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GSK2646264 1%

Phase 1

Lupus Erythematosus, Cutaneous | Small molecule | Immunology |GSK plc|Last Updated: Apr 8, 2021

Success Probability

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Trial Design

RandomizedDouble-BlindCONTROLLED
Total Trials1
Total Enrollment11

FDA Designations

No designations recorded

Clinical trial landscape

GSK2646264 1% · 1 trial · 1 indication

Phase 1 1
NCT02927457Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Clinical Effect of GSK2646264 in Cutaneous Lupus Erythematosus SubjectsLupus Erythematosus, Cutaneous
COMPLETED11 Analytics
PHASE1COMPLETED
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Clinical Effect of GSK2646264 in Cutaneous Lupus Erythematosus Subjects
Lupus Erythematosus, CutaneousUnlock trial analytics

Study Endpoints

Primary Endpoints

Number of Participants With Emergent Chemistry Results by Potential Clinical Importance (PCI) Criteria
Day 14, Day 28 and follow-up (up to Day 56)

Blood samples were collected to analyze the clinical chemistry parameters; albumin, alkaline phosphatase (ALP), alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TB), calcium, glucose, potassium (Pot) and sodium. PCI ranges were albumin (low: \<30 grams per liter), calcium (low: \<2 millimoles per liter \[mmol/L\] and high: \>2.75 mmol/L), glucose (low: \<3 mmol/L and high: \>9 mmol/L), Pot (low: \<3 mmol/L and high: \>5.5 mmol/L), sodium (low: \<130 mmol/L and high: \>150 mmol/L), ALT (high: \>=2 times upper limit of normal \[ULN\] units per liter {U/L}), AST (high: \>=2 times ULN U/L), ALP (high: \>=2 times ULN U/L) and TB (high: \>=1.5 times ULN micromoles per liter). Safety Population comprised of all participants who received at least one dose of study treatment. All participants received both treatment interventions at the same time (on different skin sites), hence data for these participants were combined.

Number of Participants With Emergent Hematology Results by PCI Criteria
Day 14, Day 28 and follow-up (up to Day 56)

PCI ranges were hematocrit \[Hct\] (high: \>0.54 proportion of red blood cell \[RBC\] in blood), hemoglobin \[Hb\] (high: \>180 grams per liter), RBC (low: \<4.2x10\^12 cells per liter and high: \>5.9x10\^12 cells per liter), lymphocytes \[Lympho\] (low: \<0.8x10\^9 cells per liter), monocytes \[Mono\] (low: \<0.14x10\^9 cells per liter and high: \>1.3x10\^9 cells per liter), neutrophils \[Neutro\] (low: \<1.5x10\^9 cells per liter), platelet count \[PC\] (low: \<100x10\^9 cells per liter and high: \>550x10\^9 cells per liter), eosinophils \[Eos\] (high: \>0.55x10\^9 cells per liter), basophils \[Baso\] (high: \>0.22x10\^9 cells per liter), white blood cell \[WBC\] (low: \<3x10\^9 cells per liter and high: \>20x10\^9 cells per liter). All participants received both treatment interventions at the same time (on different skin sites), hence data for these participants were combined.

Change From Baseline in Urine Potential of Hydrogen (pH)
Baseline (Day 1), Day 14, Day 28 and follow-up (up to Day 56)

Urine samples were collected to monitor the pH. pH is a measure of hydrogen ion concentration and is used to determine the acidity or alkalinity of urine. pH scale ranges from 0 to 14. A neutral pH is 7.0. The higher number indicates the more basic (alkaline) nature of urine and lower number indicates the more acidic urine. Day 1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. All participants received both treatment interventions at the same time (on different skin sites), hence data for these participants were combined.

Change From Baseline in Urine Specific Gravity
Baseline (Day 1), Day 14, Day 28 and follow-up (up to Day 56)

Urine samples were collected to monitor the specific gravity. Specific gravity is a measure of urine concentration and is measured using a chemical test. Specific gravity measurements provide a comparison of the amount of substances dissolved in urine as compared to pure water. If there were no solutes present, the specific gravity of urine would be 1.000 the same as pure water. Specific gravity between 1.002 and 1.035 could be considered as normal. Day 1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. All participants received both treatment interventions at the same time (on different skin sites), hence data for these participants were combined.

Number of Participants With Emergent Vital Sign Results by PCI Criteria
Day 14 and Day 28

Vital signs such as diastolic blood pressure (DBP), heart rate (HR) and systolic blood pressure (SBP) were measured in semi-supine position after 5 minutes rest for the participants. PCI ranges were SBP (lower: \<85 millimeters of mercury \[mmHg\] and upper: \>160 mmHg), DBP: (lower: \<45 mmHg and upper: \>100 mmHg) and HR (lower: \<40 beats per minute \[bpm\] and upper: \>110 bpm). All participants received both treatment interventions at the same time (on different skin sites), hence data for these participants were combined.

Change From Baseline in Electrocardiogram (ECG); HR
Baseline (Day 1), Day 14 and follow-up (up to Day 56)

Triplicate 12-lead ECGs were obtained using an ECG machine that automatically calculated the heart rate. Day 1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. All participants received both treatment interventions at the same time (on different skin sites), hence data for these participants were combined.

Change From Baseline in ECG; PR Interval, QRS Duration, QT Interval and QTcF
Baseline (Day 1), Day 14 and follow-up (up to Day 56)

Triplicate 12-lead ECGs were obtained using an ECG machine that automatically measured PR, QRS, QT, and QT interval corrected using Fridericia's formula (QTcF) intervals. Day 1 was considered as Baseline. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. All participants received both treatment interventions at the same time (on different skin sites), hence data for these participants were combined.

Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
Up to Day 56

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly/birth defect and other situations according to medical or scientific judgement or events associated with liver injury and impaired liver function.

Secondary Endpoints

Change From Baseline in Erythema, Scaling Hyperkeratosis, Edema/Infiltration, Dyspigmentation, Modified Revised Cutaneous Lupus Erythematosus Disease Area and Severity Index (RCLASI) Activity Score and Overall RCLASI Modified Score.
Baseline (Day 1), Day 14 and Day 28
Maximum Observed Concentration (Cmax) of GSK2646264 in Participants With Cutaneous Lupus Erythematosus (CLE)
Day 1 (pre-dose and 5 hours post-dose), Day 2 to Day 13, Day 14 (pre-dose), Day 21 to Day 27, Day 28 (post-dose), Day 29 to Day 42 and Follow-up (up to Day 56)
Time to Reach Maximum Observed Concentration (Tmax) of GSK2646264 in Participants With CLE
Day 1 (pre-dose and 5 hours post-dose), Day 2 to Day 13, Day 14 (pre-dose), Day 21 to Day 27, Day 28 (post-dose), Day 29 to Day 42 and Follow-up (up to Day 56)
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Group A1- Skin Sites A/C/D (A/P/A)EXPERIMENTALSkin areas A to E in group A are identified skin areas across the back of the subject. Subjects will be receiving GSK2646264 1% (A) for Area A- PV lesion, Placebo (P) for Area C- PV lesion and GSK2646264 1% for Area D- uninvolved skin once daily for 28 days according to randomisation. Skin areas B- PV lesion and E- uninvolved skin will not be assigned any treatment and will be used for the baseline biopsy.
Group A2- Skin Sites A/C/D (A/P/P)EXPERIMENTALSkin areas A to E in group A are identified skin areas across the back of the subject. Subjects will be receiving GSK2646264 1% for Area A- PV lesion, Placebo for Area C- PV lesion and Placebo for Area D- uninvolved skin once daily for 28 days according to randomisation. Skin areas B- PV lesion and E- uninvolved skin will not be assigned any treatment and will be used for the baseline biopsy.
Group A3- Skin Sites A/C/D (P/A/A)EXPERIMENTALSkin areas A to E in group A are identified skin areas across the back of the subject. Subjects will be receiving Placebo for Area A- PV lesion, GSK2646264 1% for Area C- PV lesion and GSK2646264 1% for Area D- uninvolved skin once daily for 28 days according to randomisation. Skin areas B- PV lesion and E- uninvolved skin will not be assigned any treatment and will be used for the baseline biopsy.
Group A4- Skin Sites A/C/D (P/A/P)EXPERIMENTALSkin areas A to E in group A are identified skin areas across the back of the subject. Subjects will be receiving Placebo for Area A- PV lesion, GSK2646264 1% for Area C- PV lesion and Placebo for Area D- uninvolved skin once daily for 28 days according to randomisation. Skin areas B- PV lesion and E- uninvolved skin will not be assigned any treatment and will be used for the baseline biopsy.
Group B1- Skin Sites F/ G (A/P)EXPERIMENTALIn group B, two chosen lesions will be labeled F and G based on size (F \>G). Subjects will be receiving GSK2646264 1% for lesion F and Placebo for lesion G once daily for 28 days according to randomisation. Skin area H- uninvolved skin will not be assigned any treatment and will be used for the baseline biopsy.
Group B2- Skin Sites F/ G (P/A)EXPERIMENTALIn group B, two chosen skin lesions will be labeled F and G based on size (F \>G). Subjects will be receiving Placebo for lesion F and GSK2646264 1% for lesion G once daily for 28 days according to randomisation. Skin area H- uninvolved skin will not be assigned any treatment and will be used for the baseline biopsy.

Interventions

NameTypeDescription
GSK2646264 1%DRUGA cream for topical application with a concentration of 1% GSK2646264.
PlaceboDRUGSubjects will receive matching Placebo topically.
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Eligibility Criteria

Age Range18 Years to 70 Years
SexALL
Healthy VolunteersNo
Study Sites5

Inclusion Criteria * Between 18 and 70 years of age inclusive, at the time of signing the informed consent. * Subject values for the following parameters thyroid-stimulating hormone (TSH), free thyroxine (T4), and free triiodothyronine (T3) within the normal range. * Subject has confirmed diagnosis...

Countries:Germany
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Frequently asked questions about GSK2646264 1%

What is GSK2646264 1% used for?

GSK2646264 1% is an investigational small molecule being developed for the treatment of cutaneous lupus erythematosus, a form of lupus that affects the skin. It is currently in Phase 1 clinical development and has not been approved by regulatory authorities.

Who makes GSK2646264 1%?

GSK2646264 1% is being developed by GSK plc, a global biopharmaceutical company listed on the stock exchange under the ticker GSK. The company is conducting clinical trials to evaluate the safety and efficacy of this investigational drug.

What phase is GSK2646264 1% in?

GSK2646264 1% is in Phase 1 clinical development. A Phase 1 trial has been completed, which involved 11 participants with cutaneous lupus erythematosus. The drug remains investigational and is not yet approved for any use.

What clinical trials is GSK2646264 1% in?

GSK2646264 1% has one completed clinical trial registered under NCT02927457, titled 'Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Clinical Effect of GSK2646264 in Cutaneous Lupus Erythematosus Subjects.' The study was a randomized, double-blind, controlled trial conducted in Germany with 11 participants.

Is GSK2646264 1% the same as GSK2646264?

GSK2646264 1% refers to a specific formulation or concentration of the investigational drug GSK2646264. The clinical trial NCT02927457 evaluates GSK2646264 in subjects with cutaneous lupus erythematosus, and the 1% designation indicates the concentration used in the study.