ClinicalTrials.Veeva

Menu

A Study to Examine the Effect of Tesofensine and Metoprolol on the 24-hour Mean Heart Rate

S

Saniona

Status and phase

Completed
Phase 1

Conditions

Phase 1

Treatments

Drug: Metoprolol Succinate 25 MG
Drug: Metoprolol Succinate 100 MG
Drug: Metoprolol Succinate 50 MG

Study type

Interventional

Funder types

Industry

Identifiers

Details and patient eligibility

About

A Phase 1 Study to Examine Pharmacodynamic Interaction Between Tesofensine and Metoprolol on 24-hours Mean Heart Rate

Full description

In this study, the dose-response relationship between tesofensine and metoprolol will be examined and thus the optimal dose of metoprolol to mitigate the effects of tesofensine on heart rate (HR) will be determined. HR is the primary endpoint because in the previous studies it has been shown to be the most affected safety endpoint by the effects of tesofensine.

After enrolment of 37 subjects, 2 Subjects (0115 and 0147) in dose cohort 2 experienced prolonged tachycardia (> 120 beats per minute (bpm) lasting for 30 min) documented in Holter Electrocardiogram (ECG) recording (a stopping criteria of the study). Therefore, the study was temporarily halted on 22 November 2018. Subsequent to the temporary halt, Saniona reviewed all the available data in January and February 2019 and determined that the results obtained from the completed participants were sufficiently robust to answer the questions for which the trial was designed. Therefore, Saniona decided to permanently end the trial on 20 February 2019.

Enrollment

37 patients

Sex

All

Ages

18 to 60 years old

Volunteers

Accepts Healthy Volunteers

Inclusion criteria

  1. Subject voluntarily agreed to participate in this study and signed an Independent Ethics Committee (IEC)-approved informed consent prior to performing any of the Screening procedures.
  2. Male and female subjects between 18 to 60 years of age, inclusive, at Screening.
  3. Overweight and obese subjects with a body mass index (BMI) between ≥ 27 and < 40 kg/m2 at Screening but otherwise healthy.
  4. Non-smokers (or other nicotine use) as determined by history (no nicotine use over the past 6 months) and by urine cotinine concentration (< 500 ng/mL) at Screening and admission.
  5. No clinically relevant deviation or finding in pre-study medical evaluation (medical history, physical examination, vital signs, 12-lead electrocardiogram (ECG) and clinical laboratory evaluations).
  6. Hemoglobin A1c (HbA1c) < 6.5% at Screening.
  7. Subject was willing to adhere to the contraception requirements details.

Exclusion criteria

  1. Subject had history or evidence of any clinically significant cardiovascular, gastrointestinal, endocrinologic, hematologic, hepatic, immunologic, metabolic (e.g., diabetes, metabolic acidosis), urologic, pulmonary (e.g., asthma or chronic obstructive pulmonary disease), neurologic, dermatologic, psychiatric, renal, and/or other major disease or malignancy as judged by the Investigator.

  2. Subject had any disorder that would interfere with the absorption, distribution, metabolism or excretion of drugs.

  3. Subject had a clinically significant abnormality following the Investigator's review of the physical examination, ECG and clinical study protocol (CSP)-defined clinical laboratory tests at Screening or admission to the clinical unit or had any concurrent disease or condition that, in the opinion of the Investigator, would make the subject unsuitable for participation in the clinical study. One re-test was allowed, if (a) test result(s) was outside the limits.

  4. History or presence of liver disease or liver injury, as indicated by abnormal liver function tests including:

    • Aspartate aminotransferase (AST) > 1.2 x upper limit of normal (ULN)
    • Alanine aminotransferase (ALT) > 1.1 x upper limit of normal (ULN)
  5. Subject had a pulse < 50 or > 90 beats per minute (bpm); systolic blood pressure (SBP) < 90 mmHg or > 140 mmHg; diastolic blood pressure (DBP) < 50 mmHg or > 90 mmHg (using the mean of triplicate measurements) at Screening or admission. One re-test was allowed, if (a) test result(s) was outside these limits.

  6. History of any clinically significant cardiac arrhythmia. Subject had a corrected QT interval using Fridericia's formula (QTcF) interval > 450 msec or 2nd or 3rd degree atrioventricular (AV) block, high-grade sinoatrial block or PQ interval > 0.24 seconds at Screening (using the mean of triplicate measurements). If a mean ECG parameter of a triplicate ECG exceeded the limits above, an additional triplicate ECG could have been taken. If this also gave an abnormal result, the subject was excluded. Also, the following cardiac conditions led to exclusion of the subjects: Untreated heart failure (pulmonary oedema, impaired blood flow or hypotension) and continuous or intermittent treatment leading to an increased contractility of the heart muscle (beta-receptor agonism); sick sinus syndrome; cardiogenic shock; severe peripheral arterial circulatory disturbances.

  7. Had a creatinine value exceeding the ULN.

  8. Subject had a positive test for hepatitis B surface antigen (HBsAg), or hepatitis B core antibody (indicative of active hepatitis B), hepatitis A virus antibodies (immunoglobulin M), hepatitis C virus (HCV) antibodies or human immunodeficiency virus (HIV) type 1 and/or type 2 antibodies.

  9. Use of any prescribed or non-prescribed drugs (including vitamins, natural and herbal remedies, e.g., St. John's Wort) in the 2 weeks prior to admission or 5 half-lives of the drug, whichever was longer, except for the occasional use of paracetamol (up to 2 g/day) or other non-steroidal anti-inflammatory drugs (NSAIDs) and hormonal contraception for female subjects.

  10. Subject had history of alcohol and/or illicit drug abuse within 2 years of entry.

  11. Subject had positive urine drug test (e.g., cocaine, amphetamines, barbiturates, opiates, benzodiazepines, cannabinoids) or alcohol test at Screening or at admission.

  12. History of drinking > 168 g (males) and > 84 g (females) pure alcohol per week (10 g pure alcohol = 259 mL of beer [5%] or 35 mL of spirits [35%] or 100 mL of wine [12%] within 3 months prior to admission to the clinical unit.

  13. Subject consumed more than 600 mg caffeine per day (e.g., more than 3 cups of coffee containing 200 mg caffeine per cup) within the 4 weeks before admission or the subject was unwilling to avoid consumption of coffee and caffeine-containing beverages within 48 hours prior to admission until discharge from the clinical unit.

  14. Subject was unwilling to avoid use of alcohol or alcohol-containing foods, medications or beverages, within 48 hours prior to Screening and from admission until discharge from the clinical unit.

  15. Any significant blood loss, donated 1 unit (450 mL) of blood or more, or received a transfusion of any blood or blood products within 60 days, or donated plasma within 7 days prior to the admission to the clinical unit.

  16. Participation in any clinical study within 3 months or 5 half-lives of the drug, whichever was longer, prior to the expected date of IMP administration, or participation in more than 3 clinical studies within 12 months.

  17. Subject with a relevant history or with a present psychiatric disorder, including depression, suicidal ideation, or eating disorders (e.g., bulimia or anorexia nervosa). Subjects with a medical history of relevant psychiatric disorders or known and relevant family history or evidence of anxiety disorders or depression as judged by the Investigator using the Generalized Anxiety Disorder Assessment-7 (GAD-7) and Patient Health Questionnaire-9 (PHQ-9) at Screening. Any of the following led to exclusion of the subject:

    • Subject had a GAD-7 mood scale score ≥ 10.
    • Subject had a score ≥ 10 on the PHQ-9 questionnaire.
    • Subject selected a response of "1, 2 or 3" to question number 9 on the PHQ-9 questionnaire regarding potential for suicidal thoughts or ideation (independent of the total score of the PHQ-9).
  18. Use of any agent used for weight loss within the last 3 months.

  19. More than 5% weight loss within the last 3 months.

  20. Hypo- or hyperthyroidism.

  21. Subject was pregnant or lactating.

  22. Subject was unwilling to abstain from vigorous exercise from 48 hours prior to admission until discharge.

  23. Subject had a history of hypersensitivity to the Investigational medicinal products (IMPs) or any of the excipients or to medicinal products with similar chemical structures.

  24. Any contraindication for metoprolol, e.g., severe peripheral arterial disease, untreated pheochromocytoma, concomitant intravenous administration of calcium antagonists of verapamil and diltiazem, due to the risk of hypotension, atrioventricular (AV) conduction disturbances, or left ventricular insufficiency.

  25. Subject had lactose intolerance or a rare hereditary problem of fructose intolerance, glucose galactose malabsorption or sucrase isomaltase insufficiency.

  26. Subject was unable to understand and communicate in German language or to understand the protocol requirements, instructions and study-related restrictions, the nature, scope and possible consequences of the clinical study or was unlikely to comply with the study requirements; e.g., uncooperative attitude and improbability of completing the clinical study.

  27. Subject had previously been enrolled in this clinical study.

  28. Vulnerable subjects defined as individuals whose willingness to volunteer in a clinical study may be unduly influenced by the expectation, whether justified or not, of benefits associated with participation, or of a retaliatory response from senior members of a hierarchy in case of refusal to participate (e.g., persons in detention, minors and those incapable of giving consent).

  29. Subject was the Investigator or any Sub-Investigator, research assistant, pharmacist, study coordinator, other staff or relative thereof directly involved in the conduct of the study or employee of the Sponsor or Parexel.

  30. Poor or ultra-rapid cytochrome P450 2D6 (CYP2D6) metabolizer.

Trial design

Primary purpose

Treatment

Allocation

Randomized

Interventional model

Crossover Assignment

Masking

Triple Blind

37 participants in 3 patient groups

Cohort 1 (Tesofensine 0.25mg)
Experimental group
Description:
Tesofensine 0.25 mg once daily for 23 days (loading dose of 1.0 mg for the first 3 days), plus a single dose of 25 mg, 50 mg or 100 mg metoprolol extended release (ER) in random order on Day 15, Day 18 and Day 21, respectively.
Treatment:
Drug: Metoprolol Succinate 25 MG
Drug: Metoprolol Succinate 50 MG
Drug: Metoprolol Succinate 100 MG
Cohort 2 (Tesofensine 0.50mg)
Experimental group
Description:
Tesofensine 0.50 mg once daily for 23 days (loading dose of 2.0 mg for the first 3 days), plus a single dose of 25 mg, 50 mg or 100 mg metoprolol extended release (ER) in random order on Day 15, Day 18 and Day 21, respectively.
Treatment:
Drug: Metoprolol Succinate 25 MG
Drug: Metoprolol Succinate 50 MG
Drug: Metoprolol Succinate 100 MG
Cohort 3 (Tesofensine 0.75mg)
Experimental group
Description:
Tesofensine 0.75 mg (0.25 mg + 0.50 mg) once daily for 23 days (loading dose of 2.0 mg \[4 tablets of 0.50 mg\] for the first 5 days), plus a single dose of 25 mg, 50 mg or 100 mg metoprolol extended release (ER) in random order on Day 15, Day 18 and Day 21, respectively.
Treatment:
Drug: Metoprolol Succinate 25 MG
Drug: Metoprolol Succinate 50 MG
Drug: Metoprolol Succinate 100 MG

Trial documents
2

Trial contacts and locations

1

Loading...

Data sourced from clinicaltrials.gov

Clinical trials

Find clinical trialsTrials by location
© Copyright 2025 Veeva Systems