Study Conducted to Further Understand the Elimination Pathways, Metabolite Profile and PK Profile of 14C-estetrol

NCT02720224 | Completed Phase 1 Results

• 2 other identifiers: MIT -Es0001-C1052014-000622-38
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

This study is being conducted to further understand the elimination pathways, metabolite profile and pharmacokinetic (PK) profile of carbon 14 labelled estetrol (\[14C\] estetrol).

Conditions

Contraception; Menopause

Outcome Measures

Primary Outcomes (2)

• Mass Balance of Total Radioactivity in Urine

  Amount excreted in urine (Ae\[urine\])

  From Day -1 prior study treatment intake to 312 hours post-dose

• Mass Balance of Total Radioactivity in Faeces:

  Amount excreted in faeces (Ae\[faeces\])

  From Day -1 prior study treatment intake to 312 hours post-dose

Secondary Outcomes (17)

• Maximum Concentration (Cmax) of Total Radioactivity in Plasma

  Predose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours post-dose

• Time to Maximum Concentration (Tmax) of Total Radioactivity in Plasma

  Predose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours post-dose

• Area Under the Curve From 0 Time to Last Measurable Concentration [AUC(0-last)] of Total Radioactivity in Plasma

  Predose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours post-dose

• The Elapsed Time (Tlag) of Total Radioactivity in Plasma

  Predose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours post-dose

• Cmax of Estetrol in Plasma

  Predose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours post-dose

Study Arms (1)

Estetrol

EXPERIMENTAL

A single oral dose of 15 mg carbon 14 labelled estetrol (\[14C\]-estetrol), containing approximately 2.8 MBq (76 µCi) 14C

Drug: Estetrol

Interventions

Estetrol DRUG

15 mg \[14C\]-estetrol containing approximately 2.8 MBq (76 μCi) 14C

Also known as: E4

Estetrol

Eligibility Criteria

• Age: 30 Years - 65 Years
• Sex: female
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy females of non-child bearing potential, i.e. surgically sterilised or post menopausal subjects. Postmenopausal status will be defined by an absence of menses for a minimum of 12 months and confirmed by a FSH result ≥30 IU/ml
• Negative pregnancy test at screening and Day -1
• to 65 years of age inclusive
• Body mass index between ≥18.0 and ≤30.0 kg/m2
• Must be willing and able to communicate and participate in the whole study
• Must provide written informed consent
• Must have regular bowel movements (i.e. average stool production of ≥1 and ≤3 stools per day)Must agree to use an adequate method of contraception

You may not qualify if:

• Participation in a clinical research study within the previous 3 months
• Subjects who are study site employees, or immediate family members of a study site or sponsor employee
• Subjects who have previously been enrolled in this study
• History of any drug or alcohol abuse in the past 2 years
• Regular alcohol consumption i.e. \>14 units per week (1 unit = ½ pint beer, 25 ml of 40% spirit or a 125 ml glass of wine)
• Current smokers and those who have smoked within the last 12 months. A breath carbon monoxide reading of greater than 10 ppm at screening
• Females who are pregnant or lactating
• 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 1999, shall participate in the study
• Subjects who do not have suitable veins for multiple venepunctures/cannulation as assessed at screening
• Clinically significant abnormal biochemistry, haematology or urinalysis as judged by the investigator
• Positive drugs of abuse test result
• Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results
• History or presence of clinically significant cardiovascular, renal, hepatic, chronic respiratory or gastrointestinal disease as judged by the investigator
• Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients
• Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hayfever is allowed unless it is active

Sponsors & Collaborators

• Estetra: lead
• Quotient Clinical: collaborator

Study Sites (1)

Quotient Clinical

Ruddington, Nottingham, NG11 6JS, United Kingdom

Location

MeSH Terms

Interventions

Estetrol

Intervention Hierarchy (Ancestors)

Estriol; Estrenes; Estranes; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Estradiol Congeners; Gonadal Steroid Hormones; Gonadal Hormones; Hormones; Hormones, Hormone Substitutes, and Hormone Antagonists

Results Point of Contact

• Title: Marie Mawet
• Organization: Estetra SPRL

mmawet@mithra.com

Study Officials

• Litza McKenzie, MBChB

  Quotient Clinical

  PRINCIPAL INVESTIGATOR

Publication Agreements

• PI is Sponsor Employee: No
• Restrictive Agreement: Yes

Study Design

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

Study Record Dates

• First Submitted: January 8, 2016
• First Posted: March 25, 2016
• Study Start: February 1, 2016
• Primary Completion: March 1, 2016
• Study Completion: April 1, 2016
• Last Updated: February 15, 2019
• Results First Posted: December 10, 2018

Record last verified: 2016-01

Data Sharing

• IPD Sharing: Will not share

Locations

GB (1)