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CompletedNCT01396187Updated Jan 12, 2015Results posted

Safety and Tolerability of Ascending Intravenous Doses of PF-05231023 In Adult Subjects With Type 2 Diabetes

A Phase 1 interventional study of PF-05231023 and PF-05231023 in Diabetes Mellitus, Type 2, sponsored by Pfizer. Completed at 5 sites in United States. Open to participants aged 30 Years to 70 Years. Per ClinicalTrials.gov, last updated 2015-01-12.

Sponsored by Pfizer · Phase 1, Interventional, and Treatment

Phase
Phase 1
Study type
Interventional
Enrollment
50
Allocation
Randomized
Ages
30 Years to 70 Years
Sex
All
01

Study summary

This is a trial in subjects with Type 2 diabetes mellitus to study the safety, tolerability and pharmacokinetics of multiple ascending doses of PF-05231023.

02

Conditions studied

  • Diabetes Mellitus, Type 2

Keywords

  • Type 2 diabetes
  • safety
  • multiple dose
  • intravenous
03

In context

Diabetes Mellitus, Type 2

9,590 studies on the registry are indexed under Diabetes Mellitus, Type 2; 1,332 are open to participants now.

This study's enrollment of 50 is below the median of 81 across 7,713 interventional studies indexed under Diabetes Mellitus, Type 2.

Browse Diabetes Mellitus, Type 2 studies →

Lead sponsor

Pfizer is the lead sponsor of 3,323 studies on the registry; 145 are open to participants now.

Of its 597 completed or terminated interventional studies of FDA-regulated products, 391 (65%) have results posted.

Browse Pfizer studies →

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

04

Who can participate

Ages eligible
30 Years to 70 Years
Sexes eligible
All
Accepts healthy volunteers
No

Go through the criteria one by one — yes, no or not sure — and take the list to your doctor or the study team. Kept in this browser only.

Inclusion criteria

  • Male subjects and female subjects of non-childbearing potential between the ages of 30 and 70 years, inclusive, with a historical diagnosis of type 2 diabetes mellitus, diagnosed according to the American Diabetes Association guidelines. Subjects who have other conditions but are well controlled by either diet or medications may be included as well (for example, a subject with high cholesterol level on appropriate treatment is eligible).
  • Body Mass Index (BMI) of 25 to 35.5 kg/m2, and a total body weight >50 kg (110 lbs).

Exclusion criteria

Exclusion Criteria:

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
  • Diagnosis of Type 1 diabetes mellitus.
  • Evidence of diabetic complications with significant end organ damage
05

Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Randomized
Intervention model
Parallel assignment
Masking
Triple (Participant, Care provider, Investigator)
Enrollment
50 participants (actual)

Study arms

  • Experimental
    Treatment

    Drug: PF-05231023

  • Placebo comparator
    Placebo

    Other: Placebo

Interventions

  • DrugPF-05231023

    5 mg IV twice a week for 4 weeks

  • DrugPF-05231023

    25 mg IV twice a week for 4 weeks

  • DrugPF-05231023

    100 mg IV twice a week for 4 weeks

  • DrugPF-05231023

    200 mg IV twice a week for 4 weeks

  • OtherPlacebo

    0.9% w/v sodium chloride injection, United States Pharmacopeia (USP), twice a week IV for 4 weeks

06

What researchers measure

Primary outcomes

  1. Number of Participants With Abnormal Physical Examination Findings

    Physical examination included assessment of height, weight, blood pressure, pulse rate and body temperature. Criteria for abnormal physical findings was based on investigator's discretion and were reported as adverse event (AE), as planned.

    Time frame: Baseline up to Day 42

  2. Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)

    An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to Day 77 which were absent before treatment or that worsened relative to pretreatment state.

    Time frame: Baseline up to Day 77

  3. Number of Participants With Abnormal Laboratory Values

    Criteria for laboratory tests abnormalities included: hemoglobin, hematocrit and red blood cells (RBCs)(less than \[\<\] 0.8\*lower limit of normal\[LLN\]); leucocytes (\<0.6/greater than \[\>\]1.5\*upper limit of normal \[ULN\]); platelets (\<0.5\*LLN\>\</0\>1.75\*ULN); neutrophils, lymphocytes (\<0.8\*LLN\>\</0\>1.2\*ULN); eosinophils, basophils, monocytes (\>1.2\*ULN); total bilirubin, direct bilirubin, indirect bilirubin (\>1.5\*ULN); aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (\>3\*ULN), total protein, albumin (\<0.8\*LLN\>\</0\>1.2\*ULN); creatinine, urea (\>1.3\*ULN); glucose (\<0.6\*LLN\>\</0\>1.5\*ULN); uric acid (\>1.2\*ULN); sodium, potassium, chloride, calcium, bicarbonate (\<0.9\*LLN\>\</0\>1.1\*ULN); urine RBCs, urine white blood cells (WBCs) (\> or equal\[=\]20 high-powered field), urine bacteria \>20 high-powered field. Total number of participants with any laboratory abnormalities were reported.

    Time frame: Baseline up to Day 42

  4. Number of Participants With Vital Signs Abnormalities

    Criteria for vital signs abnormalities: supine systolic blood pressure (SBP) \<90 millimeter of mercury (mm Hg), supine diastolic BP (DBP) \<50 mm Hg, supine pulse rate \<40 beats per minute (bpm), \> 120 bpm. Maximum increase or decrease from baseline in supine SBP \>=30 mm Hg and maximum increase or decrease from baseline in supine DBP \>=20 mm Hg.

    Time frame: Baseline up to Day 77

  5. Number of Participants With Electrocardiogram (ECG) Abnormalities

    Criteria for potential clinical concern in ECG parameters: maximum PR interval of greater than or equal to (\>=) 300 milliseconds (msec), maximum QRS interval \>=140 msec, maximum QTCF interval (Fridericia's Correction) of 450 to \<480 msec, 480 to \<500 msec and \>=500 msec, maximum increase of \>=25 percent (%) for baseline value of \>200 msec and \>=50% for baseline value of less than or equal to (\<=) 200 msec for PR interval, maximum increase from baseline of \>=50% for QRS interval, maximum increase from baseline of \>=30 msec to \<60 msec and maximum increase from baseline of \>60 msec in QTCF interval (Fridericia's Correction).

    Time frame: Baseline up to Day 77

  6. Number of Participants With Blood Glucose Abnormalities

    Criteria for blood glucose abnormality: Blood glucose levels \<0.6\* LLN or \>1.5\* ULN.

    Time frame: Baseline up to Day 32

Secondary outcomes

  1. Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-05231023 After Single Dose

    Participants who received PF-05231023 with C-terminal and N-terminal AUCtau were reported.

    Time frame: 0 hour (pre-dose) on Day 1, 4; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1; Day 2, 3

  2. Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05231023 After Single Dose

    Participants who received PF-05231023 with C-terminal and N-terminal Tmax were reported.

    Time frame: 0 hour (pre-dose) on Day 1, 4; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1; Day 2, 3

  3. Maximum Observed Plasma Concentration (Cmax) of PF-05231023 After Single Dose

    Participants who received PF 05231023 with C-terminal and N-terminal Cmax were reported.

    Time frame: 0 hour (pre-dose) on Day 1, 4; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1; Day 2, 3

  4. Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-05231023 at Steady State

    Participants who received PF-05231023 with C-terminal and N-terminal AUCtau at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  5. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-05231023 at Steady State

    Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) at steady state. Participants who received PF-05231023 with C-terminal and N-terminal AUClast at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  6. Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05231023 at Steady State

    Participants who received PF-05231023 with C-terminal and N-terminal Tmax at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  7. Maximum Observed Plasma Concentration (Cmax) of PF-05231023 at Steady State

    Participants who received PF 05231023 with C-terminal and N-terminal Cmax at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  8. Accumulation Ratio for Area Under the Curve From Time Zero to End of Dosing Interval of PF-05231023 (Rac)

    Rac was obtained from AUCtau at steady state (Day 25) divided by AUCtau after single dose (Day 1). AUCtau was the area under the concentration-time profile from time zero to end of dosing interval, where tau = 72 hours for Day 1 and tau = 96 hours for Day 25. Participants who received PF-05231023 with C-terminal and N-terminal Rac at steady state were reported.

    Time frame: 0 hour (pre-dose) on Day 1, 4, 25; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1, 25; Day 2, 3, 26, 29

  9. Accumulation Ratio for Maximum Observed Plasma Concentration (Rac,Cmax) of PF- 05231023

    Accumulation ratio based on maximum plasma concentration (Cmax) was calculated as: Rac,Cmax = Cmax at steady state (Day 25) divided by Cmax at first dose (Day 1). Participants who received PF-05231023 with C-terminal and N-terminal Rac,Cmax at steady state were reported.

    Time frame: 0 hour (pre-dose) on Day 1, 4, 25; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1, 25; Day 2, 3, 26, 29

  10. Plasma Terminal Half-Life (t1/2) of PF-05231023 at Steady State

    Plasma terminal half-life is the time measured for the plasma concentration to decrease by one half at the terminal phase. Participants who received PF-05231023 with C-terminal and N-terminal t1/2 at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  11. Apparent Clearance (CL) of PF-05231023 at Steady State

    Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. Participants who received PF-05231023 with C-terminal and N-terminal CL at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  12. Volume of Distribution of PF-05231023 at Steady State (Vss)

    Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Vss is the apparent volume of distribution at steady-state. PF-05231023 with C-terminal and N-terminal Vss at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  13. Minimum Observed Plasma Trough Concentration (Cmin) of PF-05231023 at Steady State

    Participants who received PF 05231023 with C-terminal and N-terminal Cmax at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

  14. Average Plasma Concentration (Cav) of PF-05231023 at Steady State

    Participants who received PF-05231023 with C-terminal and N-terminal Cmax at steady state were reported.

    Time frame: 0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29

07

Results

Posted Jan 12, 2015

Participant flow

Participants with a historical diagnosis of type 2 diabetes mellitus (T2DM), diagnosed according to the American Diabetes Association (ADA) guidelines, those with well controlled diabetes and were on stable metformin therapy were recruited in the study.

Participant flow — Overall Study
MilestonePlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
Started812101010
Completed799109
Not completed13101
Withdrew: Adverse event01000
Withdrew: Withdrawal by subject01100
Withdrew: Other11001

Outcome measures

PrimaryNumber of Participants With Abnormal Physical Examination Findings

Physical examination included assessment of height, weight, blood pressure, pulse rate and body temperature. Criteria for abnormal physical findings was based on investigator's discretion and were reported as adverse event (AE), as planned.

Time frame:
Baseline up to Day 42

No measurements were reported for this outcome.

PrimaryNumber of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to Day 77 which were absent before treatment or that worsened relative to pretreatment state.

Time frame:
Baseline up to Day 77
Reported as:
Number · participants
Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)
participantsPlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
AEs563810
SAEs00001
PrimaryNumber of Participants With Abnormal Laboratory Values

Criteria for laboratory tests abnormalities included: hemoglobin, hematocrit and red blood cells (RBCs)(less than \[\<\] 0.8\*lower limit of normal\[LLN\]); leucocytes (\<0.6/greater than \[\>\]1.5\*upper limit of normal \[ULN\]); platelets (\<0.5\*LLN\>\</0\>1.75\*ULN); neutrophils, lymphocytes (\<0.8\*LLN\>\</0\>1.2\*ULN); eosinophils, basophils, monocytes (\>1.2\*ULN); total bilirubin, direct bilirubin, indirect bilirubin (\>1.5\*ULN); aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (\>3\*ULN), total protein, albumin (\<0.8\*LLN\>\</0\>1.2\*ULN); creatinine, urea (\>1.3\*ULN); glucose (\<0.6\*LLN\>\</0\>1.5\*ULN); uric acid (\>1.2\*ULN); sodium, potassium, chloride, calcium, bicarbonate (\<0.9\*LLN\>\</0\>1.1\*ULN); urine RBCs, urine white blood cells (WBCs) (\> or equal\[=\]20 high-powered field), urine bacteria \>20 high-powered field. Total number of participants with any laboratory abnormalities were reported.

Time frame:
Baseline up to Day 42
Reported as:
Number · participants
Number of Participants With Abnormal Laboratory Values
participantsPlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
Number of Participants With Abnormal Laboratory Values8109910
PrimaryNumber of Participants With Vital Signs Abnormalities

Criteria for vital signs abnormalities: supine systolic blood pressure (SBP) \<90 millimeter of mercury (mm Hg), supine diastolic BP (DBP) \<50 mm Hg, supine pulse rate \<40 beats per minute (bpm), \> 120 bpm. Maximum increase or decrease from baseline in supine SBP \>=30 mm Hg and maximum increase or decrease from baseline in supine DBP \>=20 mm Hg.

Time frame:
Baseline up to Day 77
Reported as:
Number · participants
Number of Participants With Vital Signs Abnormalities
participantsPlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
SBP < 90 mm Hg00201
DBP< 50 mm Hg00000
Pulse rate < 40 bpm00000
Pulse rate > 120 bpm00000
SBP: Maximum increase >= 30 mm Hg31320
DBP: Maximum increase >=20 mm Hg11111
SBP: Maximum decrease>=30 mm Hg20013
DBP: Maximum Decrease >= 20 mm Hg10011
PrimaryNumber of Participants With Electrocardiogram (ECG) Abnormalities

Criteria for potential clinical concern in ECG parameters: maximum PR interval of greater than or equal to (\>=) 300 milliseconds (msec), maximum QRS interval \>=140 msec, maximum QTCF interval (Fridericia's Correction) of 450 to \<480 msec, 480 to \<500 msec and \>=500 msec, maximum increase of \>=25 percent (%) for baseline value of \>200 msec and \>=50% for baseline value of less than or equal to (\<=) 200 msec for PR interval, maximum increase from baseline of \>=50% for QRS interval, maximum increase from baseline of \>=30 msec to \<60 msec and maximum increase from baseline of \>60 msec in QTCF interval (Fridericia's Correction).

Time frame:
Baseline up to Day 77
Reported as:
Number · participants
Number of Participants With Electrocardiogram (ECG) Abnormalities
participantsPlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
Maximum PR interval >=300 msec00000
Maximum QRS Complex >=140 msec00000
Maximum QTCF interval 450 to <480 msec00002
Maximum QTCF interval 480 to <500 msec00000
Maximum QTCF interval >=500 msec00000
PR interval increase from baseline >=25/50%00000
QRS complex increase from baseline >=50%00000
QTCF interval increase from baseline 30 to <60msec11101
QTCF interval increase from baseline >=60 msec10000
PrimaryNumber of Participants With Blood Glucose Abnormalities

Criteria for blood glucose abnormality: Blood glucose levels \<0.6\* LLN or \>1.5\* ULN.

Time frame:
Baseline up to Day 32
Reported as:
Number · participants
Number of Participants With Blood Glucose Abnormalities
participantsPlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
<0.6*LLN00000
>1.5*ULN66659
SecondaryArea Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-05231023 After Single Dose

Participants who received PF-05231023 with C-terminal and N-terminal AUCtau were reported.

Time frame:
0 hour (pre-dose) on Day 1, 4; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1; Day 2, 3
Reported as:
Geometric mean · nanogram*hour per milliliter (ng*hr/mL)
Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-05231023 After Single Dose
nanogram*hour per milliliter (ng*hr/mL)PF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal12680 ± 2358780 ± 23229500 ± 22365300 ± 22
N- terminal33240 ± 22186800 ± 16844200 ± 121051000 ± 19
SecondaryTime to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05231023 After Single Dose

Participants who received PF-05231023 with C-terminal and N-terminal Tmax were reported.

Time frame:
0 hour (pre-dose) on Day 1, 4; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1; Day 2, 3
Reported as:
Median · hour
Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05231023 After Single Dose
hourPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C- terminal1.02 (0.500 to 1.50)1.26 (1.00 to 2.00)1.25 (0.883 to 2.00)1.50 (1.00 to 2.15)
N-terminal1.50 (0.500 to 2.00)1.50 (1.02 to 5.00)1.50 (1.00 to 2.97)1.50 (1.07 to 5.00)
SecondaryMaximum Observed Plasma Concentration (Cmax) of PF-05231023 After Single Dose

Participants who received PF 05231023 with C-terminal and N-terminal Cmax were reported.

Time frame:
0 hour (pre-dose) on Day 1, 4; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1; Day 2, 3
Reported as:
Geometric mean · nanogram per milliliter (ng/mL)
Maximum Observed Plasma Concentration (Cmax) of PF-05231023 After Single Dose
nanogram per milliliter (ng/mL)PF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C -terminal1270 ± 115991 ± 1723500 ± 2134390 ± 15
N -terminal1182 ± 187123 ± 1828480 ± 1835790 ± 17
SecondaryArea Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-05231023 at Steady State

Participants who received PF-05231023 with C-terminal and N-terminal AUCtau at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Geometric mean · ng*hr/mL
Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-05231023 at Steady State
ng*hr/mLPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal14810 ± 3373940 ± 27324300 ± 15453400 ± 21
N-terminal65420 ± 16317800 ± 111533000 ± 241990000 ± 22
SecondaryArea Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-05231023 at Steady State

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) at steady state. Participants who received PF-05231023 with C-terminal and N-terminal AUClast at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Geometric mean · ng*hr/mL
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-05231023 at Steady State
ng*hr/mLPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal11280 ± 2652710 ± 23294100 ± 26456700 ± 21
N-terminal121900 ± 27590400 ± 112859000 ± 203196000 ± 25
SecondaryTime to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05231023 at Steady State

Participants who received PF-05231023 with C-terminal and N-terminal Tmax at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Median · hour
Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05231023 at Steady State
hourPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal1.42 (1.02 to 1.48)1.48 (1.00 to 2.00)1.40 (1.00 to 3.00)1.01 (1.00 to 1.50)
N-terminal1.48 (1.42 to 1.48)1.45 (0.500 to 13.0)1.99 (1.37 to 24.0)1.45 (1.00 to 2.00)
SecondaryMaximum Observed Plasma Concentration (Cmax) of PF-05231023 at Steady State

Participants who received PF 05231023 with C-terminal and N-terminal Cmax at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Geometric mean · ng/mL
Maximum Observed Plasma Concentration (Cmax) of PF-05231023 at Steady State
ng/mLPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal1239 ± 235629 ± 2127240 ± 1637160 ± 13
N-terminal1839 ± 219016 ± 1737770 ± 1861160 ± 16
SecondaryAccumulation Ratio for Area Under the Curve From Time Zero to End of Dosing Interval of PF-05231023 (Rac)

Rac was obtained from AUCtau at steady state (Day 25) divided by AUCtau after single dose (Day 1). AUCtau was the area under the concentration-time profile from time zero to end of dosing interval, where tau = 72 hours for Day 1 and tau = 96 hours for Day 25. Participants who received PF-05231023 with C-terminal and N-terminal Rac at steady state were reported.

Time frame:
0 hour (pre-dose) on Day 1, 4, 25; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1, 25; Day 2, 3, 26, 29
Reported as:
Geometric mean · ratio
Accumulation Ratio for Area Under the Curve From Time Zero to End of Dosing Interval of PF-05231023 (Rac)
ratioPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal1.258 ± 201.258 ± 241.413 ± 101.173 ± 8
N-terminal2.016 ± 181.702 ± 151.818 ± 241.810 ± 14
SecondaryAccumulation Ratio for Maximum Observed Plasma Concentration (Rac,Cmax) of PF- 05231023

Accumulation ratio based on maximum plasma concentration (Cmax) was calculated as: Rac,Cmax = Cmax at steady state (Day 25) divided by Cmax at first dose (Day 1). Participants who received PF-05231023 with C-terminal and N-terminal Rac,Cmax at steady state were reported.

Time frame:
0 hour (pre-dose) on Day 1, 4, 25; 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 1, 25; Day 2, 3, 26, 29
Reported as:
Geometric mean · ratio
Accumulation Ratio for Maximum Observed Plasma Concentration (Rac,Cmax) of PF- 05231023
ratioPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal0.9992 ± 190.9392 ± 201.159 ± 131.033 ± 12
N-terminal1.626 ± 171.266 ± 231.326 ± 191.642 ± 8
SecondaryPlasma Terminal Half-Life (t1/2) of PF-05231023 at Steady State

Plasma terminal half-life is the time measured for the plasma concentration to decrease by one half at the terminal phase. Participants who received PF-05231023 with C-terminal and N-terminal t1/2 at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Mean · hour
Plasma Terminal Half-Life (t1/2) of PF-05231023 at Steady State
hourPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal (n=8, 7, 10, 8)6.484 ± 0.796857.879 ± 0.781389.563 ± 2.541910.25 ± 1.5121
N-terminal (n=9, 10, 9, 6)83.93 ± 10.92284.38 ± 8.774297.47 ± 14.53474.62 ± 13.781
SecondaryApparent Clearance (CL) of PF-05231023 at Steady State

Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. Participants who received PF-05231023 with C-terminal and N-terminal CL at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Geometric mean · liter per hour
Apparent Clearance (CL) of PF-05231023 at Steady State
liter per hourPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal0.3378 ± 260.3383 ± 230.3083 ± 150.3086 ± 23
N-terminal0.07642 ± 140.07871 ± 120.06521 ± 210.07043 ± 26
SecondaryVolume of Distribution of PF-05231023 at Steady State (Vss)

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Vss is the apparent volume of distribution at steady-state. PF-05231023 with C-terminal and N-terminal Vss at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Geometric mean · liter
Volume of Distribution of PF-05231023 at Steady State (Vss)
literPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal (n=8, 7, 10, 8)1.467 ± 191.873 ± 162.940 ± 484.110 ± 12
N-terminal (n=9, 10, 9, 6)7.320 ± 207.594 ± 156.570 ± 334.863 ± 18
SecondaryMinimum Observed Plasma Trough Concentration (Cmin) of PF-05231023 at Steady State

Participants who received PF 05231023 with C-terminal and N-terminal Cmax at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Geometric mean · ng/mL
Minimum Observed Plasma Trough Concentration (Cmin) of PF-05231023 at Steady State
ng/mLPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal0.0003894 ± 6.86670.1538 ± 11.86480.51 ± 102218.8 ± 76
N-terminal550.5 ± 331861 ± 309987 ± 2112440 ± 29
SecondaryAverage Plasma Concentration (Cav) of PF-05231023 at Steady State

Participants who received PF-05231023 with C-terminal and N-terminal Cmax at steady state were reported.

Time frame:
0 hour (pre-dose) 0.5, 1 (end of infusion), 1.5, 2, 3, 5, 9, 13 hours post-start of infusion on Day 25; Day 26, 29
Reported as:
Geometric mean · ng/mL
Average Plasma Concentration (Cav) of PF-05231023 at Steady State
ng/mLPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
C-terminal205.5 ± 331027 ± 274504 ± 156300 ± 21
N-terminal908.6 ± 164411 ± 1121290 ± 2427620 ± 22

Adverse events

Non-serious events are listed at a 2% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Placebo—0/8 (0%)5/8 (62.5%)
PF-05231023 5 mg—0/12 (0%)6/12 (50%)
PF-05231023 25 mg—0/10 (0%)3/10 (30%)
PF-05231023 100 mg—0/10 (0%)8/10 (80%)
PF-05231023 140 mg—1/10 (10%)10/10 (100%)
Most frequent serious events
Most frequent serious events
EventPlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
Femoral neck fractureInjury, poisoning and procedural complications0/80/120/100/101/10
Most frequent other events
Showing 10 of 55
Most frequent other events
EventPlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mg
DiarrhoeaGastrointestinal disorders1/80/122/102/108/10
NauseaGastrointestinal disorders2/80/122/105/104/10
HeadacheNervous system disorders4/80/120/101/104/10
Dermatitis contactSkin and subcutaneous tissue disorders1/80/120/104/101/10
Abdominal painGastrointestinal disorders0/80/121/100/103/10
ConstipationGastrointestinal disorders2/80/120/101/100/10
Upper respiratory tract infectionInfections and infestations2/80/121/100/102/10
DermatitisSkin and subcutaneous tissue disorders2/80/120/100/101/10
VomitingGastrointestinal disorders0/80/121/100/102/10
Vessel puncture site haematomaGeneral disorders0/80/120/100/102/10

Baseline characteristics

Safety analysis population included all participants who received at least 1 dose of study medication.

Age, Continuous
Age, Continuous(years)PlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mgTotal
Mean55.8 ± 4.350.2 ± 10.056.9 ± 6.959.0 ± 6.357.6 ± 9.155.7 ± 8.2
Sex: Female, Male
Sex: Female, Male(Participants)PlaceboPF-05231023 5 mgPF-05231023 25 mgPF-05231023 100 mgPF-05231023 140 mgTotal
Female2113411
Male61197639
08

Study locations

5 sites
  • Pfizer Investigational Site
    Chula Vista, California 91911, United States
  • Pfizer Investigational Site
    Miami, Florida 33169, United States
  • Pfizer Investigational Site
    South Miami, Florida 33143, United States
  • Pfizer Investigational Site
    Overland Park, Kansas 66212, United States
  • Pfizer Investigational Site
    San Antonio, Texas 78229, United States
09

References and documents

10

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jan 12, 2015, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
11

Registry details

Key details

Study ID
NCT01396187
Lead sponsor
Pfizer
Responsible party
Sponsor
First posted
Jul 18, 2011
Start date
Jul 2011
Primary completion
May 2012
Completion
May 2012
Results posted
Jan 12, 2015
Last update
Jan 12, 2015

Study contacts

Pfizer CT.gov Call Center
study director · Pfizer

Oversight

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

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