Recent Updates
Recently added Catalysts

GSK1144814

Phase 1

Schizophrenia | Small molecule | Psychiatry |GSK plc|Last Updated: Jul 7, 2017

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
Premium
Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
Premium
Trial Design
RandomizedCONTROLLEDBiomarker
Total Trials3
Total Enrollment78
FDA Designations
No designations recorded
Clinical Trials (3)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT01090440Pharmacokinetics, Effect of Food, Safety and Tolerability of a New Tablet Formulation of GSK1144814 in Healthy SubjectsPHASE1 COMPLETED 16Sep 1, 2009Oct 9, 2009Jun 22, 20171 Australia
NCT01209039A Repeat Dose Positron Emission Tomography Study With GSK1144814PHASE1 COMPLETED 41Jul 1, 2009Oct 25, 2009Jun 20, 20172 United Kingdom
NCT01381419First Time in Human Study (FTIH) With Positron Emission Tomography (PET)PHASE1 COMPLETED 21Oct 20, 2008Apr 1, 2009Jul 7, 20171 United Kingdom
Unlock Drug Trial Details
Study Endpoints
Primary Endpoints
Pharmacokinetics: tlag, Cmax, tmax, AUC(0-24), AUC(0 t), t½ and AUC(0 to infinity).
2 months
PET receptor occupancy
1 week
To assess the safety and tolerability by reviewing the number of subjects with adverse events, a review of laboratory samples and a review of vitals.
2 or 4 weeks
To review pharmacokinetic data
2 or 4 weeks
Safety and tolerability: Adverse event monitoring, vital signs (blood pressure, heart rate, respiratory rate, oral body temperature, ECGs (12 lead and Holter), clinical laboratory assessments (standard laboratory parameters).
2 months
Pharmacokinetics: time-point immediately prior to the first quantifiable plasma concentration (tlag), Cmax, time of occurrence of Cmax (tmax), AUC from time zero (pre dose) to the time of the last quantifiable concentration (AUC0-infinity),
72 hours
Volume of distribution (VT) of [11C] GR205171 in the brain at Baseline and following oral doses of GSK1144814.
7 days
NK1 receptor occupancy in the brain at Baseline and following oral doses of GSK1144814.
7 days
Secondary Endpoints
Safety and tolerability: AE monitoring, vital signs (blood pressure, heart rate, body temperature, electrocardiograms (ECGs) (12 lead and Holter), clinical laboratory assessments (standard laboratory parameters).
2 months
To assess potential induction of CYP3A4
up to 4 weeks
Unlock Study Endpoints
Study Design & Arms
AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
Three-way cross- overEXPERIMENTALThree regimens will be administered in this study: A: GSK1144814 Tablet (100mg) Fasted State; B: GSK1144814 Tablet (200mg) Fasted State and C: GSK 1144814 Tablet (100mg) Fed State (FDA high fat breakfast).
Part A, cohort 1 and 2EXPERIMENTALPart A, Cohorts 1 and 2, will investigate escalating multiple daily doses of GSK1144814 in 19 subjects
Part A, cohort 3EXPERIMENTALCohort 3 will investigate safety, tolerability and PK of a dose of GSK1144814 over a repeat treatment period of 28 days in 18 subjects and a potential drug drug interaction between GSK1144814 and the CYP3A4 sensitive substrate midazolam (in 15 subjects).
Part BEXPERIMENTALPart B will assess NK1 receptor occupancy following repeated administration of GSK1144814 given once daily until steady state is obtained
Part A, Cohort 1EXPERIMENTALIn Cohort 1, four subjects (two on active and two on placebo for first dose, and then three on active and one on placebo for subsequent doses) will be included. Subjects will be dosed at least 30 minutes apart over the dosing day and only doses administered where the predicted plasma concentration will remain below those corresponding to the MABEL.
Part A, cohort 2EXPERIMENTALIn Cohort 2, 10 subjects will be included (8 active : 2 placebo). Dosing will start once the previous cohort (Cohort 1) has completed the Treatment Phase. For Cohort 2 and any subsequent cohorts, dosing will take place on two different days when a new dose is administered such that no more than one subject receives the agreed ascending dose on the first dosing day. Doses may be split in up to three divided doses given 2 to 3 hours apart. Dosing for the first four sessions in each cohort will be staggered over 2 days. On the first day of each dosing session, only one subject will receive the highest dose for that dosing session and at least one subject each will receive placebo. The remaining subjects in the cohort will be dosed on the second day according to the randomisation plan.
Interventions
NameTypeDescription
GSK1144814DRUGThis study is an open label, randomised, three-way cross-over study to evaluate the pharmacokinetics, effect of food, safety and tolerability of a new tablet formulation of GSK1144814 in healthy male and female (non-child bearing potential) subjects. Sixteen subjects will be enrolled to provide a minimum number of 12 evaluable subjects. The doses to be administered will be 100 mg and 200mg in the fasted state, and 100mg following a high fat breakfast.
Unlock Study Design Details
Eligibility Criteria
Age Range18 Years — 65 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * 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 clinically significant abnormality or laboratory parameters significantly outside the refe...

Countries:AustraliaUnited Kingdom
Unlock Eligibility Criteria