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A Single Ascending Dose Trial Assessing Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ZP7570

Early Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Dual GLP-1/GLP-2 Receptor agonists
Registration Number
NCT03994549
Lead Sponsor
Zealand Pharma
Brief Summary

This is a randomized, double-blind, placebo-controlled, single ascending dose trial in healthy subjects, randomized to ZP7570 or placebo within each cohort.

Detailed Description

Sixty-four subjects are planned to be studied in eight cohorts in this first-in human trial. Eight subjects will be allocated to the to eight dose levels. The entire observation period comprise 28 days starting with a 96 hours in-house stay, where discharge is planned for Day 5, followed by five outpatient visits and an End of Trial Visit at Day 28. A blinded evaluation of each cohort will be performed by a Trial Safety Group to determine whether the trial will progress to the next dose level based on the stopping rules specified in protocol.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
64
Inclusion Criteria
  • Healthy male or female subject aged between 18 and 55 years, both inclusive.
  • Body Mass Index (BMI) between 18.5 and 28.0 kg/m^2, both inclusive
  • Body weight of at least 60 kg.
  • Heart rate after 5 minutes rest in supine position inside the range of 50-90 beats/min at screening
Exclusion Criteria
  • Any history of a disorder which in the investigator's opinion might jeopardize subjects safety, evaluation of results or compliance with the protocol.
  • History of gallbladder disease or cholecystectomy.
  • History of major depressive disorder or a Patient Health Questionnaire (PHQ-9) > 9 completed at screening, or a history of other severe psychiatric disorders (e.g. schizophrenia or bipolar disorder).
  • Any suicidal ideation of type 4 or 5 on the Columbia-Suicide Severity Rating Scale (C-SSRS) within 6 months prior to screening.
  • Clinically significant abnormal standard 12-lead ECG after 5 min resting in supine position at screening, including a QTcF > 450 ms (males) or QTcF > 470 ms (females), PR ≥ 220 ms and QRS ≥ 110 ms as evaluated by the investigator.
  • History of severe hypersensitivity to medicines or foods or history of severe medicinal/food induced anaphylactic reaction or contraindication to the use of Indocyanine Green (e.g. hypersensitivity to iodine).
  • Any clinically significant abnormal hematology, biochemistry, or urinalysis screening tests, as judged by the investigator.
  • TSH values outside of normal reference ranges of safety laboratory
  • Estimated glomerular filtration rate (eGFR) < 90 ml/min/1.73 m2, as defined by Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI).
  • Known or suspected hypersensitivity to IMP(s) or related products.
  • Systolic blood pressure < 90 mmHg or >139 mmHg and/or diastolic blood pressure < 50 mmHg or > 89 mmHg (one repeat test will be acceptable in case of suspected white-coat hypertension).
  • Symptoms of arterial hypotension
  • Women of childbearing potential who are not using a highly effective contraceptive method
  • Men with non-pregnant partner(s) of childbearing potential not willing to use male contraception (condom) in addition to a highly effective contraceptive method until 28 days after dosing
  • Men with pregnant partner not willing to use male contraception (condom) until 28 days after dosing, in order to avoid exposure of the embryo/fetus to seminal fluid

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
ZP7570Dual GLP-1/GLP-2 Receptor agonistsSingle subcutaneous injection
PlaceboDual GLP-1/GLP-2 Receptor agonistsSingle subcutaneous injection
Primary Outcome Measures
NameTimeMethod
Safety - Incidence of adverse events (AEs)From time zero to 28 days after dosing

The incidence, type and severity of adverse events (AEs)

Secondary Outcome Measures
NameTimeMethod
Pharmacokinetics - Area under the plasma concentration-time curve troughFrom time zero up to day 28

AUCτ, Area under the plasma concentration-time curve (AUC) from zero up to trough concentration.

Pharmacokinetics - Area under the plasma concentration-time curve infinityFrom time zero up to day 28

AUCinf, Area under the plasma concentration-time curve (AUC) from zero up to last concentration.

Pharmacokinetics - Area under the plasma concentration-time curve lastFrom time zero up to day 28

AUClast, Area under the plasma concentration-time curve (AUC) from zero up to last concentration

Pharmacokinetics - Maximum plasma concentrationFrom time zero to 28 days after dosing

Measured maximum plasma drug concentration after dosing, Cmax

Pharmacokinetics - Time to maximum plasma concentration (Tmax)From time zero to 28 days after dosing

Sampling time until reaching Cmax, Tmax

Pharmacokinetics - Half-life , t½From time zero to 28 days after dosing

Half-life of ZP7570, t½

Pharmacokinetics - Volume of distributionFrom time zero to 28 days after dosing

Apparent volume of distribution of ZP7570, Vz/f

Pharmacokinetics - Mean residence timeFrom time zero to 28 days after dosing

Mean residence time, MRT

Pharmacokinetics - Body clearanceFrom time zero to 28 days after dosing

Total body clearance, CL/f

Pharmacokinetics - Elimination rate constantFrom time zero to 28 days after dosing

Elimination rate constant, λz

Pharmacodynamics - Plasma glucose levelsTime Frame: 0-240 minutes

Plasma glucose levels included with the acetaminophen at specific timepoints relative to a Mixed Test Meal

Pharmacodynamics - Insulin concentrationsTime Frame: 0-240 minutes

Insulin concentrations included with the acetaminophen at specific timepoints relative to a Mixed Test Meal

Pharmacodynamics - Plasma acetaminophen concentration-time curvesTime Frame: 0-240 minutes

Plasma acetaminophen concentration-time curves following ingestion of acetaminophen

Pharmacodynamics - Maximum acetaminophen concentrationTime Frame: 0-240 minutes

Change from baseline acetaminophen to maximum acetaminophen

Pharmacodynamics - Time maximum acetaminophen concentrationTime Frame: 0-240 minutes

Time to maximum change in acetaminophen measure from baseline, Tmax

Safety - Safety lab, haematologyFrom time zero to 28 days after dosing

Changes in haematology parameters: Haematocrit, Haemoglobin, Erythrocytes, MCV, MCH, MCHC, platelets, Leucocytes, Neutrophile granulocytes (total count and relative), Lymphocytes (total count and relative), Monocytes (total count and relative), Eosinophile granulocytes (total count and relative), Basophile granulocytes (total count and relative)

Safety - Safety lab, clinical chemistryFrom time zero to 28 days after dosing

Changes in clinical chemistry parameters: Sodium, Potassium, Calcium, Creatinine, Urea, AST, ALT, gamma-GT, Uric acid, Total protein, Albumin, Total bilirubin, Creatine kinase, Alkaline phosphatase, LDH, Total cholesterol, LDL, HDL, Amylase, Triglycerides, Lipase

Safety - Safety lab, urinalysisFrom time zero to 28 days after dosing

Changes in urinalysis: Protein, Glucose Erythrocytes, Leucocytes, pH, ketones

Safety - Vital signs, blood pressureFrom time zero to 28 days after dosing

Changes in vital signs, blood pressure (in mmHG)

Safety - Vital signs, pulseFrom time zero to 28 days after dosing

Changes in pulse (beats per minute)

Safety - Physical examinationFrom time zero to 28 days after dosing

Changes in physical examination of body sections (head, chest and heart, abdomen, skin and mucosae, musculoskeletal system, nervous system, lymph node)

Safety - ECGFrom time zero to 28 days after dosing

Occurrence of ECG findings, Changes in ECG parameters (in ms). ECG components: Heart rate, PR, QRS, QT and QTcF.

Safety - Occurrence of Injection site reactionsFrom time zero to 28 days after dosing

Occurrence of injection site reactions

Safety - Immunogenicity: Occurrence of anti-drug antibodiesFrom time zero to 28 days after dosing

Occurrence of anti-drug antibodies

Trial Locations

Locations (1)

Profil Institut für Stoffwechselforschung GmbH

🇩🇪

Neuss, North Rhine-Westphalia, Germany

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