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A Phase 2 Study of APX-115 in Hospitalized Patients With Confirmed Mild to Moderate COVID-19.

Phase 2
Terminated
Conditions
COVID-19
Interventions
Drug: Placebo
Registration Number
NCT04880109
Lead Sponsor
Aptabio Therapeutics, Inc.
Brief Summary

This phase 2 study is to assess the safety and tolerability of APX-115 active doses compared to placebo following multiple oral dosing in hospitalized patients with confirmed, mild to moderate, symptomatic COVID-19. It is anticipated that approximately 80 patients will be randomized into the study in a 1:1 ratio to 100 mg APX-115 or placebo arm.

Detailed Description

APX-115 is a potent small molecule inhibitor of NADPH-oxidase (Nox) isozymes being developed by Aptabio Therapeutics Inc. The Nox enzymes represent a family of 7 membrane enzymes (Nox1, Nox2, Nox3, Nox4, Nox5, Duox1, and Duox2) which catalyze NADPH-dependent generation of superoxide and secondary reactive oxygen species (ROS).

ROS are often generated during virus infection, thus promoting apoptosis, lung injury, and inflammation/allergy.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
16
Inclusion Criteria
  1. Willing and able to provide informed consent themselves or through their legally authorized representative.
  2. Male or female patients, of any race or ethnicity, 18 to 80 years of age, inclusive, on the day of informed consent. Racial and ethnic minorities should be included in the study population to the greatest extent possible.
  3. Laboratory-confirmed SARS-CoV-2 infection as determined within 14 days of randomization by real time RT-PCR or other commercial or public health assay authorized by FDA or other applicable health authority .
  4. Onset of COVID-19 symptoms within 14 days prior to randomization.
  5. Have at least one of the following symptoms at screening: fever, cough, shortness of breath, myalgia, ageusia, anosmia, fatigue, or weakness.
  6. Hospitalized with COVID-19 disease (WHO COVID-19 Clinical Improvement Ordinal Scale score of 3 [hospitalized, no oxygen therapy], 4 [hospitalized, oxygen by mask or nasal prongs], or 5 [high-flow oxygen or non-invasive mechanical ventilation])
  7. Patient is aware of the investigational nature of this study and willing to comply with protocol treatments, blood tests, and other evaluations listed in the informed consent form.
Exclusion Criteria
  1. Females who are pregnant (negative pregnancy test required for all women of childbearing potential at screening) or breastfeeding.
  2. Male patients and women of childbearing potential (women who are not surgically sterile or postmenopausal defined as postmenopausal for >12 months) who are not using at least one protocol specified method of contraception.
  3. COVID-19 disease as defined by the WHO COVID-19 Clinical Improvement Ordinal Scale, scores of 6 (intubation and mechanical ventilation) or 7 (ventilation + additional organ support - pressors, renal replacement therapy, extracorporeal membrane oxygenation).
  4. Expected survival less than 72 hours.
  5. Treatment with other drugs thought to possibly have activity against SARS CoV 2 infection within 7 days or within 5 half-lives, whichever is longer, prior to enrollment or concurrently. Drugs that have received FDA emergency use authorization or COVID-19 approval are allowed.
  6. Treatment with immunosuppressants, combination of 2 or more RAS blockers, UGT inhibitors and inducers, herbal/natural supplements, potassium-sparing diuretic, and radiographic contrast agent prior to enrollment or concurrently.
  7. History of abuse of drugs or alcohol that could interfere with adherence to study requirements as judged by the investigator.
  8. Use of any other concurrent investigational drugs while participating in the present study.
  9. Patient requires frequent or prolonged use of systemic corticosteroids (≥20 mg of prednisone/day or equivalent for >4 weeks) or other immunosuppressive drugs (eg, for organ transplantation or autoimmune conditions).
  10. Known renal disease with an estimated glomerular filtration rate <30 mL/min.
  11. Patients with clinically apparent liver disease (eg, jaundice, cholestasis, hepatic synthetic impairment, or active hepatitis) or moderate or severe hepatic impairment as determined by Child-Pugh score Class B or C.
  12. Alanine aminotransaminase (ALT) or aspartate aminotransaminase (AST) >3 × upper limit of normal (ULN) AND total bilirubin levels >2 × ULN OR ALT or AST >5 × ULN.
  13. Total bilirubin >1.5 × ULN, unless the patient has known Gilbert's syndrome.
  14. Hemoglobin <9 g/dL for females or <11 g/dL for males.
  15. Absolute neutrophil count <1500/mm3.
  16. Thrombocytopenia (platelets count <100 × 109/L).
  17. Inability to swallow oral medications or a gastrointestinal disorder with diarrhea (eg, Crohn's disease) or malabsorption at screening.
  18. Any other clinically significant medical condition or laboratory abnormality that, in the opinion of the investigator, would jeopardize the safety of the patient or potentially impact patient compliance or the safety/efficacy observations in the study.
  19. History of an allergic reaction or hypersensitivity to the study drug or any component of the study drug formulation.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
APX-115APX-115Oral administration of APX-115 100mg, daily for 14 days
PlaceboPlaceboOral administration of Placebo, daily for 14 days
Primary Outcome Measures
NameTimeMethod
Incidence of Treatment-Emergent Adverse Eventsover the 60-day period

Adverse events will be assessed to evaluate the safety and tolerability of APX-115 in mild-to-moderate COVID-19 patients. Clinical laboratory evaluations, vital signs, and ECG will be used to assess adverse events.

Secondary Outcome Measures
NameTimeMethod
Time to clinical recoveryUp to 60 Days

Recovery is defined as when WHO Clinical Improvement Ordinal Scale equal to or less than 3

Time to dischargeUp to Day 60

WHO Clinical Improvement Ordinal Scale is equal to or less than 2

Time to symptomatic recoveryUp to Day 60

When none of the COVID-19 Symptom Assessment scores are higher than 1

Time to complete symptomatic recoveryUp to Day 60

When none of the COVID-19 Symptom Assessment scores are higher than 0

Change in log10 SARS-CoV-2 viral loadUp to Day 14

hange from baseline in log10 SARS-CoV-2 viral load as measured by RT-PCR by Days 5 and 14

Proportion of patients in clinical recoveryUp to Day 29

Symptom Assessment

scoring of WHO Clinical Improvement Ordinal ScaleUp to Day 29

9-point scale on key analysis days for levels ≥3

Changes from baseline in anti-inflammatory markers in bloodDay 1 and Day 14

Blood will be analyzed for changes from baseline in anti-inflammatory markers, such as C-reactive protein, ferritin, lactate dehydrogenase, D-dimer, troponin, and transforming growth factor-β.

Changes from baseline in pro-inflammatory cytokines in bloodDay 1 and 14

Blood will be analyzed for changes from baseline in pro-cytokine panel of the blood, such as interleukin (IL)-1β, IL-6, and interferon-γ.

Changes from baseline in 8-isoprostane in bloodDays 1 and 14

Blood will be analyzed for changes from baseline in 8-isoprostane.

Trough (predose) plasma concentration (Ctrough)Day 1

Trough (predose) plasma concentration (Ctrough) will be analyzed from plasma samples for pharmacokinetic assessment of APX-115.

Maximum observed plasma concentration (Cmax)Days 1, 5, and 14

Maximum observed plasma concentration (Cmax) will be analyzed from plasma samples for pharmacokinetic assessment of APX-115.

Time to Cmax (Tmax)Days 1, 5, and 14

Time to Cmax (Tmax) will be analyzed from plasma samples for pharmacokinetic assessment of APX-115.

Area under the plasma concentration versus time curve (AUC) from time zero to the Time of last quantifiable concentration (AUC0-last)Days 1, 5, and 14

Area under the plasma concentration versus time curve (AUC) from time zero to the time of last quantifiable concentration (AUC0-last) will be analyzed from plasma samples for pharmacokinetic assessment of APX-115.

AUC within a dosing interval (AUCtau, where tau = 12 hours)Days 1, 5, and 14

AUC within a dosing interval (AUCtau, where tau = 12 hours) will be analyzed from plasma samples for pharmacokinetic assessment of APX-115.

Trial Locations

Locations (3)

Alternative Research Associates, LLC

🇺🇸

Hialeah, Florida, United States

Anne Arundel Medical Center

🇺🇸

Baltimore, Maryland, United States

Millennium Physicians Group

🇺🇸

Houston, Texas, United States

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