AC0058TA is a small molecule compound that potently, selectively and irreversibly inhibits Bruton's tyrosine kinase (BTK) phosphorylation and downstream signals, resulting in inhibition of inflammatory cytokine production in monocytes and inhibition of lymphocyte activation (predominantly B-cell activation) in the preclinical studies. The nonclinical program has demonstrated that AC0058TA has the potential to interfere with signaling functions mediated by tyrosine kinases and may be useful for controlling excessive or aberrant T- and B-cell activation in autoimmune diseases. As an investigational targeted therapy for RA and SLE, AC0058TA is expected to address the unmet need of this patient population, for whom there are currently no effected therapies and there is a great unmet medical need, AC0058TA may inhibit the key pathway which involves the disease process.
This is a 2-part, randomized, double-blind, placebo-controlled, single-dose-escalation (Part 1) and multiple-dose-escalation (Part 2) study to evaluate the safety, tolerability, PK, and PD of AC0058TA administered orally to healthy subjects. Part 1 of the study will also to evaluate the effect of food on the pharmacokinetics of a single oral dose of AC0058TA.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
56
50 mg AC0058TA 100 mg AC0058TA 200 mg AC0058TA 400 mg AC0058TA
Placebo capsules
Covance Clinical Development Services
Dallas, Texas, United States
Safety and tolerability of single and multiple oral doses of AC0058TA determined by adverse events
Frequency and severity of AEs and serious AEs
Time frame: within 6 days after single dose in part 1, within 14 days after last dose in part 2.
Plasma concentrations of single dose or multiple doses of AC0058TA
Maximum observed concentration (Cmax)
Time frame: within 6 days after single dose in part 1, within 14 days after last dose in part 2.
Time to maximum observed concentration (Tmax)
Time to maximum observed concentration (Tmax)
Time frame: within 6 days after single dose in part 1, within 14 days after last dose in part 2.
Area under the concentration-time curve (AUC)
Area under the concentration-time curve (AUC)
Time frame: within 6 days after single dose in part 1, within 14 days after last dose in part 2.
The effect of food on AUC of the single-oral-dose AC0058TA
Area under the concentration-time curve (AUC)
Time frame: within 6 days after single dose in part 1
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