Solid TumorsPhase 1NCT03258515
A Study to Investigate the Effect of Single Dose of AZD6094 (600 mg) on Cardiac Repolarization in Healthy Volunteers
A Phase 1 study testing AZD6094 200 mg and Moxifloxacin in people with Solid Tumors, run by AstraZeneca at 1 site in United States.
Trial summary
This is a randomized, placebo-controlled, double-blind, 3-way crossover phase I study being conducted on healthy volunteers to investigate the effect of single dose of AZD6094 (600 mg) on cardiac repolarization under well-controlled conditions in accordance with the International Council for Harmonization (ICH) E14… Read more about this study
- Who is it for?
- Ages 18 to 55 years, men onlyHealthy volunteers can take part
- Conditions the study is for
- Solid Tumors
- What is being tested?
- AZD6094 200 mg and Moxifloxacin
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- Yes, some participants may receive a placebo
- How many people
- 45 participants
- Where
- 1 siteUnited States
- Study dates
- 6 Sep 2017to 24 Mar 2018
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- Men only
- Healthy volunteers accepted
- Adult
Who may be able to join
- Participants must fulfill the following criteria:
- Provision of signed and dated, written informed consent prior to any study specific procedure.
- Healthy vasectomized male participants with suitable veins for cannulation or repeated venipuncture, non-Japanese vasectomized male participants aged 18 to 55 years (inclusive) or male participants over 40 (and up to 55) years old not intending to father children.
- Body mass index (BMI) between 18 and 30 kg/m2 inclusive and weigh greater than 50 kg and no more than 100 kg.
- Alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin (TBL) less than or equal to the upper limit of normal for the institution.
- Have a calculated creatinine clearance (CrCL) greater than 80 mL/min using the Cockcroft-Gault formula at Screening.
- Provision of signed, written and dated informed consent for optional genetic/biomarker research. If a subject declines to participate in the genetic component of the study, there will be no penalty or loss of benefit to the subject. The subject will not be excluded from other aspects of the study described in this Clinical Study Protocol (CSP).
Who cannot join
- Participants must not be randomized if any of the following exclusion criteria are fulfilled:
- Healthy participants of Japanese ethnicity and any healthy subject that has 1 parent or grandparent (maternal or paternal) that is Japanese.
- History of any clinically important disease or disorder which, in the opinion of the Investigator, may either put the subject at risk because of participation in the study, or influence the results or the subject's ability to participate in the study.
- History or presence of gastrointestinal (GI), hepatic or renal disease or any other condition known to interfere with absorption, distribution, metabolism or excretion of drugs.
- Any clinically important illness, medical/surgical procedure or trauma within 4 weeks of the first administration of IMP.
- Planned in-patient surgery, dental procedure or hospitalization during the study.
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- Any clinically important abnormalities in clinical chemistry, hematology or urinalysis results as judged by the Investigator.
- Any positive result on screening for serum hepatitis B surface antigen, hepatitis C antibody and human immunodeficiency virus (HIV).
- Abnormal vital signs, after 10 minutes supine rest, defined as any of the following:
- SBP < 90 mmHg or ≥ 140 mmHg; DBP < 50 mmHg or ≥ 90 mmHg; HR < 45 or > 85 beats per minute.
- Any clinically important abnormalities in rhythm, conduction or morphology of the 12-lead resting ECG that may interfere with the interpretation of QTc interval changes. These include healthy participants with any of the following:
- Abnormal ST-T-wave morphology, particularly in the protocol defined primary lead (V2) or left ventricular hypertrophy.
- PR interval shortening < 120 ms (PR > 110 ms but < 120 ms is acceptable if there is no evidence of ventricular pre-excitation).
- PR interval prolongation (> 200 ms). Intermittent second (Type 1 second degree block [Wenckebach Phenomenon] while asleep is not exclusive]) or third degree atrioventricular (AV) block, or AV dissociation.
- Persistent or intermittent complete bundle branch block (BBB), incomplete bundle branch block (IBBB), or intraventricular conduction delay (IVCD) with QRS > 110 ms. Participants with QRS > 110 ms but < 115 ms are acceptable if there is no evidence of e.g. ventricular hypertrophy or pre-excitation.
- Prolonged QTcF > 450 ms or shortened QTcF < 340 ms or family history of long QT syndrome.
- A history of additional risk factors for torsades de pointes (TdP) (e.g., heart failure, hypokalemia, family history of long QT syndrome or sudden death at young age).
- Known or suspected history of drug abuse as judged by the Investigator.
- Current smokers or those who have smoked or used nicotine products within the previous 30 days.
- History of alcohol abuse or excessive intake of alcohol as judged by the Investigator.
- Excessive intake of caffeine-containing drinks or food (e.g., coffee, tea, chocolate,) as judged by the Investigator.
- Use of drugs with enzyme inducing properties such as St John's Wort within 3 weeks prior to the first administration of the IMP.
- 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 admission on Day -1.
- Use of any prescribed or non-prescribed medication including antacids, analgesics (other than use of ibuprofen up to 72 hours before dosing day), herbal remedies, megadose vitamins (intake of 20 to 600 times the recommended daily dose) and minerals during the 2 weeks before the first administration of the IMP or longer (5 times half-life) if the medication has a long half-life. No medications known to prolong the QT/QTc interval are allowed.
- Positive screen for drugs of abuse, cotinine (nicotine) and/or alcohol at Screening and before each admission to the Clinical Unit.
- History of severe allergy/hypersensitivity (including allergy to fluoroquinolone antibiotics) or ongoing clinically important allergy/hypersensitivity, as judged by the Investigator.
- History of severe allergy/hypersensitivity or ongoing clinically important allergy/hypersensitivity, as judged by the Investigator or history of hypersensitivity to drugs with a similar chemical structure or class to AZD6094.
- Plasma donation within one month of Screening or any blood donation/blood loss > 500 mL during the 3 months prior to Screening.
- Has received another new chemical entity (defined as a compound which has not been approved for marketing) within 3 months of the first administration of investigational product in this study. The period of exclusion begins 3 months after the final dose or one month after the last visit whichever is the longest. Note: participants consented and screened, but not randomized in this study or a previous Phase I study, are not excluded.
- Involvement of any Astra Zeneca or study site employee or their close relatives.
- Judgment by the Investigator that the subject should not participate in the study if they have any ongoing or recent (i.e., during the screening period) minor medical complaints that may interfere with the interpretation of study data or are considered unlikely to comply with study procedures, restrictions and requirements.
- Participants who are vegans, vegetarians or have medical dietary restrictions.
- Participants who cannot communicate reliably with the Investigator.
- Vulnerable participants, e.g., kept in detention, protected adults under guardianship, trusteeship, or committed to an institution by governmental or juridical order.
- In addition, any of the following is regarded as a criterion for exclusion from the genetic research:
- Previous bone marrow transplant.
- Non-leukocyte depleted whole blood transfusion within 120 days of the date of the genetic sample collection.
Trial locations and contacts
1 site in 1 country.
About this study
Official title: A Single-center, Randomized, Double-blind, Placebo-controlled, Three-way Crossover Phase I Study to Investigate the Effect on the QTc Interval of a Single Dose of AZD6094 (600 mg) Compared With Placebo, Using Open-label Moxifloxacin (Avelox®) as a Positive Control, in Healthy Volunteers
This is a randomized, placebo-controlled, double-blind, 3-way crossover phase I study being conducted on healthy volunteers to investigate the effect of single dose of AZD6094 (600 mg) on cardiac repolarization under well-controlled conditions in accordance with the International Council for Harmonization (ICH) E14 guidelines. An open-label Moxifloxacin (400 mg), a fluoroquinolone broad spectrum antibiotic will be used as a appositive control for the time between the start of the Q wave and the end of the T wave (QT) prolongation in accordance with ICH E14 guidelines, to establish assay sensitivity. The core study consists of screening period, 3 treatment period (AZD6094, placebo and moxifloxacin; with a minimum washout period of 14 days between each treatment period) and follow-up. The study drugs will be administered orally. The study is planned to determine effect of AZD6094 at therapeutic dose, safety and tolerability. This study provides adequate and well-controlled mechanisms to deal with potential bias, facilitate identification of effects related to investigational product (IMP) administration and tolerability issues.
Read the detailed description
The study is planned to include approximately 45 healthy non-Japanese vasectomized male participants aged 18 to 55 years (inclusive) or male participants over 40 (and up to 55) years old not intending to father children will be enrolled. The study consists of 5 visits comprised of 3 treatment periods with 6 treatment sequences and will have a minimum washout period of 14 days between each treatment period.
Visit 1: Screening period (28 days) - Assessments done on Day -1 of treatment period 1.
Visits 2 to 4: 3 Treatment periods - Participants will be resident form day before IMP (single oral dose of AZD6094 (600 mg) tablet/AZD6094 matching placebo/moxifloxacin (400 mg) capsule) dosing (Day -1) until at least 48 hours post-dose and will be discharged on Day 3.
Visit 5: Follow-up - Participants will have clinical visit 14 days after discharge from the treatment period 3.
Participants will be randomized to 6 treatment sequences (ABC, ACB, BAC, BCA, CAB and CBA). In each sequence, participants will receive single oral dose of all 3 treatments (A - AZD6094 600 mg (3X 200 mg tablet), B - Placebo tablet, C - Moxifloxacin 400 mg capsule) with a washout period (14 days) between each treatment period.
The study duration will be approximately 84 days.
- Conditions
- Solid Tumors
- Being tested
- AZD6094 200 mg, Placebo, Moxifloxacin
- Keywords
- Mesenchymal epithelial transition (MET) receptor, Small molecule kinase inhibitors, Moxifloxacin (Avelox), QT prolongation
- Medical subject headings
- Long QT Syndrome
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
AZD6094 200 mgDrug
A potent and selective small molecule mesenchymal epithelial transition (MET) kinase inhibitor with significant antitumor activity.
PlaceboOther
AZD6094 matching placebo without any pharmacological activity.
MoxifloxacinDrug
Also called Avelox
A fluoroquinolone broad-spectrum antibiotic, produces a mild, but reproducible increase in QT interval corrected (QTc) in healthy normal participants at time to reach maximum concentration (tmax - approximately 2 hours (0.5 to 4 hours)). This effect is close to the ECG interval measured from the onset of the QRS complex (onset of the QRS complex to the J point) to the offset of the T wave (QT)/QTc effect that represents the threshold of regulatory concern, around 5 ms mean QTc interval prolongation.
| Study group | Role | What they receive |
|---|---|---|
| Cohort 1 | Experimental | Participants will receive orally single dose of study drugs in the sequence of ABC.
A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg Receives: Drug: AZD6094 200 mg; Other: Placebo; Drug: Moxifloxacin |
| Cohort 2 | Experimental | Participants will receive orally single dose of study drugs in the sequence of ACB.
A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg Receives: Drug: AZD6094 200 mg; Other: Placebo; Drug: Moxifloxacin |
| Cohort 3 | Experimental | Participants will receive orally single dose of study drugs in the sequence of BAC.
A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg Receives: Drug: AZD6094 200 mg; Other: Placebo; Drug: Moxifloxacin |
| Cohort 4 | Experimental | Participants will receive orally single dose of study drugs in the sequence of BCA.
A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg Receives: Drug: AZD6094 200 mg; Other: Placebo; Drug: Moxifloxacin |
| Cohort 5 | Experimental | Participants will receive orally single dose of study drugs in the sequence of CAB.
A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg Receives: Drug: AZD6094 200 mg; Other: Placebo; Drug: Moxifloxacin |
| Cohort 6 | Experimental | Participants will receive orally single dose of study drugs in the sequence of CBA.
A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg Receives: Drug: AZD6094 200 mg; Other: Placebo; Drug: Moxifloxacin |
What is being measured
The primary outcome is the main question the study is designed to answer.
Effect of AZD6094 at single therapeutic dose (600 mg) on ventricular repolarization by analysis of change from baseline-corrected QT
To assess the effect of AZD6094 at single therapeutic dose (600mg) on ventricular repolarization by assessing the time matched baseline-adjusted, placebo subtracted QTc interval corrected for RR (R waves on electrocardiogram [ECG]) by the Fridericia formula (QTcF). The ECGs -digital (dECG) and page (pECG) would be recorded during the study for the assessment of safety. Paper ECG for safety review will be performed following the dECG recordings and at additional intervals if required.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Secondary outcomes (22)
Effect of AZD6094 at therapeutic dose (600 mg) on additional time-matched ECG variables
To assess the effect of AZD6094 at therapeutic dose (600 mg) on additional time matched ECG variables using the dECG and pECG records. The ECG variables includes Bazett corrected QT interval [QTcB], onset of the P wave to the onset of the QRS complex (PR), onset of the QRS complex to the J point (QRS), QT and time interval between corresponding points on 2 consecutive R waves on ECG (RR). Paper ECG for safety review will be performed following the dECG recordings and at additional intervals if required.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Effect of moxifloxacin 400 mg on Fridericia-corrected QT interval (QTcF) compared to placebo.
To assess the effect of moxifloxacin 400 mg on the QTcF interval compared to placebo. Paper ECG for safety review will be performed following the dECG recordings and at additional intervals if required.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Area under the plasma concentration-curve from time zero to the time of last quantifiable analyte concentration (AUC(0-∞)) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess AUC(0-∞) after administration of single oral dose of AZD6094, placebo and moxifloxacin. The pharmacokinetic (PK) sampling done post dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Area under the plasma concentration-time curve from time zero to t hours after dosing (AUC(0-t)) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess AUC(0-t) after administration of single oral dose of AZD6094, placebo and moxifloxacin. The PK sampling done post dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Observed maximum concentration (Cmax) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess Cmax after administration of single oral dose of AZD6094, placebo and moxifloxacin; Cmax will be taken directly from the individual concentration-time curve. The PK sampling done post-dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Time to reach maximum concentration (tmax) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess tmax after administration of single oral dose of AZD6094, placebo and moxifloxacin; tmax will be taken directly from the individual concentration-time curve. The PK sampling done post-dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Lag-time (tlag - from the individual concentration-time curve) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess lag-time (tlag) after administration of single oral dose of AZD6094, placebo and moxifloxacin; tlag will be taken directly from the individual concentration-time curve. The PK sampling done post-dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Terminal rate constant (λz) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess λz after administration of single oral dose of AZD6094, placebo and moxifloxacin; λz will be estimated by log-linear least squares regression of the terminal part of the concentration-time curve. The PK sampling done post-dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Terminal half-life (t½) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess t½ after administration of single oral dose of AZD6094, placebo and moxifloxacin. The PK sampling done post-dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Apparent clearance for parent drug estimated as dose divided by AUC (CL/F) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess CL/F after administration of single oral dose of AZD6094, placebo and moxifloxacin. The PK sampling done post-dose must precede with 10 minutes of rest followed by 5 minutes dECG.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Apparent volume of distribution for parent drug at terminal phase (Vz/F, extravascular administration) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
To assess apparent volume of distribution for parent drug at terminal phase (Vz/F, extravascular administration) after administration of single oral dose of AZD6094, placebo and moxifloxacin; Vz/F will be estimated by dividing the apparent clearance (CL/F) by λz. 10 min rest + 5 min dECG will always precede the PK sampling when coinciding post-dose.
Measured: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Assessment of relationship between the plasma concentration of AZD6094 and moxifloxacin and ECG variables, including baseline-adjusted and placebo-subtracted QTc interval.
To assess the effect of AZD6094 and moxifloxacin on ventricular repolarization by assessing the plasma concentration and ECG variables including baseline-adjusted and placebo subtracted QTc interval
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Number of participants with adverse events (AEs) of AZD6094
To assess AEs as a criteria of safety and tolerability. AEs will be collected from the start of Screening throughout the treatment period up to and including the Follow-up Visit (Visit 5). Serious AEs will be recorded from the time of informed consent.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose (Day -1) and post-dose (24 hours and 48 hours) and follow-up (14 days after discharge from the treatment period 3)
Systolic blood pressure [SBP]
To assess SBP as criteria of safety and tolerability variables. Blood pressure will be taken after the ECG.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Diastolic blood pressure [DBP]
To assess DBP as criteria of safety and tolerability variables. Blood pressure will be taken after the ECG.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Pulse rate
To assess pulse rate as criteria of safety and tolerability variables.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Twelve-lead (12-Lead) electrocardiograms (ECGs)
To assess the cardiovascular system functioning using 12-Lead dECG and pECG as a criteria of safety and tolerability variables.
Measured: At screening, treatment periods (pre-dose and post-dose - 30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours and 24 hours) and follow-up visits
Physical examination
To assess the physical examination as a criteria of safety and tolerability variables. Brief physical examination will be performed at pre-dose on Day -1 at each treatment period; includes assessment of general appearance, skin, cardiovascular system, respiratory and abdomen. Full physical examination includes assessment of the general appearance, skin, cardiovascular, respiratory, abdomen, head, and neck (including ears, eyes, nose, and throat), lymph nodes, thyroid, musculoskeletal and neurological systems.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Laboratory assessments of Hematology
To assess the hematology (blood cells count, differential count and hemoglobin count) as a criteria of safety and tolerability variables. A reduced safety laboratory screen will be done at Day -1 or pre-dose at Day 1 and at 48 hours post-dose for all treatment periods.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Laboratory assessments of Clinical chemistry
To assess the clinical chemistry (electrolytes, glucose (fasting), C-reactive protein (CRP), liver enzymes, total and unconjugated bilirubin; at screening alone - free thyroxine and thyroid-stimulating hormone) as a criteria of safety and tolerability variables. A reduced safety laboratory screen will be done at Day -1 or pre-dose at Day 1 and at 48 hours post-dose for all treatment periods.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Laboratory assessments of urinalysis
To assess the urinalysis (glucose, protein and blood) as a criteria of safety and tolerability variables. If urinalysis is positive for protein or blood, a microscopy test will be performed to assess red blood cells (RBC), white blood cells (WBC), casts (cellular, granular, hyaline)). A reduced safety laboratory screen will be done at Day -1 or pre-dose at Day 1 and at 48 hours post-dose for all treatment periods.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Effect of AZD6094 at therapeutic dose (600 mg) on time-matched ECG variable - heart rate (HR)
To assess the effect of AZD6094 at therapeutic dose (600 mg) on additional time matched ECG variable - HR using the dECG and pECG records. Paper ECG for safety review will be performed following the dECG recordings and at additional intervals if required.
Measured: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted23 Aug 2017
- Study start6 Sep 2017
- Primary completion24 Mar 2018
- Study completion24 Mar 2018
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (2)Papers the sponsor has linked to this study.
- Other trials for Solid TumorsStudies of the same condition, open and under way.
- More trials run by AstraZenecaThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- Double blind
- Who is masked
- Participant, Investigator
- Enrolment
- 45 participants (actual)
Sponsor and investigators
- Lead sponsor
- AstraZeneca
- Sponsor type
- Industry (pharma, biotech, devices)
- Collaborators
- Parexel
- Responsible party
- Sponsor
- Investigators
- Ronald Goldwater, MD, Principal investigator, PAREXEL Early Phase Clinical Unit Baltimore
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT03258515
- Sponsor's protocol ID
- D5084C00001
- Status last verified
- Feb 2020
- First submitted
- 11 Aug 2017
- Last updated
- 20 Feb 2020
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
Publications
Schalkwijk S, Sahota T, Verheijen RB, Harmer AR, Ahmed GF. Parent and Metabolite Concentration-QT Modeling to Evaluate QT-Interval Prolongation at Savolitinib Therapeutic Doses. AAPS J. 2021 Mar 17;23(3):46. doi: 10.1208/s12248-021-00573-1.
PubMed 33733338Sahota T, Dota CD, Vik T, Yan W, Verheijen RB, Walker S, Li Y, Goldwater R, Ghiorghiu D, Mellemgaard A, Ahmed GF. A Randomized, Double-Blind, Placebo- and Positive-Controlled, Three-Way Crossover Study in Healthy Participants to Investigate the Effect of Savolitinib on the QTc Interval. Clin Pharmacol Drug Dev. 2021 May;10(5):521-534. doi: 10.1002/cpdd.896. Epub 2021 Jan 5.
PubMed 33400845
Study at a glance
From the registry record, last updated by the sponsor on 20 Feb 2020. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Single-center, Randomized, Double-blind, Placebo-controlled, Three-way Crossover Phase I Study to Investigate the Effect on the QTc Interval of a Single Dose of AZD6094 (600 mg) Compared With Placebo, Using Open-label Moxifloxacin (Avelox®) as a Positive Control, in Healthy Volunteers
- ClinicalTrials.gov ID
- NCT03258515
- Acronym / sponsor ID
- D5084C00001
- Conditions
- Solid Tumors
- Keywords
- Mesenchymal epithelial transition (MET) receptor, Small molecule kinase inhibitors, Moxifloxacin (Avelox), QT prolongation
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 45 participants (actual)
- Lead sponsor
- AstraZenecaIndustry (pharma, biotech, devices)
- Collaborators
- Parexel
- Study start
- 6 Sep 2017 (actual)
- Primary completion
- 24 Mar 2018 (actual)
- Study completion
- 24 Mar 2018 (actual)
- First posted
- 23 Aug 2017 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This is a randomized, placebo-controlled, double-blind, 3-way crossover phase I study being conducted on healthy volunteers to investigate the effect of single dose of AZD6094 (600 mg) on cardiac repolarization under well-controlled conditions in accordance with the International Council for Harmonization (ICH) E14 guidelines. An open-label Moxifloxacin (400 mg), a fluoroquinolone broad spectrum antibiotic will be used as a appositive control for the time between the start of the Q wave and the end of the T wave (QT) prolongation in accordance with ICH E14 guidelines, to establish assay sensitivity. The core study consists of screening period, 3 treatment period (AZD6094, placebo and moxifloxacin; with a minimum washout period of 14 days between each treatment period) and follow-up. The study drugs will be administered orally. The study is planned to determine effect of AZD6094 at therapeutic dose, safety and tolerability. This study provides adequate and well-controlled mechanisms to deal with potential bias, facilitate identification of effects related to investigational product (IMP) administration and tolerability issues.
Detailed description
The study is planned to include approximately 45 healthy non-Japanese vasectomized male participants aged 18 to 55 years (inclusive) or male participants over 40 (and up to 55) years old not intending to father children will be enrolled. The study consists of 5 visits comprised of 3 treatment periods with 6 treatment sequences and will have a minimum washout period of 14 days between each treatment period.
Visit 1: Screening period (28 days) - Assessments done on Day -1 of treatment period 1.
Visits 2 to 4: 3 Treatment periods - Participants will be resident form day before IMP (single oral dose of AZD6094 (600 mg) tablet/AZD6094 matching placebo/moxifloxacin (400 mg) capsule) dosing (Day -1) until at least 48 hours post-dose and will be discharged on Day 3.
Visit 5: Follow-up - Participants will have clinical visit 14 days after discharge from the treatment period 3.
Participants will be randomized to 6 treatment sequences (ABC, ACB, BAC, BCA, CAB and CBA). In each sequence, participants will receive single oral dose of all 3 treatments (A - AZD6094 600 mg (3X 200 mg tablet), B - Placebo tablet, C - Moxifloxacin 400 mg capsule) with a washout period (14 days) between each treatment period.
The study duration will be approximately 84 days.
Study design
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- Double blind (participant, investigator)
- Number of arms
- 6
| Arm | Type | Receives |
|---|---|---|
| Cohort 1 | Experimental | Drug: AZD6094 200 mg, Other: Placebo, Drug: MoxifloxacinParticipants will receive orally single dose of study drugs in the sequence of ABC. A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg |
| Cohort 2 | Experimental | Drug: AZD6094 200 mg, Other: Placebo, Drug: MoxifloxacinParticipants will receive orally single dose of study drugs in the sequence of ACB. A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg |
| Cohort 3 | Experimental | Drug: AZD6094 200 mg, Other: Placebo, Drug: MoxifloxacinParticipants will receive orally single dose of study drugs in the sequence of BAC. A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg |
| Cohort 4 | Experimental | Drug: AZD6094 200 mg, Other: Placebo, Drug: MoxifloxacinParticipants will receive orally single dose of study drugs in the sequence of BCA. A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg |
| Cohort 5 | Experimental | Drug: AZD6094 200 mg, Other: Placebo, Drug: MoxifloxacinParticipants will receive orally single dose of study drugs in the sequence of CAB. A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg |
| Cohort 6 | Experimental | Drug: AZD6094 200 mg, Other: Placebo, Drug: MoxifloxacinParticipants will receive orally single dose of study drugs in the sequence of CBA. A - AZD6094 600 mg (3X 200 mg tablet) B - Placebo C - Moxifloxacin 400 mg |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- Male only
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (7 listed)
- Provision of signed and dated, written informed consent prior to any study specific procedure.
- Healthy vasectomized male participants with suitable veins for cannulation or repeated venipuncture, non-Japanese vasectomized male participants aged 18 to 55 years (inclusive) or male participants over 40 (and up to 55) years old not intending to father children.
- Body mass index (BMI) between 18 and 30 kg/m2 inclusive and weigh greater than 50 kg and no more than 100 kg.
- Alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin (TBL) less than or equal to the upper limit of normal for the institution.
- Have a calculated creatinine clearance (CrCL) greater than 80 mL/min using the Cockcroft-Gault formula at Screening.
Key exclusion criteria (37 listed)
- Participants must not be randomized if any of the following exclusion criteria are fulfilled:
- Healthy participants of Japanese ethnicity and any healthy subject that has 1 parent or grandparent (maternal or paternal) that is Japanese.
- History of any clinically important disease or disorder which, in the opinion of the Investigator, may either put the subject at risk because of participation in the study, or influence the results or the subject's ability to participate in the study.
- History or presence of gastrointestinal (GI), hepatic or renal disease or any other condition known to interfere with absorption, distribution, metabolism or excretion of drugs.
- Any clinically important illness, medical/surgical procedure or trauma within 4 weeks of the first administration of IMP.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| AZD6094 200 mgA potent and selective small molecule mesenchymal epithelial transition (MET) kinase inhibitor with significant antitumor activity. | Drug | Cohort 1, Cohort 2, Cohort 3, Cohort 4, Cohort 5, Cohort 6 |
| PlaceboAZD6094 matching placebo without any pharmacological activity. | Other | Cohort 1, Cohort 2, Cohort 3, Cohort 4, Cohort 5, Cohort 6 |
| MoxifloxacinAlso: AveloxA fluoroquinolone broad-spectrum antibiotic, produces a mild, but reproducible increase in QT interval corrected (QTc) in healthy normal participants at time to reach maximum concentration (tmax - approximately 2 hours (0.5 to 4 hours)). This effect is close to the ECG interval measured from the onset of the QRS complex (onset of the QRS complex to the J point) to the offset of the T wave (QT)/QTc effect that represents the threshold of regulatory concern, around 5 ms mean QTc interval prolongation. | Drug | Cohort 1, Cohort 2, Cohort 3, Cohort 4, Cohort 5, Cohort 6 |
Primary outcome
Effect of AZD6094 at single therapeutic dose (600 mg) on ventricular repolarization by analysis of change from baseline-corrected QT
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
To assess the effect of AZD6094 at single therapeutic dose (600mg) on ventricular repolarization by assessing the time matched baseline-adjusted, placebo subtracted QTc interval corrected for RR (R waves on electrocardiogram [ECG]) by the Fridericia formula (QTcF). The ECGs -digital (dECG) and page (pECG) would be recorded during the study for the assessment of safety. Paper ECG for safety review will be performed following the dECG recordings and at additional intervals if required.
22 secondary outcomes
Effect of AZD6094 at therapeutic dose (600 mg) on additional time-matched ECG variables
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Effect of moxifloxacin 400 mg on Fridericia-corrected QT interval (QTcF) compared to placebo.
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Area under the plasma concentration-curve from time zero to the time of last quantifiable analyte concentration (AUC(0-∞)) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Area under the plasma concentration-time curve from time zero to t hours after dosing (AUC(0-t)) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Observed maximum concentration (Cmax) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Time to reach maximum concentration (tmax) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Lag-time (tlag - from the individual concentration-time curve) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Terminal rate constant (λz) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Terminal half-life (t½) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Apparent clearance for parent drug estimated as dose divided by AUC (CL/F) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Apparent volume of distribution for parent drug at terminal phase (Vz/F, extravascular administration) assessment for AZD6094, its metabolites (M2 and M3) and moxifloxacin
Time frame: Treatment periods (At pre-dose (Day -1) and post-dose (30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours, 24 hours, 36 hours and 48 hours)
Assessment of relationship between the plasma concentration of AZD6094 and moxifloxacin and ECG variables, including baseline-adjusted and placebo-subtracted QTc interval.
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Number of participants with adverse events (AEs) of AZD6094
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose (Day -1) and post-dose (24 hours and 48 hours) and follow-up (14 days after discharge from the treatment period 3)
Systolic blood pressure [SBP]
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Diastolic blood pressure [DBP]
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Pulse rate
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Twelve-lead (12-Lead) electrocardiograms (ECGs)
Time frame: At screening, treatment periods (pre-dose and post-dose - 30 min, 60 min, 90 min, 2 hours to 6 hours, 8 hours, 12 hours and 24 hours) and follow-up visits
Physical examination
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Laboratory assessments of Hematology
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Laboratory assessments of Clinical chemistry
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Laboratory assessments of urinalysis
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment periods (At pre-dose on Day -1 to Day 3 (48 hours post-dose) and follow-up (14 days after discharge from the treatment Period 3)
Effect of AZD6094 at therapeutic dose (600 mg) on time-matched ECG variable - heart rate (HR)
Time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 20 Feb 2020.
- Derived from this study: PubMed 33733338Schalkwijk S, Sahota T, Verheijen RB, Harmer AR, Ahmed GF. Parent and Metabolite Concentration-QT Modeling to Evaluate QT-Interval Prolongation at Savolitinib Therapeutic Doses. AAPS J. 2021 Mar 17;23(3):46. doi: 10.1208/s12248-021-00573-1.
- Derived from this study: PubMed 33400845Sahota T, Dota CD, Vik T, Yan W, Verheijen RB, Walker S, Li Y, Goldwater R, Ghiorghiu D, Mellemgaard A, Ahmed GF. A Randomized, Double-Blind, Placebo- and Positive-Controlled, Three-Way Crossover Study in Healthy Participants to Investigate the Effect of Savolitinib on the QTc Interval. Clin Pharmacol Drug Dev. 2021 May;10(5):521-534. doi: 10.1002/cpdd.896. Epub 2021 Jan 5.
- Results of this clinical trial are available on www.astrazenecaclinicaltrials.comLink provided by the sponsor.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Ronald Goldwater, MD principal investigator
PAREXEL Early Phase Clinical Unit Baltimore
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing AZD6094 200 mg and Moxifloxacin in people with Solid Tumors, run by AstraZeneca at 1 site in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 7 inclusion and 37 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 20 Feb 2020. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Effect of AZD6094 at single therapeutic dose (600 mg) on ventricular repolarization by analysis of change from baseline-corrected QT (time frame: At screening (28 days prior to Day 1 of treatment period 1), treatment period (At pre-dose on Day -1 to Day 3, 48 hours post-dose) and follow-up (14 days after discharge from the treatment period 3)). It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT03258515, which also lists 2 linked publications.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 20 Feb 2020.