Mass Balance Study of [14C]-NT-814 Oral Suspension in Healthy Male Subjects

NCT04654897 | Completed Phase 1 FDA Drug

• 2 other identifiers: 216642020-002987-30
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

This is a single centre, open-label, non-randomised study to assess the mass balance recovery, absorption, metabolism, and excretion of a single oral dose of \[14C\]-NT-814 in healthy male subjects. It is planned to enrol 6 subjects. Each subject will receive a single dose of 120 mg \[14C\] NT-814 containing not more than (NMT) 5.6 megabecquerel (MBq) \[14C\], administered as an oral suspension in the fasted state. Subjects will remain in the study until a mass balance cumulative recovery of \>90% and \<1% of the dose administered has been collected in urine and faeces within 2 separate, consecutive 24 hour periods.

Conditions

Healthy

Outcome Measures

Primary Outcomes (6)

• Mass Balance Recovery of Total Radioactivity: CumAe(Urine)

  CumAe(Urine): cumulative amount of Total Radioactivity (TR) excreted in urine.

  Day 45 (maximum)

• Mass Balance Recovery of Total Radioactivity: Cum%Ae(Urine)

  Cum%Ae(Urine): cumulative amount of TR excreted in urine expressed as a percentage of the radioactive dose administered.

  Day 45 (maximum)

• Mass Balance Recovery of Total Radioactivity: CumAe(Faeces)

  CumAe(Faeces): cumulative amount of TR excreted in faeces.

  Day 45 (maximum)

• Mass Balance Recovery of Total Radioactivity: Cum%Ae(Faeces)

  Cum%Ae(Faeces): cumulative amount of TR excreted in faeces expressed as a percentage of the radioactive dose administered.

  Day 45 (maximum)

• Mass Balance Recovery of Total Radioactivity: CumAe(Total)

  CumAe(Total): cumulative amount of TR excreted in urine and faeces combined. The radioactivity associated with toilet tissue was also determined, and the results were reported for each subject as a single value for the whole collection period only and included in the calculation of total Ae and % of dose recovered. The data reported for total calculations excluded toilet tissue data for the 0 - 6 hours post-dose to 0 - 456 hours post-dose collection intervals and included toilet tissue data for the 0 - 480 hours post-dose collection interval.

  Day 45 (maximum)

• Mass Balance Recovery of Total Radioactivity: Cum%Ae(Total)

  Cum%Ae(Total): cumulative amount of TR excreted in urine and faeces combined expressed as a percentage of the radioactive dose administered. The radioactivity associated with toilet tissue was also determined, and the results were reported for each subject as a single value for the whole collection period only and included in the calculation of total Ae and % of dose recovered. The data reported for total calculations excluded toilet tissue data for the 0 - 6 hours post-dose to 0 - 456 hours post-dose collection intervals and included toilet tissue data for the 0 - 480 hours post-dose collection interval.

  Day 45 (maximum)

Secondary Outcomes (22)

• AUC(0-tlast) of NT-814 (in plasma)

  Day 45 (maximum)

• AUC(0-tlast) of Total Radioactivity (in plasma and whole blood)

  Day 45 (maximum)

• Cmax of NT-814 (in plasma)

  Day 45 (maximum)

• Cmax of Total Radioactivity (in plasma and whole blood)

  Day 45 (maximum)

• Ae(urine) by interval

  Day 45 (maximum)

Study Arms (1)

Elinzanetant (NT-814, BAY3427080)

EXPERIMENTAL

Subjects received a single dose of 120 mg radioactive labeled elinzanetant (\[14C\]-NT-814) orally.

Drug: [14C]-NT-814

Interventions

[14C]-NT-814 DRUG

120 mg radioactive labeled elinzanetant (\[14C\]-NT-814) oral suspension containing NMT (not more than) 5.6 MBq (megabecquerel) \[14C\].

Elinzanetant (NT-814, BAY3427080)

Eligibility Criteria

• Age: 30 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy males
• Aged 30 to 65 years inclusive at the time of signing informed consent.
• Body mass index (BMI) of 18.0 to 35.0 kg/m\^2, inclusive, as measured at screening.
• Must be able to understand the requirement of the study and be willing to participate in the whole study.
• Must have regular bowel movements (i.e., usual stool production of ≥1 and ≤3 stools per day).
• Must provide written informed consent.
• Must agree to adhere to the contraception requirements

You may not qualify if:

• Subjects who have received any IMP in a clinical research study within the 90 days prior to Day 1.
• Subjects who are, or are immediate family members of, a study site or Sponsor employee.
• Evidence of current SARS-CoV-2 infection.
• History of any drug or alcohol abuse in the past 2 years.
• Regular alcohol consumption \>21 units per week (1 unit = ½ pint beer, or a 25 mL shot of 40% spirit, 1.5 to 2 Units = 125 mL glass of wine, depending on type).
• A confirmed positive alcohol breath test at screening or admission.
• Current smokers and those who have smoked within the last 12 months.
• A confirmed breath carbon monoxide reading of greater than 10 ppm at screening or admission.
• Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months.
• Subjects with pregnant or lactating partners.
• Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 2017 \[7\], shall participate in the study.
• Subjects who do not have suitable veins for multiple venepunctures/cannulation as assessed by the Investigator or delegate at screening.
• Clinically significant abnormal clinical chemistry, haematology or urinalysis as judged by the Investigator.
• Subjects with biochemically verified Gilbert's Syndrome are allowed.
• Subjects with a presence of any of the following at screening, confirmed by a repeat test: AST, alanine aminotransferase or, gamma glutamyl transferase above the upper limit of normal.

Sponsors & Collaborators

• Bayer: lead
• Quotient Sciences: collaborator

Study Sites (1)

Quotient Sciences

Ruddington, Nottingham, NG11 6JS, United Kingdom

Location

Related Publications (1)

• Schulz SI, Schultze-Mosgau MH, Engelen A, Singh N, Pawsey S, Francke K, Lock R, Rottmann A. Mass Balance Recovery, Absorption, Metabolism, and Excretion of Elinzanetant in Healthy Human Volunteers and in vitro Biotransformation. Eur J Drug Metab Pharmacokinet. 2025 Jan;50(1):91-103. doi: 10.1007/s13318-024-00930-3. Epub 2024 Dec 24.

  PMID: 39719488 DERIVED

Related Links

• Click here to find information about studies related to Bayer Healthcare products conducted in Europe.

Study Officials

• Prinicipal Investigator

  Quotient Sciences

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Open Label, single dose

Study Record Dates

• First Submitted: November 25, 2020
• First Posted: December 4, 2020
• Study Start: September 30, 2020
• Primary Completion: October 29, 2020
• Study Completion: October 29, 2020
• Last Updated: October 28, 2021

Record last verified: 2021-10

Data Sharing

• IPD Sharing: Will not share

Locations

GB (1)