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A Bioequivalence Study of APX001 High-load and Low-load Tablets

Phase 1
Completed
Conditions
Invasive Fungal Infections
Interventions
Drug: APX001A
Registration Number
NCT05491733
Lead Sponsor
Basilea Pharmaceutica
Brief Summary

A study to learn about the bioequivalence (the biochemical similarity of two medicines that share the same active ingredient and desired outcome for patients) of the study medicine called APX001 in healthy participants.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
18
Inclusion Criteria
  • Body mass index (BMI) between 18.0 and 32.0 kg/m2, inclusive.
  • Minimum body weight of 50 kg.
  • Screening hematology, clinical chemistry, coagulation, and urinalysis consistent with overall good health and having an estimated glomerular filtration rate (eGFR) >80 mL/min, based on creatinine clearance calculation by the Cockcroft-Gault formula.
Exclusion Criteria
  • Having any uncontrolled or active major systemic disease including, but not limited to: cardiovascular, pulmonary, gastrointestinal, metabolic, urogenital, neurological, immunological, psychiatric, or neoplastic disorder with metastatic potential.
  • History or presence of neurological disorders including abnormal movements or seizures.
  • History or presence of malignancy within the past year. Subjects who have been successfully treated with no recurrence of basal cell carcinoma of the skin or carcinoma in-situ of the cervix may be enrolled.
  • Significant and/or acute illness or chronic infection, as judged by the investigator, including, but not limited to: upper airway infection, urinary tract infection, or skin infection within 30 days prior to the first study drug administration.
  • Taking any drug or herbal CYP3A modulator (e.g., erythromycin; St. John's Wort) within 4 weeks (or 5 half-lives, whichever is longer) or any other nutrients known to modulate CYP3A activity (e.g., grapefruit juice; Seville orange) within 2 weeks prior to the first admission.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
APX001A Treatment CAPX001Oral tablet with a high drug load in participants that are not fasted.
APX001A Treatment CAPX001AOral tablet with a high drug load in participants that are not fasted.
APX001 Treatment AAPX001Oral tablet with a 25% drug load (low-load) in fasted participants
APX001 Treatment AAPX001AOral tablet with a 25% drug load (low-load) in fasted participants
APX001A Treatment BAPX001AOral tablet with a high drug load in fasted participants
APX001A Treatment BAPX001Oral tablet with a high drug load in fasted participants
Primary Outcome Measures
NameTimeMethod
Maximum Observed Plasma Concentration (Cmax)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Time to Reach Maximum Observed Plasma Concentration (Tmax)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Apparent Terminal Elimination Rate Constant (λz)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Apparent Total clearance, Calculated as Dose/AUCinf (CL/F)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Apparent Volume of Distribution at Terminal Phase (Vz/F)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Number of Participants With Treatment Emergent Treatment-Related Adverse Events (AEs)Baseline through Day 14
Number of Participants With Change From Baseline in Laboratory Tests ResultsBaseline through Day 14
Number of Participants With Clinically Significant Change in Vital SignsBaseline through Day 14
Number of Participants With Clinically Significant Findings in Electrocardiogram (ECG) AbnormalitiesBaseline through Day 14
Number of Participants With Abnormalities in Physical ExaminationsBaseline through Day 14
Percentage of Area Under the Curve Extrapolated to Infinity (%AUCextra)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Plasma Decay Half-Life (t1/2)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Area Under the Curve From Time Zero to 24 hours (AUC0-24)Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (1)

Pharmaceuticals Research Associates, Inc

🇺🇸

Salt Lake City, Utah, United States

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