Clincosm LogoSign in Get a demo

A Pharmacokinetic Study of [14C]-GDC-0810 After Single Oral Administration in Healthy Female Participants

Sponsor
Genentech, Inc. (Industry)
Overall Status
Completed
CT.gov ID
NCT02802670
Collaborator
(none)
7
Enrollment
1
Location
1
Arm
1
Duration (Months)
6.9
Patients Per Site Per Month

Study Details

Study Description

Brief Summary

This is an open-label, non-randomized study to determine the excretion kinetics and mass balance of GDC-0810, and to determine metabolites present in blood, feces, and urine in healthy participants following a single 300-milligram (mg) oral dose of GDC-0810 containing approximately 100 microcuries of [14C] labeled GDC-0810 using conventional absorption, metabolism, and excretion (AME) methodology. The entire duration of the study is up to approximately 8 weeks.

Condition or Disease Intervention/Treatment Phase
Phase 1

Study Design

Study Type:
Interventional
Actual Enrollment :
7 participants
Allocation:
N/A
Intervention Model:
Single Group Assignment
Masking:
None (Open Label)
Primary Purpose:
Basic Science
Study Start Date :
May 1, 2016
Actual Primary Completion Date :
Jun 1, 2016
Actual Study Completion Date :
Jun 1, 2016

Arms and Interventions

Arm Intervention/Treatment
Experimental: GDC-0810

GDC-0810 300-mg dose administered as oral solution, containing approximately 100 microcuries of [14C]-labeled GDC-0810.

Drug: [14C]-GDC-0810
Participants will receive a single 300-mg dose of GDC-0810 containing approximately 100 microcuries of [14C]-labeled GDC-0810 on Day 1.
Other Names:
  • ARN-810; RO7056118

    		•

    Outcome Measures

    Primary Outcome Measures

    1. Cmax for [14C]-GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    2. Time to maximum concentration (Tmax) for GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    3. Tmax for [14C]-GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    4. Area under the Concentration-Time Curve (AUC) from Hour 0 to Last Measurable Concentration (AUC0-t) for GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    5. AUC0-t for [14C]-GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    6. AUC Extrapolated to Infinity (AUC0-inf) for GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    7. AUC0-inf for [14C]-GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    8. Apparent Terminal Rate Elimination Constant for GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hours post-dose on Day 1, Day 2 (24, 36 hours post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    9. Maximum Observed Concentration (Cmax) for GDC-0810 [Pre-dose [0 hour (hr)], 10, 30, 45 minutes (min), 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    10. Apparent Terminal Elimination Constant for [14C]-GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hours post-dose on Day 1, Day 2 (24, 36 hours post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    11. Apparent Terminal Elimination Half-Life (t1/2) for GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    12. t1/2 for [14C]-GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    13. Apparent Oral Clearance (CL/F) for GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    14. Apparent Volume of Distribution (Vz/F) for GDC-0810 [Pre-dose (0 hr), 10, 30, 45 mins, 1, 2, 3, 4, 6, 8, 12 hrs post-dose on Day 1, Day 2 (24, 36 hrs post-dose), Days 3, 4, 5, 6, and 7 post-dose]

    15. Amount of Total Radioactivity Excreted in Urine Over the Sampling Interval (Aeu) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 12 and 12 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 or until clinical discharge criteria met]

    16. Cumulative Aeu (Total Aeu) of [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 12 and 12 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 or until clinical discharge criteria met]

    17. Renal Clearance (CLR) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 12 and 12 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 or until clinical discharge criteria met]

    18. Percent of Total radioactivity Excreted in Urine Over Sampling (% Feu) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 12 and 12 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 or until clinical discharge criteria met]

    19. Cumulative % Feu (Total % Feu) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 12 and 12 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 or until clinical discharge criteria met]

    20. Amount of Total Radioactivity Excreted in Feces Over the Sampling Interval (Aef) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 post-dose or until clinical discharge criteria met]

    21. Cumulative Aef (Total Aef) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 post-dose or until clinical discharge criteria met]

    22. Percent of Total radioactivity Excreted in Feces Over Sampling (% Fef) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 post-dose or until clinical discharge criteria met]

    23. Cumulative % Fef (Total % Fef) for [14C]-GDC-0810 (Whenever Possible) [Pre-dose (0 hr), 0 to 24 hrs post-dose on Day 1, Days 2 (24 to 48 hrs), 3 (48 to 72 hrs), 4 (72 to 96 hrs), 5 (96 to 120 hrs), 6 (120 to 144 hrs) post-dose, and at 24-hr interval from Days 7-14 post-dose or until clinical discharge criteria met]

    Eligibility Criteria

    Criteria

    Ages Eligible for Study:
    18 Years to 65 Years
    Sexes Eligible for Study:
    Female
    Accepts Healthy Volunteers:
    Yes
    Inclusion Criteria:

    • Healthy participants with non-child bearing potential, non-pregnant, non-lactating and either post-menopausal or surgically sterile.

    • Negative pregnancy test result at Screening and at Day -1.

    • Body mass index of 18.5 to 29.9 kilogram per square meter.

    • Healthy condition documented with no clinically significant findings from laboratory evaluations, medical history, 12-lead electrocardiograms, and vital signs.

    Exclusion Criteria:

    • Significant history of metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastric, neurological, or psychiatric disorder.

    • History of significant hypersensitivity or allergy to any drug.

    • Uncontrolled hypothyroidism.

    • History or presence of clinically significant abnormal electrocardiogram.

    • History of venous thrombosis, endometrial disorders, thrombophilic condition, inflammatory bowel disease, chronic diarrhoea, active or latent tuberculosis, and Gilbert's syndrome.

    • Major surgical procedure or significant traumatic injury within 3 months prior to study participation.

    • Participation in more than one other radiolabeled investigational drug study within 12 months prior to Check-in (Day -1).

    • Exposure to significant radiation occuring within 12 months prior to Check-in (Day -1).

    • Any acute or chronic condition that would limit the participant's ability to participate in the clinical study.

    • Failure to satisfy the Investigator of fitness to participate for any other reason.

    Contacts and Locations

    Locations

    Site City State Country Postal Code
    1 Madison Wisconsin United States 53704

    Sponsors and Collaborators

    • Genentech, Inc.

    Investigators

    • Study Director: Clinical Trials, Hoffmann-La Roche

    Study Documents (Full-Text)

    None provided.

    More Information

    Publications

    None provided.
    Responsible Party:
    Genentech, Inc.
    ClinicalTrials.gov Identifier:
    NCT02802670
    Other Study ID Numbers:
    • GP29916
    First Posted:
    Jun 16, 2016
    Last Update Posted:
    Jun 16, 2016
    Last Verified:
    Jun 1, 2016

    Study Results

    No Results Posted as of Jun 16, 2016