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

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

Trial statusNot yet recruiting

Trial phasePhase 1

Trial typeInterventional

Biological sexMale

Age18-45

SponsorAlpha Biopharma (Jiangsu) Co., Ltd.

About this trial

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.

Eligibility criteria

This trial accepts healthy volunteers

Qualifiers

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;

Disqualifiers

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.

Trial design

Design model

Single group

Treatments tested in this trial

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

Treatment groups

8 Participants

are divided into 1 treatment group

Group A: Single Dose Zorifertinib GroupExperimental treatment 1 intervention

Trial outcomes

Primary outcomes

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

Time frame

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

Time frame

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)

Time frame