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GSK2982772 Modified Release

Phase 1

Autoimmune Diseases | Small molecule | Immunology |GSK plc|Last Updated: Aug 13, 2021

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Trial Design

CONTROLLED
Total Trials2
Total Enrollment78

FDA Designations

No designations recorded

Clinical trial landscape

GSK2982772 Modified Release · 2 trials · 1 indication

Phase 1 2
NCT03649412A Study to Investigate the Pharmacokinetics (PK) of Modified Release (MR) Prototype Coated Tablet Formulations of GSK2982772Autoimmune Diseases
COMPLETED33 Analytics
NCT03266172A Study to Compare the Pharmacokinetics (PK) of GSK2982772 Following Administration of Different Modified Release (MR) Formulations in Capsule and MR Tablet Formulations Relative to an Immediate Release (IR) Tablet Formulation and to Check the PK of MR Formulation in Capsule Following Repeat DosesAutoimmune Diseases
COMPLETED45 Analytics
PHASE1COMPLETED
A Study to Investigate the Pharmacokinetics (PK) of Modified Release (MR) Prototype Coated Tablet Formulations of GSK2982772
Autoimmune Diseases
NCT0364941233
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PHASE1COMPLETED
A Study to Compare the Pharmacokinetics (PK) of GSK2982772 Following Administration of Different Modified Release (MR) Formulations in Capsule and MR Tablet Formulations Relative to an Immediate Release (IR) Tablet Formulation and to Check the PK of MR Formulation in Capsule Following Repeat Doses
Autoimmune Diseases
NCT0326617245
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Study Endpoints

Primary Endpoints

Part A: Area Under the Curve From Time Zero to Infinity (AUC[0-inf]) of GSK2982772 240 mg in IR Formulation
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected at indicated time points for pharmacokinetic (PK) analysis. PK parameters were analyzed using standard non-compartmental analysis. Participants in the 'Safety Population (all participants who received at least one dose of study treatment)' for whom a PK sample was obtained and analyzed were part of PK Population.

Part A: AUC(0-inf) of GSK2982772 240 mg in MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points for PK analysis. PK parameters were analyzed using standard non-compartmental analysis.

Part A: AUC(0-inf) of GSK2982772 240 mg in MR Coated Tablet Formulation After High-fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points for PK analysis. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Area Under the Curve From Time Zero to the Last Measurable Concentration (AUC[0-t]) of GSK2982772 240 mg for IR Formulation
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t). PK parameters were analyzed using standard non-compartmental analysis.

Part A: AUC(0-t) of GSK2982772 240 mg for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t). PK parameters were analyzed using standard non-compartmental analysis.

Part A: AUC(0-t) of GSK2982772 240 mg for MR Coated Tablet Formulation After High-fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t). PK parameters were analyzed using standard non-compartmental analysis.

Part A: Area Under the Curve From Time Zero to 24 Hours (AUC[0-24]) of GSK2982772 240 mg for IR Formulation
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24). PK parameters were analyzed using standard non-compartmental analysis.

Part A: AUC(0-24) of GSK2982772 240 mg for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24). PK parameters were analyzed using standard non-compartmental analysis.

Part A: AUC(0-24) of GSK2982772 240 mg for MR Coated Tablet Formulation After High-fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24). PK parameters were analyzed using standard non-compartmental analysis.

Part A: Maximum Observed Concentration (Cmax) of GSK2982772 240 mg for IR Formulation
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Cmax. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Cmax of GSK2982772 240 mg for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Cmax. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Cmax of GSK2982772 240 mg for MR Coated Tablet Formulation After High-fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Cmax. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Concentration at 24 Hours Post-dose (C24h) of GSK2982772 240 mg for IR Formulation
24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for C24h. PK parameters were analyzed using standard non-compartmental analysis.

Part A: C24h of GSK2982772 240 mg for MR Coated Tablet Formulation
24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for C24h. PK parameters were analyzed using standard non-compartmental analysis.

Part A: C24h of GSK2982772 240 mg for MR Coated Tablet Formulation After High-fat Breakfast
24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for C24h. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Time to Cmax (Tmax) of GSK2982772 240 mg for IR Formulation
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Tmax. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Tmax of GSK2982772 240 mg for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Tmax. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Tmax of GSK2982772 240 mg for MR Coated Tablet Formulation After High-fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Tmax. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Terminal Half-life (t1/2) of GSK2982772 240 mg for IR Formulation
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for t1/2. PK parameters were analyzed using standard non-compartmental analysis.

Part A: t1/2 of GSK2982772 240 mg for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours

Blood samples were collected from participants at indicated time points and analyzed for t1/2. PK parameters were analyzed using standard non-compartmental analysis.

Part A: t1/2 of GSK2982772 240 mg for MR Coated Tablet Formulation After High-fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours

Blood samples were collected from participants at indicated time points and analyzed for t1/2. PK parameters were analyzed using standard non-compartmental analysis.

Part B: AUC(0-inf) of GSK2982772 for MR Coated Tablet Formulation After a High Fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC(0-inf). PK parameters were analyzed using standard non-compartmental analysis.

Part B: AUC(0-t) of GSK2982772 for MR Coated Tablet Formulation After a High Fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC(0-t). PK parameters were analyzed using standard non-compartmental analysis.

Part B: Cmax of GSK2982772 for MR Coated Tablet Formulation After a High Fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose post-dose

Blood samples were collected from participants at indicated time points and analyzed for Cmax. PK parameters were analyzed using standard non-compartmental analysis.

Part B: C24h of GSK2982772 for MR Coated Tablet Formulation After a High Fat Breakfast
24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for C24h. PK parameters were analyzed using standard non-compartmental analysis.

Part B: Tmax of GSK2982772 for MR Coated Tablet Formulation After a High Fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Tmax. PK parameters were analyzed using standard non-compartmental analysis.

Part B: t1/2 of GSK2982772 for MR Coated Tablet Formulation After a High Fat Breakfast
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for t1/2. PK parameters were analyzed using standard non-compartmental analysis.

Part A: Relative Bioavailability in Fed Versus Fasted Conditions (FrelFE) Based on AUC(0-inf) of GSK2982772 for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of FrelFE based on AUC of GSK2982772. Frel for AUC(0-inf) was calculated as Geometric mean of AUC(0-inf) of MR Fed/ Geometric mean of AUC(0-inf) of MR Fasted multiplied by 100.

Part A: FrelFE Based on AUC(0-t) of GSK2982772 for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of FrelFE based on AUC of GSK2982772. Frel for AUC(0-t) was calculated as Geometric mean of AUC(0-t) of MR Fed/Geometric mean of AUC(0-t) of MR Fasted multiplied by 100.

Part A: FrelFE Based on Cmax of GSK2982772 for MR Coated Tablet Formulation
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of FrelFE based on Cmax of GSK2982772. Frel for Cmax was calculated as Geometric mean of Cmax of MR Fed/Geometric mean of Cmax of MR Fasted multiplied by 100.

Part B: FrelFE of GSK2982772 Based on AUC(0-inf) for MR Coated Tablet Formulation in Fed vs Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of FrelFE based on AUC(0-inf) of GSK2982772. Frel for AUC(0-inf) was calculated as Geometric mean of AUC(0-inf) of MR Fed/ Geometric mean of AUC(0-inf) of MR Fasted multiplied by 100.

Part B: FrelFE of GSK2982772 Based on AUC (0-t) for MR Coated Tablet Formulation in Fed vs Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of FrelFE based on AUC (0-t) of GSK2982772. FrelFE for AUC (0-t) was calculated as Geometric mean of AUC (0-t) of MR Fed/ Geometric mean of AUC (0-t) of MR Fasted multiplied by 100.

Part B: FrelFE of GSK2982772 Based on Cmax for MR Coated Tablet Formulation in Fed vs Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of FrelFE based on Cmax of GSK2982772. FrelFE for Cmax was calculated as Geometric mean of Cmax of MR Fed/ Geometric mean of Cmax of MR Fasted multiplied by 100.

Part B: Frel of GSK2982772 Based on AUC (0-inf) for MR Coated Tablet Formulation in Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of Frel (dose) based on AUC (0-inf) of GSK2982772. Frel (dose) for AUC (0-inf) was calculated as Geometric mean of AUC (0-inf) of MR formulation (test dose) Fasted/ Geometric mean of AUC (0-inf) of MR Fasted formulation (reference dose) multiplied by 100.

Part B: Frel of GSK2982772 Based on AUC (0-t) for MR Coated Tablet Formulation in Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of Frel (dose) based on AUC(0-t) of GSK2982772. Frel (dose) for AUC(0-t) was calculated as Geometric mean of AUC(0-t) of MR formulation (test dose) Fasted/ Geometric mean of AUC(0-t) of MR Fasted formulation (reference dose) multiplied by 100.

Part B: Frel of GSK2982772 Based on AUC (0-24) for MR Coated Tablet Formulation in Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of Frel (dose) based on AUC(0-24) of GSK2982772. Frel (dose) for AUC(0-24) was calculated as Geometric mean of AUC(0-24) of MR formulation (test dose) Fasted/Geometric mean of AUC(0-24) of MR Fasted formulation (reference dose) multiplied by 100.

Part B: Frel of GSK2982772 Based on Cmax for MR Coated Tablet Formulation in Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of Frel dose. Frel for Cmax was calculated as Geometric mean of Cmax of MR formulation (test) Fasted/ Geometric mean of Cmax of MR Fasted Formulation (reference dose) multiplied by 100.

Part A: Relative Bioavailability (Frelformulation) Based on AUC (0-inf) of GSK2982772 240 mg
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours post-dose

Blood samples were collected at indicated time points for analysis of Frelformulation based on AUC(0-inf) of GSK2982772 in fasted state. Frel for AUC(0-inf) was calculated as Geometric mean of AUC(0-inf) of MR formulation (test) Fasted/ Geometric mean of AUC(0-inf) of Fasted of IR Formulation (reference) multiplied by 100.

Part A: Frelformulation Based on AUC (0-t) of GSK2982772 for MR Coated Tablet Formulation (240 mg)
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours

Blood samples were collected at indicated time points for analysis of Frelformulation based on AUC of GSK2982772 in fasted state. Frel for AUC (0-t) was calculated as Geometric mean of AUC(0-t) of MR Fasted formulation (test) / Geometric mean of AUC(0-t) of Fasted of IR Formulation (reference) multiplied by 100.

Part A: Frelformulation Based on AUC(0-24) of GSK2982772 for MR Coated Tablet Formulation (240 mg)
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, and 24 hours

Blood samples were collected at indicated time points for analysis of Frelformulation based on AUC of GSK2982772 in fasted state. Frel for AUC(0-24) was calculated as Geometric mean of AUC(0-24) of MR Fasted formulation (test) / Geometric mean of AUC(0-24) of Fasted of IR Formulation (reference) multiplied by 100.

Part A: Frelformulation Based on Cmax of GSK2982772 for MR Coated Tablet Formulation (240 mg)
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 36 and 48 hours

Blood samples were collected at indicated time points for analysis of Frelformulation based on Cmax of GSK2982772 in fasted state. Frel for Cmax was calculated as Geometric mean of Cmax of MR Fasted formulation (test) / Geometric mean of Cmax of Fasted Formulation of IR formulation (reference) multiplied by 100.

Area Under the Curve From Time Zero to Infinity (AUC[0-inf]) of GSK2982772 in IR Formulation: Part A
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-inf). Participants in the 'Safety Population' for whom a Pharmacokinetic (PK) sample was obtained and analyzed were part of PK Population.

AUC(0-inf) of GSK2982772 in MT Formulation :Part A
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-inf).

Area Under the Curve From Time Zero to the Last Measurable Concentration (AUC[0-t]) of GSK2982772 in IR Formulation : Part A
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t)

AUC(0-t) of GSK2982772 in MT Formulation: Part A
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t)

Area Under the Curve From Time Zero to 24 Hours (AUC[0-24]) of GSK2982772 in IR Formulation: Part A
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24)

AUC(0-24) of GSK2982772 in MT Formulation: Part A
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24)

Area Under the Curve From Time Zero to 12 Hours (AUC[0-12]) of GSK2982772 in IR Formulation: Part A
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-12)

AUC(0-12) of GSK2982772 in MT Formulation: Part A
Pre-dose, 2, 4, 6, 8, 10, and 12 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for AUC (0-12)

Maximum Observed Concentration (Cmax) of GSK2982772 in IR Formulation: Part A
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Cmax

Cmax of GSK2982772 in MT Formulation: Part A
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for Cmax

Concentration at 12 Hours Post-dose (C12hour) of GSK2982772 in Part A
12 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for C12hour.

Concentration at 24 Hours Post-dose (C24hour) of GSK2982772 in Part A
24 hours post-dose

Blood samples were collected from participants at indicated time points and analyzed for C24hour.

Relative Bioavailability (Frelformulation) Based on AUC (0-inf) of GSK2982772 in Part A
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose (reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose (test)

Blood samples were collected at indicated time points for analysis of Frelformulation. Frelformulation for AUC (0-inf) was calculated as Geometric mean of AUC (0-inf) of MT (test) / Geometric mean of AUC (0-inf) of IR Formulation (reference) multiplied by 100.

Frelformulation Based on AUC (0-24) of GSK2982772 in Part A
Pre-dose 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose (reference); Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, and 24 hours post-dose (test)

Blood samples were collected at indicated time points for analysis of Frelformulation. Frelformulation for AUC (0-24) was calculated as Geometric mean of AUC (0-24) of MT (test) / Geometric mean of AUC (0-24) of IR Formulation (reference) multiplied by 100.

Frelformulation Based on Cmax of GSK2982772 in Part A
Pre-dose,0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose(reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose(test)

Blood samples were collected at indicated time points for analysis of Frelformulation. Frel was calculated as Geometric mean of Cmax of MT Formulation (test)/ Geometric mean of Cmax of IR Formulation (reference) multiplied by 100.

Ratio of Cmax to C12hour of GSK2982772 in IR Formulation: Part A
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hour has been presented.

Ratio of Cmax to C12hour of GSK2982772 in MT Formulation: Part A
Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hour has been presented.

Ratio of Cmax to C24hour of GSK2982772 in IR Formulation: Part A
Pre-dose 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hour has been presented.

Ratio of Cmax to C24hour of GSK2982772 in MT Formulation: Part A
Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hour has been presented.

Time to Cmax (Tmax) of GSK2982772 in IR Formulation: Part A
Pre-dose 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of Tmax.

Tmax of GSK2982772 in MT Formulation: Part A
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of Tmax.

AUC(0-inf) of GSK2982772 for IR Formulation in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-inf)

AUC(0-inf) of GSK2982772 for MM Formulation in Part C: Fasted State
Pre-dose, 2, 3, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-inf).

AUC(0-t) of GSK2982772 for IR Formulation in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-t).

AUC(0-t) of GSK2982772 for MM Formulation in Part C: Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-t).

AUC(0-24) of GSK2982772 for IR Formulation in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-24)

AUC(0-24) of GSK2982772 for MM Formulation in Part C: Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-24)

AUC (0-12) of GSK2982772 for IR Formulation in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, and 12 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-12)

AUC (0-12) of GSK2982772 for MM Formulation in Part C: Fasted State
Pre-dose, 2, 4, 6, 8, 10, and 12 hours post-dose

Blood samples were collected at indicated time points for analysis of AUC (0-12)

Cmax of GSK2982772 for IR Formulation in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of Cmax

Cmax of GSK2982772 for MM Formulation in Part C: Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of Cmax

C12 of GSK2982772 in Part C: Fasted State
12 hours post-dose

Blood samples was collected at indicated time point for analysis of C12

C24 of GSK2982772 in Part C: Fasted State
24 hours post-dose

Blood samples was collected at indicated time point for analysis of C24

Ratio of Cmax to C12hour of GSK2982772 for IR Formulation in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hours has been presented.

Ratio of Cmax to C12hour of GSK2982772 for MM Formulation in Part C: Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hours has been presented.

Ratio of Cmax to C24hour of GSK2982772 for IR Formulation in Part C: Fasted State
Pre-dose,0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hours has been presented.

Ratio of Cmax to C24hour of GSK2982772 for MM Formulation in Part C: Fasted State
Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose

Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hours has been presented.

Frelformulation Based on AUC (0-t) of GSK2982772 in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose(reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose(test)

Blood samples were collected at indicated time points for analysis of Frelformulation. Frel for AUC (0-t) was calculated as Geometric mean of AUC (0-t) of MM formulation (test) / Geometric mean of AUC (0-t) of IR Formulation (reference) multiplied by 100.

Frelformulation Based on AUC (0-24) of GSK2982772 in Part C: Fasted State
Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose(reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours post-dose(test)

Blood samples were collected at indicated time points for analysis of Frelformulation. Frel for AUC (0-24) was calculated as Geometric mean of AUC (0-24) of MM Fasted formulation (test) / Geometric mean of AUC (0-24) of IR Formulation (reference) multiplied by 100.

Secondary Endpoints

Part A: Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs)
Up to Day 67
Part A: Number of Participants With Emergent Clinical Chemistry Results by Potential Clinical Importance (PCI) Criteria
Up to Day 67
Part A: Number of Participants With Emergent Hematology Results by Potential Clinical Importance Criteria
Up to Day 67
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Subjects in Part AEXPERIMENTALSubjects in Part A will receive GSK2982772 MR (Period 1, 3, 4, 5 and 6) and GSK2982772 IR (Period 2).
Subjects in Part BEXPERIMENTALSubjects in Part B will receive GSK2982772 MR.
Subjects in Part CEXPERIMENTALSubjects in Part C will receive GSK2982772 MR (Period 1, 3, 4, 5 and 6) and GSK2982772 IR (Period 2)

Interventions

NameTypeDescription
GSK2982772 Modified ReleaseDRUGGSK2982772 MR will be available as MR prototype coated tablet with unit dose strength of 240 mg in Part A. In Part B, GSK2982772 MR prototype coated tablet with unit dose strength of 120 mg (may be changed following interim review of Part B) will be administered by subjects. GSK2982772 MR will be administered orally with 240 milliliter (mL) of water.
GSK2982772 Immediate ReleaseDRUGIn part A, GSK2982772 IR tablet will be available with unit dose strength of 30 mg and the total dose administered by subjects will be 240 mg (8 tablets of dose strength 30 mg) orally with 240 mL of water
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Eligibility Criteria

Age Range18 Years to 65 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Subject at the time of participation must be 18 to 65 years of age. * Subjects who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring. * Body weight greater than or equal to 50 kilog...

Countries:United Kingdom
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Frequently asked questions about GSK2982772 Modified Release

What is GSK2982772 Modified Release used for?

GSK2982772 Modified Release is an investigational small molecule being developed for autoimmune diseases. It is a modified release formulation of GSK2982772, designed to alter the drug's release profile compared to an immediate release tablet. The drug is in Phase 1 clinical development and is not yet approved.

Who makes GSK2982772 Modified Release?

GSK2982772 Modified Release 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 pharmacokinetics of this modified release formulation in healthy volunteers.

What phase is GSK2982772 Modified Release in?

GSK2982772 Modified Release is in Phase 1 clinical development. Two Phase 1 trials have been completed, both focusing on pharmacokinetic comparisons of different modified release formulations. The drug remains investigational and has not received regulatory approval for any indication.

What clinical trials is GSK2982772 Modified Release in?

GSK2982772 Modified Release has been studied in two completed Phase 1 trials: NCT03266172, which compared the pharmacokinetics of modified release capsule and tablet formulations relative to an immediate release tablet, and NCT03649412, which investigated modified release prototype coated tablet formulations. Both trials enrolled healthy volunteers in the United Kingdom.

Is GSK2982772 Modified Release the same as GSK2982772?

GSK2982772 Modified Release is a specific formulation of the drug GSK2982772, designed to modify its release characteristics. While the active ingredient is the same, the modified release version is being studied separately to evaluate its pharmacokinetic profile compared to the immediate release formulation.