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GSK961081 for infusion

Phase 1

Pulmonary Disease, Chronic Obstructive | Small molecule | Respiratory |Theravance Biopharma, Inc.|Last Updated: Oct 6, 2021

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Trial Design

UNCONTROLLED
Total Trials1
Total Enrollment6

FDA Designations

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Clinical trial landscape

GSK961081 for infusion · 1 trial · 1 indication

Phase 1 1
NCT02663089A Phase 1 (Ph1), Single Dose (SD), GSK961081 Absorption, Distribution, Metabolism, and Excretion (ADME) Study in Healthy SubjectsPulmonary Disease, Chronic Obstructive
COMPLETED6 Analytics
PHASE1COMPLETED
A Phase 1 (Ph1), Single Dose (SD), GSK961081 Absorption, Distribution, Metabolism, and Excretion (ADME) Study in Healthy Subjects
Pulmonary Disease, Chronic ObstructiveUnlock trial analytics

Study Endpoints

Primary Endpoints

AUC(0 inf) of total drug-related material (radioactivity) in plasma after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose) and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25 , 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2

The following PK parameter will be measured: Area under the concentration-time curve from time zero (pre-dose) extrapolated to infinite time (AUC\[0 inf\])

AUC(0-t) of total drug-related material (radioactivity) in plasma after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose) and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2

The following PK parameter will be measured: Area under the concentration-time curve from time zero (pre-dose) to last time of quantifiable concentration (AUC\[0-t\]).

Cmax of total drug-related material (radioactivity) in plasma after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose) and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2

The following PK parameter will be measured: maximum observed plasma concentration (Cmax)

Tmax of total drug-related material (radioactivity) in plasma after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose) and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2

The following PK parameter will be measured: time of occurrence of Cmax (Tmax)

T1/2 of total drug-related material (radioactivity) in plasma after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose) and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2

The following PK parameter will be measured: terminal phase half-life (t1/2)

Volume of total radioactivity (drug related material) after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose)
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2
Clearance of total radioactivity (drug related material) after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose)
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2
Urinary and faecal cumulative excretion as a percentage of the total radioactive dose administered over time after a single IV microtracer of [14C] GSK961081 (concomitant with an inhaled non-radiolabelled dose) and a single oral dose of [14C] GSK961081
Pre-dose and at 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 hours post-dose during Treatment Period 1 and 2

Secondary Endpoints

AUC(0-inf) of parent GSK961081 and [14C] GSK961081 in plasma after a single IV microtracer of [14C]-GSK961081 concomitant with an inhaled non-radiolabelled GSK961081 dose and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2
AUC(0-t) of parent GSK961081 and [14C] GSK961081 in plasma after a single IV microtracer of [14C]-GSK961081 concomitant with an inhaled non-radiolabelled GSK961081 dose and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2
Cmax of parent GSK961081 and [14C] GSK961081 in plasma after a single IV microtracer of [14C]-GSK961081 concomitant with an inhaled non-radiolabelled GSK961081 dose and a single oral dose of [14C] GSK961081
Pre-dose and at 0.25, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96 and 168 hours post-dose during Treatment Period 1 and 2
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
[14C]-GSK961081 IV+GSK961081 inhalation; [14C]-GSK961081 oralEXPERIMENTALOn Day 1 of Treatment Period 1, after an overnight fast of at least 8 hours, each subject will receive \[14C\] GSK961081 4 micrograms (mcg) by IV infusion over 1 hour. Within 5 minutes after the start of infusion, subjects will take 1200 mcg non-radiolabelled GSK961081 by inhalation. After Treatment Period 1, there will be a washout of at least 2 weeks. On Day 1 of Treatment Period 2, after an overnight fast of at least 8 hours, each subject will take 200 mcg \[14C\]-GSK961081 as an oral solution.

Interventions

NameTypeDescription
[14C]-GSK961081 solution for IV infusionDRUGSubjects will receive 10 mL of solution equivalent to 4 mcg of \[14C\]-GSK961081 (approximately 6.2 kilobecquerel \[kBq\]) intravenously as a single dose over 1 hour.
[14C]-GSK961081 oral solutionDRUGSubjects will receive 10 mL of solution equivalent to 200 mcg of \[14C\]-GSK961081 (approximately 311 kBq) orally as a single dose with up to 250 mL of water.
GSK961081 dry powder for inhalationDRUGSubjects will receive single dose of 4 actuations of 300 mcg GSK961081 per actuation (1200 mcg GSK961081 total) as inhalation immediately after the start of infusion.
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Eligibility Criteria

Age Range30 Years to 55 Years
SexMALE
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Between 30 and 55 years of age inclusive, at the time of signing the informed consent. * Healthy as determined by the investigator or medically qualified designee based on a medical evaluation including medical history, physical examination, vital signs, laboratory tests, and ...

Countries:United Kingdom
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Frequently asked questions about GSK961081 for infusion

What is GSK961081 for infusion?

GSK961081 for infusion is an investigational small molecule being developed by Theravance Biopharma, Inc. (TBPH) for the treatment of chronic obstructive pulmonary disease (COPD). It is currently in Phase 1 clinical development, meaning it is still being studied in early-stage trials and is not yet approved for any use.

What is GSK961081 for infusion used for in chronic obstructive pulmonary disease?

GSK961081 for infusion is being studied for use in chronic obstructive pulmonary disease (COPD). It is an investigational small molecule in Phase 1 development, intended to address this respiratory condition. As of now, it has not been approved by regulatory authorities, and its safety and efficacy are still being evaluated in clinical trials.

Who makes GSK961081 for infusion?

GSK961081 for infusion is being developed by Theravance Biopharma, Inc., a biopharmaceutical company traded under the ticker symbol TBPH. The drug is an investigational small molecule in Phase 1 clinical development for chronic obstructive pulmonary disease (COPD).

What phase is GSK961081 for infusion in?

GSK961081 for infusion is in Phase 1 clinical development. It is an investigational small molecule being studied for chronic obstructive pulmonary disease (COPD). The drug has completed one Phase 1 trial, but it remains in early-stage development and is not yet approved for commercial use.

What clinical trials is GSK961081 for infusion in?

GSK961081 for infusion has been studied in one completed Phase 1 clinical trial, identified as NCT02663089. This was a single-dose study in healthy male subjects aged 30 years and older, conducted in the United Kingdom, to evaluate the drug's absorption, distribution, metabolism, and excretion (ADME). The trial enrolled 6 participants.