This study is a multicenter, Phase I, open-label, randomized, 2-sequence, 2-treatment, 2-period, crossover, bioequivalence study with single doses of acalabrutinib administered orally in healthy participants. The study is designed to demonstrate the bioequivalence of acalabrutinib tablet (Treatment A) compared with marketed acalabrutinib capsule (Treatment B) in the fasted state.
Eligible healthy participants will be randomized to receive either treatment sequence 1 (AB) or treatment sequence 2 (BA), as follows: * Treatment A: Acalabrutinib tablet, 100 mg, fasted state * Treatment B: Acalabrutinib capsule, 100 mg, fasted state Participants will receive fixed single doses of acalabrutinib on 2 occasions, under fasted conditions. The study will comprise: * Visit 1: A screening period of up to 28 days before first dosing. * Visit 2: Two treatment periods: * Participants will be admitted to the study center on Day -2 of Treatment Period 1 to confirm eligibility before first dosing. Eligibility criteria will be reconfirmed on Day -1 of each treatment period. * On Day 1 of Treatment Periods 1 and 2, participants will be administered the assigned treatment (A or B) as randomized, followed by a protocol defined washout period between Treatment Periods 1 and 2. * Visit 3: A Follow-up Visit/Early Termination Visit at 7 to 10 days after last administration of study drug. Each participant will be involved in the study for approximately 6 weeks.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
66
Participants will receive fixed single doses of acalabrutinib tablet in 2 treatment periods, under fasted conditions.
Participants will receive fixed single doses of acalabrutinib capsule in 2 treatment periods, under fasted conditions.
Research Site
Glendale, California, United States
Research Site
Brooklyn, Maryland, United States
Research Site
Salt Lake City, Utah, United States
Area under plasma concentration time curve from zero to infinity (AUCinf) of Acalabrutinib
To compare the AUCinf of acalabrutinib capsule with the tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Area under the plasma concentration time curve from zero to the last quantifiable concentration (AUClast) of Acalabrutinib
To compare the AUClast of acalabrutinib capsule with the tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Maximum observed plasma (peak) drug concentration (Cmax) of Acalabrutinib
To compare the Cmax of acalabrutinib capsule with the tablet
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Area under plasma concentration time curve from zero to infinity (AUCinf) of ACP-5862
To compare the AUCinf of acalabrutinib capsule with the tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Area under the plasma concentration time curve from zero to the last quantifiable concentration (AUClast) of ACP-5862
To compare the AUClast of acalabrutinib capsule with the tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Maximum observed plasma (peak) drug concentration (Cmax) of ACP-5862
To compare the Cmax of acalabrutinib capsule with the tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Time to reach peak or maximum concentration (tmax) following drug administration for acalabrutinib and ACP-5862
To compare the tmax of acalabrutinib capsule with the acalabrutinib tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Half life associated with terminal slope (λz) of a semi logarithmic concentration time curve (t½λz) for acalabrutinib and ACP-5862
To compare the t½λz of acalabrutinib capsule with the acalabrutinib tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Mean residence time of the unchanged drug in the systemic circulation from zero to infinity (MRT) for acalabrutinib and ACP-5862
To compare the MRT of acalabrutinib capsule with the acalabrutinib tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Terminal rate constant, estimated by log linear least squares regression of the terminal part of the concentration time curve (λz) for acalabrutinib and ACP-5862
To compare the λz of acalabrutinib capsule with the acalabrutinib tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Metabolite (ACP-5862) to parent (acalabrutinib) ratio based on AUCinf and/or AUClast (M:P[AUC])
To compare the M:P\[AUC\] of acalabrutinib capsule with the tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Metabolite (ACP-5862) to parent (acalabrutinib) ratio based on Cmax (M:P [Cmax])
To compare the M:P\[Cmax\] of acalabrutinib capsule with the tablet.
Time frame: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, and 48 hours post-dose
Number of participants with adverse events and serious adverse events
Comparison of the safety and tolerability of single doses of acalabrutinib capsule with the tablet.
Time frame: From screening day (Day -28) until Follow-up/end of treatment visit (at 7 to 10 days after last study drug administration)