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NCT Number: NCT06754761

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

This is an open-label, two-part study in participants with NSCLC, ovarian cancer, or endometrial cancer and will be conducted at multiple study sites.

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

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. 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 B, and following the Follow-up Visit, participants may be allowed further access to Ceralasertib if in the opinion of the investigator and medical monitor they may derive clinical benefit.

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Key information

Conditions

Neoplasm Adnexal Diseases Bronchial Neoplasms Carcinoma, Bronchogenic Carcinoma, Non-Small-Cell Lung Endocrine Gland Neoplasms Endocrine System Diseases Endometrial Neoplasms Female Urogenital Diseases Female Urogenital Diseases and Pregnancy Complications Genital Diseases Genital Diseases, Female Genital Neoplasms, Female Gonadal Disorders Lung Diseases Lung Neoplasms Neoplasms Neoplasms by Site Ovarian Diseases Ovarian Neoplasms Respiratory Tract Diseases Respiratory Tract Neoplasms Thoracic Neoplasms Urogenital Diseases Urogenital Neoplasms Uterine Diseases Uterine Neoplasms

Age range

18 year and older

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Research Site, Liverpool, United Kingdom

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Who can participate

Healthy volunteers accepted: No

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

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

Age

  • 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

  • Sufficient ECOG performance status, life expectancy, and ability to swallow and retain oral medication
  • Adequate organ and marrow function
  • Willingness and ability to comply with study and follow-up procedures.
  • Able and willing to stay in hospital for specified residential periods following administration of Ceralasertib/[14C]-Ceralasertib
  • Regular bowel movements
  • Participants with NSCLC must have appropriately documented NSCLC diagnosis, mutation status, treatment history, and disease status according to protocol-specified eligibility criteria
  • Participants with Ovarian cancer must have appropriately documented ovarian cancer diagnosis, mutation status, treatment history, and disease status according to protocol-specified eligibility criteria 9. Participants with Endometrial cancer must have appropriately documented endometrial cancer diagnosis, treatment history, and disease status according to protocol-specified eligibility criteria 10. 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 11. 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:
  • History of Diagnosis of protocol-specified medical conditions
  • Spinal cord compression or brain metastasis prior to start of study intervention unless asymptomatic and stable
  • Persistent toxicities (CTCAE Grade ≥ 2), with the exception of alopecia and vitiligo, caused by previous anticancer therapy.
  • History of allogenic organ transplant or autoimmune or inflammatory disorders requiring use of immunosuppressive medications with some protocol specified conditions/exceptions
  • Any medical or surgical condition that would preclude adequate absorption of Ceralasertib
  • Inadequate cardiac function / status or other cardiovascular diseases
  • Participants with active infection requiring systemic antibiotics, antifungal or antiviral drugs
  • 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
  • Protocol-specified prior/concomitant therapy exclusions
  • Protocol-specified prior/concurrent clinical study experience
  • Other Exclusions including but not limited to tobacco/nicotine and/or alcohol use, or drug/alcohol abuse history
  • Not currently pregnant, breast-feeding, or planning to become pregnant

Treatment and study plan

[14C] AZD6738

Drug

radiolabeled AZD6738 / ceralasertib

AZD6738 / ceralasertib

Drug

Ceralasertib (AZD6738) is a potent, selective inhibitor of the serine/threonine-specific protein kinase ATR

Primary outcomes

  1. 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

  2. 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

  3. 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

  4. 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

  5. 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

  6. 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

  7. 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

  8. 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

  9. 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

  10. 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)

    Pharmacokinetic activity of ceralasertib present in urine

Secondary outcomes

  1. 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)

  2. To assess the safety of Ceralasertib in participants with NSCLC, ovarian cancer, or endometrial cancer (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

Study contacts

Contact information is provided by the study sponsor or research team.

AstraZeneca Clinical Study Information Center

CONTACT

[email protected]

1-877-240-9479

Sponsors and collaborators

Lead sponsor

AstraZeneca

Industry

Registry information

Official study title

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 Non-small Cell Lung Cancer, Ovarian Cancer, or Endometrial Cancer

Important dates

Study start
2025
Primary completion
2025
Study completion
2025
First posted
Jan 1, 2025
Registry last updated
Jan 1, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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