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First-in-Human Study of BCX9930 in Healthy Volunteers and Patients With PNH

Phase 1
Completed
Conditions
Paroxysmal Nocturnal Hemoglobinuria
Interventions
Drug: Placebo
Registration Number
NCT04330534
Lead Sponsor
BioCryst Pharmaceuticals
Brief Summary

This is a 3-part Phase 1 dose-ranging study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of single (Part 1) and multiple (Part 2) ascending doses of BCX9930 in healthy subjects and in subjects with paroxysmal nocturnal hemoglobinuria (PNH; Part 3). Pharmacokinetics is an analysis of how the body handles the study drug BCX9930 and pharmacodynamics is an analysis of the activity that the study drug BCX9930 may have in the body.

Detailed Description

Up to 6 sequential ascending dose cohorts are planned to be dosed in a sequential manner in Part 1 of the study. Eight subjects will be treated with a single dose of the study drug per dose cohort (6 subjects per cohort will receive BCX9930 and 2 subjects per cohort will receive matching placebo). Escalation to the next higher dose level will occur only after completion of a review of clinical safety and pharmacokinetics by the Sponsor and PI.

Up to 7 ascending, multiple dose cohorts will be enrolled in a sequential manner in Part 2 of the study. In Cohorts 1 through 3, twelve subjects will be treated with either a 7-day or 14-day course of study drug (10 subjects per cohort will receive BCX9930 and 2 subjects per cohort will receive matching placebo) administered orally. In Cohorts 4 through 7, twelve subjects will be treated with a 3-day course of study drug (10 subjects per cohort will receive BCX9930 and 2 subjects per cohort will receive matching placebo) administered orally. The daily dose may be split into 2 times daily (BID) or 3 times daily (TID) dosing for the multiple ascending dose part as needed. Escalation to the next higher dose level in Part 2 will occur only after completion of a review of clinical safety and pharmacokinetics by the Sponsor and PI.

Part 3 of the study consists of up to 2 sequential ascending multiple dose cohorts of up to 8 subjects; each cohort may enroll up to 4 subjects with PNH who are naïve to both eculizumab and ravulizumab and up to 4 subjects with PNH who are currently being treated with either eculizumab or ravulizumab. In each cohort, subjects will receive one daily dose of BCX9930 on Days 1 to 14 and a higher daily dose on Days 15 to 28. Cohort 2 will start after independent data monitoring committee (DMC) review of Cohort 1 data and communication of their evaluation to Part 3 investigators. In South Africa, subjects that have clinical benefit from BCX9930 will be allowed to continue dosing for up to 48 weeks.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
168
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
BCX9930BCX9930Parts 1, 2 and 3
PlaceboPlaceboParts 1 and 2 only
Primary Outcome Measures
NameTimeMethod
Change from baseline in temperaturePart 3: Day 44 or Week 50 (South Africa only)
Change from baseline in respiratory ratePart 3: Day 44 or Week 50 (South Africa only)
Change in Electrocardiogram (PR interval)Part 3: Day 44 or Week 50 (South Africa only)
Change in Electrocardiogram (QRS interval)Part 3: Day 44 or Week 50 (South Africa only)
Incidence of graded treatment-emergent adverse eventsPart 3:Day 44 or Week 50 (South Africa only)
Incidence of graded urinalysis abnormalitiesPart 3: Day 44 or Week 50 (South Africa only)
Change from baseline in heart ratePart 3: Day 44 or Week 50 (South Africa only)
Incidence of graded laboratory chemistry abnormalitiesPart 3:Day 44 or Week 50 (South Africa only)
Incidence of graded coagulation abnormalitiesPart 3: Day 44 or Week 50 (South Africa only)
Incidence of graded hematology abnormalitiesPart 3: Day 44 or Week 50 (South Africa only)
Change from baseline in blood pressurePart 3: Day 44 or Week 50 (South Africa only)
Change in Electrocardiogram (RR interval)Part 3:Day 44 or Week 50 (South Africa only)
Change in Electrocardiogram (QT interval)Part 3:Day 44 or Week 50 (South Africa only)
Secondary Outcome Measures
NameTimeMethod
Plasma BCX9930 AUCinfplasma PK parameters are based on blood sampling through Day 4 for Part 1
Plasma BCX9930 Cmaxplasma PK parameters are based on blood sampling through Day 4 for Part 1; through Day 6, 14 or 18 for Part 2 (Day depends on dosing duration); and through Day 28 for Part 3
Plasma BCX9930 Tmaxplasma PK parameters are based on blood sampling through Day 4 for Part 1; through Day 6, 14 or 18 for Part 2 (Day depends on dosing duration); and through Day 28 for Part 3
Plasma BCX9930 t1/2plasma PK parameters are based on blood sampling through Day 4 for Part 1; through Day 6, 14 or 18 for Part 2 (Day depends on dosing duration); and through Day 28 for Part 3
Plasma BCX9930 AUCtauplasma PK parameters are based on blood sampling through Day 6, 14 or 18 for Part 2 (Day depends on dosing duration); and through Day 28 for Part 3
Serum AP complement activityPart 1:through Study Day 4; through Day 6, 14 or 18 for Part 2 (Day depends on dosing duration); and Part 3 through Day 28 or Week 48 (South Africa only)
Plasma Factor BbPart 1:through Study Day 4; through Day 6, 14 or 18 for Part 2 (Day depends on dosing duration); and Part 3 through Day 28 or Week 48 (South Africa only)
Number of blood transfusionsPart 3:baseline through Day 28 or Week 50 (South Africa only)
Lactate dehydrogenasePart 3: absolute and change from baseline through Day 28 or Week 50 (South Africa only)
HemoglobinPart 3: absolute and change from baseline through Day 28 or Week 50 (South Africa only)
Absolute reticulocyte countPart 3: values and change from baseline through Day 28 or Week 50 (South Africa only)
HaptoglobinPart 3: absolute and change from baseline through Day 28 or Week 50 (South Africa only)

Trial Locations

Locations (1)

Study Site

🇬🇧

London, United Kingdom

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