Human ADME Study of [14C]-Ceralasertib (AZD6738) and Absolute Bioavailability of Ceralasertib

August 31, 2026 updated by: AstraZeneca

A Phase I, Open-label Study to Assess the Absolute Bioavailability of Ceralasertib (AZD6738) and Absorption, Distribution, Metabolism, and Excretion (ADME) of [14C]-Ceralasertib in Patients With Advanced Solid Tumours

This is an open-label, two-part study in participants with solid tumours and will be conducted at multiple study sites.

Participants will be assessed for study eligibility prior to admission to the study site.

Participants may be enrolled in either Part A or Part B of the study or in both.

Part A will assess the absolute bioavailability, determine the excretory routes of [14C]-Ceralasertib, and evaluate the PK parameters of a Ceralasertib oral dose and a radiolabelled IV microdose of [14C]-Ceralasertib.

Participants will be admitted to the study site pre-dose Part A and will remain at the study site for excreta (urine and faeces) collections, PK sampling and safety assessments. A washout period days will be observed between dosing in Part A and Part B if participants are taking part in both parts of the study.

Part B will assess the ADME of [14C]-Ceralasertib.

Participants will be readmitted to the study site for Part B and will remain at the study site for excreta (urine, faeces, and any vomitus) collections, PK sampling, and safety assessments.

Participants will return to the study site for a Follow-up Visit after the last dose of Ceralasertib which will include routine safety assessments.

After the completion of Parts A and/or B, and following the Follow-up Visit, participants may be allowed further access to Ceralasertib if in the opinion of the investigator they may derive clinical benefit.

Study Overview

Status

Status

Indicates the current recruitment status or the expanded access status.
Terminated

Conditions

Conditions

The disease, disorder, syndrome, illness, or injury that is being studied. On ClinicalTrials.gov, conditions may also include other health-related issues, such as lifespan, quality of life, and health risks.

Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.

Study Type

Study Type

Describes the nature of a clinical study. Study types include interventional studies (also called clinical trials), observational studies (including patient registries), and expanded access.
Interventional

Enrollment (Actual)

Enrollment

The number of participants in a clinical study. The "anticipated" enrollment is the target number of participants that the researchers need for the study.
2

Phase

Phase

The stage of a clinical trial studying a drug or biological product, based on definitions developed by the U.S. Food and Drug Administration (FDA). The phase is based on the study's objective, the number of participants, and other characteristics. There are five phases: Early Phase 1 (formerly listed as Phase 0), Phase 1, Phase 2, Phase 3, and Phase 4. Not Applicable is used to describe trials without FDA-defined phases, including trials of devices or behavioral interventions.
  • Phase 1

Contacts and Locations

This section provides the contact details for those conducting the study, and information on where this study is being conducted.

Study Contact

Study Contact

The name and contact information for the person who can answer enrollment questions for a clinical study. Each location where the study is being conducted may also have a specific contact, who may be better able to answer those questions.

Study Locations

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Eligibility Criteria

The key requirements that people who want to participate in a clinical study must meet or the characteristics they must have. Eligibility criteria consist of both inclusion criteria (which are required for a person to participate in the study) and exclusion criteria (which prevent a person from participating). Types of eligibility criteria include whether a study accepts healthy volunteers, has age or age group requirements, or is limited by sex.

Ages Eligible for Study

  • Adult
  • Older Adult

Accepts Healthy Volunteers

No

Description

Inclusion Criteria:

  • Participants are eligible to be included in the study only if all of the following criteria apply:

Age

  1. Male or female ≥ 18 years of age (or the legal age of consent in the jurisdiction in which the study is taking place), at the time of signing the ICF.

    Type of Participant and Disease Characteristics

  2. Sufficient ECOG performance status, life expectancy, and ability to swallow and retain oral medication
  3. Adequate organ and marrow function
  4. Willingness and ability to comply with study and follow-up procedures.
  5. Able and willing to stay in hospital for specified residential periods following administration of Ceralasertib/[14C]-Ceralasertib
  6. Regular bowel movements
  7. Locally advanced or metastatic solid tumour, for which standard therapy does not exist or has proven to be ineffective or intolerable.
  8. Sex and Contraceptive/Barrier Requirements: Contraceptive use by men or women should be consistent with local regulations regarding the methods of contraception for those participating in clinical studies
  9. Informed Consent: patient must be capable of giving signed informed consent as described in Appendix A which includes compliance with the requirements and restrictions listed in the ICF and in this protocol.

Exclusion Criteria:

  • Participants are excluded from the study if any of the following criteria apply:

    1. History of Diagnosis of protocol-specified medical conditions
    2. Spinal cord compression or brain metastasis prior to start of study intervention unless asymptomatic and stable
    3. Persistent toxicities (CTCAE Grade ≥ 2), with the exception of alopecia and vitiligo, caused by previous anticancer therapy.
    4. Any medical or surgical condition that would preclude adequate absorption of Ceralasertib
    5. Inadequate cardiac function / status or other cardiovascular diseases
    6. Participants with active infection requiring systemic antibiotics, antifungal or antiviral drugs
    7. Any evidence of severe or uncontrolled systemic disease, as judged by the investigator that would make it undesirable for the participant to participate in the study or would jeopardise compliance with the protocol
    8. Protocol-specified prior/concomitant therapy exclusions
    9. Protocol-specified prior/concurrent clinical study experience
    10. Other Exclusions including but not limited to tobacco/nicotine and/or alcohol use, or drug/alcohol abuse history
    11. Not currently pregnant, breast-feeding, or planning to become pregnant

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

  • Primary Purpose: Basic Science
  • Allocation: N/A
  • Interventional Model: Single Group Assignment
  • Masking: None (Open Label)

Arms and Interventions

Participant Group / Arm

Participant Group / Arm

A group or subgroup of participants in a clinical trial that receives a specific intervention/treatment, or no intervention, according to the trial's protocol.
Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.
Experimental: Primary Treatment Arm - AZD6738
Part A - oral dose of Ceralasertib and a radiolabelled IV microdose of [14C]-Ceralasertib Part B - oral dose of [14C]-Ceralasertib
Drug: [14C] AZD6738
radiolabeled AZD6738 / ceralasertib
Drug: AZD6738 / ceralasertib
Ceralasertib (AZD6738) is a potent, selective inhibitor of the serine/threonine-specific protein kinase ATR

What is the study measuring?

Primary Outcome Measures

Primary Outcome Measures

In a clinical study's protocol, the planned outcome measure that is the most important for evaluating the effect of an intervention/treatment. Most clinical studies have one primary outcome measure, but some have more than one.
Outcome Measure
Measure Description
Time Frame
To determine the rates and major excretory routes of Ceralasertib and its metabolites after IV dose of [14C]-Ceralasertib (Part A) and a oral dose of [14C]-Ceralasertib (Part B)
Time Frame: Through end of Part B, approximately 10 weeks including screening period
[14C]-Ceralasertib (Part A) or total radioactivity (Part B) recovery in urine and faeces
Through end of Part B, approximately 10 weeks including screening period
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
AUCinf
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
AUClast
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Cmax
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
tmax
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
t1/2(lambda)z
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Ratio of AUCinf of plasma Ceralasertib relative to AUCinf of plasma total radioactivity
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Ratio of AUCinf of whole blood total radioactivity relative to AUCinf of plasma total radioactivity
Through end of the part B, approximately 10 weeks (Including screening period)
To evaluate absolute bioavailability Ceralasertib and PK of Ceralasertib and [14C]-Ceralasertib after administration of oral dose of Ceralasertib and IV [14C]-Ceralasertib (Part A)
Time Frame: Through end of Part A, approximately 5 weeks including screening period
Absolute bioavailability (F) of Ceralasertib and PK parameters and recovery in urine and faeces
Through end of Part A, approximately 5 weeks including screening period
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Urine Ae
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Urine - Ae
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Urine CumAe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Urine - CumAe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Urine Fe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Urine - Fe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Urine CumFe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Urine - CumFe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Faeces Ae
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Faeces - Ae
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Faeces CumAe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Faeces - CumAe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Faeces Fe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Faeces - Fe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Faeces CumFe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Faeces - CumFe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Total (Urine+Faeces) Ae
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Total (Urine + Faeces) Ae
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Total (Urine+Faeces) CumAe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Total (Urine + Faeces) CumAe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Total (Urine+Faeces) Fe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Total (Urine + Faeces) Fe
Through end of the part B, approximately 10 weeks (Including screening period)
To characterise the PK of Ceralasertib and total radioactivity following oral dose of [14C]-Ceralasertib including the extent of distribution into blood cells (Part B) - Total (Urine+Faeces) CumFe
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Total (Urine + Faeces) CumFe
Through end of the part B, approximately 10 weeks (Including screening period)

Secondary Outcome Measures

Secondary Outcome Measures

In a clinical study's protocol, a planned outcome measure that is not as important as the primary outcome measure for evaluating the effect of an intervention but is still of interest. Most clinical studies have more than one secondary outcome measure.
Outcome Measure
Measure Description
Time Frame
To provide biologic samples for metabolic profiling and identification after oral dose of [14C]-Ceralasertib (Part B)
Time Frame: Through end of the part B, approximately 10 weeks (Including screening period)
Quantification and identification of major metabolites of Ceralasertib in plasma and excreta (will be reported separately)
Through end of the part B, approximately 10 weeks (Including screening period)
To assess the safety of Ceralasertib in participants with advanced solid tumours (Parts A and B)
Time Frame: Through study completion, approximately 9 - 11 weeks, with screening included
Incidence and severity of AEs Incidence of laboratory abnormalities, based on haematology, clinical chemistry, and urinalysis test results 12-lead ECG parameters Vital signs measurements Physical examinations
Through study completion, approximately 9 - 11 weeks, with screening included

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Sponsor

Sponsor

The organization or person who initiates the study and who has authority and control over the study.
AstraZeneca

Publications and helpful links

The person responsible for entering information about the study voluntarily provides these publications. These may be about anything related to the study.

Helpful Links

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start (Actual)

Study Start

The actual date on which the first participant was enrolled in a clinical study. The "anticipated" study start date is the date that the researchers think will be the study start date.
September 22, 2025

Primary Completion (Actual)

Primary Completion

The date on which the last participant in a clinical study was examined or received an intervention to collect final data for the primary outcome measure. Whether the clinical study ended according to the protocol or was terminated does not affect this date. For clinical studies with more than one primary outcome measure with different completion dates, this term refers to the date on which data collection is completed for all the primary outcome measures. The "anticipated" primary completion date is the date that the researchers think will be the primary completion date for the study.
October 21, 2025

Study Completion (Actual)

Study Completion

The date on which the last participant in a clinical study was examined or received an intervention/treatment to collect final data for the primary outcome measures, secondary outcome measures, and adverse events (that is, the last participant's last visit). The "anticipated" study completion date is the date that the researchers think will be the study completion date.
October 21, 2025

Study Registration Dates

First Submitted

First Submitted

The date on which the study sponsor or investigator first submitted a study record to ClinicalTrials.gov. There is typically a delay of a few days between the first submitted date and the record's availability on ClinicalTrials.gov (the first posted date).
November 4, 2024

First Submitted That Met QC Criteria

First Submitted That Met QC Criteria

The date on which the study sponsor or investigator first submits a study record that is consistent with National Library of Medicine (NLM) quality control (QC) review criteria. The sponsor or investigator may need to revise and submit a study record one or more times before NLM's QC review criteria are met. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
December 23, 2024

First Posted (Actual)

First Posted

The date on which the study record was first available on ClinicalTrials.gov after National Library of Medicine (NLM) quality control (QC) review has concluded. There is typically a delay of a few days between the date the study sponsor or investigator submitted the study record and the first posted date.
January 1, 2025

Study Record Updates

Last Update Posted (Actual)

Last Update Posted

The most recent date on which changes to a study record were made available on ClinicalTrials.gov. There may be a delay between when the changes were submitted to ClinicalTrials.gov by the study's sponsor or investigator (the last update submitted date) and the last update posted date.
September 3, 2026

Last Update Submitted That Met QC Criteria

Last Update Submitted That Met QC Criteria

The most recent date on which the study sponsor or investigator submitted changes to a study record that are consistent with National Library of Medicine (NLM) quality control (QC) review criteria. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
August 31, 2026

Last Verified

Last Verified

The most recent date on which the study sponsor or investigator confirmed the information about a clinical study on ClinicalTrials.gov as accurate and current. If a study with a recruitment status of recruiting; not yet recruiting; or active, not recruiting has not been confirmed within the past 2 years, the study's recruitment status is shown as unknown.
August 1, 2026

More Information

Terms related to this study

Keywords

Additional Relevant MeSH Terms

Other Study ID Numbers

Other Study ID Numbers

Identifiers or ID numbers other than the NCT number that are assigned to a clinical study by the study's sponsor, funders, or others. These numbers may include unique identifiers from other trial registries and National Institutes of Health grant numbers.
  • D533BC00002

Plan for Individual participant data (IPD)

Plan to Share Individual Participant Data (IPD)?

YES

IPD 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 Vivli.org. 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.

IPD Sharing Time Frame

AstraZeneca will meet or exceed data availability as per the commitments made to the EFPIA PhRMA Data Sharing Principles. For details of our timelines, please rerefer to our disclosure commitment at https://astrazenecagrouptrials.pharmacm.com/ST/Submission/Disclosure.

IPD Sharing Access Criteria

When a request has been approved AstraZeneca will provide access to the anonymized individual patient-level data via secure research environment Vivli.org.

Signed Data Usage Agreement (non-negotiable contract for data accessors) must be in place before accessing requested information.

Drug and device information, study documents

Studies a U.S. FDA-regulated drug product

No

Studies a U.S. FDA-regulated device product

No

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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