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Safety and Pharmacokinetics of Sustained-release Depot Tacrolimus: A First-in-human Study

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
 
ClinicalTrials.gov Identifier: NCT03626714
Recruitment Status : Completed
First Posted : August 13, 2018
Results First Posted : June 11, 2019
Last Update Posted : August 13, 2019
Sponsor:
Collaborator:
National Institute of Allergy and Infectious Diseases (NIAID)
Information provided by (Responsible Party):
Auritec Pharmaceuticals

Study Type Interventional
Study Design Intervention Model: Single Group Assignment;   Masking: None (Open Label);   Primary Purpose: Treatment
Conditions Organ Transplant Rejection
Psoriasis
Intervention Drug: Sustained Release Injectable Tacrolimus
Enrollment 8
Recruitment Details  
Pre-assignment Details  
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description All subjects will be treated with a single dose injection of sustained-release Tacrolimus.
Period Title: Overall Study
Started 8
Completed 8
Not Completed 0
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description All subjects will be treated with a single dose injection of sustained-release Tacrolimus.
Overall Number of Baseline Participants 8
Hide Baseline Analysis Population Description
[Not Specified]
Age, Continuous  
Mean (Full Range)
Unit of measure:  Years
Number Analyzed 8 participants
34.37
(22 to 43)
Sex: Female, Male  
Measure Type: Count of Participants
Unit of measure:  Participants
Number Analyzed 8 participants
Female
4
  50.0%
Male
4
  50.0%
Ethnicity (NIH/OMB)  
Measure Type: Count of Participants
Unit of measure:  Participants
Number Analyzed 8 participants
Hispanic or Latino
6
  75.0%
Not Hispanic or Latino
2
  25.0%
Unknown or Not Reported
0
   0.0%
Race (NIH/OMB)  
Measure Type: Count of Participants
Unit of measure:  Participants
Number Analyzed 8 participants
American Indian or Alaska Native
0
   0.0%
Asian
0
   0.0%
Native Hawaiian or Other Pacific Islander
0
   0.0%
Black or African American
3
  37.5%
White
5
  62.5%
More than one race
0
   0.0%
Unknown or Not Reported
0
   0.0%
Region of Enrollment  
Measure Type: Number
Unit of measure:  Participants
United States Number Analyzed 8 participants
8
1.Primary Outcome
Title Number of Subjects That Experienced Treatment-related Adverse Events [Safety and Tolerability]
Hide Description

Adverse events were documented at each study visit according to the criteria set forth in the Toxicity Grading Scale for Healthy Adult and Adolescent Volunteers Enrolled in Preventive Vaccine Clinical Trials as follows:

Grade 1 (mild); Grade 2 (moderate); Grade 3 (severe); Grade 4 (potentially life-threatening).

Time Frame 60 days
Hide Outcome Measure Data
Hide Analysis Population Description
[Not Specified]
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description:
All subjects were subcutaneously injected a single dose (0.1 mg/kg) of sustained-release tacrolimus.
Overall Number of Participants Analyzed 8
Measure Type: Count of Participants
Unit of Measure: Participants
Tenderness at Injection Site - Grade 1
6
  75.0%
Burning Pain at Injection Site - Grade 1
6
  75.0%
Erythema/Redness at Injection Site - Grade 1
3
  37.5%
Induration/Swelling at Injection Site - Grade 1
2
  25.0%
Tenderness at Injection Site - Grade 2
1
  12.5%
2.Primary Outcome
Title Drug Concentrations in Blood Samples at Individual Time-points
Hide Description The concentrations of tacrolimus in blood samples were measured at baseline, day 1 (1 hr, 3 hrs, 6 hrs, 12 hrs, and 24 hrs), followed by days 3, 7, 14, 21, 30, 37, 44, 51 and 60.
Time Frame 60 days
Hide Outcome Measure Data
Hide Analysis Population Description
[Not Specified]
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description:
All subjects were subcutaneously injected a single dose (0.1 mg/kg) of sustained-release tacrolimus.
Overall Number of Participants Analyzed 8
Mean (Standard Deviation)
Unit of Measure: ng/mL
Baseline 0  (0)
Day 1, hour 1 0.667  (0.505)
Day 1, hour 3 0.956  (0.556)
Day 1 hour 6 1.30  (0.623)
Day 1, hour 12 1.84  (0.548)
Day 1, hour 24 1.54  (0.484)
Day 3 1.24  (0.397)
Day 7 0.775  (0.365)
Day 14 0.341  (0.158)
Day 21 0.320  (0.127)
Day 30 0.302  (0.091)
Day 37 0.282  (0.074)
Day 44 0.260  (0.082)
Day 51 0.269  (0.091)
Day 60 0.260  (0.072)
3.Primary Outcome
Title Mean Blood Concentration-time Curve - Cmax
Hide Description Maximum observed tacrolimus whole blood concentration
Time Frame 60 days
Hide Outcome Measure Data
Hide Analysis Population Description
[Not Specified]
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description:
All subjects were subcutaneously injected a single dose (0.1 mg/kg) of sustained-release tacrolimus.
Overall Number of Participants Analyzed 8
Mean (Standard Deviation)
Unit of Measure: ng/mL
1.92  (0.527)
4.Primary Outcome
Title Mean Blood Concentration-time Curve - Tmax
Hide Description Time to maximum observed tacrolimus whole blood concentration
Time Frame 60 days
Hide Outcome Measure Data
Hide Analysis Population Description
[Not Specified]
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description:
All subjects were subcutaneously injected a single dose (0.1 mg/kg) of sustained-release tacrolimus.
Overall Number of Participants Analyzed 8
Mean (Standard Deviation)
Unit of Measure: Hour
14.3  (6.36)
5.Primary Outcome
Title Blood Concentration-time Curve [AUC]
Hide Description Area under the concentration-time curve
Time Frame 60 days
Hide Outcome Measure Data
Hide Analysis Population Description
[Not Specified]
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description:
All subjects were subcutaneously injected a single dose (0.1 mg/kg) of sustained-release tacrolimus.
Overall Number of Participants Analyzed 8
Mean (Standard Deviation)
Unit of Measure: hour*ng/mL
568  (171)
6.Primary Outcome
Title Terminal Elimination Half-life [t1/2]
Hide Description The apparent terminal elimination half-life was calculated.
Time Frame 60 days
Hide Outcome Measure Data
Hide Analysis Population Description
[Not Specified]
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description:
All subjects were subcutaneously injected a single dose (0.1 mg/kg) of sustained-release tacrolimus.
Overall Number of Participants Analyzed 8
Mean (Standard Deviation)
Unit of Measure: hours
1100  (803)
Time Frame For this single-dose experimental study, adverse event data was collected from subjects for up to 60 days.
Adverse Event Reporting Description [Not Specified]
 
Arm/Group Title Experimental: Sustained Release Injectable Tacrolimus
Hide Arm/Group Description All subjects were subcutaneously injected a single dose (0.1 mg/kg) of sustained-release tacrolimus.
All-Cause Mortality
Experimental: Sustained Release Injectable Tacrolimus
Affected / at Risk (%)
Total   0/8 (0.00%) 
Show Serious Adverse Events Hide Serious Adverse Events
Experimental: Sustained Release Injectable Tacrolimus
Affected / at Risk (%)
Total   0/8 (0.00%) 
Show Other (Not Including Serious) Adverse Events Hide Other (Not Including Serious) Adverse Events
Frequency Threshold for Reporting Other Adverse Events 0%
Experimental: Sustained Release Injectable Tacrolimus
Affected / at Risk (%)
Total   8/8 (100.00%) 
Blood and lymphatic system disorders   
Elevated Bilirubin   2/8 (25.00%) 
Decreased Hemoglobin   3/8 (37.50%) 
Decreased Platelets   1/8 (12.50%) 
Hypercalcemia   1/8 (12.50%) 
Hyponatremia   1/8 (12.50%) 
Gastrointestinal disorders   
Elevated Alt/Ast   1/8 (12.50%) 
Elevated Aspartate   3/8 (37.50%) 
General disorders   
Hyperglycemia   3/8 (37.50%) 
Hypoglycemia   1/8 (12.50%) 
Bruising   1/8 (12.50%) 
Musculoskeletal and connective tissue disorders   
Odontalgia left upper wisdom tooth   1/8 (12.50%) 
Renal and urinary disorders   
Hematuria   1/8 (12.50%) 
Hypokalemia   1/8 (12.50%) 
Indicates events were collected by systematic assessment
The study’s main limitations include the small sample size (n=8) and the short duration (60 days).
Certain Agreements
Principal Investigators are NOT employed by the organization sponsoring the study.
There is NOT an agreement between Principal Investigators and the Sponsor (or its agents) that restricts the PI's rights to discuss or publish trial results after the trial is completed.
Results Point of Contact
Layout table for Results Point of Contact information
Name/Title: Sarjan Shah
Organization: Auritec
Phone: 9092109715
EMail: sshah@auritecpharma.com
Layout table for additonal information
Responsible Party: Auritec Pharmaceuticals
ClinicalTrials.gov Identifier: NCT03626714     History of Changes
Other Study ID Numbers: RTB-010
U44AI069674 ( U.S. NIH Grant/Contract )
First Submitted: July 31, 2018
First Posted: August 13, 2018
Results First Submitted: May 20, 2019
Results First Posted: June 11, 2019
Last Update Posted: August 13, 2019