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

NCT05491733 | Completed Phase 1 FDA Drug

• 2 other identifiers: APX001-108C4791008
• Study Type: interventional
• Target: 18
• Locations: 1 country
• Sites: 1

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.

Conditions

Invasive Fungal Infections

Keywords

fosmanogepix; candida; aspergillus; scedosporium; fusarium; mucorales; rhizopus

Outcome Measures

Primary Outcomes (15)

• 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

• 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

• 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

• 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 Results

  Baseline through Day 14

• Number of Participants With Clinically Significant Change in Vital Signs

  Baseline through Day 14

• Number of Participants With Clinically Significant Findings in Electrocardiogram (ECG) Abnormalities

  Baseline through Day 14

• Number of Participants With Abnormalities in Physical Examinations

  Baseline through Day 14

Study Arms (3)

APX001 Treatment A

ACTIVE COMPARATOR

Oral tablet with a 25% drug load (low-load) in fasted participants

Drug: APX001; Drug: APX001A

APX001A Treatment B

EXPERIMENTAL

Oral tablet with a high drug load in fasted participants

Drug: APX001; Drug: APX001A

APX001A Treatment C

EXPERIMENTAL

Oral tablet with a high drug load in participants that are not fasted.

Drug: APX001; Drug: APX001A

Interventions

APX001 DRUG

Low-load oral tablet

Also known as: fosmanogepix

APX001 Treatment A; APX001A Treatment B; APX001A Treatment C

APX001A DRUG

High-load oral tablet

Also known as: fosmanogepix

APX001 Treatment A; APX001A Treatment B; APX001A Treatment C

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Basilea Pharmaceutica: lead

Study Sites (1)

Pharmaceuticals Research Associates, Inc

Salt Lake City, Utah, 84124, United States

Location

MeSH Terms

Conditions

Invasive Fungal Infections; Torulopsis

Interventions

APX001A

Condition Hierarchy (Ancestors)

Mycoses; Bacterial Infections and Mycoses; Infections

Study Officials

• Marc Engelhardt

  Basilea Pharmaceutica International Ltd, Allschwil

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR
• Expanded Access: Yes

Study Record Dates

• First Submitted: August 4, 2022
• First Posted: August 8, 2022
• Study Start: March 2, 2021
• Primary Completion: May 13, 2021
• Study Completion: June 23, 2021
• Last Updated: July 11, 2024

Record last verified: 2024-07

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)