Material Balance of [14C]Zorifertinib in Healthy Adult Male Participants in China

NCT07620951 | Not Yet Recruiting Phase 1

• 1 other identifier: AZD3759-CIT-101
• Study Type: interventional
• Target: 8
• Locations: 1 country
• Sites: 1

Brief Summary

This is a single-center, single-dose, open-label, Phase I study to evaluate the mass balance, biotransformation, pharmacokinetic characteristics, excretion pathways, and safety of a single oral 200 mg/5 µCi dose of \[14C\]Zorifertinib in healthy Chinese adult male participants. The study includes a screening period (Day -14 to Day -1) and a dosing and observation period (Day 1 to Day 14). Blood, urine, and feces samples will be collected to measure radioactivity, drug concentrations, and metabolites. Safety will be assessed by adverse events, vital signs, laboratory tests, 12-lead ECG, and ophthalmic examinations. The target total radioactivity recovery is ≥90% of the administered dose.

Conditions

EGFR Mutant Advanced Non-small Cell Lung Cancer; Central Nervous System (CNS) Metastases

Outcome Measures

Primary Outcomes (11)

• Total radioactive recovery and cumulative total radioactive recovery in urine and feces at each time interval

  Pre-dose up to 312 hours after dosing, or until termination criteria met

• Percentage of total radioactivity exposure (%AUC), percentage of parent drug and its metabolites (%Dose), and metabolite identification

  Percentage of total radioactivity exposure (%AUC) accounted for by parent drug and its metabolites in plasma. Percentage of administered dose (%Dose) accounted for by parent drug and its metabolites in urine and faeces. Identification of metabolites in plasma, urine, and feces

  Pre-dose up to 312 hours after dosing, or until termination criteria met

• Peak Plasma Concentration (Cmax)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Time to Peak Concentration (Tmax)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Area under the plasma concentration versus time curve (AUC)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Elimination Half-Life (t1/2)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Terminal Rate Constant (λz)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Apparent Volume of Distribution (Vz/F)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Apparent Clearance (CLz/F)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Mean Residence Time (MRT)

  Pharmacokinetic parameters of total radioactivity in plasma and whole blood (if applicable)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Whole blood / plasma total radioactivity ratio

  Pre-dose up to 120 hours after dosing,or until termination criteria met

Secondary Outcomes (9)

• Peak Plasma Concentration (Cmax)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Time to Peak Concentration (Tmax)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Area under the plasma concentration versus time curve (AUC)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Elimination Half-Life (t1/2)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

• Terminal Rate Constant (λz)

  Pre-dose up to 120 hours after dosing,or until termination criteria met

Study Arms (1)

Single Dose Zorifertinib Group

EXPERIMENTAL

Drug: [14C]Zorifertinib Oral Formulation

Interventions

[14C]Zorifertinib Oral Formulation DRUG

Single oral administration of 200 mg/5 µCi \[¹⁴C\]Zorifertinib in healthy male subjects under fasting condition

Single Dose Zorifertinib Group

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy Chinese males;
• Age at the time of signing the informed consent form: 18-45 years (inclusive);
• Body mass index (BMI) ranging from 19-26 kg/m2 (inclusive), with a body weight of no less than 50 kg;
• Fully understand the purpose and requirements of this study and voluntarily sign the informed consent form;
• Be able to communicate well with the investigators and complete the trial according to the protocol.
• The 14C content in plasma and urine samples obtained during screening are within general environmental 14C background levels. Directly analyzed plasma samples must have values ≤150 pMC, and urine samples containing petroleum-based carbon carriers must have values ≤50 pMC.

You may not qualify if:

• Ancillary Examinations:
• Abnormal findings from comprehensive physical examination, vital signs, laboratory tests (hematology, blood biochemistry, coagulation function, urinalysis, routine stool + occult blood, thyroid function), 12-lead ECG, chest X-ray (posteroanterior view), abdominal ultrasound, digital rectal examination, etc., that are judged by the investigator as clinically significant.
• Resting corrected QT interval (Fridericia correction, QTcF = QT/RR1/3) obtained from 12-lead ECG \>450 ms in males, or other abnormalities judged by the investigator as clinically significant.
• Positive result for any of the following: hepatitis B surface antigen or hepatitis B e antigen, hepatitis C virus antibody, Treponema pallidum antibody, or human immunodeficiency virus antigen/antibody combination test (HIV-Ag/Ab).
• Abnormal findings from ophthalmic examination (slit lamp, intraocular pressure, fundus photography) that are clinically significant.
• Medication History:
• Use of any drugs that inhibit or induce the drug-metabolizing enzyme CYP3A4 within 30 days prior to the screening period.
• Use of any prescription drugs, over-the-counter drugs, herbal medicines, or food supplements (e.g., vitamins, calcium supplements) within 14 days prior to the screening period.
• Medical and Surgical History:
• History of any clinically serious disease or condition that the investigator believes may affect the trial results, including but not limited to circulatory, respiratory, endocrine, nervous, digestive, urinary, hematologic, immune, psychiatric, or metabolic diseases;
• History of dysphagia or any condition that may affect drug absorption, e.g., gastrectomy, cholecystectomy, gastric bypass, duodenotomy, colectomy, inflammatory bowel disease;
• History of organic heart disease, heart failure, myocardial infarction, angina pectoris, arrhythmia, ventricular tachycardia, clinically symptomatic AV block, long QT syndrome, or family history of long QT syndrome (evidenced by genetic proof or sudden cardiac death of a close relative at a young age);
• Major surgery within 6 months prior to the screening period, or surgical incision not fully healed; Major surgery includes, but is not limited to, any procedure with significant bleeding risk, prolonged general anesthesia, incisional biopsy, or significant traumatic injury;
• Allergic constitution, e.g., known history of allergy to two or more substances; Or judged by the investigator as potentially allergic to the investigational drug;
• Hemorrhoids or perianal diseases with regular/ongoing hematochezia, irritable bowel syndrome, inflammatory bowel disease.

Sponsors & Collaborators

• Alpha Biopharma (Jiangsu) Co., Ltd.: lead

Study Sites (1)

The First Affiliated Hospital of Soochow University

Suzhou, Jiangsu, 215000, China

Location

MeSH Terms

Conditions

Neoplasm Metastasis

Condition Hierarchy (Ancestors)

Neoplastic Processes; Neoplasms; Pathologic Processes; Pathological Conditions, Signs and Symptoms

Study Officials

• Liyan Miao, Ph.D.

  The First Affiliated Hospital of Soochow University

  PRINCIPAL INVESTIGATOR

Central Study Contacts

John Ge, M.D.

CONTACT

+86 (0)21-63862197; john.ge@alphabiopharma.com.cn

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 20, 2026
• First Posted: June 2, 2026
• Study Start: June 1, 2026
• Primary Completion (Estimated): August 1, 2026
• Study Completion (Estimated): August 1, 2026
• Last Updated: June 3, 2026

Record last verified: 2026-05

Locations

CN (1)