A Study to Assess the Effects of Itraconazole, Rifampicin, and Omeprazole on Pharmacokinetics of Adavosertib
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ClinicalTrials.gov Identifier: NCT04959266 |
Recruitment Status :
Recruiting
First Posted : July 13, 2021
Last Update Posted : June 30, 2022
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Condition or disease | Intervention/treatment | Phase |
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Advanced Solid Tumours | Drug: Adavosertib Drug: Itraconazole Drug: Rifampicin Drug: Omeprazole | Phase 1 |
The study will include 3 arms consisting of a screening period of up to 28 days (Day -28 to Day -1), an intervention period (12 days for arm A, 17 days for arm B, and 12 days for arm C), and a follow-up end of treatment [EOT] visit (within 3 days after a 4-day washout period relative to the last dose of adavosertib).
Arm A of this study follows a non-randomised, open-label, 2-intervention design. Patients will receive the following 2 study interventions: a single oral dose of adavosertib alone, and a single oral dose of adavosertib administered concomitantly with itraconazole.
Arm B of this study follows a non-randomised, open-label, 2-intervention design. Patients will receive the following 2 study interventions: a single oral dose of adavosertib alone, and a single oral dose of adavosertib administered concomitantly with rifampicin.
Arm C of this study follows a non-randomised, open-label, 2-intervention design. Patients will receive the following 2 study interventions: a single oral dose of adavosertib alone, and a single oral dose of adavosertib administered concomitantly with omeprazole.
Study Type : | Interventional (Clinical Trial) |
Estimated Enrollment : | 70 participants |
Allocation: | Non-Randomized |
Intervention Model: | Crossover Assignment |
Masking: | None (Open Label) |
Primary Purpose: | Other |
Official Title: | A Phase I, Open-label, Non-randomised Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor), Rifampicin (a CYP3A4 Inducer), and Omeprazole (a Proton Pump Inhibitor) on the Pharmacokinetics of a Single Oral Dose of Adavosertib in Patients With Advanced Solid Tumours |
Actual Study Start Date : | June 28, 2021 |
Estimated Primary Completion Date : | November 9, 2022 |
Estimated Study Completion Date : | November 9, 2022 |

Arm | Intervention/treatment |
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Experimental: Arm A
Patients will receive a single oral dose of adavosertib alone, and a single oral dose of adavosertib concomitantly with itraconazole.
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Drug: Adavosertib
Patients will receive a single dose of Adavosertib orally in arm A, B, and C. Drug: Itraconazole Patients will receive Itraconazole orally once daily for 7 days in arm A. |
Experimental: Arm B
Patients will receive a single oral dose of adavosertib alone, and a single oral dose of adavosertib concomitantly with rifampicin.
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Drug: Adavosertib
Patients will receive a single dose of Adavosertib orally in arm A, B, and C. Drug: Rifampicin Patients will receive Rifampicin orally once daily for 13 days in arm B. |
Experimental: Arm C
Patients will receive a single oral dose of adavosertib alone, and a single oral dose of adavosertib concomitantly with omeprazole.
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Drug: Adavosertib
Patients will receive a single dose of Adavosertib orally in arm A, B, and C. Drug: Omeprazole Patients will receive Omeprazole orally once daily for 5 days in arm C. |
- Ratios of geometric means of Cmax (maximum observed plasma concentration) when administered in combination with itraconazole/rifampicin/omeprazole relative to adavosertib alone [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of the effect of itraconazole (arm A)/rifampicin (arm B)/omeprazole (arm C) on the Cmax of adavosertib following oral dosing in patients with advanced solid tumours.
- Ratios of geometric means of AUCinf (Area under plasma concentration-time curve from time zero to infinity) when administered in combination with itraconazole/rifampicin/omeprazole relative to adavosertib alone [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of the effect of itraconazole (arm A)/rifampicin (arm B)/omeprazole (arm C) on the AUCinf of adavosertib following oral dosing in patients with advanced solid tumours.
- Ratios of geometric means of AUClast (Area under the plasma concentration-time curve from zero to time of last quantifiable concentration) when administered in combination with itraconazole/rifampicin/omeprazole relative to adavosertib alone [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of the effect of itraconazole (arm A)/rifampicin (arm B)/omeprazole (arm C) on the AUClast of adavosertib following oral dosing in patients with advanced solid tumours.
- Summary of Adavosertib plasma concentrations with time [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of pharmacokinetics (PK) for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of Cmax [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of Cmax for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of AUCinf [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of AUCinf for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of AUClast [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of AUClast for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of tmax (Time to reach maximum observed concentration following drug administration) [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of tmax for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of λz (Terminal elimination rate constant) [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of λz for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of t½λz (Half-life associated with terminal slope (λz) of a semi-logarithmic concentration-time curve) [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of t½λz for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of CL/F (Apparent total body clearance of drug from plasma after extravascular administration) [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of CL/F for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of Vss/F (Volume of distribution (apparent) at steady state following extravascular administration) [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of Vss/F for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of Vz/F (Apparent volume of distribution during the terminal phase after extravascular administration) [ Time Frame: Arm A: Days 1-4 and 9-12; Arm B: Days 1-4 and 14-17; Arm C: Days 1-4 and 9-12 ]Assessment of Vz/F for adavosertib when administered alone and in combination with itraconazole (arm A) /rifampicin (arm B) /omeprazole (arm C).
- Descriptive statistics of Ctrough (Observed lowest drug concentration reached before the next dose is administered) [ Time Frame: Arm A: Days 9-11; Arm B: Days 14-17; Arm C: Day 9 ]Assessment of Ctrough for itraconazole, rifampicin and omeprazole when administered in combination with adavosertib.
- Number of patients with serious and non-serious adverse events [ Time Frame: From screening to end of study [within 30 (±7) days of last adavosertib dose] ]Assessment of the safety and tolerability of adavosertib when dosed with itraconazole (arm A), rifampicin (arm B), and omeprazole (arm C).

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Ages Eligible for Study: | 18 Years to 130 Years (Adult, Older Adult) |
Sexes Eligible for Study: | All |
Accepts Healthy Volunteers: | No |
Inclusion Criteria:
- Histologically or cytologically documented, locally advanced or metastatic solid tumour, excluding lymphoma, for which standard therapy does not exist or has proven ineffective or intolerable.
- Eastern Cooperative Oncology Group performance status score of 0 or 1.
- Predicted life expectancy ≥ 12 weeks.
- Patients must have normal organ and marrow function at baseline, within 7 days prior to study drug administration.
- Males and females of childbearing potential who agree to use contraceptive measures must be consistent with clinical study protocol.
Exclusion Criteria:
- Persistent toxicities (Common Terminology Criteria for Adverse Events [CTCAE] Grade > 2) caused by previous anticancer therapy, excluding alopecia and CTCAE Grade 2 peripheral neuropathy.
- Refractory nausea and vomiting, chronic gastrointestinal disease, inability to swallow the formulated product, or previous significant bowel resection that would preclude adequate absorption, distribution, metabolism, or excretion of adavosertib, itraconazole, rifampicin, and omeprazole.
- Any significant cardiac diseases currently or within the last 6 months such as: (a) unstable angina pectoris (b) acute myocardial infarction, congestive heart failure (c) conduction abnormality not controlled with pacemaker or medication (d) significant ventricular or supraventricular arrhythmias.
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Any of the following:
- History or current evidence of congenital long QT syndrome;
- concomitant medications known to prolong QT interval or history of medicationrelated QT prolongation.
- Known to have tested positive for human immunodeficiency virus or active tuberculosis infection.
- Known active hepatitis infection, positive hepatitis C antibody, hepatitis B virus surface antigen or hepatitis B virus core antibody, at screening.
- Any evidence of diseases (such as severe or uncontrolled systemic diseases, including uncontrolled hypertension, renal transplant, active infections, and active bleeding diseases) which prohibit participating in the study.
- Spinal cord compression or brain metastases unless asymptomatic, stable, and not requiring steroids for at least 4 weeks prior to start of study intervention.
- Receipt of live virus and live bacterial vaccines whilst the patient is receiving the study intervention and during the 30-day follow-up period. Inactivated flu vaccines are permitted.
- Use of an anti-cancer treatment drug ≤ 21 days (≤ 6 weeks for nitroureas or mitomycin C) or use of an investigational product within 5 half-lives prior to the first dose of adavosertib.
- Patient uses drugs that are sensitive to CYP3A4 substrates or CYP3A4 substrates with a narrow therapeutic index, or are moderate to strong inhibitors/inducers of CYP3A4 which cannot be discontinued 2 weeks or 5 halflives (whichever is longer) prior to Day 1 of dosing.
- Patients with a known hypersensitivity to adavosertib, itraconazole, rifampicin, and omeprazole or any of the excipients of the product.
- Currently pregnant (confirmed with positive pregnancy test) or breast-feeding.

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT04959266
Contact: AstraZeneca Clinical Study Information Center | 1-877-240-9479 | information.center@astrazeneca.com |
United States, Connecticut | |
Research Site | Withdrawn |
New Haven, Connecticut, United States, 06510 | |
United States, Georgia | |
Research Site | Not yet recruiting |
Newnan, Georgia, United States, 30265 | |
United States, New Hampshire | |
Research Site | Not yet recruiting |
Lebanon, New Hampshire, United States, 03756 | |
United States, Oregon | |
Research Site | Recruiting |
Portland, Oregon, United States, 97213 | |
United States, Texas | |
Research Site | Recruiting |
Austin, Texas, United States, 78758 | |
Research Site | Recruiting |
Dallas, Texas, United States, 75230 | |
Spain | |
Research Site | Not yet recruiting |
Madrid, Spain, 28029 | |
Research Site | Not yet recruiting |
Madrid, Spain, 28031 | |
Research Site | Recruiting |
Madrid, Spain, 28034 | |
Research Site | Not yet recruiting |
Madrid, Spain, 28040 | |
Research Site | Recruiting |
Madrid, Spain, 28041 | |
Research Site | Not yet recruiting |
Malaga, Spain, 29010 | |
Research Site | Not yet recruiting |
Pozuelo de Alarcon, Spain, 28223 |
Responsible Party: | AstraZeneca |
ClinicalTrials.gov Identifier: | NCT04959266 |
Other Study ID Numbers: |
D601HC00006 |
First Posted: | July 13, 2021 Key Record Dates |
Last Update Posted: | June 30, 2022 |
Last Verified: | June 2022 |
Individual Participant Data (IPD) Sharing Statement: | |
Plan to Share IPD: | Yes |
Plan Description: | Qualified researchers can request access to anonymized individual patient-level data from AstraZeneca group of companies sponsored clinical trials via the request portal. All requests will be evaluated as per the AZ disclosure commitment: https://astrazenecagrouptrials.pharmacm.com/ST/Submission/Disclosure. Yes, indicates that AZ are accepting requests for IPD, but this does not mean all requests will be shared. |
Time Frame: | AstraZeneca will meet or exceed data availability as per the commitments made to the EFPIA Pharma Data Sharing Principles. For details of our timelines, please refer to our disclosure commitment at: https://astrazenecagrouptrials.pharmacm.com/ST/Submission/Disclosure |
Access Criteria: | When a request has been approved AstraZeneca will provide access to the de-identified individual patient-level data in an approved sponsored tool. Signed Data Sharing Agreement (non-negotiable contract for data accessors) must be in place before accessing requested information. Additionally, all users will need to accept the terms and conditions of the SAS MSE to gain access. For additional details, please review the Disclosure Statements at: https://astrazenecagrouptrials.pharmacm.com/ST/Submission/Disclosure |
URL: | https://astrazenecagroup-dt.pharmacm.com/DT/Home |
Studies a U.S. FDA-regulated Drug Product: | Yes |
Studies a U.S. FDA-regulated Device Product: | No |
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