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Safety, Tolerability, and Pharmacokinetics of XXB750 in Healthy Participants

Phase 1
Completed
Conditions
XXB750 in Healthy Participants
Interventions
Other: Placebo
Registration Number
NCT06558097
Lead Sponsor
Novartis Pharmaceuticals
Brief Summary

This study was a randomized, participant and investigator-blinded, placebo-controlled, single-ascending dose study, consisting of 9 sequential dose cohorts (1 mg, 3 mg, 10 mg, 30 mg, 60 mg, 120 mg, 240 mg, 450 mg and 600 mg) and a Japanese ethnic sensitivity cohort (240 mg dose)

Detailed Description

Eligible healthy participants with normal blood pressure (SBP: 110-139 mmHg; DBP: 70-89 mmHg) were randomized into dose cohorts 1 - 240 mg. Eligible healthy participants with elevated blood pressure (SBP: 139 - 159 mmHg; DBP: 75 - 95 mmHg) were randomized into dose cohorts 450 and 600 mg. Each participant received a subcutaneous single dose of either XXB750 or placebo. In total, the duration of the study was 151 days, including the full Screening period of up to 28 days, safety, pharmacokinetics and pharmacodynamics assessments over a period of 91 days, and a 30-day safety follow up call after the end of study visit.

Sentinel dosing will be applied in this FIH study at each new dose level to ensure participant's safety and minimize the number of participants that may experience symptomatic hypotension, especially for sustained periods of time attributing to the long acting nature of XXB750 and the sustained pharmacological effects on BP at higher doses. The 10-day safety monitoring for the sentinel cohort is considered sufficient based on the predicted mean Tmax (4.5 days) in humans.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
77
Inclusion Criteria
  • Healthy male and female participants age 18 to 50 years of age included, and in good health as determined by past medical history, physical examination, vital signs, electrocardiogram, and laboratory tests at screening.
  • Participants must weigh at least 50 kg to participate in the study, and must have a body mass index (BMI) within the range of 18 - 32 kg/m2. BMI = Body weight (kg) / [Height (m)]2
  • For ethnic Japanese cohort: participants must be defined as being of first, second or third generation ethnic origin, with each set of parents qualifying as Japanese under the prior generation.
Exclusion Criteria
  • Any surgical or medical condition which significantly altered the distribution, metabolism, or excretion of drugs, or which jeopardized the participant's participation in the study.
  • Known history or current clinically significant arrhythmias.
  • Women of child-bearing potential were excluded from this study.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
XXB750 s.c 3 mgXXB750Single SC dose of XXB750 3 mg
PlaceboPlaceboPlacebo to XXB750
XXB750 s.c 10 mgXXB750Single SC dose of XXB750 10 mg
XXB750 s.c 30 mgXXB750Single SC dose of XXB750 30 mg
XXB750 s.c 60 mgXXB750Single SC dose of XXB750 60 mg
XXB750 s.c 1 mgXXB750Single SC dose of XXB750 1 mg
XXB750 s.c 120 mgXXB750Single SC dose of XXB750 120 mg
XXB750 s.c 240 mgXXB750Single SC dose of XXB750 240 mg
XXB750 s.c 240 mg Japanese cohortXXB750Single SC dose of XXB750 240 mg in the Japanese cohort
Placebo for Japanese cohortPlaceboPlacebo to XXB750 in the Japanese cohort
XXB750 s.c 450 mg (HBP)XXB750Single SC dose of XXB750 450 mg (High Blood Pressure Cohort)
XXB750 s.c 600 mg (HBP)XXB750Single SC dose of XXB750 600 mg (High Blood Pressure Cohort)
Placebo to High Blood Pressure cohortPlaceboPlacebo to XXB750 in High Blood Pressure cohorts
Primary Outcome Measures
NameTimeMethod
Number of participants with Adverse EventsUp to 121 days

To evaluate the safety and tolerability of single ascending SC doses of XXB750 in healthy participants.

Adverse events may include abnormal vital signs, safety laboratory tests, physical exam tests and ECG parameters that include clinical signs or symptoms, are considered clinically significant or require therapy.

Secondary Outcome Measures
NameTimeMethod
Pharmacokinetics parameters: TmaxUp to 91 days

To evaluate the pharmacokinetics: Time to maximum concentation (Tmax) of XXB750 in healthy participants following a single SC dose of XXB750.

Pharmacokinetics parameters: Vz/FUp to 91 days

To evaluate the pharmacokinetics: Vd/F of XXB750 in healthy participants following a single SC dose of XXB750.

Pharmacokinetics parameters: CmaxUp to 91 days

To evaluate the pharmacokinetics: Peak plasma concentration (Cmax) of XXB750 in healthy participants following a single SC dose of XXB750.

Pharmacokinetics parameters: AUClastUp to 91 days

To evaluate the pharmacokinetics: Area under the plasma concentration curve (AUClast) of XXB750 in healthy participants following a single SC dose of XXB750.

Pharmacokinetics parameters: AUCinfUp to 91 days

To evaluate the pharmacokinetics: Area under the curve (AUCinf) of XXB750 in healthy participants following a single SC dose of XXB750.

Pharmacokinetics parameters: T1/2Up to 91 days

To evaluate the pharmacokinetics: Half-life (T1/2) of XXB750 in healthy participants following a single SC dose of XXB750.

Pharmacokinetics parameters: CL/FUp to 91 days

To evaluate the pharmacokinetics: Apparent clearance (CL/F) of XXB750 in healthy participants following a single SC dose of XXB750.

Trial Locations

Locations (1)

Novartis Investigative Site

🇺🇸

Cypress, California, United States

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