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This is a single-centre, single-dose, dose-escalation, placebo and positive drug-controlled Phase I clinical study in healthy Chinese subjects to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic profile of octreotide injection in healthy Chinese subjects.
This single centre study will be comprised of 6 cohorts. The single ascending dose part is comprises of 4 cohorts(5 mg, 10 mg, 20 mg, 30 mg).
The other 2 cohorts are octreotide long-acting release ( Sandostatin LAR® ) 20 mg and Sandostatin® 0.1 mg.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 5 mg cohort | Experimental | Subjects will be randomly assigned 4:1 to single dose of either SYHX2008(octreotide long-acting injection) or placebo at dose of 5 mg (8 active : 2 placebo). |
|
| 10 mg cohort | Experimental | Subjects will be randomly assigned 4:1 to single dose of either SYHX2008 or placebo at dose of 10 mg (8 active : 2 placebo). |
|
| 20 mg cohort | Experimental | Subjects will be randomly assigned 4:1 to single dose of either SYHX2008 or placebo at dose of 20 mg (8 active : 2 placebo). |
|
| 30 mg cohort | Experimental | Subjects will be randomly assigned 4:1 to single dose of either SYHX2008 or placebo at dose of 30 mg (8 active : 2 placebo). |
|
| Octreotide long-acting release ( Sandostatin LAR®) 20 mg cohort | Experimental | Subjects will be treated with single dose of octreotide long-acting release ( Sandostatin LAR®) at dose of 20 mg. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| SYHX2008 injection | Drug | Subcutaneous administration on Day 1. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Incidence and severity of adverse events | Throughout the study period, with an average of 60 days. |
| Measure | Description | Time Frame |
|---|---|---|
| Area under the plasma concentration-time curve (AUC) | AUC from pre-dose to time 't' (AUC[0-t]) and pre-dose to infinite time (AUC[0-infinity]) of Octreotide | Pre-dose, 0.5 hour, 1 hour, 2 hour, 4 hour, 8 hour, 12 hour, 24 hour, 48 hour, 96 hour, 168 hour, 336 hour, 576 hour, 1008 hour, 1416 hour. |
| Maximum plasma concentration (Cmax) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Yang NA Lin, PhD | Beijing Anzhen Hospital | Principal Investigator |
| Shan NA Jing, PhD | Beijing Anzhen Hospital | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Beijing Anzhen Hospital, Capital Medical University | Beijing | Beijing Municipality | 100000 | China |
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| ID | Term |
|---|---|
| D000172 | Acromegaly |
| ID | Term |
|---|---|
| D001849 | Bone Diseases, Endocrine |
| D001847 | Bone Diseases |
| D009140 | Musculoskeletal Diseases |
| D006964 | Hyperpituitarism |
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| ID | Term |
|---|---|
| D007267 | Injections |
| D015282 | Octreotide |
| ID | Term |
|---|---|
| D004333 | Drug Administration Routes |
| D004358 | Drug Therapy |
| D013812 | Therapeutics |
| D010456 | Peptides, Cyclic |
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|
| Sandostatin® 0.1mg cohort | Experimental | Subjects will be treated with single dose of Sandostatin® at dose of 0.1mg. |
|
| Octreotide Acetate Microspheres for Injection injection | Drug | Intramuscular administration on Day 1. |
|
| Sandostatin ® injection | Drug | Subcutaneous administration on Day 1. |
|
| Placebo to SYHX2008 injection | Drug | Subcutaneous administration on Day 1. |
|
Maximum octreotide plasma concentration (Cmax) of Octreotide |
| Pre-dose, 0.5 hour, 1 hour, 2 hour, 4 hour, 8 hour, 12 hour, 24 hour, 48 hour, 96 hour, 168 hour, 336 hour, 576 hour, 1008 hour, 1416 hour. |
| Time to maximum plasma concentration (Tmax) | Time to maximum octreotide plasma concentration (Tmax) of Octreotide | Pre-dose, 0.5 hour, 1 hour, 2 hour, 4 hour, 8 hour, 12 hour, 24 hour, 48 hour, 96 hour, 168 hour, 336 hour, 576 hour, 1008 hour, 1416 hour. |
| Terminal elimination half-life (t1/2) | Plasma decay half-life is the time measured for the octreotide plasma concentration to decrease by one half. | Pre-dose, 0.5 hour, 1 hour, 2 hour, 4 hour, 8 hour, 12 hour, 24 hour, 48 hour, 96 hour, 168 hour, 336 hour, 576 hour, 1008 hour, 1416 hour. |
| Apparent systemic clearance (CL/F) | CL/F is the volume of plasma cleared of octreotide per unit time. | Pre-dose, 0.5 hour, 1 hour, 2 hour, 4 hour, 8 hour, 12 hour, 24 hour, 48 hour, 96 hour, 168 hour, 336 hour, 576 hour, 1008 hour, 1416 hour. |
| Apparent volume of distribution (Vz/F) | Vz/F is the apparent volume of distribution of octreotide during the terminal elimination phase . | Pre-dose, 0.5 hour, 1 hour, 2 hour, 4 hour, 8 hour, 12 hour, 24 hour, 48 hour, 96 hour, 168 hour, 336 hour, 576 hour, 1008 hour, 1416 hour. |
| Insulin-like growth factor-1 (IGF-1) concentrations over time. | IGF-1 levels will be collected over time to compare the suppressive ability of octreotide. | Pre-dose, 1 hour, 4 hour, 12 hour, 24 hour, 48 hour, 96 hour, 168 hour, 336 hour, 576 hour, 1008 hour, 1416 hour. |
| D010900 |
| Pituitary Diseases |
| D007027 | Hypothalamic Diseases |
| D001927 | Brain Diseases |
| D002493 | Central Nervous System Diseases |
| D009422 | Nervous System Diseases |
| D004700 | Endocrine System Diseases |
| D047028 |
| Macrocyclic Compounds |
| D011083 | Polycyclic Compounds |
| D010455 | Peptides |
| D000602 | Amino Acids, Peptides, and Proteins |