RP3128 is a calcium release activated calcium (CRAC) channel modulator. The purpose of this study is to evaluate the safety, tolerability and pharmacokinetics of single and multiple ascending dose(s) of RP3128 in healthy volunteers and to evaluate the effect on late phase asthmatic response to allergen challenge in patients with mild asthma.
The study consists of three parts; Part 1: single ascending dose (SAD), Part 2: multiple ascending dose (MAD) in healthy volunteers and Part 3: proof of concept (POC) study in mild asthmatics. There will be 5 cohorts in SAD and 3 cohorts in MAD, the doses used in the MAD will be based on emerging safety, tolerability and pharmacokinetics (PK) from Part 1 (SAD). POC is a randomized, placebo- controlled, double blind, two period cross-over, proof of concept study in male and female of non child bearing potential with history of mild asthma. the highest identified dose of RP3128 in Part 2 (MAD) will be considered for POC
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
57
Inflamax Research Inc.
Mississauga, Ontario, Canada
Number of Participants With Adverse Events
Number of Participants With Abnormal Laboratory Values and/or Adverse Events That Are Related to Treatment
Time frame: Baseline through 2 weeks
Peak Plasma Concentration (Cmax)
Cmax after administration of RP3128/ placebo in part 1 and part 2
Time frame: Pre-dose through 48 hours post dose
Measurement of Cytokines
Levels of cytokines following LPS (lipopolysaccharide) or CD3/CD28 stimulation.
Time frame: Predose and Day 7 in Part 2
Fractional Exhaled Nitric Oxide (FeNo)
Change in FeNo after administration of RP3128/ placebo in part 3
Time frame: Prechallenge to 3, 8 and 24 hours post challenge in Part 3
Area Under Effective Concentration (AUEC)
AUEC0-3h, AUEC3-8h after administration of RP3128/ placebo in part 3
Time frame: 0 to 3 hours and 3 to 8 hours post allergen challenge in Part 3
Cell Count
Absolute and % counts of sputum eosinophils and neutrophils
Time frame: 8 and 24 hours post allergen challenge in Part 3
Area Under the Plasma-Concentration
AUC0-t after administration of RP3128/ placebo in part 1 and part 2
Time frame: Pre-dose through 48 hours post dose
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