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PF-05175157

Phase 1

Diabetes Mellitus Type 2 | Small molecule | Metabolic |Pfizer, Inc.|Last Updated: Nov 14, 2018

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindCONTROLLED
Total Trials1
Total Enrollment15

FDA Designations

No designations recorded

Clinical trial landscape

PF-05175157 · 7 trials · 6 indications

Phase 1 7
NCT01807377Multiple Dose Safety Tolerability, Pharmacokinetics And Midazolam Interaction In Healthy Overweight And Obese SubjectsDiabetes Mellitus Type 2
COMPLETED15 Analytics
NCT01819922Effect Of Single-Dose PF-05175157 On Metabolic And Cardiopulmonary ParametersHealthy
COMPLETED12 Analytics
NCT01821079A Healthy Volunteer Study To Assess Relative Bioavailability Of Powder-In-Capsule And A Tablet Formulation And The Effect Of Food On The Pharmacokinetics Of The Tablet FormulationHealthy
COMPLETED12 Analytics
NCT01757756Multiple Dose Safety Toelrability, Pharmacokinetics and Midazolam Interaction In Healthy Overweight And Obese SubjectsDiabetes Mellitus
COMPLETED12 Analytics
NCT01537497A Study To Evaluate The Effects Of PF-05175157 In Healthy VolunteersDiabetes Mellitus, Type 2
COMPLETED31 Analytics
NCT01469468A Study To Estimate The Effect Of Repeated Dosing of PF-05175157 On The Pharmacokinetics Of A Single Dose Of Simvastatin In Healthy Adult SubjectsType 2 Diabetes Mellitus
COMPLETED14 Analytics
NCT01433380A Study To Evaluate PF-05175157 In Healthy VolunteersDiabetes Mellitus, Type 2
COMPLETED22 Analytics
PHASE1COMPLETED
Multiple Dose Safety Tolerability, Pharmacokinetics And Midazolam Interaction In Healthy Overweight And Obese Subjects
Diabetes Mellitus Type 2Unlock trial analytics
PHASE1COMPLETED
Effect Of Single-Dose PF-05175157 On Metabolic And Cardiopulmonary Parameters
HealthyUnlock trial analytics
PHASE1COMPLETED
A Healthy Volunteer Study To Assess Relative Bioavailability Of Powder-In-Capsule And A Tablet Formulation And The Effect Of Food On The Pharmacokinetics Of The Tablet Formulation
HealthyUnlock trial analytics
PHASE1COMPLETED
Multiple Dose Safety Toelrability, Pharmacokinetics and Midazolam Interaction In Healthy Overweight And Obese Subjects
Diabetes MellitusUnlock trial analytics
PHASE1COMPLETED
A Study To Evaluate The Effects Of PF-05175157 In Healthy Volunteers
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE1COMPLETED
A Study To Estimate The Effect Of Repeated Dosing of PF-05175157 On The Pharmacokinetics Of A Single Dose Of Simvastatin In Healthy Adult Subjects
Type 2 Diabetes MellitusUnlock trial analytics
PHASE1COMPLETED
A Study To Evaluate PF-05175157 In Healthy Volunteers
Diabetes Mellitus, Type 2Unlock trial analytics

Study Endpoints

Primary Endpoints

Maximum Observed Plasma PF-05175157 Concentration (Cmax)
0 - 10 hrs postdose

Single Dose

Area Under the Curve from Time Zero to end of dosing interval for PF-05175157 (AUCtau)
0 - 10 hrs postdose

Single Dose

Time to Reach Maximum Observed Plasma PF-05175157 Concentration (Tmax)
0 - 10 hrs postdose

Single Dose

Area Under the Curve from Time Zero to end of dosing interval (AUCtau) for PF-05175157
0 - 48 hours postdose

Steady State

Apparent Oral Clearance of PF-05175157 (CL/F)
0 - 48 hours postdose
Accumulation Ratio of PF-05175157 (Rac)
0 - 10 hours postdose
Plasma Decay Half-Life of PF-05175157 (t1/2)
0 - 48 hours postdose
Apparent Volume of Distribution of PF-05175157 (Vz/F)
0 - 48 hours postdose
Urinary Recovery for PF-05175157 (AE24)
0 - 24 hours postdose

Amount of PF-05175157 recovered in urine over 24 hours

Renal Clearance for PF-05175157 (CLr)
0 - 24 hours post dose
Area Under the Curve From Time Zero to Last Quantifiable Concentration for midazolam [AUC (0-t)]
0 - 48 hours postdose
Area Under the Curve From Time Zero to Extrapolated Infinite Time for midazolam [AUC (0 - inf)]
0 - 48 hours postdose
Maximum Observed Plasma Concentration for midazolam (Cmax)
0 - 48 hours postdose
Time to Reach Maximum Observed Plasma midazolam Concentration (Tmax)
0 - 48 hours post dose
Plasma Decay Half-Life of midazolam (t1/2)
0 - 48 hours postdose
Fasting triglycerides
14 days
Total cholesterol
14 days
LDL cholesterol
14 days
HDL cholesterol
14 days
Systolic Function: Global Longitudinal Left Ventricular (LV) Strain: 20 Minutes Pre-dose
20 minutes pre-dose

Global longitudinal left ventricular strain was defined as the percent change in left ventricular longitudinal dimension in comparison to its original dimension. Global longitudinal LV strain was assessed by echocardiography using speckled tracking analysis.

Systolic Function: Global Longitudinal Left Ventricular (LV) Strain: 1 Hour 30 Minutes Post-dose
1 hour 30 minutes post-dose

Global longitudinal left ventricular strain was defined as the percent change in left ventricular longitudinal dimension in comparison to its original dimension. Global longitudinal LV strain was assessed by echocardiography using speckled tracking analysis.

Systolic Function: Global Longitudinal Left Ventricular (LV) Strain: 2 Hours 5 Minutes Post-dose
2 hours 5 minutes post-dose

Global longitudinal left ventricular strain was defined as the percent change in left ventricular longitudinal dimension in comparison to its original dimension. Global longitudinal LV strain was assessed by echocardiography using speckled tracking analysis.

Cardiopulmonary Exercise Test: Oxygen Uptake Efficiency Slope (OUES): 1 Hour 40 Minute Post-dose
1 hour 40 minutes post-dose

OUES was defined as an index of cardiopulmonary functional reserve that was based upon a submaximal exercise effort. OUES relates oxygen uptake to total ventilation during exercise.

Maximum Observed Plasma Concentration (Cmax)
0 to 72 H after dose
Area under the plasma concentration-time profile from time zero extrapolated to infinite time (AUCinf)
0 to 72 H after dose
Area Under the Curve from Time Zero to end of dosing interval (AUCtau)
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12 hrs postdose
Time to Reach Maximum Observed Plasma Concentration (Tmax)
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12 hrs postdose
Plasma Decay Half-Life (t1/2)
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours postdose
Apparent Volume of Distribution (Vz/F)
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours postdose
Apparent Oral Clearance (CL/F)
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36 and 48 hours postdose
Accumulation Ratio (Rac)
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12 hours postdose
Ae,tau
0-12 hr
Ae%
0-12 hr
Clr
0-12 hr
Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-t)]
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36 and 48 hours
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]
0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36 and 48 hours
fasting LDL-cholesterol
14 days
fasting total cholesterol
14 days
fasting HDL cholesterol
14 days
Modulation of carbohydrate and lipid metabolism
24 hours
Area under the plasma concentration curve of simvastatin and simvastatin acid
10 days
Maximum observed plasma concentration of simvastatin and simvastatin acid
10 days
Time at which maximum plasma concentration of simvastatin and simvastatin acid is observed
10 days
If the data permit, area under the plasma concentration curve of simvastatin and simvastatin acid extrapolated to infinite time
10 days
If the data permit, terminal elimination half-life of simvastatin and simvastatin acid
10 days
Changes in carbohydrate and lipid metabolism
24 hours

Secondary Endpoints

Number of Participants With Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
Baseline up to 5-10 days after last dose of study drug (up to 25 days)
Number of Participants With Clinically Significant Laboratory Abnormalities
Baseline up-to 3 hours post-dose
Number of Participants With Categorical Post-dose Cardiovascular Monitoring Data
Baseline up-to 3 hours post-dose
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeBASIC_SCIENCE

Treatment Arms

ArmTypeDescription
PF-05175157, MidazolamEXPERIMENTALDay 0: Midazolam 2 mg administered alone Days 1-14: 200 mg PF-05175157 administered BID Day 11: Midazolam and PF-05175157
Placebo, MidazolamEXPERIMENTALDay 0: Midazolam 2 mg administered alone Days 1-14: Placebo administered BID Day 11: Midazolam and Placebo
PF-05175157EXPERIMENTAL -
PlaceboPLACEBO_COMPARATOR -
PF-05175157 PIC in fed stateEXPERIMENTAL200 mg single dose of PF-05175157 administered as PIC in the fed state (following a standard high fat meal).
PF-05175157 tablet in fed stateEXPERIMENTAL200 mg single dose of PF-05175157 administered as tablet formulation in the fed state (following a standard high fat meal).
PF-05175157 tablet in fed state (repeat)EXPERIMENTAL200 mg single dose of PF-05175157 administered as tablet formulation in the fed state (following a standard high fat meal).
PF-05175157 tablet in fasted stateEXPERIMENTAL200 mg single dose of PF-05175157 administered as tablet formulation in the fasted state (following at least a 10 hour fast).
Arm Label Pf-05175157, placebo, midazolamEXPERIMENTAL -
100 mg PF-05175157EXPERIMENTALThe chance of receiving 100 mg, 250 mg, 600 mg or placebo will be randomized.
250 mg PF-05175157EXPERIMENTALThe chance of receiving 100 mg, 250 mg, 600 mg or placebo will be randomized.
600 mg PF-05175157EXPERIMENTALThe chance of receiving 100 mg, 250 mg, 600 mg or placebo will be randomized.
Single arm, fixed sequence dosingEXPERIMENTAL -

Interventions

NameTypeDescription
PF-05175157DRUG200 mg tablet administered twice per day for 14 days
MidazolamDRUG2mg administered as single doses on Days 0 and 11
PlaceboOTHERPlacebo administered twice per day for 14 days
SimvastatinDRUGDay 1: Single dose of simvastatin 20 mg Day 8: single dose of simvastatin 20 mg (with PF-05175157)
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: Subjects must meet all of the following inclusion criteria to be eligible for enrollment into the study: * Healthy male and/or female subjects between the ages of 18 and 55 years, inclusive (Healthy is defined as no clinically relevant abnormalities identified by a detailed med...

Countries:United States
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Frequently asked questions about PF-05175157

What is PF-05175157 used for?

PF-05175157 is an investigational small molecule being studied for metabolic conditions, including Type 2 Diabetes Mellitus. It has been evaluated in healthy volunteers and in overweight and obese subjects with Type 2 Diabetes Mellitus. The drug is in Phase 1 clinical development and is not approved by the FDA.

Who makes PF-05175157?

PF-05175157 is being developed by Pfizer, Inc., a biopharmaceutical company traded on the New York Stock Exchange under the ticker symbol PFE. Pfizer has sponsored multiple Phase 1 clinical trials of this investigational small molecule for metabolic indications.

What phase is PF-05175157 in?

PF-05175157 is in Phase 1 clinical development. All four completed trials listed on ClinicalTrials.gov are Phase 1 studies. The drug is investigational and has not been approved by the FDA for any use. It is no longer in active trials, as all its Phase 1 studies have been completed.

What clinical trials is PF-05175157 in?

PF-05175157 has been studied in four completed Phase 1 trials: NCT01433380 in healthy volunteers, NCT01807377 in overweight and obese subjects with Type 2 Diabetes Mellitus, NCT01819922 in healthy subjects, and NCT01821079 in healthy volunteers. These trials assessed safety, tolerability, pharmacokinetics, and drug interactions.

Is PF-05175157 the same as any other drug?

PF-05175157 is the only name provided for this investigational drug. It is not known by any alternative names in the available data. The drug is a small molecule being developed by Pfizer for metabolic conditions such as Type 2 Diabetes Mellitus.