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GSK2126458

Phase 1

Idiopathic Pulmonary Fibrosis | Small molecule | Respiratory |GSK plc|Last Updated: Nov 21, 2019

Success Probability

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials1
Total Enrollment17

FDA Designations

No designations recorded

Clinical trial landscape

GSK2126458 · 2 trials · 2 indications

Phase 1 2
NCT01725139A Proof of Mechanism Study With GSK2126458 in Patients With Idiopathic Pulmonary Fibrosis (IPF)Idiopathic Pulmonary Fibrosis
COMPLETED17 Analytics
NCT00972686Dose-Escalation Study of GSK2126458Solid Tumours
COMPLETED79 Analytics
PHASE1COMPLETED
A Proof of Mechanism Study With GSK2126458 in Patients With Idiopathic Pulmonary Fibrosis (IPF)
Idiopathic Pulmonary FibrosisUnlock trial analytics
PHASE1COMPLETED
Dose-Escalation Study of GSK2126458
Solid TumoursUnlock trial analytics

Study Endpoints

Primary Endpoints

Pharmacodynamic (PD) endpoints pAKT/AKT in platelet-rich plasma and BAL cells, [18F]-FDG-PET/CT
Baseline, Day 1, mid-study BAL visit (Day 5-9) and final dosing day (Day 7, 8, 9 or 10) for each cohort

Pharmacodynamic will be measured by inhibition of pAKT/AKT in platelet-rich plasma and BAL cells, as well as inhibition of glucose uptake as measured by thoracic\[18F\]-FDG-PET/CT

Area under the curve (AUC) in blood for GSK2126458
Day 1, mid-study PET visit (Day 4-8), mid-study BAL visit (Day 5-9) and final dosing day post-dose (Day 7, 8, 9 or 10) for each cohort

GSK2126458 PK parameters in blood in order to define the blood and pulmonary PK/PD relationship for GSK2126458 in IPF subjects

Maximum observed concentration (Cmax) in blood for GSK2126458
Day 1, mid-study PET visit (Day 4-8), mid-study BAL visit (Day 5-9) and final dosing day post-dose (Day 7, 8, 9 or 10) for each cohort

GSK2126458 PK parameters in blood in order to define the blood and pulmonary PK/PD relationship for GSK2126458 in IPF subjects

Pre-dose (trough) concentration at the end of the dosing interval (Ctrough) in blood for GSK2126458
Day 1, mid-study PET visit (Day 4-8), mid-study BAL visit (Day 5-9) and final dosing day post-dose (Day 7, 8, 9 or 10) for each cohort

GSK2126458 PK parameters in blood in order to define the blood and pulmonary PK/PD relationship for GSK2126458 in IPF subjects

Concentration of GSK2126458 in bronchoalveolar lavage fluid (BALF)
Baseline BAL visit and mid-study BAL visit (Day 5-9).

GSK2126458 concentration in BALF in order to define the pulmonary PK/PD relationship for GSK2126458 in IPF subjects

Adverse events (AEs) and changes in laboratory values and vital signs. Pharmacokinetic parameter values for GSK2126458, Change from baseline in protein markers in tumor and/or blood. Blood glucose and insulin levels. Tumor response, RECIST defined
Subjects continue on study until disease progression or consent withdrawal

Secondary Endpoints

Safety and tolerability of GSK2126458 as assessed by number of subjects with adverse events (AE)s
Baseline up to final dosing day (Day 7, 8, 9 or 10) for each cohort
Safety and tolerability of GSK2126458 as assessed by change from baseline in vital signs
Day 1, final dosing day (Day 7, 8, 9 or 10) and follow-up (10-14 days post last dose), for each cohort
Safety and tolerability of GSK2126458 as assessed by change from baseline in clinical laboratory parameters
Day 1, mid-study BAL visit (Day 5-9), final dosing day (Day 7, 8, 9 or 10) and follow-up (10-14 days post last dose) for each cohort
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Cohort 1-GSK2126458EXPERIMENTALSubjects will be randomized in 3:1 ratio to receive either GSK2126458 (0.25 mg twice daily \[bid\]) or placebo for approximately 8 days (7 to 10 days dosing)
Cohort 1-PlaceboPLACEBO_COMPARATORSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or matching placebo for approximately 8 days (7 to 10 days dosing)
Cohort 2-GSK2126458EXPERIMENTALSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or placebo for approximately 8 days (7 to 10 days dosing). GSK2126458 dose will be decided from Cohort 1 and which could be escalated or deescalated or repeated from Cohort 1 dosing.
Cohort 2-PlaceboPLACEBO_COMPARATORSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or matching placebo for approximately 8 days (7 to 10 days dosing).
Cohort 3- GSK2126458EXPERIMENTALSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or placebo for approximately 8 days (7 to 10 days dosing). GSK2126458 dose will be decided from Cohort 2 and which could be escalated or deescalated or repeated from Cohort 2 dosing.
Cohort 3-PlaceboPLACEBO_COMPARATORSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or matching placebo for approximately 8 days (7 to 10 days dosing).
Cohort 4- GSK2126458EXPERIMENTALSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or placebo for approximately 8 days (7 to 10 days dosing). GSK2126458 dose will be decided from Cohort 3 and which could be escalated or deescalated or repeated from Cohort 3 dosing.
Cohort 4- PlaceboPLACEBO_COMPARATORSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or matching placebo for approximately 8 days (7 to 10 days dosing).
Cohort 5- GSK2126458EXPERIMENTALSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or placebo for approximately 8 days (7 to 10 days dosing). GSK2126458 dose will be decided from Cohort 4 and which could be escalated or deescalated or repeated from Cohort 4 dosing.
Cohort 5- PlaceboPLACEBO_COMPARATORSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or matching placebo for approximately 8 days (7 to 10 days dosing).
Cohort 6- GSK2126458EXPERIMENTALSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or placebo for approximately 8 days (7 to 10 days dosing). GSK2126458 dose will be decided from Cohort 4 and which could be escalated or deescalated or repeated from Cohort 5 dosing.
Cohort 6- PlaceboPLACEBO_COMPARATORSubjects will be randomized in 3:1 ratio to receive either GSK2126458 bid or matching placebo for approximately 8 days (7 to 10 days dosing).
GSK2126458EXPERIMENTALGSK2126458 will be dosed continuously (every day) for the duration a 28 day cycle. The 28 day cycles will continue until the subjects withdraw from the study.

Interventions

NameTypeDescription
GSK2126458DRUGGSK2126458 will be available as film coated tablet of dose strength 0.25 mg and 0.5 mg
PlaceboDRUGMatching placebo will be available
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Eligibility Criteria

Age Range45 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites1

Inclusion Criteria: * Diagnosis of IPF as determined by a responsible and experienced chest physician and based on established criteria defined by the American Thoracic Society/European Respiratory Society: American Thoracic Society/European Respiratory Society International Multidisciplinary Conse...

Countries:United KingdomUnited StatesNetherlands
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Frequently asked questions about GSK2126458

What is GSK2126458 used for?

GSK2126458 is an investigational small molecule being studied for Idiopathic Pulmonary Fibrosis and Solid Tumours. It is in Phase 1 clinical development and is not approved by the FDA. The drug is being developed by GSK plc.

Who makes GSK2126458?

GSK2126458 is being developed by GSK plc, a pharmaceutical company listed on the stock exchange under the ticker GSK. The drug is currently in Phase 1 clinical trials for Idiopathic Pulmonary Fibrosis and Solid Tumours.

What phase is GSK2126458 in?

GSK2126458 is in Phase 1 clinical development. It is an investigational drug and has not been approved by the FDA. Clinical trials for the drug have been completed, including studies in Solid Tumours and Idiopathic Pulmonary Fibrosis.

What clinical trials is GSK2126458 in?

GSK2126458 has been studied in two completed Phase 1 clinical trials. NCT00972686 was a dose-escalation study in Solid Tumours with 79 participants. NCT01725139 was a proof of mechanism study in Idiopathic Pulmonary Fibrosis with 17 participants.

Is GSK2126458 the same as omipalisib?

GSK2126458 is also known by the name omipalisib. It is an investigational small molecule being developed by GSK plc for Idiopathic Pulmonary Fibrosis and Solid Tumours. The drug is currently in Phase 1 clinical development.