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This study aims to evaluate the pharmacokinetic interaction between HL237 and tacrolimus in healthy male subjects.
To evaluate the pharmacokinetic interaction by comparing of pharmacokinetic parameters when administered HL237(or tacrolimus) between with tacrolimus(or HL237) and without tacrolimus(or HL237).
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Single arm | Experimental | This single arm is conducted in fixed-sequence(Treatment A ->(washout period) -> Treatment B -> Treatment C -> Maintenance treatment). Treatment A : tacrolimus 5mg po single dose, Treatment B : HL237 400mg bid for 4 days, Treatment C: tacrolimus 5mg po single dose and HL237 400 mg bid, Maintenance treatment : HL237 400mg bid for 2 days |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| HL237 tablet | Drug | HL237 400mg will be administered orally twice a day. |
| |
| Measure | Description | Time Frame |
|---|---|---|
| Peak plasma concentration at steady state(Cmax,ss) of HL237 | Comparison of pharmacokinetic parameters between when administered tacrolimus with HL237 and without HL237 | 0(before dosing), 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 hour(after dosing) on day 21 and day 22 |
| Area under the plasma concentration versus time curve during a dosage interval(AUCÏ„) of HL237 | Comparison of pharmacokinetic parameters between when administered tacrolimus with HL237 and without HL237 | 0(before dosing), 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 hour(after dosing) on day 21 and day 22 |
| Peak whole-blood concentration(Cmax) of tacrolimus | Comparison of pharmacokinetic parameters between when administered tacrolimus with HL237 and without HL237 | 0(before dosing), 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72hour(after dosing) on day 1 and day 22 |
| Area under the whole-blood concentration versus time curve from time zero to time of last measurable concentration(AUClast) of tacrolimus | Comparison of pharmacokinetic parameters between when administered tacrolimus with HL237 and without HL237 | 0(before dosing), 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72hour(after dosing) on day 1 and day 22 |
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Inclusion Criteria:
Exclusion Criteria:
Subject with serious cardiovascular, respiratory, hepatology, renal, hematologic, gastrointestinal, immunologic, dermal, neurologic, or psychological disease or history of such disease
Subject with symptoms of acute disease within 28 days prior to investigational products dosing
Subject with medical history which able to affect absorption, distribution, metabolism and excretion of drug
Subject with hypersensitive reaction to following drug or history of clinically significant hypersensitive reaction to following drug
Subject with clinically significant active chronic disease
Subject with genetic deficiency such as galactose intolerance, Lapp lactose deficiency or glucosegalactose malabsorption
Subjects who showed one or more of the following in a screening test including a retest
Positive test results for hepatitis B virus surface antigen, anti-hepatitis C virus antibody, anti-Human Immunodeficiency virus antibody or venereal disease research laboratory test
Use of any prescription medication within 14 days prior to study medication dosing
Use of any over-the-counter(OTC) medication within 7 days prior to study medication dosing
Subject with clinically significant allergic disease (except for mild allergic rhinitis and mild allergic dermatitis that are not needed to administer drug)
Subject who is not able to taking standard meals provided by the institution
Subject with whole blood donation within 60 days, component blood donation within 20 days
Subjects receiving blood transfusion within 30 days prior to study medication dosing
Participation in any clinical investigation within 6 months prior to study medication dosing
Use of any medication effected on drug enzyme induction or inhibition such as barbitals within 30 days prior to study medication dosing
Subjects who have continuously consumed grapefruit juice or caffeine (grapefruit juice or caffeine > 5 cups/day), or who can't refrain from intake during hospitalization
Subjects who have continued to drink alcohol (alcohol> 30 g/day) or who can't quit drinking during hospitalization
Severe heavy smoker(cigarette > 10 cigarettes per day) or subjects who can't quit smoking during hospitalization
Subjects that the investigator deems unsuitable for participation in the clinical trial due to laboratory test results or other excuse such as non-responding to request or instruction by investigator
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| The Korea Univertisy Anam Hospital | Seoul | South Korea |
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| ID | Term |
|---|---|
| D016559 | Tacrolimus |
| ID | Term |
|---|---|
| D018942 | Macrolides |
| D007783 | Lactones |
| D009930 | Organic Chemicals |
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Fixed-sequential
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| tacrolimus capsule |
| Drug |
tacrolimus 5mg will be administered orally once a day. |
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