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Phase 1 Completed N=109 Randomized Quadruple-blind Treatment

A First in Human Study to Evaluate Safety, Tolerability, and Pharmacology of PF-06826647 in Healthy Subjects and Subjects With Plaque Psoriasis

Source: ClinicalTrials.gov NCT03210961 ↗
Enrolled (actual)
109
Serious AEs
0.0%
Results posted
Mar 2020
Primary outcomePrimary: Number of Participants With Vital Signs Data Meeting Pre-Specified Criteria (Single Ascending Dose [SAD] Period) — 2; 2; 1; 0 Participants

Summary

This first in human study will evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of PF-06826647 in healthy subjects and subjects with plaque psoriasis.

Outcome Measures

OutcomeResultp-value
PRIMARY
Number of Participants With Vital Signs Data Meeting Pre-Specified Criteria (Single Ascending Dose [SAD] Period)
2; 2; 1; 0; 1; 0
PRIMARY
Number of Participants With Vital Signs Data Meeting Pre-Specified Criteria (Multiple Ascending Dose [MAD] Period)
1; 0; 0; 0; 1; 0
PRIMARY
Number of Participants With Vital Signs Data Meeting Pre-Specified Criteria (Psoriasis Cohorts)
0; 1; 1; 0; 3; 5
PRIMARY
Number of Participants With Physical Examination Data Meeting Pre-Specified Criteria (SAD Period)
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With Physical Examination Data Meeting Pre-Specified Criteria (MAD Period)
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With Physical Examination Data Meeting Pre-Specified Criteria (Psoriasis Cohorts)
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With Electrocardiogram (ECG) Data Meeting Pre-Specified Criteria (SAD Period)
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With ECG Data Meeting Pre-Specified Criteria (MAD Period)
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With ECG Data Meeting Pre-Specified Criteria (Psoriasis Cohorts)
0; 0; 0; 0; 0; 0
PRIMARY
Number of Participants With Treatment-Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs), and Who Withdrew Due to Adverse Events (AEs) (SAD Period)
1; 0; 0; 0; 1; 0
PRIMARY
Number of Participants With TEAEs, SAEs, and Who Withdrew Due to AEs (MAD Period)
2; 0; 2; 1; 1; 1
PRIMARY
Number of Participants With TEAEs, SAEs, and Who Withdrew Due to AEs (Psoriasis Cohorts)
7; 12; 5; 5; 5; 3
PRIMARY
Number of Participants With Laboratory Abnormalities (SAD Period)
0; 0; 0; 0; 1; 0
PRIMARY
Number of Participants With Laboratory Abnormalities (MAD Period)
0; 0; 0; 1; 0; 0
PRIMARY
Number of Participants With Laboratory Abnormalities (Psoriasis Cohorts)
2; 3; 1; 1; 1; 0
PRIMARY
Change in 24 Hour Creatinine Clearance From Day -1 on Day 10 (MAD Period)
-21.0; -32.0; -62.4; 0.2; -52.5; -11.4
SECONDARY
Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) (SAD Period)
47.63; 369.3; 848.4; 1582; 3056; 11790
SECONDARY
Secondary: Dose Normalized AUCinf (AUCinf[dn]) (SAD Period)
15.86; 36.93; 28.28; 15.82; 7.636; 7.370
SECONDARY
Area Under the Concentration-Time Profile From Time 0 to 24 Hours (AUC24) (SAD Period)
43.10; 347.8; 543.2; 1158; 2519; 9318
SECONDARY
Area Under the Concentration-Time Profile From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) (SAD Period)
40.25; 354.8; 638.5; 1375; 2767; 9921
SECONDARY
Dose Normalized AUClast (AUClast[dn]) (SAD Period)
13.40; 35.48; 21.28; 13.75; 6.919; 6.200
SECONDARY
Maximum Plasma Concentration (Cmax) (SAD Period)
7.844; 47.09; 77.93; 166.8; 404.8; 1218
SECONDARY
Dose Normalized Cmax (Cmax[dn]) (SAD Period)
2.617; 4.709; 2.597; 1.668; 1.012; 0.7618
SECONDARY
Time for Cmax (Tmax) (SAD Period)
2.00; 2.00; 2.00; 2.00; 2.00; 2.00
SECONDARY
Terminal Elimination Half-Life ((t½) (SAD Period)
3.620; 6.032; 19.69; 38.77; 16.25; 22.21
SECONDARY
Mean Residence Time (MRT) (SAD Period)
5.596; 7.761; 16.97; 21.23; 10.56; 9.417
SECONDARY
Apparent Volume of Distribution (Vz/F) (SAD Period)
312.1; 226.1; 902.9; 2671; 2732; 2877
SECONDARY
Apparent Clearance (CL/F) (SAD Period)
62.98; 27.08; 35.36; 63.21; 130.8; 135.4
SECONDARY
Area Under the Plasma Concentration-Time Profile Over the Dosing Interval τ (AUCτ) (MAD Period Day 1)
662.8; 1803; 1646; 4424; 6038; 17090
SECONDARY
Dose Normalized AUCτ (AUCτ[dn]) (MAD Period Day 1)
22.10; 18.03; 8.229; 11.07; 15.10; 14.23
SECONDARY
Cmax (MAD Period Day 1)
83.53; 267.2; 289.8; 585.9; 695.5; 2023
SECONDARY
Cmax(dn) (MAD Period Day 1)
2.787; 2.672; 1.450; 1.468; 1.741; 1.686
SECONDARY
Tmax (MAD Period Day 1)
3.00; 4.00; 4.00; 3.00; 4.00; 2.00
SECONDARY
AUCτ (MAD Period Day 10)
752.9; 1952; 2010; 5420; 7194; 14890
SECONDARY
AUCτ(dn) (MAD Period Day 10)
25.06; 19.52; 10.04; 13.56; 18.00; 12.41
SECONDARY
Cmax (MAD Period Day 10)
85.34; 263.2; 339.5; 667.3; 887.0; 1855
SECONDARY
Cmax(dn) (MAD Period Day 10)
2.844; 2.632; 1.701; 1.669; 2.220; 1.547
SECONDARY
Tmax (MAD Period Day 10)
4.00; 4.00; 4.00; 4.00; 4.00; 4.00
SECONDARY
Average Concentration at Steady State (Cav) (MAD Period Day 10)
31.36; 81.28; 167.6; 226.0; 299.7; 619.9
SECONDARY
Lowest Concentration Observed During the Dosing Interval τ (Cmin) (MAD Period Day 10)
6.273; 10.40; 55.01; 24.77; 29.50; 62.26
SECONDARY
Terminal Elimination Half-Life ((t½) (MAD Period Day 10)
8.802; 12.72; 26.93; 7.500; 7.433; 34.33
SECONDARY
MRT (MAD Period Day 10)
10.56; 9.872; 17.14; 9.622; 7.996; 9.165
SECONDARY
Peak Trough Ratio (PTR) (MAD Period Day 10)
13.61; 25.31; 6.951; 26.92; 30.09; 29.76
SECONDARY
Observed Accumulation Ratio Based on AUC (Rac) (MAD Period Day 10)
1.085; 1.082; 1.328; 1.225; 1.191; 0.8711
SECONDARY
Observed Accumulation Ratio Based on Cmax (Rac,Cmax) (MAD Period Day 10)
0.9295; 0.9852; 1.282; 1.139; 1.275; 0.9176
SECONDARY
Vz/F (MAD Period Day 10)
433.5; 643.6; 3224; 758.9; 519.2; 2944
SECONDARY
CL/F (MAD Period Day 10)
39.86; 51.27; 99.47; 73.78; 55.62; 80.63
SECONDARY
Cumulative Amount of Drug Recovered Unchanged in Urine From Time 0 to the Dosing Interval τ Hours Post-Dose (Aeτ) (MAD Period Day 10)
0.2204; 1.072; 2.560; 3.134; 2.931; 14.73
SECONDARY
Percentage of Dose Recovered Unchanged in Urine From Time 0 to the Dosing Interval τ Hours Post-Dose (Aeτ%) (MAD Period Day 10)
0.7344; 1.072; 1.280; 0.7827; 0.7333; 1.228
SECONDARY
Renal Clearance (Clr) (MAD Period Day 10)
0.2928; 0.5500; 1.274; 0.5777; 0.4076; 0.9909
SECONDARY
AUCτ (Psoriasis Cohorts)
2401; 7664
SECONDARY
AUCτ(dn) (Psoriasis Cohorts)
24.01; 19.17
SECONDARY
Cmax (Psoriasis Cohorts)
296.6; 869.8
SECONDARY
Cmax(dn) (Psoriasis Cohorts)
2.966; 2.176
SECONDARY
Tmax (Psoriasis Cohorts)
4.00; 4.00
SECONDARY
Cav (Psoriasis Cohorts)
100.2; 319.3
SECONDARY
Cmin (Psoriasis Cohorts)
21.92; 38.12
SECONDARY
Terminal Elimination Half-Life ((t½) (Psoriasis Cohorts)
7.796; 6.809
SECONDARY
MRT (Psoriasis Cohorts)
11.27; 9.444
SECONDARY
PTR (Psoriasis Cohorts)
13.52; 22.81
SECONDARY
Vz/F (Psoriasis Cohorts)
408.1; 461.2
SECONDARY
CL/F (Psoriasis Cohorts)
41.61; 52.21
SECONDARY
Change From Baseline in Psoriasis Area and Severity Index (PASI) Score at Day 28
-11.13; -24.18; -14.62

Eligibility Criteria

Healthy Participants:

Inclusion Criteria

  • Healthy male subjects between ages of 18-55 years
  • Healthy female subjects of non-childbearing potential between the ages of 18-55 years
  • Body Mass Index (BMI) of 17.5 to 30.5kg/m2; and a total body weight >50kg (110lbs).
  • No evidence of active or latent or inadequately treated infection with Mycobacterium tuberculosis (TB)
  • (Optional) Japanese subjects who have four Japanese biologic grandparents born in Japan

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)
  • Pregnant female subjects; breastfeeding female subjects; female subjects of childbearing potential
  • Fertile male subjects who are unwilling or unable to use a highly effective method of contraception as outlined in this protocol for the duration of the study and for at least 28 days after the last dose of investigational product
  • Have a clinically significant infection currently or within 6 months of first dose of study drug

Psoriasis Participants:

Inclusion Criteria

  • Healthy male subjects between ages of 18-65 years
  • Healthy female subjects of non-childbearing potential between the ages of 18-65 years
  • Have a diagnosis of plaque psoriasis for at least 6 months prior to first study dose
  • Have plaque-type psoriasis covering at least 15% of total body surface area (BSA) at Day-1(prior to randomization in the study
  • No evidence of active or latent or inadequately treated infection with Mycobacterium tuberculosis (TB)

Exclusion Criteria

  • Currently have non-plaque forms of psoriasis, eg, erythrodermic, guttate, or pustular psoriasis
  • Have a clinically significant infection currently or within 6 months of first dose of study drug, or a history of chronic or recurrent infectious disease
  • Pregnant female subjects; breastfeeding female subjects; female subjects of childbearing potential
  • Fertile male subjects who are unwilling or unable to use a highly effective method of contraception as outlined in this protocol for the duration of the study and for at least 28 days after the last dose of investigational product
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT03210961). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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