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Darapladib China PK

12 mei 2017 bijgewerkt door: GlaxoSmithKline

A Study to Evaluate the Pharmacokinetics, Pharmacodynamics and Safety of 160 mg Enteric-coated Micronised Free Base Darapladib in Healthy Chinese Subjects.

This study is to evaluate pharmacokinetics (PK), pharmacodynamics (PD) and safety of 160 mg enteric-coated micronised free base darapladib in healthy Chinese subjects.

Studie Overzicht

Toestand

Voltooid

Conditie

Interventie / Behandeling

Gedetailleerde beschrijving

SB-480848 (darapladib) is a novel selective and orally active inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) being developed by GlaxoSmithKline (GSK) for the treatment of atherosclerosis.

This will be an open label study where each Subject will participate in 2 study sessions, a single dose session and a repeat dose session. All Subjects will receive 160 mg of enteric coated micronised free-base darapladib as a single dose and as repeated daily doses for 28 days.

The purpose of this study is to evaluate the pharmacokinetics (PK) and pharmacodynamics (PD) and safety of single and repeat oral dose of darapladib in healthy Chinese Subjects. The primary endpoints for safety are: clinical safety data from spontaneous adverse event reporting, 12-lead electrocardiogram recording, vital sign measurement, nursing/physician observation and clinical laboratory tests. The primary PK parameters of interest are area under plasma concentration time curve (AUC) and maximum plasma concentration (Cmax) of darapladib, while the secondary PK parameters of interest are: time of occurrence of Cmax (Tmax) and apparent terminal phase half-life (t1/2) of darapladib as well as AUC, Cmax, Tmax and t1/2 of the metabolite, SB-553253. Finally, the PD endpoint of interest is plasma Lp PLA2 activity, as expressed in terms of percent inhibition relative to baseline.

Studietype

Ingrijpend

Inschrijving (Werkelijk)

24

Fase

  • Fase 1

Contacten en locaties

In dit gedeelte vindt u de contactgegevens van degenen die het onderzoek uitvoeren en informatie over waar dit onderzoek wordt uitgevoerd.

Studie Locaties

      • Shanghai, China, 200030
        • GSK Investigational Site

Deelname Criteria

Onderzoekers zoeken naar mensen die aan een bepaalde beschrijving voldoen, de zogenaamde geschiktheidscriteria. Enkele voorbeelden van deze criteria zijn iemands algemene gezondheidstoestand of eerdere behandelingen.

Geschiktheidscriteria

Leeftijden die in aanmerking komen voor studie

18 jaar tot 45 jaar (Volwassen)

Accepteert gezonde vrijwilligers

Nee

Geslachten die in aanmerking komen voor studie

Allemaal

Beschrijving

Inclusion Criteria:

  • Healthy Chinese males or females aged between 18 and 45 years of age inclusive, at the time of signing the informed consent. (Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, laboratory tests and cardiac monitoring. A Subject with a clinical abnormality or laboratory parameters which is/are not specifically listed in the inclusion or exclusion criteria, outside the reference range for the population being studied may be included only if the Investigator (in consultation with the GSK Medical Monitor if required) agree and document that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures. )
  • Of Chinese origin - defined as being born in mainland China, having four ethnic Chinese grandparents.
  • Body weight ≥50 kg and BMI within the range 19 to 24 kg/m2 (inclusive).
  • A female Subject is eligible to participate if she is of:

Non-childbearing potential defined as pre-menopausal females with a documented tubal ligation or hysterectomy [for this definition, "documented" refers to the outcome of the investigator's/designee's review of the Subject's medical history for study eligibility, as obtained via a verbal interview with the Subject or from the Subject's medical records]; or postmenopausal defined as 12 months of spontaneous amenorrhea [in questionable cases a blood sample with simultaneous follicle stimulating hormone (FSH) >40 MlU/ml and estradiol < 40 pg/ml (<147 pmol/L) is confirmatory].

Child-bearing potential with negative pregnancy test as determined by urine human chorionic gonadotropin (hCG) test at screening or prior to dosing and Agrees to use 1 of the contraception methods listed in Section 4.3.1 from the time of Screening to sufficiently minimize the risk of pregnancy at that point. Female Subjects must agree to use contraception until the follow-up contact.

  • Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form
  • Alanine aminotransferase (ALT), alkaline phosphatise (ALP) and bilirubin ≤1.5x upper limit of normal (ULN) (isolated bilirubin >1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin <35%).
  • Based on single or averaged QTc values of triplicate ECGs obtained over a brief recording period:

QT duration corrected for heart rate by Bazett's formula (QTcB) or QT duration corrected for heart rate by Fridericia's formula (QTcF) <450 msec; QTc <480 msec in Subjects with Bundle Branch Block.

Exclusion Criteria:

  • Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
  • History of regular alcohol consumption within 6 months of the study defined as: an average weekly intake of >14 drinks for males or >7 drinks for females. One drink is equivalent to 12 g of alcohol: 12 ounces (360 ml) of beer, 5 ounces (150 ml) of wine or 1.5 ounces (45 ml) of 80 proof distilled spirits.
  • Consumption of grapefruit or grapefruit juice within 7 days prior to first dose of study medication.
  • History of sensitivity to heparin or heparin-induced thrombocytopenia.
  • History of asthma, anaphylaxis or anaphylactoid reactions, severe allergic responses.
  • History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy that, in the opinion of the investigator or GSK Medical Monitor, contraindicates their participation.
  • Unable to refrain from the use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St John's Wort) within 7 days (or 14 days if the drug is a potential enzyme inducer) or 5 half-lives (whichever is longer) prior to the first dose of study medication.
  • A positive test for Hepatitis B surface antigen (HBsAg) or positive Hepatitis C antibody result, or positive test for human immunodeficiency virus (HIV) antibody or Syphilis antibody at Screening.
  • A positive pre-study drug/alcohol screen.
  • Pregnant females as determined by positive urine hCG test at screening or prior to dosing.
  • A chest X-ray or computed tomography (CT) scan that reveals evidence of clinical significant abnormalities eg, tuberculosis. A chest X-ray must be taken at Day-1 if a chest X-ray or CT scan is not available within 6 months prior to that day.
  • Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
  • Lactating females.
  • The Subject has participated in a clinical trial and has received an investigational product within the following time period prior to the first dosing day in the current study: 30 days, 5 half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
  • Exposure to more than 4 new chemical entities within 12 months prior to the first dosing day.
  • Unwillingness or inability to follow the procedures outlined in the protocol.

Studie plan

Dit gedeelte bevat details van het studieplan, inclusief hoe de studie is opgezet en wat de studie meet.

Hoe is de studie opgezet?

Ontwerpdetails

  • Primair doel: Behandeling
  • Toewijzing: NVT
  • Interventioneel model: Opdracht voor een enkele groep
  • Masker: Geen (open label)

Wapens en interventies

Deelnemersgroep / Arm
Interventie / Behandeling
Experimenteel: darapladib 160mg
drug
drug

Wat meet het onderzoek?

Primaire uitkomstmaten

Uitkomstmaat
Maatregel Beschrijving
Tijdsspanne
Adverse event
Tijdsspanne: Up to 12 weeks
An AE is any untoward medical occurrence in a patient or clinical investigation Subject, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product.
Up to 12 weeks
12-lead ECG
Tijdsspanne: Up to 12 weeks
12-lead ECGs will be obtained at designated timepoint during the study, using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTc intervals.
Up to 12 weeks
Vital sign measurement
Tijdsspanne: Up to 12 weeks
Systolic and diastolic blood pressure and pulse rate
Up to 12 weeks
clinical laboratory examination
Tijdsspanne: Up to 12 weeks
Hematology, clinical chemistry, urinalysis and additional parameters to be tested
Up to 12 weeks
AUC0-t for darapladib
Tijdsspanne: Up to 12 weeks
Area under the concentration-time curve from time zero (pre-dose) to last time of quantifiable concentration
Up to 12 weeks
AUC 0-∞ for Darapdlib
Tijdsspanne: Up to 12 weeks
Area under the concentration-time curve from time zero (pre-dose) extrapolated to infinite time
Up to 12 weeks
Cmax for darapladib
Tijdsspanne: Up to 12 weeks
Area under the concentration-time curve from time zero (pre-dose) extrapolated to infinite time
Up to 12 weeks
Rcmax for darapladib
Tijdsspanne: Up to 12 weeks
Accumulation ratios Cmax accumulation ratio
Up to 12 weeks
Ro for darapladib
Tijdsspanne: Up to 12 weeks
Accumulation ratios Cmax accumulation ratio
Up to 12 weeks
Nursing/physician observation
Tijdsspanne: Up to 12 weeks
The physical examination will include assessments of the skin, lungs, cardiovascular system, and abdomen (liver and spleen).
Up to 12 weeks

Secundaire uitkomstmaten

Uitkomstmaat
Maatregel Beschrijving
Tijdsspanne
Tmax for darapladib
Tijdsspanne: Up to 12 weeks
Time of occurrence of Cmax for darapladib
Up to 12 weeks
T1/2 for darapladib
Tijdsspanne: Up to 12 weeks
Terminal phase half-life for darapladib
Up to 12 weeks
AUC0-t for darapladib metabolite SB-553253 (as data permit).
Tijdsspanne: Up to 12 weeks
Area under the concentration-time curve from time zero (pre-dose) to last time of quantifiable concentration for the pharmacologically active metabolite SB-553253
Up to 12 weeks
AUC0-∞ for darapladib metabolite SB-553253 (as data permit).
Tijdsspanne: Up to 12 weeks
Area under the concentration-time curve from time zero (pre-dose) extrapolated to infinite time the pharmacologically active metabolite SB-553253
Up to 12 weeks
Cmax for darapladib metabolite SB-553253 (as data permit).
Tijdsspanne: Up to 12 weeks
Maximum observed concentration for the pharmacologically active metabolite SB-553253
Up to 12 weeks
T1/2 for darapladib metabolite SB-553253 (as data permit).
Tijdsspanne: Up to 12 weeks
Terminal phase half-life for the pharmacologically active metabolite SB-553253
Up to 12 weeks
Tmax for darapladib metabolite SB-553253 (as data permit).
Tijdsspanne: Up to 12 weeks
Time of occurrence of Cmax for the pharmacologically active metabolite SB-553253
Up to 12 weeks
Plasma Lp-PLA2 activity
Tijdsspanne: Up to 12 weeks
Percent inhibition relative to baseline of Plasma Lp-PLA2
Up to 12 weeks

Medewerkers en onderzoekers

Hier vindt u mensen en organisaties die betrokken zijn bij dit onderzoek.

Sponsor

Publicaties en nuttige links

De persoon die verantwoordelijk is voor het invoeren van informatie over het onderzoek stelt deze publicaties vrijwillig ter beschikking. Dit kan gaan over alles wat met het onderzoek te maken heeft.

Studie record data

Deze datums volgen de voortgang van het onderzoeksdossier en de samenvatting van de ingediende resultaten bij ClinicalTrials.gov. Studieverslagen en gerapporteerde resultaten worden beoordeeld door de National Library of Medicine (NLM) om er zeker van te zijn dat ze voldoen aan specifieke kwaliteitscontrolenormen voordat ze op de openbare website worden geplaatst.

Bestudeer belangrijke data

Studie start (Werkelijk)

23 oktober 2013

Primaire voltooiing (Werkelijk)

4 januari 2014

Studie voltooiing (Werkelijk)

4 januari 2014

Studieregistratiedata

Eerst ingediend

20 juni 2013

Eerst ingediend dat voldeed aan de QC-criteria

27 november 2013

Eerst geplaatst (Schatting)

4 december 2013

Updates van studierecords

Laatste update geplaatst (Werkelijk)

15 mei 2017

Laatste update ingediend die voldeed aan QC-criteria

12 mei 2017

Laatst geverifieerd

1 mei 2017

Meer informatie

Termen gerelateerd aan deze studie

Plan Individuele Deelnemersgegevens (IPD)

Bent u van plan om gegevens van individuele deelnemers (IPD) te delen?

Ja

Beschrijving IPD-plan

Patient-level data for this study will be made available through www.clinicalstudydatarequest.com following the timelines and process described on this site.

Bestudeer gegevens/documenten

  1. Formulier geïnformeerde toestemming
    Informatie-ID: 117326
    Informatie opmerkingen: For additional information about this study please refer to the GSK Clinical Study Register
  2. Specificatie gegevensset
    Informatie-ID: 117326
    Informatie opmerkingen: For additional information about this study please refer to the GSK Clinical Study Register
  3. Leerprotocool
    Informatie-ID: 117326
    Informatie opmerkingen: For additional information about this study please refer to the GSK Clinical Study Register
  4. Gegevensset individuele deelnemers
    Informatie-ID: 117326
    Informatie opmerkingen: For additional information about this study please refer to the GSK Clinical Study Register
  5. Geannoteerd casusrapportformulier
    Informatie-ID: 117326
    Informatie opmerkingen: For additional information about this study please refer to the GSK Clinical Study Register
  6. Statistisch analyseplan
    Informatie-ID: 117326
    Informatie opmerkingen: For additional information about this study please refer to the GSK Clinical Study Register
  7. Klinisch onderzoeksrapport
    Informatie-ID: 117326
    Informatie opmerkingen: For additional information about this study please refer to the GSK Clinical Study Register

Deze informatie is zonder wijzigingen rechtstreeks van de website clinicaltrials.gov gehaald. Als u verzoeken heeft om uw onderzoeksgegevens te wijzigen, te verwijderen of bij te werken, neem dan contact op met register@clinicaltrials.gov. Zodra er een wijziging wordt doorgevoerd op clinicaltrials.gov, wordt deze ook automatisch bijgewerkt op onze website .

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