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This is a phase 1 randomized,double-blind,placebo-controlled study with single oral dose of globalagliatin hydrochloride (SY-004) administered to chinese healthy subjects to evaluated the safety, tolerability, pharmacokinetics and pharmacodynamics of globalagliatin hydrochloride (SY-004).
Glucokinase is a characteristic hexokinase isoenzyme in hepatocytes that catalyzes the first step in glucose metabolism. In addition to its role in glucose metabolism, glucokinase is expressed in pancreatic islet beta cells where it acts as a "glucose sensor" for insulin release. Activation of glucokinase increases the glucose sensitivity of insulin secretion, effectively lowering the glucose threshold for insulin secretion. Because of its potential to enhance insulin secretion and affect hepatic glucose metabolism, is being investigated for use as a treatment for hyperglycaemia,glubalagliatin( the active ingredient in SY-004 capsule) is being investigated for use as a treatment for T2DM patients. This is a phase 1 randomized,double-blind,placebo-controlled study with single oral dose of SY-004 administered to chinese healthy subjects to evaluated the safety, tolerability, pharmacokinetics and pharmacodynamics of SY-004.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| SY-004 2mg | Experimental | SY-004 (globalagliatin hydrochloride) 2mg by mouth, single dose |
|
| SY-004 20mg&placebo | Placebo Comparator | SY-004 (globalagliatin hydrochloride) 20mg or placebo by mouth, single dose |
|
| SY-004 40mg&placebo | Placebo Comparator | SY-004 (globalagliatin hydrochloride) 40mg or placebo by mouth, single dose |
|
| SY-004 80mg&placebo | Placebo Comparator | SY-004 (globalagliatin hydrochloride) 80mg or placebo by mouth, single dose |
|
| SY-004 120mg&placebo | Placebo Comparator | SY-004(globalagliatin hydrochloride) 120mg or placebo by mouth, single dose |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| globalagliatin hydrochloride | Drug | orally administration, single dose |
|
| Measure | Description | Time Frame |
|---|---|---|
| Safety and tolerability of single dose of SY-004 | number of patients with adverse events and changes from baseline in vital signs, ECG and clinical labs (blood chemistry, hematology and urinalysis) | 14 day post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| AUC of SY-004 following oral administration of single ascending dose | to measure the study drug concentration in blood and urine samples to be collected after drug administration. | up to 168 hours post-dose |
| Cmax of SY-004 following oral administration of single ascending dose. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Lei Yang | Yabao pharmaceutical Group Co. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| The First Affiliated Hospital of Nanjing Medical University | Nanjing | Jiangsu | China |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 35093240 | Derived | Zhao Y, Xie L, Zhang H, Zhou S, Liu Y, Chen J, Wang L, Wang L, Zhuo L, Wang Y, Ou N, Shao F. Tolerability, Safety, Pharmacokinetics, and Pharmacodynamics of SY-004, a Glucokinase Activator, in Healthy Chinese Adults: A Randomized, Phase Ia, Single-Ascending Dose Study. Clin Ther. 2022 Feb;44(2):269-281. doi: 10.1016/j.clinthera.2021.12.009. Epub 2022 Jan 29. |
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| ID | Term |
|---|---|
| D006943 | Hyperglycemia |
| D003920 | Diabetes Mellitus |
| ID | Term |
|---|---|
| D044882 | Glucose Metabolism Disorders |
| D008659 | Metabolic Diseases |
| D009750 | Nutritional and Metabolic Diseases |
| D004700 | Endocrine System Diseases |
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|
| placebo | Drug | orally administration, single dose |
|
to measure the study drug concentration in blood and urine samples to be collected after drug administration. |
| up to 168 hours post-dose |
| T1/2 of SY-004 following oral administration of single ascending dose | to measure the study drug concentration in blood and urine samples to be collected after drug administration. | up to 168 hours post-dose |
| CL/F of SY-004 following oral administration of single ascending dose | to measure the study drug concentration in blood and urine samples to be collected after drug administration. | up to 168 hours post-dose |
| glucose levels following single dose of SY-004 | FPG AUC | up to 48 hours post-dose |
| insulin secretion following single dose of SY-004 | insulin changes | up to 11 hours post-dose |
| C-peptide secretion following single dose of SY-004 | C-peptide change | up to 11 hour post-dose |