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Fig 1.

CONSORT flow diagram.

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Fig 2.

General design of chronic weight loss studies.

Baseline body weight and body composition measurements were made during the period Day -18 to -13 (left Black Arrow). Treatment with GSK457 was begun on Day -8 or -7 (Green Arrow). Subcutaneous exendin-4 AlbudAb dosing began on Day 0 (Red Arrow) and ended on Day 28 for the DIO study (right Black Arrow) and on Day 14 for the db/db study (middle Black Arrow); final body composition measurements were also made on that day. Blood was collected on the following day for serum chemistry, HbA1c and hormone analyses, and tissues were collected for histopathology (Blue Arrows).

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Fig 3.

Clinical Study Design Schematic.

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Table 1.

Clinical Study Design and Main Inclusion-Exclusion Criteria.

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Table 2.

Endpoints and Associated Procedures.

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Fig 4.

GSK457 + exendin-4 AlbudAb combination treatment returned DIO C57BL/6NTac mice to the body weight of age-matched lean control mice after 28 days.

GSK457 administration began on Day -7 (baseline) and exendin-4 AlbudAb SC dosing began on Day 0. An asterisk (*) indicates a significant difference from vehicle (p < 0.05). The small dots/dashed line indicates the additive weight loss.

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Fig 5.

GSK457 + exendin-4 AlbudAb combination treatment reduced glucose and HbA1c levels in db/db mice after 14 days.

GSK457 treatment began on Day -8 and exendin-4 AlbudAb SC dosing began on Day 0. Blood was collected on Day 15 to measure (A) serum glucose levels (mg/dL) and (B) HbA1c (change (Δ) in %, normalized to control). An asterisk (*) indicates a significant difference from vehicle (p < 0.05).

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Table 3.

Clinical Study: Demographic and Baseline Characteristics.

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Fig 6.

Mean weight, weighted mean glucose AUC (0–24 h), mean % HbA1c and mean fasting plasma glucose in T2D subjects taking liraglutide and GSK457 or placebo in Part B of the clinical study.

Panel A shows the mean weight (± SE) from the Screening visit to the Follow-up visit and it includes the 3-month liraglutide Stabilization period and the 6-week Treatment period. Panels B and C show the weighted mean glucose AUC (0–24 h) and % HbA1c (± SE), respectively, at Baseline (Day -1) and at the end of the 6-week Treatment period (Day 42). Panel D shows the mean fasting plasma glucose (± SE) from the safety labs from the Screening visit to the Follow-up visit and it includes the 3-month liraglutide Stabilization period and the 6-week Treatment period. In all panels, the GSK457 group is shown as red symbols and lines and the placebo group as blue symbols and lines.

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Fig 7.

Mean weight, weighted mean glucose AUC (0–24 h), mean % HbA1c and mean fasting plasma glucose in T2D subjects taking metformin and GSK457 or placebo in Part C of the clinical study.

Panel A shows the mean weight (± SE) from the Screening visit to the Follow-up visit and it includes the 1-month metformin Stabilization period and the 6-week Treatment period. Panels B and C show the weighted mean glucose AUC (0–24 h) and % HbA1c (± SE), respectively, at baseline (Day -1) and at the end of the 6-week Treatment period (Day 42). Panel D shows the mean fasting plasma glucose (± SE) from the safety labs from the Screening visit to the Follow-up visit and it includes the 1-month metformin Stabilization period and the 6-week Treatment period. In all panels, the GSK457 group is shown as red symbols and lines and the placebo group as blue symbols and lines.

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Table 4.

Adverse Events during the Treatment Period Reported by More than 1 Subject.

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