NCT05667688

Brief Summary

This is a Phase 1b, parallel single-dose study to evaluate the pharmacokinetics (PK) and pharmacodynamics (PD) of Tinlarebant when administered as an oral dose to elderly healthy volunteers. This study will evaluate 2 dose levels in 2 cohorts comprising up to a total of 16 participants (8 per cohort). Dose levels will be evaluated in parallel.

Trial Health

87
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
15

participants targeted

Target at below P25 for phase_1

Timeline
Completed

Started Nov 2022

Shorter than P25 for phase_1

Geographic Reach
1 country

1 active site

Status
completed

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

First Submitted

Initial submission to the registry

November 15, 2022

Completed
13 days until next milestone

Study Start

First participant enrolled

November 28, 2022

Completed
1 month until next milestone

First Posted

Study publicly available on registry

December 28, 2022

Completed
7 days until next milestone

Primary Completion

Last participant's last visit for primary outcome

January 4, 2023

Completed
14 days until next milestone

Study Completion

Last participant's last visit for all outcomes

January 18, 2023

Completed
Last Updated

February 23, 2023

Status Verified

February 1, 2023

Enrollment Period

1 month

First QC Date

November 15, 2022

Last Update Submit

February 21, 2023

Conditions

Healthy VolunteerDry Age-related Macular Degeneration

Outcome Measures

Primary Outcomes (16)

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Area under the plasma concentration versus time curve from time 0 to the last time point with quantifiable concentration (AUC0-t)

    Up to 168 hours

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Area under the plasma concentration versus time curve from time 0 extrapolated to infinity (AUC0-inf)

    Up to 168 hours

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Maximum observed plasma concentration (Cmax)

    Up to 168 hours

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Time of maximum observed plasma concentration (Tmax)

    Up to 168 hours

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Apparent plasma terminal elimination half-life (t1/2)

    Up to 168 hours

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Terminal elimination rate constant (λz)

    Up to 168 hours

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Apparent total body clearance (CL/F)

    Up to 168 hours

  • To measure the pharmacokinetics (PK) of tinlarebant in plasma following a single oral dose in healthy volunteers aged 50-85.

    Apparent volume of distribution (Vz/F)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Time of minimal RPB4 levels post-dose (Tmin)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Maximal suppression to RBP4 expressed as minimum concentration of RBP4 (Cmin)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Maximal suppression to RBP4 expressed as percent (%) of baseline concentration of RBP4 (C%bmin)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Level of RBP4 at 12 hours as concentration (C12h)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Level of RBP4 at 12 hours as percent of baseline concentration (C%b12h)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Level of RBP4 at 24 hours as concentration (C24h)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Level of RBP4 at 24 hours as percent of baseline concentration (C%b24h)

    Up to 168 hours

  • To measure the concentrations of retinol-binding protein 4 (RBP4), a pharmacodynamic (PD) biomarker, in plasma following a single oral dose in healthy volunteers aged 50-85

    Half-life for recovery of RBP4 to baseline levels (PDt1/2)

    Up to 168 hours

Secondary Outcomes (16)

  • To investigate the systemic and ocular safety and tolerability of a single oral dose of tinlarebant in healthy adult volunteers aged 50-85.

    Up to 15 days

  • To investigate the systemic and ocular safety and tolerability of a single oral dose of tinlarebant in healthy adult volunteers aged 50-85.

    Up to 15 days

  • To investigate the systemic and ocular safety and tolerability of a single oral dose of tinlarebant in healthy adult volunteers aged 50-85.

    Up to 15 days

  • To investigate the systemic and ocular safety and tolerability of a single oral dose of tinlarebant in healthy adult volunteers aged 50-85.

    Up to 15 days

  • To investigate the systemic and ocular safety and tolerability of a single oral dose of tinlarebant in healthy adult volunteers aged 50-85.

    Up to 15 days

  • +11 more secondary outcomes

Other Outcomes (1)

  • To measure the concentration of retinol, a PD biomarker , in serum following a single oral dose of tinlarebant in healthy volunteers aged 50-85.

    Up to 168 hours

Study Arms (2)

Cohort 1: 5 mg, fasted

ACTIVE COMPARATOR

A single dose (5 mg) of tinlarebant will be administered to each study participant on study Day 1.

Drug: Tinlarebant (LBS-008)

Cohort 2: 10 mg, fasted

ACTIVE COMPARATOR

A single dose (10 mg) of tinlarebant will be administered to each study participant on study Day 1.

Drug: Tinlarebant (LBS-008)

Interventions

Tinlarebant (LBS-008)DRUG

A single dose of Tinlarebant (LBS-008) will be administered to each study participant on study Day 1.

Cohort 1: 5 mg, fastedCohort 2: 10 mg, fasted

Eligibility Criteria

Age50 Years - 85 Years
Sexall
Healthy VolunteersYes
Age GroupsAdult (18-64), Older Adult (65+)

You may qualify if:

  • Must have given written informed consent before any study-related activities are carried out and must be able to understand the full nature and purpose of the trial, including possible risks and adverse effects.

You may not qualify if:

  • The volunteer is considered by the Investigator to be in stable health
  • Presence of CS cardiovascular, pulmonary, hepatic, renal, haematologic, gastrointestinal, endocrine, immunologic, dermatologic, neurologic, oncologic, or psychiatric disease, or any other condition that, in the opinion of the Investigator, would jeopardise the safety of the participant or the validity of the study results.
  • Had a CS new illness within 1 month prior to the screening visit, with the exception of fully resolved gastrointestinal illness at least 14 days prior to the screening visit, fully resolved minor colds (e.g., only cold and flu-like symptoms) that occurred within 1 month prior to the screening visit, and fully resolved corona virus disease 2019 (COVID-19) infections if resolved at least 14 days prior to the screening visit and 30 days prior to confinement to the clinical facility.
  • A history of uncontrolled hypertension, coronary artery disease, or any other significant cardiovascular disease.
  • A history of uncontrolled diabetes. Volunteers with fully resolved gestational diabetes will be eligible to participate in the study.
  • A history of unexplained loss of consciousness, epilepsy or other seizure disorder, or cerebrovascular disease.

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Study Sites (1)

Nucleus Network

Melbourne, Australia

Location

Study Officials

  • Sam Francis

    Nucleus Network - Melbourne

    PRINCIPAL INVESTIGATOR

Study Design

Study Type
interventional
Phase
phase 1
Allocation
NON RANDOMIZED
Masking
NONE
Purpose
BASIC SCIENCE
Intervention Model
PARALLEL
Sponsor Type
INDUSTRY
Responsible Party
SPONSOR

Study Record Dates

First Submitted

November 15, 2022

First Posted

December 28, 2022

Study Start

November 28, 2022

Primary Completion

January 4, 2023

Study Completion

January 18, 2023

Last Updated

February 23, 2023

Record last verified: 2023-02

Data Sharing

IPD Sharing
Will not share

After completion of the study, data may be considered for reporting at a scientific meeting or for publication in a scientific journal. In these cases, the sponsor will be responsible for these activities and will work with the investigators to determine how the manuscript is written and edited, the number and order of authors, the publication to which it will be submitted, and any other related issues. The sponsor has final approval authority of all such issues. Data are the property of the sponsor and cannot be published without their prior authorization, but data and any publication thereof will not be unduly withheld.

Locations

AU(1)