The primary objectives of this study are to evaluate the safety and tolerability of opevesostat in the treatment of male Chinese participants with metastatic castration-resistant prostate cancer (mCRPC) and to characterize the pharmacokinetic profile of opevesostat. There are no formal hypotheses to be tested in this study.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
14
Tablets to be taken orally.
Tablets to be taken orally
Tablets to be taken orally.
Peking University First Hospital-Urology ( Site 0001)
Beijing, Beijing Municipality, China
Sun Yat-sen University Cancer Center-Neurosurgery department ( Site 0003)
Guangzhou, Guangdong, China
Tongji Hospital Tongji Medical,Science & Technology ( Site 0002)
Wuhan, Hubei, China
Number of Participants Who Experience an Adverse Event (AE)
An AE is defined as any untoward medical occurrence associated with the use of a drug in a participant, whether or not considered drug related. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product and does not imply any judgment about causality.
Time frame: Up to approximately 20 months
Number of Participants Who Discontinue Study Intervention Due to an AE
An AE is defined as any untoward medical occurrence associated with the use of a drug in a participant, whether or not considered drug related. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product and does not imply any judgment about causality.
Time frame: Up to approximately 20 months
Maximum Plasma Concentration (Cmax) of opevesostat
Blood samples will be collected at pre-specified timepoints to determine the Cmax of opevesostat.
Time frame: Day 1 and Day 8: predose and 0.5, 1, 2, 3, 4, 6, 9, and 12 hours postdose, Day 29, Day 57, and Day 89: pre-dose
Time to Maximum Plasma Concentration (Tmax) of opevesostat
Blood samples will be collected at pre-specified timepoints to determine the Tmax of opevesostat.
Time frame: Day 1 and Day 8: predose and 0.5, 1, 2, 3, 4, 6, 9, and 12 hours postdose, Day 29, Day 57, and Day 89: pre-dose
Area Under the Curve from Time 0 to 12 hours postdose (AUC0-12) of opevesostat
Blood samples will be collected at pre-specified timepoints to determine the AUC0-12 of opevesostat.
Time frame: Day 1 and Day 8: predose and 0.5, 1, 2, 3, 4, 6, 9, and 12 hours postdose, Day 29, Day 57, and Day 89: pre-dose
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Tablet to be taken orally as a rescue medication.
Apparent Volume of Distribution (Vz/F) of opevesostat
Blood samples will be collected at pre-specified timepoints to determine the Vz/F of opevesostat.
Time frame: Day 1 and Day 8: predose and 0.5, 1, 2, 3, 4, 6, 9, and 12 hours postdose, Day 29, Day 57, and Day 89: pre-dose
Oral Clearance (CL/F) of opevesostat
Blood samples will be collected at pre-specified timepoints to determine the CL/F of opevesostat.
Time frame: Day 1 and Day 8: predose and 0.5, 1, 2, 3, 4, 6, 9, and 12 hours postdose, Day 29, Day 57, and Day 89: pre-dose
Half-Life (t1/2) of opevesostat
Blood samples will be collected at pre-specified timepoints to determine the t1/2 of opevesostat.
Time frame: Day 1 and Day 8: predose and 0.5, 1, 2, 3, 4, 6, 9, and 12 hours postdose, Day 29, Day 57, and Day 89: pre-dose
Prostate-specific Antigen (PSA) Response Rate
The PSA response rate is defined as the percentage of participants in the analysis population with a reduction in PSA level of ≥50% measured twice ≥3 weeks apart.
Time frame: Up to approximately 37 months
Radiographic Progression-free Survival (rPFS) Per Prostate Cancer Working Group (PCWG)-modified Response Evaluation Criteria in Solid Tumors Version 1.1 (RECIST 1.1)
rPFS is defined as the time from first dose of study intervention to radiographic progression per PCWG-modified RECIST 1.1 as assessed by the investigator OR death due to any cause, whichever occurs first.
Time frame: Up to approximately 37 months
Objective Response Rate (ORR) Per PCWG-modified RECIST 1.1
ORR is defined as the percentage of participants who have a best overall response of either confirmed Complete Response (CR: disappearance of all target lesions) or a confirmed Partial Response (PR: at least a 30% decrease in the sum of diameters of target lesions) per PCWG-modified RECIST 1.1 as assessed by the investigator.
Time frame: Up to approximately 37 months
Duration of Response (DOR) Per PCWG-modified RECIST 1.1
For participants who demonstrate a confirmed Complete Response (CR: disappearance of all target lesions) or Partial Response (PR: at least a 30% decrease in the sum of diameters of target lesions) per PCWG-modified RECIST 1.1, DOR is defined as the time from first documented evidence of confirmed CR or PR until disease progression or death from any cause, whichever occurs first.
Time frame: Up to approximately 37 months
Overall Survival (OS)
OS is defined as time from first dose of study intervention to death due to any cause.
Time frame: Up to approximately 37 months
Blood Concentrations of Steroids
Blood samples collected at multiple timepoints after the administration of opevesostat will be used to determine the blood concentrations of steroids.
Time frame: At designated timepoints (up to approximately 37 months)