This is a trial of up to 60-day duration for safety, tolerability, and pharmacokinetics in healthy volunteers administered deupirfenidone (LYT-100) alone or in combination with nintedanib .
The purpose of this research is to investigate the effects of deupirfenidone (LYT-100) when co-administered with nintedanib to determine if there are any drug-drug interactions. In particular, the study will investigate the safety, tolerability and pharmacokinetics of LYT-100 co-administered with nintedanib. Eligible participants will be admitted to the Clinical Research Unit for 31 days, will be administered nintedanib and/or LYT-100 for 30 days, and will provide blood samples and have assessments during this time. Participants will return for a safety follow-up visit 30 days after taking the last dose of study drug.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
24
Nintedanib 150 MG will be administered every 12 hours from Days 1 to 20. LYT-100 will be titrated from 275 MG three times a day on Days 8 to 10, to 550 MG three times a day on Days 11 to 13, to 825 MG three times a day on Days 14 to 30.
Nucleus Network Pty Ltd (Commercial Rd and St Kilda Rd) - VIC
Melbourne, Victoria, Australia
AUC of LYT-100 and Nintedanib
The area under the curve will be calculated from the first observed to last measurable plasma concentration. For nintedanib, dosing begins on Day 1 and ends on Day 20. For LYT-100, dosing begins on Day 8 and ends on Day 30.
Time frame: Blood samples for PK analysis were collected on Days 7, 13, 20, and 30 to assess the steady-state plasma PK profiles of nintedanib and/or LYT-100
Tmax of LYT-100 and Nintedanib
The time to maximum concentration (Tmax) will be calculated from the first observed to last measurable plasma concentration. For nintedanib, dosing begins on Day 1 and ends on Day 20. For LYT-100, dosing begins on Day 8 and ends on Day 30.
Time frame: Blood samples for PK analysis were collected on Days 7, 13, 20, and 30 to assess the steady-state plasma PK profiles of nintedanib and/or LYT-100
Cmax of LYT-100 and Nintedanib
The maximum observed plasma concentration (Cmax) will be calculated from the first observed to last measurable plasma concentration. For nintedanib, dosing begins on Day 1 and ends on Day 20. For LYT-100, dosing begins on Day 8 and ends on Day 30.
Time frame: Blood samples for PK analysis were collected on Days 7, 13, 20, and 30 to assess the steady-state plasma PK profiles of nintedanib and/or LYT-100
Number of Subjects With Abnormal Vital Signs (Blood Pressure)
Systolic and Diastolic blood pressure measured in millimeters of mercury (mmHg) to determine if there is abnormal blood pressure
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Vital Signs (Heart Rate)
Heart rate is measured in beats per minute (bpm) to determine if there is an abnormal heart rate
Time frame: Screening through Follow-up Visit on Day 60
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Number of Subjects With Abnormal Vital Signs (Respiration Rate)
Respiration rate is measured in breaths per minute (bpm) to determine if the respiration rate is abnormal
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Vital Signs (Body Temperature)
Tympanic body temperature is measured in degrees Celsius to determine if the body temperature is abnormal
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Electrocardiograms
Number of participants with an abnormal ECG and/or that have a QTcF\>450 ms
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Physical Examinations
A physical examination is performed to determine if any physical abnormalities are detected
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Laboratory Values (Hematology)
Hematology parameters to be tested are hemoglobin, hematocrit, erythrocytes, platelets, and leukocytes.
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Laboratory Values (Serum Chemistry)
Serum chemistry parameters to be tested are C-reactive protein, urea, creatinine, total and direct bilirubin, urate, albumin, globulin, alkaline phosphatase, creatine phosphokinase, troponin 1, aspartate aminotransferase, alanine aminotransferase, gamma-glutamyl transpeptidase, glucose, sodium, potassium, calcium, chloride, phosphate, bicarbonate
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Laboratory Values (Coagulation)
Coagulation parameters to be tested are international normalized ratio, prothrombin time, activated partial thromboplastin time
Time frame: Screening through Follow-up Visit on Day 60
Number of Subjects With Abnormal Laboratory Values (Urinalysis)
Urinalysis parameters to be tested are micro protein, nitrite, pH, trial specific gravity, ketone bodies, urobilinogen, blood, urine leukocyte esterase, appearance uri acm, micro glucose, bilirubin
Time frame: Screening through Follow-up Visit on Day 60