Pharmacokinetics (PK) Drug Interaction Study of Milademetan and Itraconazole or Posaconazole in Healthy Participants

An Open-label, Randomized, 2-period, 2-sequence Study to Evaluate the Single-dose Pharmacokinetics of Milademetan When Administered Alone or Concomitantly With Itraconazole or Posaconazole in Healthy Subjects

Status

Completed

Phases

Early Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT03614455

Enrollment

Registered

2018-08-03

Start date

2018-07-13

Completion date

2018-10-01

Last updated

2019-02-12

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Pharmacokinetics

Brief summary

This will be an open-label, randomized, 3-treatment, 2-period, 2-sequence study in healthy subjects to evaluate the single-dose PK of milademetan when given as monotherapy and when administered with steady-state levels of the strong CYP3A4 inhibitors itraconazole or posaconazole. The duration of the study for each individual subject will be approximately 49 days from the start of Screening through Study Discharge. Subjects will remain in-house for up to 23 days, including 22 overnight stays.

Interventions

DRUGMilademetan

Milademetan 100 mg capsule for oral administration

DRUGItraconazole

Itraconazole (200 mg) oral solution (20 mL of 10 mg/mL)

DRUGPosaconazole

Posaconazole (200 mg) oral suspension (5 mL of 40 mg/mL)

Study design

Allocation

RANDOMIZED

Intervention model

SEQUENTIAL

Primary purpose

BASIC_SCIENCE

Masking

NONE

Intervention model description

Prior to dosing on Day 1 of Treatment Period 1, subjects will be assigned to 1 of 2 sequences (sequences AB or AC), according to a pre-generated randomization scheme.

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

Healthy participants with no clinically significant medical history or physical examination findings and who also meet all protocol-defined inclusion and

Exclusion criteria

summarized as follows: Inclusion Criteria: * Has negative urine test for drugs of abuse, alcohol and tobacco * If female, is surgically sterile or postmenopausal * If male, agrees to protocol-defined contraceptive methods * Has adequate hematologic, hepatic, and renal function as defined by the protocol * Is able and willing to follow all study procedures * Has provided a signed informed consent

Design outcomes

Primary

Measure	Time frame	Description
Maximum plasma concentration (Cmax) of milademetan	pre-dose and then at 0.5, 1, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose	Categories: alone (A), in sequence AB, in sequence AC
Area under the plasma concentration-time curve extrapolated to infinity (AUCinf) of milademetan	within 168 hours postdose	Categories: alone (A), in sequence AB, in sequence AC

Secondary

Measure	Time frame	Description
Terminal elimination half-life (t½) of milademetan	within 168 hours postdose	Categories: alone (A), in sequence AB, in sequence AC
Time to reach maximum plasma concentration (Tmax) of milademetan	pre-dose and then at 0.5, 1, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose	Categories: alone (A), in sequence AB, in sequence AC
Apparent volume of distribution (Vz/F)	within 168 hours postdose	Categories: alone (A), in sequence AB, in sequence AC
Apparent total body clearance (CL/F) of milademetan	within 168 hours postdose	Categories: alone (A), in sequence AB, in sequence AC
Area under the plasma concentration-time curve from time 0 to the time of last measurable concentration (AUC0-t) for milademetan	within 168 hours postdose	Categories: alone (A), in sequence AB, in sequence AC

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 15, 2026