Trial Outcomes & Findings for Bioequivalence Study of Saxagliptin and Glucophage Combination Formulations in Healthy Subjects (A) (NCT NCT00899470)
NCT ID: NCT00899470
Last Updated: 2015-06-01
Results Overview
Cmax of single-dose saxagliptin (2.5 mg), either coadministered with metformin IR (500 mg), or administered as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
24 participants
Primary outcome timeframe
Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hr
Results posted on
2015-06-01
Participant Flow
85 participants were enrolled and 24 were treated on study. 61 participants discontinued before randomization and treatment due to: no longer meeting study criteria (n=36), withdraw of consent (n=3), study was full (n=15), participant did not call for results (n=1), completed alternate status (n=5), or did not show for check-up (n=1)
Participant milestones
| Measure |
S+M (Fasted)> S/M (Fed)> S/M (Fasted)>S+M (Fed)
Participants were randomized to receive oral co-administration of a 2.5 mg tablet of saxagliptin plus a 500 mg tablet of metformin immediate release (IR) under fasted conditions (S + M \[fasted\]) followed by a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions (S/M \[fed\]) followed by S/M under fasting conditions (S/M \[fasted\]) followed by S + M under fed conditions (S + M \[fed\])
|
S/M (Fasted)> S+M (Fasted)> S+M (Fed)> S/M (Fed)
Participants were randomized to receive S/M (fasted) followed by S + M (fasted) followed by S + M (fed) followed by S/M (fed)
|
S+M (Fed)> S/M (Fasted) >S/M (Fed)> S+M (Fasted)
Participants were randomized to receive S + M (fed) followed by S/M (fasted) followed by S/M (fed) followed by S+M (fasted)
|
S/M (Fed)> S+M (Fed)> S+M (Fasted)> S/M (Fasted)
Participants were randomized to receive S/M (fed) followed by S+M (fed) followed by S+M (fasted) followed by S/M (fasted)
|
|---|---|---|---|---|
|
First Therapy
STARTED
|
6
|
6
|
6
|
6
|
|
First Therapy
COMPLETED
|
6
|
6
|
6
|
6
|
|
First Therapy
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
First Washout Period
STARTED
|
6
|
6
|
6
|
6
|
|
First Washout Period
COMPLETED
|
6
|
6
|
6
|
6
|
|
First Washout Period
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Second Therapy
STARTED
|
6
|
6
|
6
|
6
|
|
Second Therapy
COMPLETED
|
6
|
6
|
6
|
6
|
|
Second Therapy
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Second Washout
STARTED
|
6
|
6
|
6
|
6
|
|
Second Washout
COMPLETED
|
6
|
6
|
6
|
6
|
|
Second Washout
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Third Therapy
STARTED
|
6
|
6
|
6
|
6
|
|
Third Therapy
COMPLETED
|
6
|
6
|
6
|
6
|
|
Third Therapy
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Third Washout
STARTED
|
6
|
6
|
6
|
6
|
|
Third Washout
COMPLETED
|
6
|
6
|
6
|
6
|
|
Third Washout
NOT COMPLETED
|
0
|
0
|
0
|
0
|
|
Fourth Therapy
STARTED
|
6
|
6
|
6
|
6
|
|
Fourth Therapy
COMPLETED
|
6
|
6
|
6
|
6
|
|
Fourth Therapy
NOT COMPLETED
|
0
|
0
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Bioequivalence Study of Saxagliptin and Glucophage Combination Formulations in Healthy Subjects (A)
Baseline characteristics by cohort
| Measure |
All Treated Participants
n=24 Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|
|
Age, Continuous
|
28 years
STANDARD_DEVIATION 7 • n=5 Participants
|
|
Sex: Female, Male
Female
|
7 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
17 Participants
n=5 Participants
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
Cmax of single-dose saxagliptin (2.5 mg), either coadministered with metformin IR (500 mg), or administered as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Saxagliptin Mean Maximum Observed Plasma Concentration (Cmax)
|
8.57 ng/mL
Standard Deviation 2.572
|
8.61 ng/mL
Standard Deviation 2.266
|
11.36 ng/mL
Standard Deviation 2.875
|
11.51 ng/mL
Standard Deviation 3.781
|
—
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
AUC (0-T) for single-dose saxagliptin (2.5 mg), either coadministered with metformin IR (500 mg), or administered as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Saxagliptin Mean Area Under the Plasma Concentration Time Curve From Time Zero To Time of Last Quantifiable Concentration (AUC [0-T]}
|
48.57 ng*h/mL
Standard Deviation 12.864
|
49.69 ng*h/mL
Standard Deviation 12.330
|
54.59 ng*h/mL
Standard Deviation 12.407
|
55.83 ng*h/mL
Standard Deviation 12.735
|
—
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
AUC (0-T) for single-dose saxagliptin (2.5 mg), either coadministered with metformin IR (500 mg), or administered as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Saxagliptin Mean Area Under the Plasma Concentration Time Curve From Time Zero To Infinity (AUC [0-INF])
|
50.66 ng*h/mL
Standard Deviation 13.322
|
51.74 ng*h/mL
Standard Deviation 12.736
|
56.56 ng*h/mL
Standard Deviation 12.778
|
57.86 ng*h/mL
Standard Deviation 13.222
|
—
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
T-half and T-max for single-dose saxagliptin (2.5 mg), either coadministered with metformin IR (500 mg) or administered as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Saxagliptin Mean Plasma Half-life (T-half) and Mean Time of Maximum Observed Plasma Concentration (T-max)
T-max
|
1.78 hours
Standard Deviation 1.210
|
1.23 hours
Standard Deviation 0.829
|
1.37 hours
Standard Deviation 0.842
|
1.42 hours
Standard Deviation 0.862
|
—
|
|
Saxagliptin Mean Plasma Half-life (T-half) and Mean Time of Maximum Observed Plasma Concentration (T-max)
T-half
|
5.86 hours
Standard Deviation 1.367
|
5.55 hours
Standard Deviation 1.135
|
5.75 hours
Standard Deviation 1.119
|
5.72 hours
Standard Deviation 1.146
|
—
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
Cmax of single-dose metformin IR (500 mg), either coadministered with saxagliptin (2.5 mg) or administerd as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Metformin Mean Cmax
|
1030.22 ng/mL
Standard Deviation 293.970
|
1042.52 ng/mL
Standard Deviation 314.365
|
993.32 ng/mL
Standard Deviation 198.653
|
1027.70 ng/mL
Standard Deviation 208.974
|
—
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
AUC (0-T for single-dose metformin (500 mg), either coadministered with saxagliptin (2.5 mg) or administerd as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Metformin Mean AUC (0-T)
|
7403.01 ng*h/mL
Standard Deviation 1822.749
|
7575.23 ng*h/mL
Standard Deviation 1832.807
|
7176.78 ng*h/mL
Standard Deviation 1216.854
|
7502.46 ng*h/mL
Standard Deviation 1402.256
|
—
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
AUC (0-INF) for single-dose metformin IR (500 mg), either coadministered with saxagliptin (2.5 mg) or administerd as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Metformin Mean AUC(0-INF)
|
7494.67 ng*h/mL
Standard Deviation 1792.921
|
7689.57 ng*h/mL
Standard Deviation 1761.119
|
7246.89 ng*h/mL
Standard Deviation 1215.675
|
7574.17 ng*h/mL
Standard Deviation 1397.335
|
—
|
PRIMARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
T-half and T-max for single-dose metformin IR (500 mg), either coadministered with saxagliptin (2.5 mg), or administerd as FDC 2.5 mg saxagliptin/500 mg metformin IR, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Metformin T-half and T-max
T-Half
|
9.87 hours
Standard Deviation 5.561
|
12.03 hours
Standard Deviation 9.014
|
8.62 hours
Standard Deviation 3.069
|
8.61 hours
Standard Deviation 3.288
|
—
|
|
Metformin T-half and T-max
T-max
|
3.18 hours
Standard Deviation 0.919
|
3.08 hours
Standard Deviation 0.762
|
3.96 hours
Standard Deviation 0.204
|
3.87 hours
Standard Deviation 0.680
|
—
|
SECONDARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
Cmax of the saxagliptin metabolite BMS-510849, following single-dose saxagliptin (2.5 mg) coadministered with metformin IR (500 mg) or administered as an FDC 2.5 mg saxagliptin/500 mg metformin IR tablet, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
BMS-510849 Mean Cmax
|
16.32 ng/mL
Standard Deviation 5.094
|
16.10 ng/mL
Standard Deviation 4.967
|
18.40 ng/mL
Standard Deviation 4.140
|
18.72 ng/mL
Standard Deviation 4.280
|
—
|
SECONDARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
AUC (0-T) for the saxagliptin metabolite BMS-510849, following single-dose saxagliptin (2.5 mg) coadministered with metformin IR (500 mg) or administration as an FDC 2.5 mg saxagliptin/500 mg metformin IR tablet, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
BMS-510849 Mean AUC (0-T)
|
112.35 ng*h/mL
Standard Deviation 20.053
|
113.87 ng*h/mL
Standard Deviation 24.141
|
120.31 ng*h/mL
Standard Deviation 22.719
|
123.05 ng*h/mL
Standard Deviation 24.821
|
—
|
SECONDARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
AUC (0-T)= for the saxagliptin metabolite BMS-510849, following single-dose saxagliptin (2.5 mg) coadministered with metformin IR (500 mg) or administered as an FDC 2.5 mg saxagliptin/500 mg metformin IR tablet, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
BMS-510849 Mean AUC (0-INF)
|
120.72 ng*h/mL
Standard Deviation 19.826
|
122.74 ng*h/mL
Standard Deviation 24.805
|
129.02 ng*h/mL
Standard Deviation 22.988
|
131.88 ng*h/mL
Standard Deviation 25.908
|
—
|
SECONDARY outcome
Timeframe: Day 1: 0 hr, 0.25 hr, 0.5 hr, 0.75 hr, 1 hr, 1.5 hr, 2 hr, 3 hr, 4 hr, 6 hr, 8 hr, 12 hr, 18 hr, Day 2: 0 hr, 12 hr, Day 3: 0 hrPopulation: PK data set, all participants who received study drug
T-half and Tmax of the saxagliptin metabolite BMS-510849, following single-dose saxagliptin (2.5 mg) coadministered with metformin IR (500 mg) or administerd as an FDC 2.5 mg saxagliptin/500 mg metformin IR tablet, under fasted and fed conditions.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
BMS-510849 Mean T-half and T-max
T-max
|
2.40 hours
Standard Deviation 0.965
|
2.30 hours
Standard Deviation 0.965
|
2.35 hours
Standard Deviation 0.774
|
2.53 hours
Standard Deviation 0.727
|
—
|
|
BMS-510849 Mean T-half and T-max
T-Half
|
6.53 hours
Standard Deviation 1.346
|
6.93 hours
Standard Deviation 1.284
|
6.73 hours
Standard Deviation 1.380
|
6.62 hours
Standard Deviation 1.238
|
—
|
SECONDARY outcome
Timeframe: From Day 1 through Day 45, including up to 56 days after last dose of study medicationPopulation: All Treated Participants
AE=any new untoward medical occurrence or worsening of a pre-existing medical condition which does not necessarily have a causal relationship with this treatment. SAE=any untoward medical occurrence that at any dose: results in death, is life-threatening, requires inpatient hospitalization or causes prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, results in development of drug dependency or drug abuse, is an important medical event.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
n=24 Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Number of Participants With at Least 1 Adverse Event (AE), Death, Serious AE (SAE), or AEs Leading to Discontinuation
Participants with at least 1 AE
|
6 participants
|
3 participants
|
4 participants
|
1 participants
|
7 participants
|
|
Number of Participants With at Least 1 Adverse Event (AE), Death, Serious AE (SAE), or AEs Leading to Discontinuation
Death
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
|
Number of Participants With at Least 1 Adverse Event (AE), Death, Serious AE (SAE), or AEs Leading to Discontinuation
SAE
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
|
Number of Participants With at Least 1 Adverse Event (AE), Death, Serious AE (SAE), or AEs Leading to Discontinuation
AE leading to discontinuation
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
SECONDARY outcome
Timeframe: From Day 1 through Day 45, including up to 56 days after last dose of study medicationPopulation: All Treated Participants
High=greater than Upper Normal Limit (ULN), Low=lower than Lower Normal Limit (LLN). LLN/ULN= Leukocytes: \<0.9 x LLN/ \>1.2 x ULN; blood urea nitrogen (BUN): \>1.1 x ULN; creatinine: \>1.33 x BL; phosphorous (P): \<0.75 x LLN/ \>1.2 5 x ULN; creatinine kinase (CK): \>1.5 x ULN; urine blood=use ≥2 x BL if value ≥2+ or BL1+
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
n=24 Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Number of Participants With Laboratory Marked Abnormalities
High leukocytes
|
0 participants
|
0 participants
|
1 participants
|
0 participants
|
1 participants
|
|
Number of Participants With Laboratory Marked Abnormalities
High BUN
|
0 participants
|
1 participants
|
0 participants
|
0 participants
|
1 participants
|
|
Number of Participants With Laboratory Marked Abnormalities
High creatinine
|
0 participants
|
0 participants
|
1 participants
|
0 participants
|
1 participants
|
|
Number of Participants With Laboratory Marked Abnormalities
Low phosphorus
|
0 participants
|
1 participants
|
0 participants
|
0 participants
|
1 participants
|
|
Number of Participants With Laboratory Marked Abnormalities
High CK
|
0 participants
|
0 participants
|
1 participants
|
0 participants
|
1 participants
|
|
Number of Participants With Laboratory Marked Abnormalities
High urine blood
|
0 participants
|
1 participants
|
0 participants
|
0 participants
|
1 participants
|
SECONDARY outcome
Timeframe: Period 1 Day 1, Period 2 Day 1, Period 3 Day 1, Period 4 Day 1, Period 4 Day 3Population: All Treated Participants
PR interval, QRS complex, width of QRS, QT interval, and QT corrected for heart rate adjusting for heart rate using either Bazett formula or Fridericia formula were measured. ECG abnormalities were judged to be of medical importance by the Investigator.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Number of Participants With Clinically Relevant Electrocardiogram (ECG) Abnormalities
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
—
|
SECONDARY outcome
Timeframe: Period 1 Day 1, Period 2 Day 1, Period 3 Day 1, Period 4 Day 1, Period 4 Day 3Population: All Treated Participants
Mean systolic and diastolic blood pressure, heart rate, respiration, and temperature were assessed.Vital sign abnormalities abnormalities were judged to be of medical importance by the Investigator.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Number of Participants With Clinically Relevant Vital Sign Abnormalities
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
—
|
SECONDARY outcome
Timeframe: Screen, Period 1 Day -1, prior to dischargePopulation: All Treated Participants
A physical examination was conducted which included height and weight measurements, from which the Body Mass Index was determined. Physical examination abnormalities were judged to be of medical importance by the Investigator.
Outcome measures
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 Participants
Participants received a single oral dose of a fixed-dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 Participants
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 Participants
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
All Treated Participants
Participants were randomized to received 1 of 4 treatments 1)oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions, 2) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions, 3) oral co-administration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fed conditions, or 4) a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions. Participants received all 4 treatments in 1 of 4 sequences: 1-4-2-3, 2-1-3-4, 3-2-4-1, or 4-3-1-2, with a washout period between treatments of at least 1 week.
|
|---|---|---|---|---|---|
|
Number of Participant With Clinically Relevant Physical Examination Abnormalities
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
—
|
Adverse Events
Coadministration of Saxagliptin and Metformin IR (Fasted)
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Saxagliptin/Metformin FDC (Fasted)
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Coadministration of Saxagliptin and Metformin IR (Fed)
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Saxagliptin/Metformin FDC (Fed)
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Coadministration of Saxagliptin and Metformin IR (Fasted)
n=24 participants at risk
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin immediate release (IR) under fasted conditions
|
Saxagliptin/Metformin FDC (Fasted)
n=24 participants at risk
Participants received a single oral dose of a fixed dose combination (FDC) tablet of 2.5 mg saxagliptin/500 mg metformin IR under fasting conditions
|
Coadministration of Saxagliptin and Metformin IR (Fed)
n=24 participants at risk
Participants received oral coadministration of a 2.5 mg tablet of saxagliptin and a 500 mg tablet of metformin IR under fed conditions
|
Saxagliptin/Metformin FDC (Fed)
n=24 participants at risk
Participants received a single oral dose of an FDC tablet of 2.5 mg saxagliptin/500 mg metformin IR under fed conditions
|
|---|---|---|---|---|
|
Cardiac disorders
PALPITATIONS
|
0.00%
0/24
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
|
Nervous system disorders
HEADACHE
|
4.2%
1/24
|
4.2%
1/24
|
0.00%
0/24
|
4.2%
1/24
|
|
Nervous system disorders
DIZZINESS
|
0.00%
0/24
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
|
Gastrointestinal disorders
NAUSEA
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
0.00%
0/24
|
|
Gastrointestinal disorders
DIARRHOEA
|
0.00%
0/24
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
|
Gastrointestinal disorders
ABDOMINAL PAIN UPPER
|
4.2%
1/24
|
0.00%
0/24
|
0.00%
0/24
|
0.00%
0/24
|
|
Gastrointestinal disorders
GASTROINTESTINAL PAIN
|
0.00%
0/24
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
|
Ear and labyrinth disorders
EAR PAIN
|
0.00%
0/24
|
0.00%
0/24
|
0.00%
0/24
|
4.2%
1/24
|
|
Renal and urinary disorders
NEPHROLITHIASIS
|
4.2%
1/24
|
0.00%
0/24
|
0.00%
0/24
|
0.00%
0/24
|
|
Blood and lymphatic system disorders
LYMPH NODE PAIN
|
0.00%
0/24
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
|
Skin and subcutaneous tissue disorders
RASH
|
4.2%
1/24
|
0.00%
0/24
|
0.00%
0/24
|
0.00%
0/24
|
|
Respiratory, thoracic and mediastinal disorders
COUGH
|
4.2%
1/24
|
0.00%
0/24
|
0.00%
0/24
|
0.00%
0/24
|
|
Respiratory, thoracic and mediastinal disorders
RHINORRHOEA
|
4.2%
1/24
|
0.00%
0/24
|
0.00%
0/24
|
0.00%
0/24
|
|
Respiratory, thoracic and mediastinal disorders
NASAL CONGESTION
|
0.00%
0/24
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
|
Respiratory, thoracic and mediastinal disorders
OROPHARYNGEAL PAIN
|
4.2%
1/24
|
4.2%
1/24
|
4.2%
1/24
|
4.2%
1/24
|
|
Respiratory, thoracic and mediastinal disorders
INCREASED UPPER AIRWAY SECRETION
|
4.2%
1/24
|
0.00%
0/24
|
0.00%
0/24
|
0.00%
0/24
|
|
General disorders
FATIGUE
|
8.3%
2/24
|
0.00%
0/24
|
4.2%
1/24
|
0.00%
0/24
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee Bristol-Myers Squibb Co. agreements with investigators vary; constant is our right to embargo communications regarding trial results prior to public release for a period ≤60 days from submittal for review. We will not prohibit investigators from publishing, but will prohibit the disclosure of previously undisclosed confidential information other than study results, and request postponement of single-center publications until after disclosure of the clinical trial's primary publication.
- Publication restrictions are in place
Restriction type: OTHER