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Pharmacokinetics Study of XG005 Capsule

Phase 1
Completed
Conditions
Pain
Interventions
Registration Number
NCT04499209
Lead Sponsor
Xgene Pharmaceutical Group
Brief Summary

This was a Phase 1, single-center, randomized, placebo-controlled, 2-period, ascending single-dose study assessing the PK, safety, and tolerability of single ascending doses of XG005 (Period 1) and the naproxen and pregabalin combination (Period 2), in 5 dose groups each with 10 subjects.

Detailed Description

Period 1 was double-blind and randomized 8 subjects (1:1 allocation ratio by gender) to XG005 and 2 subjects (1:1 allocation ratio by gender) to placebo. Subjects were enrolled sequentially into a total of 5 ascending dose levels pending safety review, and PK review where possible, of Period 1 of the prior dose level. Sentinel dose participants (1 for XG005 and 1 for placebo) were included as the first dose administered at each dose level in Period 1.

In Period 2, all subjects in the last three XG005 dose groups received approximate molar equivalents of naproxen and pregabalin corresponding to XG005 doses after a 7-day washout period. Period 2 was open-label with 10 subjects per group.

PK blood samples in each treatment period were collected at 0 (pre-dosing), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hrs after drug administration.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
50
Inclusion Criteria
  • BMI range of 18-30 kg/m2
  • Medically healthy subjects
  • Creatinine clearance ≥ 80 mL/min
Exclusion Criteria
  • History or presence of significant diseases
  • History or presence of alcoholism or drug abuse
  • Consumption of alcohol 48 hours prior each dose
  • Hypersensitivity or idiosyncratic reaction to the study drug
  • Abnormal diet (for whatever reason) during the 30 days prior to the first dosing;
  • Donation (standard donation amount or more) of blood or blood products
  • Plasma donation within 7 days prior to the study;
  • Participation in another clinical trial within 30 days prior to the first dose;
  • Female subjects who are pregnant or lactating;
  • Hemoglobin < 120 g/L

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Period 1- XG005XG005XG005 capsule in 4 dose level
Period 2- Naproxen and PregabalinCombination of Naproxen and PregabalinCombination of Naproxen and Pregabalin
Period 1- PlaceboPlacebosXG005 matching placebo
Primary Outcome Measures
NameTimeMethod
Terminal clearance (CL/F)Day1 to Day 4
Terminal Elimination Rate Constant (kel)Day1 to Day 4
Maximum concentration (Cmax)Day1 to Day 4
Time to maximum concentration (Tmax)Day1 to Day 4
Area under the concentration-time curve from time 0 to last measurable time-point (AUC0-t)Day1 to Day 4
Terminal half-life (t1/2)Day1 to Day 4
Area under the concentration-time curve from time 0 to infinity (AUC0-inf)Day1 to Day 4
Volume of distribution (Vd/F)Day1 to Day 4
Secondary Outcome Measures
NameTimeMethod
respiratory rateDay -1 to Day 8

vital signs

temperatureDay -1 to Day 8

vital signs

physical examinationDay -1 to Day 8

Cardiovascular, Ears, Nose and Throat, Eyes, Gastrointestinal, Head, Lymph Nodes, Musculoskeletal, Neurological, Respiratory, Skin

electrocardiogram (ECG) parameters;Day -1 to Day 8

ECG-PR, RR, QRS, QT, and QTc intervals

clinical laboratory parameters -chemistryDay -1 to Day 8

BUN, Creatinine, Total bilirubin, Total protein, Alkaline phosphatase, Uric Acid, Estimated creatinine clearance, Creatine Phosphokinase (CPK), AST (SGOT), ALT (SGPT), Glucose, Sodium, Potassium

clinical laboratory parameters- hematologyDay -1 to Day 8

Hemoglobin, Hematocrit, Red Blood Cell Count, White Blood Cell Count with differential, Platelet Count

incidence and severity of adverse events (AEs)Day -1 to Day 8
blood pressureDay -1 to Day 8

vital signs

heart rateDay -1 to Day 8

vital signs

clinical laboratory parameters urinalysisDay -1 to Day 8

* pH • Specific gravity • Protein

* Glucose • Ketones • Bilirubin

* Blood • Nitrite • Urobilinogen

* Leukocytes

Trial Locations

Locations (1)

Linear Clinical Research Ltd

🇦🇺

Nedlands, Western Australia, Australia

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