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Darapladib China PK

12 mai 2017 mis à jour par: 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.

Aperçu de l'étude

Statut

Complété

Les conditions

Intervention / Traitement

Description détaillée

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.

Type d'étude

Interventionnel

Inscription (Réel)

24

Phase

  • La phase 1

Contacts et emplacements

Cette section fournit les coordonnées de ceux qui mènent l'étude et des informations sur le lieu où cette étude est menée.

Lieux d'étude

      • Shanghai, Chine, 200030
        • GSK Investigational Site

Critères de participation

Les chercheurs recherchent des personnes qui correspondent à une certaine description, appelée critères d'éligibilité. Certains exemples de ces critères sont l'état de santé général d'une personne ou des traitements antérieurs.

Critère d'éligibilité

Âges éligibles pour étudier

18 ans à 45 ans (Adulte)

Accepte les volontaires sains

Non

Sexes éligibles pour l'étude

Tout

La description

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.

Plan d'étude

Cette section fournit des détails sur le plan d'étude, y compris la façon dont l'étude est conçue et ce que l'étude mesure.

Comment l'étude est-elle conçue ?

Détails de conception

  • Objectif principal: Traitement
  • Répartition: N / A
  • Modèle interventionnel: Affectation à un seul groupe
  • Masquage: Aucun (étiquette ouverte)

Armes et Interventions

Groupe de participants / Bras
Intervention / Traitement
Expérimental: darapladib 160mg
drug
drug

Que mesure l'étude ?

Principaux critères de jugement

Mesure des résultats
Description de la mesure
Délai
Adverse event
Délai: 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
Délai: 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
Délai: Up to 12 weeks
Systolic and diastolic blood pressure and pulse rate
Up to 12 weeks
clinical laboratory examination
Délai: Up to 12 weeks
Hematology, clinical chemistry, urinalysis and additional parameters to be tested
Up to 12 weeks
AUC0-t for darapladib
Délai: 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
Délai: 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
Délai: 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
Délai: Up to 12 weeks
Accumulation ratios Cmax accumulation ratio
Up to 12 weeks
Ro for darapladib
Délai: Up to 12 weeks
Accumulation ratios Cmax accumulation ratio
Up to 12 weeks
Nursing/physician observation
Délai: 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

Mesures de résultats secondaires

Mesure des résultats
Description de la mesure
Délai
Tmax for darapladib
Délai: Up to 12 weeks
Time of occurrence of Cmax for darapladib
Up to 12 weeks
T1/2 for darapladib
Délai: Up to 12 weeks
Terminal phase half-life for darapladib
Up to 12 weeks
AUC0-t for darapladib metabolite SB-553253 (as data permit).
Délai: 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).
Délai: 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).
Délai: 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).
Délai: 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).
Délai: Up to 12 weeks
Time of occurrence of Cmax for the pharmacologically active metabolite SB-553253
Up to 12 weeks
Plasma Lp-PLA2 activity
Délai: Up to 12 weeks
Percent inhibition relative to baseline of Plasma Lp-PLA2
Up to 12 weeks

Collaborateurs et enquêteurs

C'est ici que vous trouverez les personnes et les organisations impliquées dans cette étude.

Parrainer

Publications et liens utiles

La personne responsable de la saisie des informations sur l'étude fournit volontairement ces publications. Il peut s'agir de tout ce qui concerne l'étude.

Dates d'enregistrement des études

Ces dates suivent la progression des dossiers d'étude et des soumissions de résultats sommaires à ClinicalTrials.gov. Les dossiers d'étude et les résultats rapportés sont examinés par la Bibliothèque nationale de médecine (NLM) pour s'assurer qu'ils répondent à des normes de contrôle de qualité spécifiques avant d'être publiés sur le site Web public.

Dates principales de l'étude

Début de l'étude (Réel)

23 octobre 2013

Achèvement primaire (Réel)

4 janvier 2014

Achèvement de l'étude (Réel)

4 janvier 2014

Dates d'inscription aux études

Première soumission

20 juin 2013

Première soumission répondant aux critères de contrôle qualité

27 novembre 2013

Première publication (Estimation)

4 décembre 2013

Mises à jour des dossiers d'étude

Dernière mise à jour publiée (Réel)

15 mai 2017

Dernière mise à jour soumise répondant aux critères de contrôle qualité

12 mai 2017

Dernière vérification

1 mai 2017

Plus d'information

Termes liés à cette étude

Plan pour les données individuelles des participants (IPD)

Prévoyez-vous de partager les données individuelles des participants (DPI) ?

Oui

Description du régime IPD

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

Données/documents d'étude

  1. Formulaire de consentement éclairé
    Identifiant des informations: 117326
    Commentaires d'informations: For additional information about this study please refer to the GSK Clinical Study Register
  2. Spécification du jeu de données
    Identifiant des informations: 117326
    Commentaires d'informations: For additional information about this study please refer to the GSK Clinical Study Register
  3. Protocole d'étude
    Identifiant des informations: 117326
    Commentaires d'informations: For additional information about this study please refer to the GSK Clinical Study Register
  4. Ensemble de données de participant individuel
    Identifiant des informations: 117326
    Commentaires d'informations: For additional information about this study please refer to the GSK Clinical Study Register
  5. Formulaire de rapport de cas annoté
    Identifiant des informations: 117326
    Commentaires d'informations: For additional information about this study please refer to the GSK Clinical Study Register
  6. Plan d'analyse statistique
    Identifiant des informations: 117326
    Commentaires d'informations: For additional information about this study please refer to the GSK Clinical Study Register
  7. Rapport d'étude clinique
    Identifiant des informations: 117326
    Commentaires d'informations: For additional information about this study please refer to the GSK Clinical Study Register

Ces informations ont été extraites directement du site Web clinicaltrials.gov sans aucune modification. Si vous avez des demandes de modification, de suppression ou de mise à jour des détails de votre étude, veuillez contacter register@clinicaltrials.gov. Dès qu'un changement est mis en œuvre sur clinicaltrials.gov, il sera également mis à jour automatiquement sur notre site Web .

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