Study to Evaluate Bioavailability of Apremilast Oral Suspension Relative to Tablet and to Assess Effect of Food on the Pharmacokinetics (PK) of the Oral Suspension
Summary
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Maximum Observed Plasma Concentration (Cmax) of Apremilast |
323; 274; 215 | — |
| PRIMARY Area Under the Concentration-time Curve From Time Zero to the Last Measured Time Point (AUC0-t) for Apremilast |
3130; 2740; 3160 | — |
| PRIMARY Area Under the Concentration-time Curve From Time Zero to Infinity (AUC0-∞) for Apremilast |
3160; 2760; 3190 | — |
| PRIMARY Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast |
2.00; 2.00; 5.00 | 0.1508 |
| PRIMARY Terminal Elimination Half-life (T1/2) of Apremilast |
7.89; 8.51; 7.54 | — |
| PRIMARY Apparent Clearance of Apremilast From Plasma After Extravascular Administration (CL/F) |
9.51; 10.9; 9.42 | — |
| PRIMARY Apparent Volume of Distribution of Apremilast During the Terminal Phase (Vz/F) |
108; 133; 102 | — |
| PRIMARY Lag Time (Tlag) of Apremilast |
0.00; 0.00; 0.00 | — |
| PRIMARY Relative Bioavailability (F) of Apremilast Oral Suspension Formulation |
87.6; 101 | — |
| SECONDARY Number of Participants With Treatment-emergent Adverse Events |
8; 10; 6; 4; 7; 4 | — |
Eligibility Criteria
Inclusion Criteria
Subjects must satisfy ALL of the following criteria to be eligible for enrollment into the study:
- Must understand and voluntarily sign a written Informed Consent (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 QTcF value ≤ 450 msec.
- Contraception Requirements:
- Must comply with the following acceptable forms of contraception. All female of childbearing potential (FCBP) 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 Visits 1 and 2. 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 of the following additional barrier methods: (a) diaphragm with spermicide; (b) cervical cap with spermicide; or (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 any healthy subject from enrollment into the study:
- 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.
- Use of any prescribed systemic or topical medication within 30 days of the first dose administration.
- Use of any non-prescribed systemic or topical medication (including vitamin/mineral supplements, and herbal medicines) within 14 days of the first dos
Data sourced from ClinicalTrials.gov (NCT02641353). 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.