Phase 1 Completed N=144 Randomized Treatment

A Study to Evaluate the Pharmacokinetic Exposure of 2 Formulations of Apremilast in Healthy Adults

Healthy Volunteers

Source: ClinicalTrials.gov NCT02777554 ↗

Enrolled (actual)

144

Serious AEs

0.0%

Results posted

Jul 2021

Primary outcomePrimary: Part 1: Peak Maximum Plasma Concentration (Cmax) of Apremilast — 451; 459 ng/mL

Summary

The purpose of this study is to evaluate the relative bioavailability of apremilast once-daily formulation relative to a twice daily formulation when administered as multiple doses (Part 1), and when administered as a single dose under fasting and fed conditions (Part 2). Information on safety and tolerability will also be obtained.

Outcome Measures

Outcome	Result	p-value
PRIMARY Part 1: Peak Maximum Plasma Concentration (Cmax) of Apremilast	451; 459	—
PRIMARY Part 1: Area Under the Concentration-time Curve From Time Zero to 24 Hours Postdose (AUC0-24) of Apremilast	6370; 6090	—
PRIMARY Part 2: Peak Maximum Plasma Concentration (Cmax) of Apremilast	379; 402; 436; 496	—
PRIMARY Part 2: Area Under the Plasma Concentration-time Curve From Time Zero to the Last Observable Concentration (AUC0-t) of Apremilast	7030; 6650; 7580; 7400	—
PRIMARY Part 2: Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast	7100; 6680; 7600; 7450	—
SECONDARY Number of Participants With Treatment-emergent Adverse Events	50; 47; 2; 4; 3; 2	—

Eligibility Criteria

Inclusion Criteria

Subjects must satisfy the following criteria to be enrolled in the study (Part 1 and Part 2):

Must understand and voluntarily sign a written Informed consent form (ICF) prior to any study-related procedures being performed.
Must be able to communicate with the investigator, understand and comply with the requirements of the study, and agree to adhere to restrictions and examination schedules.
Male and female subjects of any race between 18 to 55 years of age (inclusive), and in good health as determined by the Investigator at the time of signing the informed consent document.
Have a body mass index (BMI) between 18 and 33 kg/m^2 (inclusive).
No clinically significant laboratory test results as determined by the investigator.
At the screening visit, must be afebrile, with supine systolic blood pressure (BP): 90 to 140 mmHg, supine diastolic BP: 50 to 90 mmHg, and pulse rate: 40 to 110 bpm. Eligibility criteria for vital signs performed during check-in and/or predose on Day 1 will be at the discretion of the Investigator.
Must have a normal or clinically acceptable 12-lead electrocardiogram (ECG). Subjects must have a QT interval corrected using the Fridericia formula (QTcF) value ≤ 450 msec.
Female subjects
Must have a negative pregnancy test
If postmenopausal: must have follicular stimulating hormone (FSH) test result > 40 IU/L and a negative pregnancy test
Contraception Requirements:

Must comply with the following acceptable forms of contraception. All Female of child bearing potential (FCBP)1 must use one of the approved contraceptive options as described below while taking apremilast and for at least 28 days after administration of the last dose of the apremilast. At the time of study entry, and at any time during the study when a FCBP's contraceptive measures or ability to become pregnant changes, the Investigator will educate the subject regarding contraception options and the correct and consistent use of effective contraceptive methods in order to successfully prevent pregnancy.

All FCBP must have a negative pregnancy test at Screening and Day -1 of each Treatment Period. All FCBP subjects who engage in activity in which conception is possible must use one of the approved contraceptive options described below:

Option 1: Any one of the following highly effective methods: hormonal contraception (oral, injection, implant, transdermal patch, vaginal ring); intrauterine device (IUD); tubal ligation; or partner's vasectomy; OR Option 2: Male or female condom (latex condom or non-latex condom NOT made out of natural [animal] membrane [for example, polyurethane]); Plus one additional barrier(c) contraceptive sponge with spermicide.

Male subjects (including those who have had a vasectomy) who engage in activity in which conception is possible must use barrier contraception (latex or non-latex condoms NOT made out of natural [animal] membrane [for example, polyurethane]) while on Investigational Product (IP) and for at least 28 days after the last dose of IP.

Must agree to refrain from donating sperm, blood or plasma (other than for this study) while participating in this study and for at least 28 days after the last dose of investigational product.
Subject is willing and able to adhere to the study visit schedule and other protocol requirements.

Exclusion Criteria

The presence of any of the following will exclude a subject from enrollment:

History of any clinically significant and relevant neurological, psychiatric, gastrointestinal, renal, hepatic, cardiovascular, psychological, pulmonary, metabolic, endocrine, hematological, allergic disease, drug allergies, or other major disorders.
Any condition which places the subject at unacceptable risk if he were to participate in the study, or confounds the ability to interpret data from the study.

1 A female of childbearing potential is a sexually mature female who 1) has not undergone a hysterectomy (the s

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Data sourced from ClinicalTrials.gov (NCT02777554). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.