Esta página foi traduzida automaticamente e a precisão da tradução não é garantida. Por favor, consulte o versão em inglês para um texto fonte.

GSK1349572 Drug Interaction Study With Efavirenz

21 de setembro de 2017 atualizado por: 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.

Visão geral do estudo

Descrição detalhada

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

Tipo de estudo

Intervencional

Inscrição (Real)

12

Estágio

  • Fase 1

Contactos e Locais

Esta seção fornece os detalhes de contato para aqueles que conduzem o estudo e informações sobre onde este estudo está sendo realizado.

Locais de estudo

    • New York
      • Buffalo, New York, Estados Unidos, 14202
        • GSK Investigational Site

Critérios de participação

Os pesquisadores procuram pessoas que se encaixem em uma determinada descrição, chamada de critérios de elegibilidade. Alguns exemplos desses critérios são a condição geral de saúde de uma pessoa ou tratamentos anteriores.

Critérios de elegibilidade

Idades elegíveis para estudo

18 anos a 65 anos (Adulto, Adulto mais velho)

Aceita Voluntários Saudáveis

Não

Gêneros Elegíveis para o Estudo

Tudo

Descrição

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

Plano de estudo

Esta seção fornece detalhes do plano de estudo, incluindo como o estudo é projetado e o que o estudo está medindo.

Como o estudo é projetado?

Detalhes do projeto

  • Finalidade Principal: Tratamento
  • Alocação: N / D
  • Modelo Intervencional: Atribuição de grupo único
  • Mascaramento: Nenhum (rótulo aberto)

Armas e Intervenções

Grupo de Participantes / Braço
Intervenção / Tratamento
Experimental: 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.
Outros nomes:
  • SUSTIVA. SUSTIVA is a registered trademark of Bristol-Myers Squibb

O que o estudo está medindo?

Medidas de resultados primários

Medida de resultado
Descrição da medida
Prazo
Plasma GSK1349572 PK parameters: AUC (0-24)
Prazo: 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
Prazo: 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
Prazo: 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)
Prazo: 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
Prazo: 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
Prazo: 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
Prazo: 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
Prazo: 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

Medidas de resultados secundários

Medida de resultado
Descrição da medida
Prazo
Safety and tolerability parameters
Prazo: 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
Prazo: 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
Prazo: 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
Prazo: 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
Prazo: 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
Prazo: 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
Prazo: 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

Colaboradores e Investigadores

É aqui que você encontrará pessoas e organizações envolvidas com este estudo.

Patrocinador

Colaboradores

Datas de registro do estudo

Essas datas acompanham o progresso do registro do estudo e os envios de resumo dos resultados para ClinicalTrials.gov. Os registros do estudo e os resultados relatados são revisados ​​pela National Library of Medicine (NLM) para garantir que atendam aos padrões específicos de controle de qualidade antes de serem publicados no site público.

Datas Principais do Estudo

Início do estudo (Real)

16 de março de 2010

Conclusão Primária (Real)

26 de maio de 2010

Conclusão do estudo (Real)

26 de maio de 2010

Datas de inscrição no estudo

Enviado pela primeira vez

4 de março de 2010

Enviado pela primeira vez que atendeu aos critérios de CQ

1 de abril de 2010

Primeira postagem (Estimativa)

2 de abril de 2010

Atualizações de registro de estudo

Última Atualização Postada (Real)

25 de setembro de 2017

Última atualização enviada que atendeu aos critérios de controle de qualidade

21 de setembro de 2017

Última verificação

1 de setembro de 2017

Mais Informações

Essas informações foram obtidas diretamente do site clinicaltrials.gov sem nenhuma alteração. Se você tiver alguma solicitação para alterar, remover ou atualizar os detalhes do seu estudo, entre em contato com register@clinicaltrials.gov. Assim que uma alteração for implementada em clinicaltrials.gov, ela também será atualizada automaticamente em nosso site .

Se inscrever