Clinical trial NCT05491733: A Bioequivalence Study of APX001 High-load and Low-load Tablets
Official title: A 3-Treatment, 3-Period, 6-Sequence Randomized Crossover Single-Dose Study Evaluating the Bioequivalence of High-Load and Low-Load Oral Tablet Formulations of Apx001 and the Effect of Food on the Absorption of Apx001 From the High-Load Tablet In Healthy Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Invasive Fungal Infections
Keywords: fosmanogepix
candida
aspergillus
scedosporium
fusarium
mucorales
rhizopus
Lead sponsor: Basilea Pharmaceutica
Sponsor class: INDUSTRY
First posted: 2022-08-08
Enrollment: 18
Sex: ALL
Minimum age (years): 18
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: BASIC_SCIENCE

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.


Eligibility criteria: 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.

Primary outcomes:
measure: Maximum Observed Plasma Concentration (Cmax)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Time to Reach Maximum Observed Plasma Concentration (Tmax)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Area Under the Curve From Time Zero to 24 hours (AUC0-24)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Percentage of Area Under the Curve Extrapolated to Infinity (%AUCextra)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Plasma Decay Half-Life (t1/2)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Apparent Terminal Elimination Rate Constant (λz)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Apparent Total clearance, Calculated as Dose/AUCinf (CL/F)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Apparent Volume of Distribution at Terminal Phase (Vz/F)
timeFrame: Predose, 0.5, 1, 2, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 36, 48, 168, and 312 hours post dose
measure: Number of Participants With Treatment Emergent Treatment-Related Adverse Events (AEs)
timeFrame: Baseline through Day 14
measure: Number of Participants With Change From Baseline in Laboratory Tests Results
timeFrame: Baseline through Day 14
measure: Number of Participants With Clinically Significant Change in Vital Signs
timeFrame: Baseline through Day 14
measure: Number of Participants With Clinically Significant Findings in Electrocardiogram (ECG) Abnormalities
timeFrame: Baseline through Day 14
measure: Number of Participants With Abnormalities in Physical Examinations
timeFrame: Baseline through Day 14
Secondary outcomes:
Other outcomes:
Locations:
city: Salt Lake City
country: United States
facility: Pharmaceuticals Research Associates, Inc
state: Utah
Study officials:
affiliation: Basilea Pharmaceutica International Ltd, Allschwil
name: Marc Engelhardt
role: STUDY_DIRECTOR
References: