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GSK1360707 is a potent re-uptake inhibitor of the neurotransmitters dopamine, norepinephrine and serotonin

Phase 1

Depressive Disorder | Small molecule | Psychiatry |GSK plc|Last Updated: Jun 27, 2017

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLED
Total Trials1
Total Enrollment12

FDA Designations

No designations recorded

Clinical trial landscape

GSK1360707 is a potent re-uptake inhibitor of the neurotransmitters dopamine, norepinephrine and serotonin · 1 trial · 1 indication

Phase 1 1
NCT01153802An Open Label Positron Emission Tomography Study in Healthy Male Subjects to Investigate Brain DAT and SERT Occupancy,Pharmacokinetics and Safety of Single Oral Doses of GSK1360707, Using 11C- PE2I and 11C-DASB as PET LigandsDepressive Disorder
COMPLETED12 Analytics
PHASE1COMPLETED
An Open Label Positron Emission Tomography Study in Healthy Male Subjects to Investigate Brain DAT and SERT Occupancy,Pharmacokinetics and Safety of Single Oral Doses of GSK1360707, Using 11C- PE2I and 11C-DASB as PET Ligands
Depressive DisorderUnlock trial analytics

Study Endpoints

Primary Endpoints

To estimate the degree of DAT occupancy in brain regions of interest (ROIs)following oral doses of GSK1360707 in healthy male subjects-To estimate the degree of SERT occupancy in brain ROIs following total oral doses of GSK1360707 in healthy male subject
6-7 weeks.
To evaluate the relationship between the plasma concentration and the resultant DAT occupancy by GSK1360707.To evaluate the relationship between the plasma concentration and the resultant SERT occupancy by GSK1360707.
6 - 7 weeks

Secondary Endpoints

To further assess the safety and tolerability of total oral doses of GSK1360707 including the maximal tolerated dose in the FTIH study (150 mg PO)-To further assess the pharmacokinetics of GSK1360707 in healthy male subjects
6-7 weeks.
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Healthy Male VolunteersEXPERIMENTALAll the 12 subjects enrolled in the study were exposed to at least one dose of GSK1360707 15 mg, 30 mg, 60 mg, 90 mg, 120 mg and 150 mg. All the subjects completed the study. The initial dose, given in the study as a single-dose was 15 mg GSK1360707. The remaining subjects were dosed either as a single or split dose, as determined by the PET and tolerability data collected in the preceding subjects. The total dose did not exceed 150 mg per day, the maximum total dose given in the FTIH study.

Interventions

NameTypeDescription
GSK1360707 is a potent re-uptake inhibitor of the neurotransmitters dopamine, norepinephrine and serotoninDRUGThis is an open label, adaptive design, daily dosing, non-randomized PET occupancy study in healthy adult males.A range of doses may be evaluated. The initial dose, given in the study as a single dose was 150mg GSK1360707. The remaining subjects will be dosed either as a single or split dose, as determined by the PET and tolerability data collected in the preceding subjects. The total dose will not exceed 150mg per day, the maximum total dose given in the FTIH study.If dosing is conducted as a single dose, the dose will be administered after the baseline scan, If a dosing is performed in a split dose manner, dosing will occur after the baseline scan, and up to 12 hours later. The time period between doses will be determined by emerging PET occupancy data. Subsequent doses, if any, will be chosen based on the observed scan results. No single dose, or total dose split over 2 dosing sessions, will exceed the maximum dose in the FTIH study.
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Eligibility Criteria

Age Range35 Years to 55 Years
SexMALE
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * 1\. Healthy as determined by a responsible physician, based on a medical evaluation including medical history, physical examination, laboratory tests and cardiac monitoring. A subject with a clinical abnormality or laboratory parameters outside the reference range for the popu...

Countries:United Kingdom
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Frequently asked questions about GSK1360707 is a potent re-uptake inhibitor of the neurotransmitters dopamine, norepinephrine and serotonin

What is GSK1360707?

GSK1360707 is an investigational small molecule developed by GSK plc for depressive disorder. It acts as a re-uptake inhibitor of the neurotransmitters dopamine, norepinephrine and serotonin. It has been studied in a single Phase 1 clinical trial and is not approved for any indication.

What does GSK1360707 target?

GSK1360707 targets the re-uptake of three neurotransmitters: dopamine, norepinephrine and serotonin. By inhibiting their re-uptake, it is designed to increase the availability of these neurotransmitters. This mechanism is being explored in the context of depressive disorder.

Who is developing GSK1360707?

GSK1360707 is being developed by GSK plc, which trades under the ticker GSK. The company sponsored the Phase 1 trial of the drug.

What phase is GSK1360707 in?

GSK1360707 is in Phase 1 clinical development. One Phase 1 trial has been completed, and no active trials are currently listed. The drug remains investigational and has not been approved for any indication.

What clinical trials is GSK1360707 in?

GSK1360707 has been evaluated in one completed Phase 1 trial, NCT01153802. This open-label PET study enrolled 12 healthy male subjects in the United Kingdom to investigate brain DAT and SERT occupancy, pharmacokinetics and safety after single oral doses.