Study to Assess the Effect of Rifampicin (CYP Inducer) on Blood Levels and Safety of Olaparib in Patients With Advanced Solid Tumours
A Non-randomised, Open-label, Sequential, Multicentre, Two-part, Phase I Study to Assess the Effect of Rifampicin, a CYP Inducer, on the Pharmacokinetics of Olaparib Following Oral Dosing of a Tablet Formulation in Patients With Advanced Solid Tumours
研究概览
研究类型
注册 (实际的)
阶段
- 阶段1
联系人和位置
参与标准
资格标准
适合学习的年龄
接受健康志愿者
有资格学习的性别
描述
Inclusion Criteria:-
For inclusion in the study, patients should fulfil the following criteria:
- Provision of written informed consent prior to any study-specific procedures.
- Patients aged greater than or equal to 18 years.
- Histologically or, where appropriate, cytologically confirmed malignant solid tumour refractory or resistant to standard therapy or for which no suitable effective standard therapy exists.
4 Patients must have normal organ and bone marrow function measured within 28 days prior to administration of investigational product (IP) as defined below: Haemoglobin (Hb) greater than or equal to 10.0 g/dL, with no blood transfusions in the previous 28 days.
Absolute neutrophil count (ANC) greater than or equal to 1.5 x 109/L. White blood cells (WBC) greater than 3 x 109/L. Platelet count greater than or equal to 100 x 109/L. Total bilirubin less than or equal to 1.5 x institutional upper limit of normal (ULN) (except in the case of Gilbert's disease).
Aspartate aminotransferase (AST), alanine aminotransferase (ALT) less than or equal to 2.5 x institutional ULN unless liver metastases are present, in which case it must be less than or equal to 5x ULN, Serum creatinine less than or equal to 1.5 x institutional ULN.
5. Calculated serum creatinine clearance greater than 50 mL/min (using Cockroft-Gault formula or by 24 hour urine collection).
6. Eastern Cooperative Oncology Group (ECOG) performance status less than or equal to 2.
7. Patients must have a life expectancy of greater than or equal to 16 weeks. 8. Evidence of non-childbearing status for women of childbearing potential, or post menopausal status: negative urine or serum pregnancy test within 28 days of study treatment, confirmed prior to treatment on Day 1 of Part A. Post-menopausal is defined as: Amenorrheic for 1 year or more following cessation of exogenous hormonal treatments.
Luteinising hormone and follicle stimulating hormone levels in the post menopausal range for women under 50 years of age.
Radiation-induced oophorectomy with last menses greater than 1 year ago. Chemotherapy-induced menopause with greater than 1 year interval since last menses.
Surgical sterilisation (bilateral oophorectomy or hysterectomy). 9. Patients are willing and able to comply with the protocol for the duration of the study including undergoing treatment and scheduled visits and examinations.
10. Patients must be on a stable concomitant medication regimen (with the exception of electrolyte supplements), defined as no changes in medication or in dose within the 2 weeks prior to start of olaparib dosing, except for bisphosphonates, denosumab, and corticosteroids, which should be at a stable dose for at least 4 weeks prior to the start of olaparib dosing.
Exclusion Criteria:- Patients should not enter the study if any of the following exclusion criteria are fulfilled.
- Involvement in the planning and/or conduct of the study (applies to AstraZeneca staff, its agents, and/or staff at the study site).
- Previous enrolment in the present study.
- Participation in another clinical study with an IP during the last 14 days (or a longer period depending on the defined characteristics of the agents used).
- Patients receiving any systemic chemotherapy or radiotherapy (except for palliative reasons) within 2 weeks prior to study treatment (or a longer period depending on the defined characteristics of the agents used). The patient can receive a stable dose of bisphosphonates or denosumab for bone metastases, before and during the study, as long as these were started at least 4 weeks prior to treatment.
- Patients who have received or are receiving inhibitors or inducers of CYP3A4.
- Toxicities (greater than or equal to Common Toxicity Criteria for Adverse Events [CTCAE] Grade 2) caused by previous cancer therapy, excluding alopecia.
- Any intake of grapefruit, grapefruit juice, Seville oranges, Seville orange marmalade, or other products containing grapefruit or Seville oranges within 7 days of the first administration of the IP until the end of Part A.
- Patients with brain metastases. A scan to confirm the absence of brain metastases is not required.
- Major surgery within 2 weeks of starting study treatment and patients must have recovered from any effects of major surgery.
- Patients considered a poor medical risk due to a serious uncontrolled medical disorder, non malignant systemic disease, uncontrolled seizures, or active uncontrolled infection. Examples include, but are not limited to, uncontrolled ventricular arrhythmia, recent (within 3 months) myocardial infarction, uncontrolled major seizure disorder, unstable spinal cord compression, superior vena cava syndrome, extensive bilateral interstitial lung disease on high resolution computer tomography (HRCT) scan, or any psychiatric disorder that prohibits obtaining informed consent.
- Patients who have diabetes mellitus.
- Patients who have gastric, gastro-oesophageal, or oesophageal cancer .
- Patients unable to swallow orally administered medication and patients with gastrointestinal disorders or significant gastrointestinal resection likely to interfere with the absorption of olaparib.
- Breastfeeding women.
- Immunocompromised patients, eg, patients who are known to be serologically positive for human immunodeficiency virus (HIV).
- Patients with known active hepatic disease (eg, hepatitis B or C).
- Patients with a known hypersensitivity to rifampicin or any of the excipients of the product.
- Patients with a known hypersensitivity to olaparib or any of the excipients of the product.
- Resting electrocardiogram (ECG) at screening with measurable QT interval (QT) corrected for heart rate (QTc) greater than 470 msec at 2 or more time points within a 24 hour period or family history of long QT syndrome.
- Concomitant medication contraindicated for use with rifampicin (including, but not limited to): atazanavir, darunavir, fosamprenavir, ritonavir-boosted saquinavir, saquinavir, or tipranavir.
- Patients who have jaundice.
- Patients who weigh less than 50 kg.
- Clinical judgment by the investigator that the patient should not participate in the study.
学习计划
研究是如何设计的?
设计细节
- 分配:不适用
- 介入模型:单组作业
- 屏蔽:无(打开标签)
武器和干预
参与者组/臂 |
干预/治疗 |
|---|---|
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实验性的:Olaparib alone, olaparib+rifampicin
Sequential treatments of olaparib alone followed by olaparib+rifampicin, with a washout period inbetween.
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Blood sampling to measure olaparib, rifampicin and 4β-hydroxycholesterol
Rifampicin (CYP inducer) 600mg taken once daily from Day 5 to Day 14 (Part A)
Olaparib 300mg tablet taken on Days 1 and 14 (Part A).
Part B dosing is 300mg olaparib bi-daily
|
研究衡量的是什么?
主要结果指标
结果测量 |
措施说明 |
大体时间 |
|---|---|---|
|
Pharmacokinetics of olaparib by assessment of maximum plasma olaparib concentration (Cmax)
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of maximum plasma olaparib concentration (Cmax).
Olaparib doses are first without, then with rifampicin.
|
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
|
Pharmacokinetics of olaparib by assessment of area under the plasma concentration time curve from zero to infinity (AUC)
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of area under the plasma concentration time curve from zero to infinity (AUC). Olaparib doses are first without, then with rifampicin. |
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
|
Pharmacokinetics of olaparib by assessment of area under the plasma concentration time curve from zero to the last measurable time point, AUC0-t, if AUC is not adequately estimable.
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of area under the plasma concentration time curve from zero to the last measurable time point, AUC0-t, if AUC is not adequately estimable.
Olaparib doses are first without, then with rifampicin.
|
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
次要结果测量
结果测量 |
措施说明 |
大体时间 |
|---|---|---|
|
Pharmacokinetics of olaparib by assessment of time to reach maximum plasma concentration for olaparib (tmax).
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of time to reach maximum plasma concentration for olaparib (tmax).
Olaparib doses are first without, then with rifampicin.
|
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
|
Pharmacokinetics of olaparib by assessment of olaparib area under the plasma concentration time curve from zero to the last measurable time point (AUC0-τ).
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of olaparib area under the plasma concentration time curve from zero to the last measurable time point (AUC0-τ).
Olaparib doses are first without, then with rifampicin.
|
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
|
Pharmacokinetics of olaparib by assessment of olaparib apparent clearance (CL/F).
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of olaparib apparent clearance (CL/F).
Olaparib doses are first without, then with rifampicin.
|
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
|
Pharmacokinetics of olaparib by assessment of olaparib apparent volume of distribution (Vz/F).
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of olaparib apparent volume of distribution (Vz/F).
Olaparib doses are first without, then with rifampicin.
|
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
|
Pharmacokinetics of olaparib by assessment of olaparib terminal half-life (t1/2).
大体时间:Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
Rate and extent of absorption of olaparib following single oral doses of olaparib tablet formulation by assessment of olaparib terminal half-life (t1/2).
Olaparib doses are first without, then with rifampicin.
|
Blood samples are collected on olaparib dosing days (Day 1 and 14) at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A.
|
|
Pharmacokinetics of rifampicin by assessment of plasma concentrations of rifampicin during rifampicin dosing period.
大体时间:Rifampicin is dosed daily from Days 5 to 17 in Part A. Blood samples are collected on Days 5, 9, 14 and 17 at 2 hours post rifampicin dose
|
Rate and extent of absorption of rifampicin following multiple doses of rifampicin by assessment of plasma concentrations of rifampicin during rifampicin dosing period.
|
Rifampicin is dosed daily from Days 5 to 17 in Part A. Blood samples are collected on Days 5, 9, 14 and 17 at 2 hours post rifampicin dose
|
|
Demonstration of induction of CYP by assessment of plasma concentrations of 4β-hydroxycholesterol during rifampicin dosing period.
大体时间:Blood samples are collected on Days 5, 9, 14 and 17 at pre-dose of rifampicin in Part A
|
Demonstration of CYP induction by assessment of plasma concentrations of 4β-hydroxycholesterol during rifampicin dosing period.
|
Blood samples are collected on Days 5, 9, 14 and 17 at pre-dose of rifampicin in Part A
|
|
Assessment of the safety and tolerability of olaparib by collection of adverse event reports
大体时间:Part A: From baseline, every visit until 30 days after last dose. Part B, from start to 12 months after the last patient has entered Part B
|
Assessment of adverse events (AEs) graded by Common Terminology Criteria for Adverse Events (CTCAE) v4.0
|
Part A: From baseline, every visit until 30 days after last dose. Part B, from start to 12 months after the last patient has entered Part B
|
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Determine safety and tolerability of olaparib by assessment of 12 lead electrocardiograms
大体时间:Part A: baseline, Days -1, 17 (and within 30 days post last olaparib dose if not in Part B).
|
Assessment of standard 12 lead electrocardiograms (ECGs)
|
Part A: baseline, Days -1, 17 (and within 30 days post last olaparib dose if not in Part B).
|
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Determine safety and tolerability of olaparib by physical examination
大体时间:Part A: baseline, Day -1 and within 30 days after last dose. Part B: Day 1.
|
Assessment of physical examination
|
Part A: baseline, Day -1 and within 30 days after last dose. Part B: Day 1.
|
|
Determine safety and tolerability of olaparib by assessment of vital signs
大体时间:Part A: baseline, Days 1,2 and 3. Part B: Days 1,8,15,22,29 then every 4 weeks. Final assessment within 30 days after last dose.
|
Assessment of standard vital signs (including blood pressure, pulse)
|
Part A: baseline, Days 1,2 and 3. Part B: Days 1,8,15,22,29 then every 4 weeks. Final assessment within 30 days after last dose.
|
|
Determine safety and tolerability of olaparib by assessment of clinical chemistry results
大体时间:Part A: baseline, Days -1, 9, 14, 17. Part B: Days 1,8,15,22,29 then every 4 weeks. Final assessment within 30 days after last dose.
|
Assessment of laboratory parameters (clinical chemistry)
|
Part A: baseline, Days -1, 9, 14, 17. Part B: Days 1,8,15,22,29 then every 4 weeks. Final assessment within 30 days after last dose.
|
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Determine safety and tolerability of olaparib by assessment of haematology results
大体时间:Part A: baseline, Days -1, 9, 14, 17. Part B: Days 1,8,15,22,29 then every 4 weeks. Final assessment within 30 days after last dose.
|
Assessment of laboratory parameters (haematology)
|
Part A: baseline, Days -1, 9, 14, 17. Part B: Days 1,8,15,22,29 then every 4 weeks. Final assessment within 30 days after last dose.
|
|
Determine safety and tolerability of olaparib by assessment of urinalysis results
大体时间:Part A: baseline, Days -1, 14, 17. Part B: Day 1 only
|
Assessment of laboratory parameters (urinalysis)
|
Part A: baseline, Days -1, 14, 17. Part B: Day 1 only
|
合作者和调查者
赞助
调查人员
- 研究主任:Anitra Fielding、AstraZeneca Senior Research Physician
- 首席研究员:Luc Dirix、GZA Ziekenhuizen campus Sint-Augustinus
出版物和有用的链接
研究记录日期
研究主要日期
学习开始
初级完成 (实际的)
研究完成 (实际的)
研究注册日期
首次提交
首先提交符合 QC 标准的
首次发布 (估计)
研究记录更新
最后更新发布 (估计)
上次提交的符合 QC 标准的更新
最后验证
更多信息
与本研究相关的术语
其他相关的 MeSH 术语
其他研究编号
- D0816C00008
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