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NCT02783300: Meteor 1

An Open-label, Dose Escalation Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics and Clinical Activity of GSK3326595 in Participants With Solid Tumors and Non-Hodgkin's Lymphoma

Completed Phase 1 Results posted Last updated 10 March 2025
What this trial tests

Phase 1 trial testing GSK3326595 in Neoplasms in 297 participants. Completed in 30 August 2023.

Timeline
30 August 2016
Primary endpoint
30 August 2023
30 August 2023

Quick facts

Lead sponsorGlaxoSmithKline
PhasePhase 1
StatusCompleted
Study typeINTERVENTIONAL
Allocationnon randomized
Designparallel
Maskingnone
Primary purposetreatment
Enrollment297
Start date30 August 2016
Primary completion30 August 2023
Estimated completion30 August 2023
Sites15 locations across France, Canada, United States, Netherlands

Drugs / interventions tested

Conditions studied

Sponsor

GlaxoSmithKline — full company profile →

Who can join

18 and older, any sex, with Neoplasms. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Part 1: Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) Primary · Up to 30 months

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. SAE is defined as any untoward medical occurrence that, at any dose resulted in death, was life-threatening, required inpatient hospitalization or prolongation of existing hospitalization, resulted in persistent disability/incapacity, or is a congenital anomaly/birth defect, other situations which involved medical or scientific judgment or is associated with liver injury and impaired liver function. SAEs are

Any AEs
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD7
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD19
Part 1: GSK3326595 600mg QD3
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID7
Part 1: GSK3326595 150mg BID6
Part 1: GSK3326595 200mg BID3
Any SAEs
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD4
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD10
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID2
Part 1: GSK3326595 150mg BID3
Part 1: GSK3326595 200mg BID3
Part 1: Number of Participants Withdrawn Due to AEs Primary · Up to 30 months

The data for number of participants withdrawn due to AEs have been presented.

GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD2
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD2
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID1
Part 1: Number of Participants With Dose Limiting Toxicities (DLTs) Primary · Up to 21 days

DLT is considered to be clinically relevant AE by investigator if it met at least one of the criteria: Grade(G)3 neutropenia for \>=5 days/G4 neutropenia of any duration, G3 or greater febrile neutropenia, G4 or greater anemia of any duration and thrombocytopenia, or G3 thrombocytopenia with bleeding, Alanine aminotransferase (ALT) \>3x upper limit of normal (ULN)+bilirubin, \>=2xULN or ALT between 3-5 X ULN with bilirubin \< 2Xuln but with hepatitis symptoms/rash, G3 nausea/vomiting/diarrhea that does not improve within 72 hour, G4 or greater nausea/vomiting/diarrhea, G3 or greater hypertensi

GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD2
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID1
Part 1: GSK3326595 200mg BID1
Part 1: Number of Participants With Dose Modifications of GSK3326595 Primary · Up to 30 months

The number of participants who experienced any dose modifications (interruptions and reductions) of GSK3326595 have been presented.

Dose interruptions
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD5
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD18
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID5
Part 1: GSK3326595 150mg BID4
Part 1: GSK3326595 200mg BID2
Dose reductions
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD16
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID2
Part 1: GSK3326595 150mg BID2
Part 1: GSK3326595 200mg BID3
Part 1: Number of Participants With Worst Case Change From Baseline in Clinical Chemistry Parameters Primary · Baseline (Day 1) and up to 30 months

Blood samples were collected for evaluation of clinical chemistry parameters. The summaries of worst-case change from Baseline with respect to normal range have been presented for only those laboratory tests that are gradable by Common Terminology Criteria for Adverse Events (CTCAE) version 5.0. The number of participants with decreases to low, changes to normal or no changes from Baseline, and increases to high values have been presented. Participants were counted twice if the participants have values that changed 'To Low' and 'To High', so the percentages may not add to 100%.

Alanine Aminotransferase, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD2
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD4
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID1
Part 1: GSK3326595 200mg BID1
Alanine Aminotransferase, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD4
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD13
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID6
Part 1: GSK3326595 150mg BID4
Part 1: GSK3326595 200mg BID2
Alanine Aminotransferase, increases to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD1
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD2
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID1
Part 1: GSK3326595 150mg BID1
Part 1: GSK3326595 200mg BID0
Albumin, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD4
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD12
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID2
Part 1: GSK3326595 150mg BID5
Part 1: GSK3326595 200mg BID1
Albumin, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD3
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD7
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID5
Part 1: GSK3326595 150mg BID1
Part 1: GSK3326595 200mg BID2
Albumin, increases to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD0
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Alkaline Phosphatase, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD0
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Alkaline Phosphatase, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD7
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD17
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID4
Part 1: GSK3326595 150mg BID5
Part 1: GSK3326595 200mg BID3
Part 1: Number of Participants With Worst Case Change From Baseline in Hematology Parameters Primary · Baseline (Day 1) and up to 30 months

Blood samples were collected for evaluation of hematology parameters. The summaries of worst-case change from Baseline with respect to normal range have been presented for only those laboratory tests that are gradable by CTCAE v5.0. The number of participants with decreases to low, changes to normal or no changes from Baseline, and increases to high values have been presented. Participants were counted twice if the participants have values that changed 'To Low' and 'To High', so the percentages may not add to 100%.

Basophils, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD0
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Basophils, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD6
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD19
Part 1: GSK3326595 600mg QD3
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID7
Part 1: GSK3326595 150mg BID6
Part 1: GSK3326595 200mg BID2
Basophils, increases to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD1
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD0
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID1
Eosinophils, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD2
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD1
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Eosinophils, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD5
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD16
Part 1: GSK3326595 600mg QD3
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID6
Part 1: GSK3326595 150mg BID6
Part 1: GSK3326595 200mg BID0
Eosinophils, increases to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD2
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID1
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID3
Mean Corpuscular Hemoglobin, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD2
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD1
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID2
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID1
Mean Corpuscular Hemoglobin, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD5
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD17
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID5
Part 1: GSK3326595 150mg BID6
Part 1: GSK3326595 200mg BID1
Part 1: Number of Participants With Worst Case Change From Baseline in Coagulation Parameters Primary · Baseline (Day 1) and up to 30 months

Blood samples were collected for evaluation of coagulation parameters. The summaries of worst-case change from Baseline with respect to normal range have been presented for only those laboratory tests that are gradable by CTCAE v4.0. The number of participants with decreases to low, changes to normal or no changes from Baseline, and increases to high values have been presented. Participants were counted twice if the participants have values that changed 'To Low' and 'To High', so the percentages may not add to 100%.

Partial Thromboplastin Time, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD1
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Partial Thromboplastin Time, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD4
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD8
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID4
Part 1: GSK3326595 150mg BID1
Part 1: GSK3326595 200mg BID1
Partial Thromboplastin Time, increases to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD3
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD6
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID1
Part 1: GSK3326595 150mg BID3
Part 1: GSK3326595 200mg BID1
Prothrombin Intl. Normalized Ratio, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD1
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Prothrombin Intl. Normalized Ratio, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD4
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD8
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID2
Part 1: GSK3326595 150mg BID2
Part 1: GSK3326595 200mg BID2
Prothrombin Intl. Normalized Ratio, increases to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD3
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD10
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID5
Part 1: GSK3326595 150mg BID4
Part 1: GSK3326595 200mg BID1
Prothrombin Time, decreases to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD1
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Prothrombin Time, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD3
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD9
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID4
Part 1: GSK3326595 150mg BID3
Part 1: GSK3326595 200mg BID3
Part 1: Number of Participants With Worst Case Change From Baseline in Urinalysis Parameters Primary · Baseline (Day 1) and up to 30 months

Urine samples were collected for evaluation of urinalysis parameters. The summaries of worst-case change from Baseline with respect to normal range have been presented for only those laboratory tests that are gradable by CTCAE v5.0. The number of participants with no change or change to negative and change to positive have been presented.

Occult Blood, No Change or Change to Negative
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD5
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD12
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID4
Part 1: GSK3326595 150mg BID4
Part 1: GSK3326595 200mg BID1
Occult Blood, Change to Positive
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD2
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD7
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID3
Part 1: GSK3326595 150mg BID2
Part 1: GSK3326595 200mg BID2
Protein, No Change or Change to Negative
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD4
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD11
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID2
Part 1: GSK3326595 150mg BID4
Part 1: GSK3326595 200mg BID1
Protein, Change to Positive
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD3
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD8
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID5
Part 1: GSK3326595 150mg BID2
Part 1: GSK3326595 200mg BID2
Ketones, No Change or Change to Negative
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD5
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD11
Part 1: GSK3326595 600mg QD2
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID3
Part 1: GSK3326595 150mg BID3
Part 1: GSK3326595 200mg BID3
Ketones, Change to Positive
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD2
Part 1: GSK3326595 300mg QD1
Part 1: GSK3326595 400mg QD8
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID4
Part 1: GSK3326595 150mg BID3
Part 1: GSK3326595 200mg BID0
Glucose, No Change or Change to Negative
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD7
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD18
Part 1: GSK3326595 600mg QD3
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID7
Part 1: GSK3326595 150mg BID5
Part 1: GSK3326595 200mg BID3
Glucose, Change to Positive
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD1
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID1
Part 1: GSK3326595 200mg BID0
Part 1: Changes From Baseline in Urine Potential of Hydrogen (pH) Primary · Baseline (Day 1) and up to week 132

Urine samples were collected from participants to assess urine pH levels.

Baseline
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)5.00± NA
Part 1: GSK3326595 25mg QD5.50± NA
Part 1: GSK3326595 50mg QD7.00± NA
Part 1: GSK3326595 100mg QD6.50± NA
Part 1: GSK3326595 200mg QD6.00± 0.886
Part 1: GSK3326595 300mg QD6.17± 0.289
Part 1: GSK3326595 400mg QD6.11± 0.698
Part 1: GSK3326595 600mg QD5.67± 0.764
Part 1: GSK3326595 50mg Twice Daily (BID)6.50± NA
Part 1: GSK3326595 100mg BID5.79± 1.075
Part 1: GSK3326595 150mg BID5.75± 0.524
Part 1: GSK3326595 200mg BID6.17± 0.764
CFB to Day 8
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0.00± NA
Part 1: GSK3326595 25mg QD0.00± NA
Part 1: GSK3326595 50mg QD-1.00± NA
Part 1: GSK3326595 100mg QD0.50± NA
Part 1: GSK3326595 200mg QD0.17± 0.516
Part 1: GSK3326595 300mg QD-0.25± 0.354
Part 1: GSK3326595 400mg QD-0.28± 0.548
Part 1: GSK3326595 600mg QD0.83± 0.764
Part 1: GSK3326595 50mg Twice Daily (BID)0.50± NA
Part 1: GSK3326595 100mg BID-0.07± 1.239
Part 1: GSK3326595 150mg BID0.08± 0.492
Part 1: GSK3326595 200mg BID0.33± 1.258
CFB to Day 15
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0.00± NA
Part 1: GSK3326595 25mg QD0.00± NA
Part 1: GSK3326595 50mg QD-1.00± NA
Part 1: GSK3326595 100mg QD0.50± NA
Part 1: GSK3326595 200mg QD0.21± 0.488
Part 1: GSK3326595 300mg QD-0.17± 0.289
Part 1: GSK3326595 400mg QD-0.24± 0.731
Part 1: GSK3326595 600mg QD0.00± 1.000
Part 1: GSK3326595 50mg Twice Daily (BID)0.00± NA
Part 1: GSK3326595 100mg BID-0.29± 0.859
Part 1: GSK3326595 150mg BID0.10± 0.548
Part 1: GSK3326595 200mg BID1.00± NA
CFB to Week 4 Day 1
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0.00± NA
Part 1: GSK3326595 25mg QD0.00± NA
Part 1: GSK3326595 50mg QD0.00± NA
Part 1: GSK3326595 100mg QD0.50± NA
Part 1: GSK3326595 200mg QD-0.20± 0.447
Part 1: GSK3326595 300mg QD-0.75± 0.354
Part 1: GSK3326595 400mg QD-0.13± 0.611
Part 1: GSK3326595 600mg QD0.67± 1.041
Part 1: GSK3326595 50mg Twice Daily (BID)-0.50± NA
Part 1: GSK3326595 100mg BID-0.21± 0.488
Part 1: GSK3326595 150mg BID0.10± 0.548
Part 1: GSK3326595 300mg QD (Food Effect)-0.10± 0.849
CFB to Week 6 Day 1
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0.00± NA
Part 1: GSK3326595 25mg QD0.00± NA
Part 1: GSK3326595 50mg QD0.00± NA
Part 1: GSK3326595 100mg QD0.50± NA
Part 1: GSK3326595 200mg QD-0.17± 0.577
Part 1: GSK3326595 300mg QD0.00± 0.000
Part 1: GSK3326595 400mg QD-0.43± 0.799
Part 1: GSK3326595 600mg QD0.25± 1.061
Part 1: GSK3326595 50mg Twice Daily (BID)-0.50± NA
Part 1: GSK3326595 100mg BID-0.29± 1.035
Part 1: GSK3326595 150mg BID-0.08± 0.492
Part 1: GSK3326595 200mg BID0.00± 0.707
CFB to Week 8
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0.00± NA
Part 1: GSK3326595 25mg QD-0.50± NA
Part 1: GSK3326595 100mg QD0.50± NA
Part 1: GSK3326595 200mg QD-1.17± 1.155
Part 1: GSK3326595 300mg QD-0.75± 0.354
Part 1: GSK3326595 400mg QD-0.19± 0.630
Part 1: GSK3326595 600mg QD1.00± 0.707
Part 1: GSK3326595 100mg BID0.75± 0.645
Part 1: GSK3326595 150mg BID-0.20± 0.274
Part 1: GSK3326595 200mg BID0.00± 0.000
Part 1: GSK3326595 300mg QD (Food Effect)0.44± 0.682
CFB to Week 12
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0.00± NA
Part 1: GSK3326595 200mg QD0.00± 0.500
Part 1: GSK3326595 300mg QD-0.50± NA
Part 1: GSK3326595 400mg QD-0.11± 0.546
Part 1: GSK3326595 600mg QD1.00± 1.414
Part 1: GSK3326595 100mg BID0.38± 0.629
Part 1: GSK3326595 150mg BID0.00± NA
Part 1: GSK3326595 200mg BID-0.25± 1.061
Part 1: GSK3326595 300mg QD (Food Effect)0.08± 1.021
CFB to Week 16
GroupValue95% CI
Part 1: GSK3326595 200mg QD-0.25± 1.061
Part 1: GSK3326595 300mg QD0.00± NA
Part 1: GSK3326595 400mg QD0.14± 0.690
Part 1: GSK3326595 600mg QD0.50± 1.414
Part 1: GSK3326595 100mg BID0.33± 0.289
Part 1: GSK3326595 150mg BID0.00± NA
Part 1: GSK3326595 200mg BID0.00± 0.000
Part 1: GSK3326595 300mg QD (Food Effect)-0.13± 0.250
Part 1: Changes From Baseline in Urine Specific Gravity Primary · Baseline (Day 1) and up to week 132

Urine samples were collected from participants to assess urine specific gravity.

Baseline
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1.02± NA
Part 1: GSK3326595 25mg QD1.03± NA
Part 1: GSK3326595 50mg QD1.01± NA
Part 1: GSK3326595 100mg QD1.02± NA
Part 1: GSK3326595 200mg QD1.02± 0.008
Part 1: GSK3326595 300mg QD1.02± 0.006
Part 1: GSK3326595 400mg QD1.02± 0.007
Part 1: GSK3326595 600mg QD1.02± 0.004
Part 1: GSK3326595 50mg Twice Daily (BID)1.01± NA
Part 1: GSK3326595 100mg BID1.02± 0.006
Part 1: GSK3326595 150mg BID1.03± 0.008
Part 1: GSK3326595 200mg BID1.02± 0.008
CFB to Day 8
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)-0.01± NA
Part 1: GSK3326595 25mg QD0.00± NA
Part 1: GSK3326595 50mg QD0.01± NA
Part 1: GSK3326595 100mg QD0.01± NA
Part 1: GSK3326595 200mg QD0.00± 0.010
Part 1: GSK3326595 300mg QD0.00± 0.004
Part 1: GSK3326595 400mg QD0.00± 0.007
Part 1: GSK3326595 600mg QD0.00± 0.010
Part 1: GSK3326595 50mg Twice Daily (BID)0.00± NA
Part 1: GSK3326595 100mg BID0.00± 0.008
Part 1: GSK3326595 150mg BID0.00± 0.006
Part 1: GSK3326595 200mg BID0.00± 0.009
CFB to Day 15
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)-0.01± NA
Part 1: GSK3326595 25mg QD-0.01± NA
Part 1: GSK3326595 50mg QD0.01± NA
Part 1: GSK3326595 100mg QD0.00± NA
Part 1: GSK3326595 200mg QD0.00± 0.010
Part 1: GSK3326595 300mg QD-0.01± 0.005
Part 1: GSK3326595 400mg QD0.00± 0.007
Part 1: GSK3326595 600mg QD0.00± 0.005
Part 1: GSK3326595 50mg Twice Daily (BID)0.01± NA
Part 1: GSK3326595 100mg BID0.00± 0.010
Part 1: GSK3326595 150mg BID0.00± 0.004
Part 1: GSK3326595 200mg BID0.00
CFB to Week 4 Day 1
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)-0.01± NA
Part 1: GSK3326595 25mg QD-0.01± NA
Part 1: GSK3326595 50mg QD0.00± NA
Part 1: GSK3326595 100mg QD0.00± NA
Part 1: GSK3326595 200mg QD0.00± 0.007
Part 1: GSK3326595 300mg QD0.00± 0.004
Part 1: GSK3326595 400mg QD0.00± 0.008
Part 1: GSK3326595 600mg QD0.00± 0.002
Part 1: GSK3326595 50mg Twice Daily (BID)0.01± NA
Part 1: GSK3326595 100mg BID0.00± 0.007
Part 1: GSK3326595 150mg BID0.00± 0.007
Part 1: GSK3326595 300mg QD (Food Effect)0.00± 0.007
CFB to Week 6 Day 1
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)-0.01± NA
Part 1: GSK3326595 25mg QD-0.01± NA
Part 1: GSK3326595 50mg QD0.01± NA
Part 1: GSK3326595 100mg QD0.01± NA
Part 1: GSK3326595 200mg QD0.00± 0.008
Part 1: GSK3326595 300mg QD-0.01± 0.004
Part 1: GSK3326595 400mg QD0.00± 0.010
Part 1: GSK3326595 600mg QD0.00± 0.006
Part 1: GSK3326595 50mg Twice Daily (BID)0.01± NA
Part 1: GSK3326595 100mg BID0.00± 0.012
Part 1: GSK3326595 150mg BID0.00± 0.004
Part 1: GSK3326595 200mg BID-0.01± 0.007
CFB to Week 8
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)-0.01± NA
Part 1: GSK3326595 25mg QD0.00± NA
Part 1: GSK3326595 100mg QD0.01± NA
Part 1: GSK3326595 200mg QD0.00± 0.008
Part 1: GSK3326595 300mg QD-0.01± 0.004
Part 1: GSK3326595 400mg QD0.00± 0.008
Part 1: GSK3326595 600mg QD0.00± 0.006
Part 1: GSK3326595 100mg BID0.00± 0.006
Part 1: GSK3326595 150mg BID0.00± 0.004
Part 1: GSK3326595 200mg BID-0.01± 0.007
Part 1: GSK3326595 300mg QD (Food Effect)0.00± 0.007
CFB to Week 12
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)-0.01± NA
Part 1: GSK3326595 200mg QD0.00± 0.005
Part 1: GSK3326595 300mg QD-0.01
Part 1: GSK3326595 400mg QD0.00± 0.008
Part 1: GSK3326595 600mg QD-0.01± 0.008
Part 1: GSK3326595 100mg BID0.00± 0.010
Part 1: GSK3326595 150mg BID-0.01± NA
Part 1: GSK3326595 200mg BID-0.01± 0.004
Part 1: GSK3326595 300mg QD (Food Effect)0.00± 0.006
CFB to Week 16
GroupValue95% CI
Part 1: GSK3326595 200mg QD0.00± 0.011
Part 1: GSK3326595 300mg QD-0.02± NA
Part 1: GSK3326595 400mg QD0.00± 0.006
Part 1: GSK3326595 600mg QD-0.01± 0.004
Part 1: GSK3326595 100mg BID-0.01± 0.008
Part 1: GSK3326595 150mg BID0.00± NA
Part 1: GSK3326595 200mg BID0.00± 0.004
Part 1: GSK3326595 300mg QD (Food Effect)0.00± 0.004
Part 1: Number of Participants With Maximum Grade Worst Case Increase Post-baseline Relative to Baseline in Vital Signs Primary · Baseline (Day 1) and up to 30 months

The abnormal vital sign ranges are: Heart Rate:- Low (\<60 beats per minute (bpm)), Normal (\>=60 bpm to \<=100 bpm), High (\>100 bpm); Temperature:- Low (\<=35 degree Celsius (°C)), Normal (\>35 °C and \<38 °C), High (\>=38 °C); Systolic Blood Pressure:- Low (\<90 millimeter of mercury (mmHg)), Normal (\>=90 mmHg to \<120 mmHg), High (\>=120 mmHg); Diastolic Blood Pressure:- Low (\<60 mmHg), Normal (\>=60 mmHg to \<80 mmHg), High (\>=80 mmHg). Participants were counted in the worst-case category and their value changes to (low, normal or high), unless there is no change in their category. Par

Heart Rate, changes to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD1
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD2
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID1
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Heart Rate, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD5
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD12
Part 1: GSK3326595 600mg QD3
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID3
Part 1: GSK3326595 150mg BID6
Part 1: GSK3326595 200mg BID2
Heart Rate, changes to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD1
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD6
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID3
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID1
Temperature, changes to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD0
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID0
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Temperature, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)1
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD6
Part 1: GSK3326595 300mg QD3
Part 1: GSK3326595 400mg QD17
Part 1: GSK3326595 600mg QD3
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID6
Part 1: GSK3326595 150mg BID6
Part 1: GSK3326595 200mg BID3
Temperature, changes to high
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD1
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD2
Part 1: GSK3326595 600mg QD0
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID1
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Systolic Blood Pressure, changes to low
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD0
Part 1: GSK3326595 50mg QD0
Part 1: GSK3326595 100mg QD0
Part 1: GSK3326595 200mg QD0
Part 1: GSK3326595 300mg QD0
Part 1: GSK3326595 400mg QD3
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)0
Part 1: GSK3326595 100mg BID1
Part 1: GSK3326595 150mg BID0
Part 1: GSK3326595 200mg BID0
Systolic Blood Pressure, changes to normal or no changes
GroupValue95% CI
Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)0
Part 1: GSK3326595 25mg QD1
Part 1: GSK3326595 50mg QD1
Part 1: GSK3326595 100mg QD1
Part 1: GSK3326595 200mg QD5
Part 1: GSK3326595 300mg QD2
Part 1: GSK3326595 400mg QD9
Part 1: GSK3326595 600mg QD1
Part 1: GSK3326595 50mg Twice Daily (BID)1
Part 1: GSK3326595 100mg BID5
Part 1: GSK3326595 150mg BID5
Part 1: GSK3326595 200mg BID1
Part 3: Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) Primary · Up to 10 months

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. SAE is defined as any untoward medical occurrence that, at any dose resulted in death, was life-threatening, required inpatient hospitalization or prolongation of existing hospitalization, resulted in persistent disability/incapacity, or was a congenital anomaly/birth defect, other situations which involve medical or scientific judgment or is associated with liver injury and impaired liver function. SAEs are

Any AEs
GroupValue95% CI
Part 3: GSK3326595 100mg + Pembrolizumab 200mg9
Any SAEs
GroupValue95% CI
Part 3: GSK3326595 100mg + Pembrolizumab 200mg5

Adverse events — posted to ClinicalTrials.gov

Time frame: All-cause mortality, non-serious adverse events (non-SAEs) and serious adverse events (SAEs) were collected up to 30 months for part 1, 42 months for part 2 and 10 months for part 3.. Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Part 1: GSK3326595 12.5 Milligram (mg) Once a Day (QD)
Serious: 0/1 (0%)
Deaths: 1/1
Part 1: GSK3326595 25mg QD
Serious: 0/1 (0%)
Deaths: 1/1
Part 1: GSK3326595 50mg QD
Serious: 0/1 (0%)
Deaths: 1/1
Part 1: GSK3326595 100mg QD
Serious: 0/1 (0%)
Deaths: 0/1
Part 1: GSK3326595 200mg QD
Serious: 4/8 (50%)
Deaths: 7/8
Part 1: GSK3326595 300mg QD
Serious: 1/3 (33%)
Deaths: 3/3
Part 1: GSK3326595 400mg QD
Serious: 10/19 (53%)
Deaths: 13/19
Part 1: GSK3326595 600mg QD
Serious: 1/3 (33%)
Deaths: 3/3
Part 1: GSK3326595 50mg Twice Daily (BID)
Serious: 0/1 (0%)
Deaths: 1/1
Part 1: GSK3326595 100mg BID
Serious: 2/7 (29%)
Deaths: 6/7
Part 1: GSK3326595 150mg BID
Serious: 3/6 (50%)
Deaths: 6/6
Part 1: GSK3326595 200mg BID
Serious: 3/3 (100%)
Deaths: 3/3
Part 1: GSK3326595 300mg QD (Food Effect)
Serious: 6/15 (40%)
Deaths: 8/15
Part 2: GSK3326595 400mg (TNBC)
Serious: 13/22 (59%)
Deaths: 16/22
Part 2: GSK3326595 400mg (mTCC)
Serious: 7/16 (44%)
Deaths: 10/16
Part 2: GSK3326595 400mg (GBM)
Serious: 15/29 (52%)
Deaths: 22/29
Part 2: GSK3326595 400mg (ER+BC)
Serious: 10/37 (27%)
Deaths: 31/37
Part 2: GSK3326595 400mg (HPV+)
Serious: 13/28 (46%)
Deaths: 25/28
Part 2: GSK3326595 400mg (ACC)
Serious: 15/34 (44%)
Deaths: 20/34
Part 2: GSK3326595 300mg (ACC)
Serious: 5/16 (31%)
Deaths: 2/16
Part 2: GSK3326595 400mg (NHL P53 Mutant)
Serious: 4/6 (67%)
Deaths: 4/6
Part 2: GSK3326595 300mg (NHL P53 Mutant)
Serious: 2/2 (100%)
Deaths: 1/2
Part 2: GSK3326595 400mg (NHL P53 Wild Type)
Serious: 4/8 (50%)
Deaths: 5/8
Part 2: GSK3326595 300mg (NHL P53 Wild Type)
Serious: 0/2 (0%)
Deaths: 1/2
Part 2: GSK3326595 400mg (NHL P53 Unknown)
Serious: 4/11 (36%)
Deaths: 7/11
Part 2: GSK3326595 300mg (NSCLC)
Serious: 0/7 (0%)
Deaths: 3/7
Part 3: GSK3326595 100mg + Pembrolizumab 200mg
Serious: 5/10 (50%)
Deaths: 6/10

Serious adverse events (114 terms)

ReactionSystemPart 1: GSK3326595 12.5 Mi…Part 1: GSK3326595 25mg QDPart 1: GSK3326595 50mg QDPart 1: GSK3326595 100mg QDPart 1: GSK3326595 200mg QDPart 1: GSK3326595 300mg QDPart 1: GSK3326595 400mg QDPart 1: GSK3326595 600mg QDPart 1: GSK3326595 50mg Tw…Part 1: GSK3326595 100mg BIDPart 1: GSK3326595 150mg BIDPart 1: GSK3326595 200mg BIDPart 1: GSK3326595 300mg Q…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 3: GSK3326595 100mg +…
AnaemiaBlood and lymphatic system disorders
DyspnoeaRespiratory, thoracic and mediastinal disorders
Acute kidney injuryRenal and urinary disorders
PneumoniaInfections and infestations
DehydrationMetabolism and nutrition disorders
Pleural effusionRespiratory, thoracic and mediastinal disorders
PneumothoraxRespiratory, thoracic and mediastinal disorders
HypoxiaRespiratory, thoracic and mediastinal disorders
PainGeneral disorders
VomitingGastrointestinal disorders
Brain oedemaNervous system disorders
Intracranial pressure increasedNervous system disorders
ThrombocytopeniaBlood and lymphatic system disorders
Respiratory failureRespiratory, thoracic and mediastinal disorders
Escherichia infectionInfections and infestations
Pyelonephritis acuteInfections and infestations
SepsisInfections and infestations
Skin infectionInfections and infestations
Staphylococcal infectionInfections and infestations
Urinary tract infectionInfections and infestations
PyrexiaGeneral disorders
FatigueGeneral disorders
General physical health deteriorationGeneral disorders
Oedema peripheralGeneral disorders
Atrial fibrillationCardiac disorders
Other adverse events (86 terms — click to expand)

ReactionSystemPart 1: GSK3326595 12.5 Mi…Part 1: GSK3326595 25mg QDPart 1: GSK3326595 50mg QDPart 1: GSK3326595 100mg QDPart 1: GSK3326595 200mg QDPart 1: GSK3326595 300mg QDPart 1: GSK3326595 400mg QDPart 1: GSK3326595 600mg QDPart 1: GSK3326595 50mg Tw…Part 1: GSK3326595 100mg BIDPart 1: GSK3326595 150mg BIDPart 1: GSK3326595 200mg BIDPart 1: GSK3326595 300mg Q…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 2: GSK3326595 400mg (…Part 2: GSK3326595 300mg (…Part 3: GSK3326595 100mg +…
NauseaGastrointestinal disorders
FatigueGeneral disorders
AlopeciaSkin and subcutaneous tissue disorders
AnaemiaBlood and lymphatic system disorders
DysgeusiaNervous system disorders
Decreased appetiteMetabolism and nutrition disorders
VomitingGastrointestinal disorders
StomatitisGastrointestinal disorders
AstheniaGeneral disorders
HeadacheNervous system disorders
DyspnoeaRespiratory, thoracic and mediastinal disorders
DiarrhoeaGastrointestinal disorders
Dry skinSkin and subcutaneous tissue disorders
Oedema peripheralGeneral disorders
ConstipationGastrointestinal disorders
Back painMusculoskeletal and connective tissue disorders
Weight decreasedInvestigations
ThrombocytopeniaBlood and lymphatic system disorders
PruritusSkin and subcutaneous tissue disorders
Platelet count decreasedInvestigations
Abdominal painGastrointestinal disorders
CoughRespiratory, thoracic and mediastinal disorders
ArthralgiaMusculoskeletal and connective tissue disorders
MyalgiaMusculoskeletal and connective tissue disorders
PyrexiaGeneral disorders
DizzinessNervous system disorders
Pain in extremityMusculoskeletal and connective tissue disorders
Blood bilirubin increasedInvestigations
Vision blurredEye disorders
Dry mouthGastrointestinal disorders
RashSkin and subcutaneous tissue disorders
Neutrophil count decreasedInvestigations
PneumoniaInfections and infestations
Urinary tract infectionInfections and infestations
NeutropeniaBlood and lymphatic system disorders
HypokalaemiaMetabolism and nutrition disorders
DyspepsiaGastrointestinal disorders
Gastrooesophageal reflux diseaseGastrointestinal disorders
Peripheral sensory neuropathyNervous system disorders
Rash maculo-papularSkin and subcutaneous tissue disorders

Most-reported serious reactions: Anaemia, Dyspnoea, Acute kidney injury, Pneumonia, Dehydration, Pleural effusion, Pneumothorax, Hypoxia.

Data from ClinicalTrials.gov NCT02783300 adverse events section.

Sponsor's own description

This first time in human (FTIH) open-label, dose escalation study will assess the safety, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary clinical activity of GSK3326595 in participants with advanced or recurrent solid tumors, as well as clinical activity in participants with a subset of solid tumors and non-Hodgkin's lymphoma (NHL).

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

  1. Integrative Molecular Characterization of Malignant Pleural Mesothelioma.
    Hmeljak J, Sanchez-Vega F, Hoadley KA, Shih J, et al · · 2018 · cited 495× · PMID 30322867 · DOI 10.1158/2159-8290.cd-18-0804
  2. Pancreatic cancer organoids recapitulate disease and allow personalized drug screening.
    Driehuis E, van Hoeck A, Moore K, Kolders S, et al · · 2019 · cited 358× · PMID 31818951 · DOI 10.1073/pnas.1911273116
  3. Human organoids in basic research and clinical applications.
    Tang XY, Wu S, Wang D, Chu C, et al · · 2022 · cited 298× · PMID 35610212 · DOI 10.1038/s41392-022-01024-9
  4. WD40 repeat domain proteins: a novel target class?
    Schapira M, Tyers M, Torrent M, Arrowsmith CH. · · 2017 · cited 256× · PMID 29026209 · DOI 10.1038/nrd.2017.179
  5. Epigenetics and Cancer Stem Cells: Unleashing, Hijacking, and Restricting Cellular Plasticity.
    Wainwright EN, Scaffidi P. · · 2017 · cited 250× · PMID 28718414 · DOI 10.1016/j.trecan.2017.04.004
  6. Protein arginine methyltransferases: promising targets for cancer therapy.
    Hwang JW, Cho Y, Bae GU, Kim SN, et al · · 2021 · cited 205× · PMID 34006904 · DOI 10.1038/s12276-021-00613-y
  7. Targeting Epigenetics in Cancer.
    Bennett RL, Licht JD. · · 2018 · cited 184× · PMID 28992434 · DOI 10.1146/annurev-pharmtox-010716-105106
  8. PRMT5 control of cGAS/STING and NLRC5 pathways defines melanoma response to antitumor immunity.
    Kim H, Kim H, Feng Y, Li Y, et al · · 2020 · cited 181× · PMID 32641491 · DOI 10.1126/scitranslmed.aaz5683

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Data sources for this page

Drug Landscape aggregates and links these public records for informational use only. Always verify against the primary source before clinical or regulatory decisions. Canonical URL: https://druglandscape.com/trial/NCT02783300.

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing