A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of BPI-21668

Study Overview
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Brief Summary
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This study is an open-label, single arm, dose escalation and dose expansion phase 1 study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of BPI-21668 in solid tumor patients. In dose escalation phase, biomarker status is not required, but in dose expansion phase patients are required to harbor PIK3CA mutation.

Official Title
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A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of BPI-21668 in Advanced Solid Tumor Patients

Conditions
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Advanced Solid Tumor

Intervention / Treatment
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* Drug: BPI-21668


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Age ≥18 and ≤70 years, male and female patients; Life expectancy ≥ 12 weeks; ECOG performance score 0-1; Locally advanced or relapsed/metastatic solid tumor patients, who had disease progression after standard therapy, intolerable to standard therapy or for whom no standard therapy exists, PIK3CA mutation status is required for dose expansion phase; Evaluable lesion required for dose escalation phase and measurable lesion as per RECIST 1.1 required for dose expansion phase; Adequate organ function; Signed informed consent. Exclusion Criteria: Prior use of PI3K、mTOR or AKT inhibitor; Prior other malignant tumor; Unstable, symptomatic primary CNS tumors/metastasis or leptomeningeal metastases ; Type I or type II diabetes; Inadequate wash-out of prior anti-cancer therapies; Cardiac disorders; Instable systemic diseases; Acute or chronic pancreatitis; Pregnancy or lactation; Other protocol specified criteria.

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 70 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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No

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Allocation: Non-Randomized
Intervention Model: Sequential Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Dose Escalation<br>Oral tablets taken in escalating levels to determine MTD/RP2D. Each treatment cycle will be 28 days in duration with BPI-21668 administered, once daily (QD). | Drug: BPI-21668<br>* Subjects will receive BPI-21668 until disease progression<br>|
| Experimental: Dose Expansion<br>Oral tablets administered at MTD/RP2D. Each treatment cycle will be 28 days in duration with BPI-21668 administered, once daily (QD). | Drug: BPI-21668<br>* Subjects will receive BPI-21668 until disease progression<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| The adverse events (AEs) | Safety and tolerability will be assessed by monitoring frequency, duration and severity of adverse events (AEs). | Through the Phase I, approximately 24 months | 
| Determine the Maximum Tolerated Dose (MTD) | The MTD will be based on DLT. | Through the Phase I, approximately 24 months | 
| Determine the recommended Phase II dose (RP2D) | The RP2D will be based on DLT. | Through the Phase I, approximately 24 months | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Evaluate the pharmacokinetics of BPI-21668 | Based on blood plasma concentration | Through the Phase I, approximately 24 months | 
| Determination of anti-tumor activity of BPI-21668 | Efficacy assessments (tumor evaluation) will be performed per RECIST1.1 | Through the Phase I, approximately 24 months |