Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
This study is a three part study to assess the safety and efficacy of LEZ763 on normal healthy volunteers and patients with Type 2 Diabetes.
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| LEZ763 | Experimental | Part I- Healthy volunteers enrolled into 6 single-ascending dose cohorts Part II- Healthy volunteers enrolled into 5 multiple-ascending dose cohorts. Part III- LEZ763 will be given orally once daily for 28 days in a randomized and blinded manner |
|
| Placebo | Placebo Comparator | Part I : Healthy volunteers enrolled in 6 single ascending dose cohorts to receive matching placebo of LEZ763. Part II: Healthy volunteers enrolled in 5 multiple ascending dose cohorts to receive matching placebo of LEZ763. Part III- Placebo will be given orally once daily for 28 days to patients assigned to placebo in a randomized and blinded manner |
|
| Sitagliptin | Active Comparator | Sitaglitpin will be given orally once daily for 28 days to patients assigned to this treatment in a randomized and blinded manner |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Placebo | Drug | Placebo will be given orally once daily for 28 days to patients assigned to placebo in a randomized and blinded manner |
|
| Measure | Description | Time Frame |
|---|---|---|
| Number of Patients with adverse events, serious adverse events and death | An adverse event is the appearance or worsening of any undesirable sign, symptom, or medical condition occurring after starting the study drug even if the event is not considered to be related to study drug. Adverse events will also be determined on the basis of clinical laboratory assessments, electrocardiographic evaluations and vital signs determinations. | Day 28 |
| Pharmacokinetics of LEZ763 (Part I): area under the plasma concentration-time curve from time zero to infinity (AUCinf) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4 |
| Pharmacokinetics of LEZ763 (Part I): area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration (AUClast) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4 |
| Pharmacokinetics of LEZ763 (Part I): Terminal elimination half-life (T1/2) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4 |
| Pharmacokinetics of LEZ763 (Part I): Apparent systemic (or total body) clearance from plasma following extravascular administration (CL/F) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose |
| Measure | Description | Time Frame |
|---|---|---|
| Area under the serum Glucagon-like-peptide 1 (GLP-1) curve (AUC0-24 hours) | GLP-1 Biomarker measures will be evaluated at pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose | Pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day -1, Day 1, Day 27, and Day 28 |
Not provided
Inclusion criteria:
Normal Healthy Volunteers
Type II Diabetic Patients
Exclusion criteria:
All subjects:
Normal Healthy Volunteers
• History of diabetes, or adrenal disorders.
Type II Diabetic Patients
Not provided
Not provided
Not provided
Not provided
Not provided
| Name | Affiliation | Role |
|---|---|---|
| Novartis Pharmaceuticals | Novartis Pharmaceuticals | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Novartis Investigative Site | Chula Vista | California | 91910 | United States | ||
| Novartis Investigative Site |
Not provided
| Label | URL |
|---|---|
| Results for CLEZ763X2201 from the Novartis Clinical Trials website | View source |
Not provided
Not provided
| ID | Term |
|---|---|
| D003924 | Diabetes Mellitus, Type 2 |
| D003920 | Diabetes Mellitus |
| ID | Term |
|---|---|
| D044882 | Glucose Metabolism Disorders |
| D008659 | Metabolic Diseases |
| D009750 | Nutritional and Metabolic Diseases |
| D004700 | Endocrine System Diseases |
Not provided
Not provided
| ID | Term |
|---|---|
| D000068900 | Sitagliptin Phosphate |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Sitagliptin | Drug | Sitaglitpin will be given orally once daily for 28 days to patients assigned to this treatment in a randomized and blinded manner |
|
| LEZ763 | Drug | LEZ763 will be given orally once daily for 28 days in a randomized and blinded manner |
|
| pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4 |
| Pharmacokinetics of LEZ763 (Part I) : Observed maximum plasma concentration (Cmax) following drug administration | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single and multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4 |
| Pharmacokinetics of LEZ763 (Part I): time to reach the maximum concentration after drug administration (Tmax) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4 |
| Pharmacokinetics of LEZ763 (Part II) : Observed maximum plasma concentration (Cmax) following drug administration | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 10 |
| Pharmacokinetics of LEZ763 (Part II): time to reach the maximum concentration after drug administration (Tmax) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 10 |
| Pharmacokinetics of LEZ763 (Part II): Accumulation ratio(Racc) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27 |
| Pharmacokinetics of LEZ763 (Part III) : Observed maximum plasma concentration (Cmax) following drug administration | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27 |
| Pharmacokinetics of LEZ763 (Part III): time to reach the maximum concentration after drug administration (Tmax) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27 |
| Pharmacokinetics of LEZ763 (Part III): Area under the plasma concentration-time curve from time zero to the end of the dosing interval tau (AUCtau) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single and multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27 |
| Pharmacokinetics of LEZ763 (Part III): Accumulation ratio(Racc) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single and multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27 |
| Pharmacokinetics of LEZ763 and Sitagliptin (Part III): Observed maximum plasma concentration (Cmax) following drug administration | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day 28 |
| Pharmacokinetics of LEZ763 and Sitagliptin (Part III): Area under the plasma concentration-time curve from time zero to the end of the dosing interval tau (AUCtau) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day 28 |
| Pharmacokinetics of LEZ763 and Sitagliptin (Part III): Time to reach the maximum concentration after drug administration (Tmax) | Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses | pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day 28 |
| Area under the effect curve (AUC0-4h) over the 4-hour post-dose period to measure glucose response following a standard mixed meal test | 4 hour post-dose Day 27 |
| 2-hour value of post-prandial glucose |
| Day 1 of Part I, Day 1 and day 10 of Part II |
| Change from baseline in Fasting C-peptide at Day 27 (Part III) | Baseline, Day 27 |
| Change from baseline in Fasting Insulin at Day 27 (Part III) | Baseline , Day 27 |
| Change from baseline in fasting plasma glucose at Day 27 (Part III) | Baseline , Day 27 |
| Change From Baseline in peak glucose level following meal Test at Day 27 (Part III) | Baseline , Day 27 |
| Peak effect (Emax) on postprandial GLP-1 (Part III) | Baseline , Day 27 |
| Change from baseline in Peptide YY (PYY) (Part III) | Baseline , Day 27 |
| Change from baseine in Gastric inhibit polypeptide (GIP) (Part III) | Baseline , Day 27 |
| Miami |
| Florida |
| 33126 |
| United States |
| Novartis Investigative Site | Orlando | Florida | 32809 | United States |
| Novartis Investigative Site | Cincinnati | Ohio | 45227 | United States |
| Novartis Investigative Site | Knoxville | Tennessee | 37920 | United States |
| Novartis Investigative Site | San Antonio | Texas | 78209 | United States |
| D011719 |
| Pyrazines |