This study will evaluate the bioavailability, palatability, safety and tolerability of entrectinib in healthy volunteers. Part 1 of the study will explore the performance of entrectinib multi-particle formulation. Part 2 will evaluate the effect of drug substance particle size on entrectinib bioavailability.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
31
Test formulation 1 (T1): Multi-particulate formulation 1: entrectinib film-coated mini-tablets
Test formulation 2 (T2): Multi-particulate formulation 2: entrectinib film-coated mini-tablets
Reference formulation (R): entrectinib hard capsules
Quotient Clinical Ltd, Clinical Research Unit
Nottingham, United Kingdom
Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC0-inf) of Entrectinib
Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)
AUC0-inf of Entrectinib Active Metabolite M5
Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)
Maximum Plasma Concentration (Cmax) of Entrectinib
Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)
Cmax of Entrectinib Active Metabolite M5
Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)
Percentage of Participants With Treatment-Emergent Adverse Events (TEAEs)
An adverse event (AE) is any untoward medical occurrence in a subject administered a pharmaceutical product and which does not necessarily have to have a causal relationship with the treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a pharmaceutical product, whether or not considered related to the pharmaceutical product. Preexisting conditions which worsen during a study are also considered as adverse events. Treatment-emergent adverse events (TEAEs) are AEs that were not present before the first dose of study drug or that were present before the first dose of study drug but worsened in intensity during exposure to study drug.
Time frame: From Day -1 to Day 5 of each periods (each period=7 days)
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Test formulation (T): entrectinib HPMC capsules