentration (Cmax)
ng/mlABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Sitagliptin + Atorvastatin: Sitagliptin Maximum Plasma Concentration (Cmax)428 ± 201420 ± 137370 ± 217
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.56
Other pre-specifiedRelative Change in Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity

AUC of sitagliptin when administered with atorvastatin divided by AUC of sitagliptin when administered alone

Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ratio
Relative Change in Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity
ratioABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Relative Change in Sitagliptin Area Under the Plasma Concentration-time Curve (AUC) From 0 to Infinity0.96 (0.81 to 1.11)0.98 (0.88 to 1.07)0.97 (0.87 to 1.08)
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.97
Other pre-specifiedRelative Change in Sitagliptin Maximum Plasma Concentration (Cmax)

Cmax of sitagliptin when administered with atorvastatin divided by Cmax of sitagliptin when administered alone

Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ratio
Relative Change in Sitagliptin Maximum Plasma Concentration (Cmax)
ratioABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Relative Change in Sitagliptin Maximum Plasma Concentration (Cmax)0.96 (0.75 to 1.17)1.0 (0.79 to 1.21)0.93 (0.76 to 1.11)
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.86
PrimarySitagliptin Monotherapy: Sitagliptin Renal Clearance (CLr)
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ml/min
Sitagliptin Monotherapy: Sitagliptin Renal Clearance (CLr)
ml/minABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Sitagliptin Monotherapy: Sitagliptin Renal Clearance (CLr)254 ± 176232 ± 62359 ± 182
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.21
SecondarySitagliptin + Atorvastatin: Sitagliptin Renal Clearance (CLr)
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ml/min
Sitagliptin + Atorvastatin: Sitagliptin Renal Clearance (CLr)
ml/minABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Sitagliptin + Atorvastatin: Sitagliptin Renal Clearance (CLr)280 ± 124226 ± 66339 ± 188
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.22
Other pre-specifiedRelative Change in Sitagliptin Renal Clearance (CLr)

CLr of sitagliptin when administered with atorvastatin divided by CLr of sitagliptin when administered alone

Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours
Reported as:
Mean · ratio
Relative Change in Sitagliptin Renal Clearance (CLr)
ratioABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Relative Change in Sitagliptin Renal Clearance (CLr)1.22 (0.97 to 1.48)0.99 (0.82 to 1.16)1.0 (0.81 to 1.18)
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.14
Other pre-specifiedAtorvastatin Area Under the Plasma Concentration Time Curve (AUC) Over the Dosing Interval (0-24 Hours)
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ng*h/ml
Atorvastatin Area Under the Plasma Concentration Time Curve (AUC) Over the Dosing Interval (0-24 Hours)
ng*h/mlABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Atorvastatin Area Under the Plasma Concentration Time Curve (AUC) Over the Dosing Interval (0-24 Hours)44.4 ± 28.035.4 ± 35.649.0 ± 37.1
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.29
Other pre-specifiedAtorvastatin Maximum Plasma Concentration (Cmax)
Time frame:
0, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24 hours post-dose
Reported as:
Mean · ng/ml
Atorvastatin Maximum Plasma Concentration (Cmax)
ng/mlABCB1 Group 1ABCB1 Group 2ABCB1 Group 3
Atorvastatin Maximum Plasma Concentration (Cmax)8.6 ± 6.27.5 ± 7.610.6 ± 7.4
Statistical analysis
  • ABCB1 Group 1 vs ABCB1 Group 2 vs ABCB1 Group 3 · ANOVA · p = 0.43

Adverse events

Collected over Pharmacokinetic study periods. Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Overall Study Population—0/33 (0%)24/33 (72.7%)
Most frequent other events
Most frequent other events
EventOverall Study Population
HeadacheGeneral disorders11/33
HypoalbuminemiaGeneral disorders8/33
LightheadednessGeneral disorders3/33
Increased liver function testsHepatobiliary disorders3/33
Pain at IV siteGeneral disorders3/33
Muscle painMusculoskeletal and connective tissue disorders2/33
NauseaGastrointestinal disorders2/33
DiarrheaGastrointestinal disorders2/33
Nasal congestionGeneral disorders2/33
Dry mouthGeneral disorders2/33

Baseline characteristics

Age, Categorical
Age, Categorical(Participants)Overall Study Population
<=18 years0
Between 18 and 65 years33
>=65 years0
Age Continuous
Age Continuous(years)Overall Study Population
Mean33 ± 10
Sex: Female, Male
Sex: Female, Male(Participants)Overall Study Population
Female16
Male17
08

Study locations

1 site
  • University of Colorado Denver
    Aurora, Colorado 80045, United States
09

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jan 24, 2013, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
10

Registry details

Key details

Study ID
NCT01112670
Lead sponsor
University of Colorado, Denver
Collaborators
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Responsible party
Sponsor
First posted
Apr 28, 2010
Start date
Nov 2009
Primary completion
Jul 2011
Completion
Jul 2011
Results posted
Jan 8, 2013
Last update
Jan 24, 2013

Study contacts

Christina L Aquilante, PharmD
principal investigator · University of Colorado, Denver

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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