Safety, Pharmacokinetics, Bioavailability, Food Effect, Drug-Drug Interaction Study of APX001 Administered Orally

Basilea Pharmaceutica

Status and phase: Completed; Phase 1

Conditions: Fungal Infection

Treatments: Drug: Cytochrome P450 substrates; Drug: APX001 multiple oral doses 1; Drug: APX001 single oral dose fed; Drug: APX001 single oral dose 3; Drug: Matching placebo control; Drug: APX001 multiple oral doses 3; Drug: APX001 single oral dose 1; Drug: APX001 single IV dose; Drug: APX001 single oral dose fasted; Drug: APX001 multiple oral doses 2; Drug: APX001 single oral dose 2

Study type: Interventional

Funder types: Industry

Identifiers

NCT02957929

C4791002 (Other Identifier)

APX001-102

Details and patient eligibility

About

This is a Phase l double-blind, placebo-controlled, randomized study to investigate the safety, tolerability, pharmacokinetics, bioavailability and food effect of single doses of APX001 administered intravenously and orally, followed by an evaluation of the safety, tolerability, pharmacokinetics and drug-drug interaction potential of multiple doses of APX001 administered orally.

Enrollment: 46 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Women of childbearing potential must agree to avoid pregnancy during the study and to use contraception at least 2 weeks before the start of the study until 3 months after the last dose of study drug.
• Males with partner(s) of childbearing potential must agree to use appropriate barrier contraception from the screening period until 3 months after the last dose of study drug.
• Screening hematology, clinical chemistry, coagulation and urinalysis consistent with overall good health.
• No significantly abnormal findings on physical examination, ECG and vital signs.
• Willing and able to provide written informed consent.

Exclusion criteria

• 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 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.
• Use of prescription medication within 14 days prior to the first dose of study drug and throughout the study.
• Use of non-prescription or over-the-counter medications within 7 days prior to the first dose of study drug and throughout the study.
• Positive results on any of the following Screening laboratory tests: serum pregnancy test, urine alcohol test, urine drugs of abuse, hepatitis B surface antigen, hepatitis C antibody, and human immunodeficiency virus (HIV) antibody.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: Double Blind

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46 participants in 9 patient groups

Cohort 1a, Period A

Experimental group

Description:

single intravenous dose, crossover

Treatment:

Drug: APX001 single IV dose

Drug: Matching placebo control

Cohort 1a, Period B

Experimental group

Description:

single oral dose, crossover

Treatment:

Drug: Matching placebo control

Drug: APX001 single oral dose 1

Cohort 1a, Period C

Experimental group

Description:

single oral dose

Treatment:

Drug: APX001 single oral dose 2

Drug: Matching placebo control

Cohort 1a, Period D

Experimental group

Description:

single oral dose, crossover

Treatment:

Drug: Matching placebo control

Drug: APX001 single oral dose 3

Cohort 1b, Period E

Experimental group

Description:

Single oral dose under fasted conditions, crossover

Treatment:

Drug: APX001 single oral dose fasted

Drug: Matching placebo control

Cohort 1b, Period F

Experimental group

Description:

Single oral dose under fed conditions, crossover

Treatment:

Drug: Matching placebo control

Drug: APX001 single oral dose fed

Cohort 2

Experimental group

Description:

Multiple oral doses

Treatment:

Drug: Matching placebo control

Drug: APX001 multiple oral doses 1

Cohort 3

Experimental group

Description:

Multiple oral doses

Treatment:

Drug: APX001 multiple oral doses 2

Drug: Matching placebo control

Cohort 4

Experimental group

Description:

Multiple oral doses in presence of CYP probe substrates

Treatment:

Drug: APX001 single IV dose

Drug: APX001 multiple oral doses 3

Drug: Cytochrome P450 substrates