Phase I Study of Kukoamine B Mesilate in Healthy Volunteers

Study Overview
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Brief Summary
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The purpose of this study is to assess safety, tolerance and pharmacokinetics of a single intravenous injection Kukoamine B Mesilate in health volunteer

Official Title
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Randomized, Double-blind Placebo-controlled Phase I Study to Assess Safety, Tolerance and Pharmacokinetics of a Single Intravenous Injection Kukoamine B Mesilate in Healthy Volunteers

Conditions
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Healthy

Intervention / Treatment
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* Drug: Kukoamine B Mesilate


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Gender: male or female, each sex ratio does not exceed 2/3; 18-45 years (including upper and lower limit), the general situation is good; Body mass index (BMI) in 19-28 (including upper and lower limit of the range), BW ≥ 50kg (female) and 60kg (male); Nearly half of the year, no child care program and agreed to take effective measures to contraception during the study period, women of childbearing age blood pregnancy test was negative; Subjects to fully understand the purpose, properties, method and reactions may occur of test drug trials.Voluntarily signed the informed consents, and agreed to abide by the requirements of clinical protocols. Exclusion Criteria: Primary disease in important organs; Mental or physical disability; Familial hereditary disease; Screening supine blood pressure (after 5 minutes of rest) systolic or diastolic blood pressure greater than 90 140mmHg, beyond the scope of 50 90mmHg, Or pulse (HR) beyond 50bpm 100bpm Abnormal results of any clinically meaningful physical examination, vital signs, ECG or clinical laboratory; History of immunodeficiency diseases, including HIV antibody positive; Detection of antibody positive, hepatitis B surface antigen or antibody to hepatitis C / syphilis positive; Alcohol and drug abusers; Smoking and drinking are (drinking 14 units of alcohol per week: 1 unit = beer 285 ml, or liquor 25 ml, or wine 1 cup. numbers of daily smoking ≥ 5) and / or not smoking and drinking in the test period; Any discharge period may affect the study drug, or in the past 3 months participated in any drug clinical trials; Before entering the group 4 weeks using any prescription drugs before entering the group, or use of any non prescription drugs within 2 weeks (vitamins, herbal tonics, food additives), or into the group within 2 weeks before taking effect of drug metabolizing enzymes in food, such as grapefruit or grapefruit drink. Can the use of acetaminophen, but must record report in CRF; The last 3 months had a history of blood donation or significant blood loss (more than 400ml); There are drugs, the clinical significance of the history of food allergy and atopic allergic diseases (asthma, urticaria, eczema dermatitis) or a known drug to test drugs or similar drug allergy test; Lactating women, pregnant women or unable to take effective contraceptive measures; Researchers believe that the other is not suitable to take the test factors participants.

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 45 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Triple


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Kukoamine B Mesilate 0.005mg/kg<br>Pre-test,open study: Kukoamine B Mesilate 0.005mg/kg single-dose and intravenous(IV) drip for 1 hour in healthy volunteers. | Drug: Kukoamine B Mesilate<br>* Kukoamine B Mesilate or placebo single-dose and intravenous(IV) drip for 1 hour in healthy volunteers.<br>|
| Experimental: Kukoamine B Mesilate 0.02mg/kg + Placebo<br>Dose Escalation: Kukoamine B Mesilate 0.02mg/kg single-dose and intravenous(IV) drip for 1 hour in healthy volunteers. Placebo: single and intravenous(IV) drip for 1 hour in healthy volunteers. | Drug: Kukoamine B Mesilate<br>* Kukoamine B Mesilate or placebo single-dose and intravenous(IV) drip for 1 hour in healthy volunteers.<br>|
| Experimental: Kukoamine B Mesilate 0.04mg/kg +Placebo<br>Dose Escalation: Kukoamine B Mesilate 0.04mg/kg single-dose and intravenous(IV) drip for 1 hour in healthy volunteers. Placebo: single and intravenous(IV) drip for 1 hour in healthy volunteers. | Drug: Kukoamine B Mesilate<br>* Kukoamine B Mesilate or placebo single-dose and intravenous(IV) drip for 1 hour in healthy volunteers.<br>|
| Experimental: Kukoamine B Mesilate 0.08mg/kg + Placebo<br>Dose Escalation: Kukoamine B Mesilate 0.08mg/kg single-dose and intravenous(IV) drip for 1 hour in healthy volunteers. Placebo: single and intravenous(IV) drip for 1 hour in healthy volunteers. | Drug: Kukoamine B Mesilate<br>* Kukoamine B Mesilate or placebo single-dose and intravenous(IV) drip for 1 hour in healthy volunteers.<br>|
| Experimental: Kukoamine B Mesilate 0.12mg/kg + Placebo<br>Dose Escalation: Kukoamine B Mesilate 0.12mg/kg single-dose and intravenous(IV) drip for 1 hour in healthy volunteers. Placebo: single and intravenous(IV) drip for 1 hour in healthy volunteers. | Drug: Kukoamine B Mesilate<br>* Kukoamine B Mesilate or placebo single-dose and intravenous(IV) drip for 1 hour in healthy volunteers.<br>|
| Experimental: Kukoamine B Mesilate 0.24mg/kg + Placebo<br>Dose Escalation: Kukoamine B Mesilate 0.24mg/kg single-dose and intravenous(IV) drip for 1 hour in healthy volunteers. Placebo: single and intravenous(IV) drip for 1 hour in healthy volunteers. | Drug: Kukoamine B Mesilate<br>* Kukoamine B Mesilate or placebo single-dose and intravenous(IV) drip for 1 hour in healthy volunteers.<br>|
| Experimental: Kukoamine B Mesilate 0.48mg/kg + Placebo<br>Dose Escalation: Kukoamine B Mesilate 0.48mg/kg single-dose and intravenous(IV) drip for 1 hour in healthy volunteers. Placebo: single and intravenous(IV) drip for 1 hour in healthy volunteers. | Drug: Kukoamine B Mesilate<br>* Kukoamine B Mesilate or placebo single-dose and intravenous(IV) drip for 1 hour in healthy volunteers.<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Incidence of adverse events. | AE,physical examination,monitoring of vital signs, Laboratory examination,ECG etc. | 7 days | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Pharmacokinetic parameters (t1/2,AUC0-inf,AUClast and Cmax;Fe0-48h(%),CLr24h) | Blood:（Pre Test）0,20min,40min after initiation of drug administration and 0,10min,20min,30min,45min,1h,1.5h,2h,2.5h,3h,4h,6h,8h,12h,24h after the end of administration;(Formal Test) 0,20min,40min after initiation of drug administration and 0,30min,1h,2h,3h,4h,6h,8h,12h,16h,24h after the end of administration; Urine:(Pre Test) 0,0-4h,4-8h,8-12h,12-24h,24-48h after initiation of drug administration;(Formal Test) 0,0-5h,5-9h,9-13h,13-25h,25-49h after initiation of drug administration . | 48h | 

 Terms related to the study
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Keywords Provided by Centre Hospitalier Valida
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Healthy