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GSK1349572 Drug Interaction Study With Efavirenz

21 septembre 2017 mis à jour par: ViiV Healthcare

A Phase 1, Open Label, Single Sequence, Three Period Study to Evaluate the Single Dose Pharmacokinetics of GSK1349572 100mg Versus 50mg and the Effect of Efavirenz 600mg Once Daily on the Pharmacokinetics, Safety and Tolerability of GSK1349572 50mg Once Daily in Healthy Adult Subjects (ING114005)

GSK1349572 is an integrase inhibitor that is currently in Phase 2 clinical trials for the treatment of HIV infection. As GSK1349572 development progresses, it may be dosed with non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) including efavirenz (EFV, Sustiva). Efavirenz is a known inducer of CYP3A4. GSK1349572 is primarily metabolized via UGT1A1, however it also has a CYP component to its metabolism, thus a drug interaction between GSK1349572 and EFV is likely. A previous study showed that another NNRTI, etravirine which is also a known inducer of CYP3A and UGT, reduced GSK1349572 exposure significantly. GSK1349572 is not an inhibitor or inducer of CYP3A and is not expected to have impact on pharmacokinetics (PK) of EFV.

This study will investigate the dose proportionality between single doses of 50mg and 100mg of GSK1349572 and will compare steady-state plasma PK, safety and tolerability of GSK1349572 50 mg every 24h (q24h) with and without efavirenz 600 mg q24h. Approximately 12 subjects will receive a single dose of GSK1349572 100 mg (Treatment A) in Period 1 followed by a washout of greater than or equal to 6 days. In Period 2 subjects will receive GSK1349572 50mg q24h for 5 days (Treatment B). Subjects will then be administered GSK1349572 50mg q24h in the morning in combination with EFV 600 mg q24h (Treatment C) in the evening for 14 days in Period 3. There will be no washout between Periods 2 and 3. Safety evaluations and serial PK samples for GSK1349572 will be collected during each treatment period. A follow-up visit will occur 7-14 days after the last dose of study drug.

This study will be conducted at one center in the US, with healthy adult male and female subjects.

Aperçu de l'étude

Description détaillée

ViiV Healthcare is the new sponsor of this study, and GlaxoSmithKline is in the process of updating systems to reflect the change in sponsorship.

Type d'étude

Interventionnel

Inscription (Réel)

12

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

    • New York
      • Buffalo, New York, États-Unis, 14202
        • 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 65 ans (Adulte, Adulte plus âgé)

Accepte les volontaires sains

Non

Sexes éligibles pour l'étude

Tout

La description

Inclusion Criteria:

  • AST, ALT, alkaline phosphatase and bilirubin less than or equal to 1.5xULN (isolated bilirubin >1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin <35%).
  • Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, laboratory tests and cardiac monitoring.
  • Male or female between 18 and 65 years of age inclusive, at the time of signing the informed consent.
  • 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; 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].
  • Body weight greater than or equal to 50 kg for males and 45 kg for females and BMI within the range 18.5- 31.0 kg/m2 (inclusive).
  • Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form.

Exclusion Criteria:

  • The subject has a positive pre-study drug/alcohol screen. A minimum list of drugs that will be screened for include amphetamines, barbiturates, cocaine, opiates, cannabinoids and benzodiazepines.
  • 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).
  • 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.
  • 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, unless in the opinion of the Investigator and GSK Medical Monitor the medication will not interfere with the study procedures or compromise subject safety.
  • If heparin is used during PK sampling, subjects with a history of sensitivity to heparin or heparin-induced thrombocytopenia should not be enrolled.
  • History of regular alcohol consumption within 6 months of the study defined as an average weekly intake of >14 drinks/week for men or >7 drinks/week for women. One drink is equivalent to (12 g alcohol) = 5 ounces (150 ml) of wine or 12 ounces (360 ml) of beer or 1.5 ounces (45 ml) of 80 proof distilled spirits.
  • Has a history or regular use of tobacco- or nicotine-containing products within 3 months prior to screening.
  • Consumption of red wine, seville oranges, grapefruit or grapefruit juice from 7 days prior to the first dose of study medication.
  • Pregnant females as determined by positive serum or urine human chorionic gonadotrophin (hCG) test at screening or prior to dosing.
  • Lactating females.
  • Unwillingness or inability to follow the procedures outlined in the protocol.
  • Subjects with a pre-existing condition interfering with normal gastrointestinal anatomy or motility, hepatic and/or renal function, that could interfere with the absorption, metabolism, and/or excretion of the study drugs. Subjects with a history of cholecystectomy, peptic ulceration, inflammatory bowel disease or pancreatitis should be excluded.
  • History/evidence of symptomatic arrhythmia, angina/ischemia, coronary artery bypass grafting (CABG) surgery or percutaneous transluminal coronary angioplasty (PCTA) or any clinically significant cardiac disease.
  • History/evidence of clinically significant pulmonary disease.
  • History of significant renal or hepatobiliary diseases. Subjects with a history of nephrolithiasis will be excluded.
  • History of severe or serious psychiatric disease ever requiring hospitalization, history of suicidal ideation or suicidal attempt, or undergoing psychiatric treatment will be excluded from study participation.
  • A positive pre-study Hepatitis B surface antigen or positive Hepatitis C antibody result within 3 months of screening.
  • A positive test for HIV antibody.
  • History of 2nd degree or higher AV block.
  • History of Gilbert's disease.
  • Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
  • The subject's systolic blood pressure is outside the range of 90-140mmHg, or diastolic blood pressure is outside the range of 45-90mmHg or heart rate is outside the range of 50-100bpm for female subjects or 45-100 bpm for male subjects.
  • Exclusion criteria for screening ECG per 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: Cohort 1
Subjects will receive a single dose of GSK1349572 100 mg in Period 1 followed by a washout of at least 6 days. Subjects will then receive GSK1349572 50 mg once a day for 5 days in Period 2. Period 3 will begin immediately after Period 2. In Period 3 subjects will receive GSK1349572 50 mg once a day in the morning and Efavirenz 600 mg once a day at bedtime for 14 days. There will be a screening visit up to 30 days before Period 1 and a follow up visit 7-14 days after the end of Period 3.
GSK1349572 is an experimental drug under development for the treatment of HIV. It is in the class of integrase inhibitors.
Efavirenz is a drug that has been approved by the FDA for the treatment of HIV. It is in the class of non-nucleoside reverse trancriptase inhibitors.
Autres noms:
  • SUSTIVA. SUSTIVA is a registered trademark of Bristol-Myers Squibb

Que mesure l'étude ?

Principaux critères de jugement

Mesure des résultats
Description de la mesure
Délai
Plasma GSK1349572 PK parameters: AUC (0-24)
Délai: 24 hours
Plasma GSK1349572 PK parameters: AUC(0-24), Cmax, and C24, and dose-normalized AUC(0-24), Cmax, and C24 following single dose administration of 100mg and 50mg.
24 hours
Plasma GSK1349572 PK parameters: Cmax
Délai: 24 hours
Plasma GSK1349572 PK parameters: AUC(0-24), Cmax, and C24, and dose-normalized AUC(0-24), Cmax, and C24 following single dose administration of 100mg and 50mg.
24 hours
Plasma GSK1349572 PK parameters: C24
Délai: 24 hours
Plasma GSK1349572 PK parameters: AUC(0-24), Cmax, and C24, and dose-normalized AUC(0-24), Cmax, and C24 following single dose administration of 100mg and 50mg.
24 hours
Plasma GSK1349572 steady-state AUC (0-tau)
Délai: 19 days
Plasma GSK1349572 steady-state AUC(0-tau), Cmax, C0, Ctau, and Cmin following administration of GSK1349572 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days
Plasma GSK1349572 steady-state Cmax
Délai: 19 days
Plasma GSK1349572 steady-state AUC(0-tau), Cmax, C0, Ctau, and Cmin following administration of GSK1349572 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days
Plasma GSK1349572 steady-state C0
Délai: 19 days
Plasma GSK1349572 steady-state AUC(0-tau), Cmax, C0, Ctau, and Cmin following administration of GSK1349572 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days
Plasma GSK1349572 steady-state Ctau
Délai: 19 days
Plasma GSK1349572 steady-state AUC(0-tau), Cmax, C0, Ctau, and Cmin following administration of GSK1349572 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days
Plasma GSK1349572 steady-state Cmin
Délai: 19 days
Plasma GSK1349572 steady-state AUC(0-tau), Cmax, C0, Ctau, and Cmin following administration of GSK1349572 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days

Mesures de résultats secondaires

Mesure des résultats
Description de la mesure
Délai
Safety and tolerability parameters
Délai: 4 weeks
Safety and tolerability parameters, including adverse event, concurrent medication, clinical laboratory, ECG, and vital signs assessments.
4 weeks
Plasma GSK1349572 single dose PK parameters: tmax
Délai: 24 hours
Plasma GSK1349572 single dose PK parameters: tmax and tlag, following administration of GSK1349572 100mg and 50mg.
24 hours
Plasma GSK1349572 single dose PK parameters: tlag
Délai: 24 hours
Plasma GSK1349572 single dose PK parameters: tmax and tlag, following administration of GSK1349572 100mg and 50mg.
24 hours
Plasma GSK1349572 steady-state PK parameters: tmax
Délai: 19 days
Plasma GSK1349572 steady-state PK parameters: tmax, tmin, CL/F, and t½, following 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days
Plasma GSK1349572 steady-state PK parameters: tmin
Délai: 19 days
Plasma GSK1349572 steady-state PK parameters: tmax, tmin, CL/F, and t½, following 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days
Plasma GSK1349572 steady-state PK parameters: CL/F
Délai: 19 days
Plasma GSK1349572 steady-state PK parameters: tmax, tmin, CL/F, and t½, following 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days
Plasma GSK1349572 steady-state PK parameters: t½
Délai: 19 days
Plasma GSK1349572 steady-state PK parameters: tmax, tmin, CL/F, and t½, following 50mg q24h for 5 days and following co-administration with EFV 600mg q24h for 14 days.
19 days

Collaborateurs et enquêteurs

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

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Collaborateurs

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)

16 mars 2010

Achèvement primaire (Réel)

26 mai 2010

Achèvement de l'étude (Réel)

26 mai 2010

Dates d'inscription aux études

Première soumission

4 mars 2010

Première soumission répondant aux critères de contrôle qualité

1 avril 2010

Première publication (Estimation)

2 avril 2010

Mises à jour des dossiers d'étude

Dernière mise à jour publiée (Réel)

25 septembre 2017

Dernière mise à jour soumise répondant aux critères de contrôle qualité

21 septembre 2017

Dernière vérification

1 septembre 2017

Plus d'information

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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