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A Dose Escalation Study to Assess the Safety and Tolerability of HMPL-453 in Patients With Advanced Solid Malignancies

Phase 1
Terminated
Conditions
Solid Tumor
Interventions
Registration Number
NCT02966171
Lead Sponsor
Hutchison Medipharma Limited
Brief Summary

This is a first-time-in-human, phase I, open-label, dose-escalation study of HMPL-453 in patients with advanced or metastatic solid malignancies who have failed or are intolerable to standard therapies or for whom no standard therapies exist. There are preliminary two stages in this study: a dose-escalation stage (stage 1) and a dose-expansion stage (stage 2). We will decide whether to conduct stage 2 or not one month after the last patient included in stage 1.

Detailed Description

Dose-escalation stage (stage 1): Patients participating in the dose-escalation stage will take a single dose of HMPL-453 on Day 1 and will be followed for one week for safety observations. After one week of observation, if no safety issues occur, patients can continue multiple dosing of HMPL-453 QD and start on the DLT assessment cycles. Each cycle consists of 28-days. Patients are required to draw blood samples for PK and safety analysis at specific time points during the treatment.

The 3+3 design will be employed for the dose escalation and MTD determination. To limit the number of patients being exposed to potentially ineffective doses, one patient will be enrolled and dosed in the initial dose cohort. If there are no DLT or \< 2 CTCAE grade 2 toxicities occur in the first treatment cycle, then the study will be escalated to the next dose cohort. Otherwise, the trial will revert to a standard 3+3 design.

Dose-Expansion Stage (Stage 2): This stage is to further evaluate the safety, tolerability, PD profile, and preliminary anti-tumor activity of HMPL-453 at the RP2D in approximately 10 patients with advanced solid tumor. Patients with FGFR dysregulated advanced solid tumors, including but not limited to, advanced gastric cancer, advanced urothelial bladder cancer, or advanced cholangiocarcinoma (patients with cancers of the gallbladder or ampulla of Vater are not eligible) are preferred to be enrolled.

Expansion stage will begin after dose-escalation stage is completed and the MTD/RP2D has been determined. Patients will receive HMPL-453 with 28-day treatment cycles until disease progression, death, intolerable toxicity, no longer benefiting from the study treatment per investigator's discretion, or withdrawal of consent, whichever comes first.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
14
Inclusion Criteria
  • In the dose escalation stage, patients with locally advanced, or metastatic solid tumor who have failed, or intolerable to, standard therapies or for whom no standard therapies exist will be enrolled.
  • In the dose expansion stage, patients with locally advanced, or metastatic solid tumor and FGFR dysregulation who have failed or intolerable to standard therapies or no standard therapies exist are to be enrolled.
  • In the dose escalation stage: evaluable or measurable disease according to RECIST Version 1.1. In the dose expansion stage: measurable disease according to RECIST Version 1.1.
  • Life expectancy of at least 12 weeks.
  • ECOG performance status of 0 or 1
Exclusion Criteria
  • Prior or current treatment with any selective FGFR inhibitor.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
HMPL-453HMPL-453Two strengths of HMPL-453 tablets (25 mg and 100 mg based on the free base) will be used for clinical studies. The drug products are coated tablets, which are packaged in white induction sealed HDPE bottles. HMPL-453 will be administered to patients as oral tablet(s) on a daily basis, untill disease progression, intolerable toxicity, or death. Dose levels are to be potentially tested in this study include 25, 50, 100, 200, 300, 400, and 500 mg/day.
Primary Outcome Measures
NameTimeMethod
Incidence of DLTs by the NCI CTCAE v4.03Cycle 1 (DLT assessment window, 28 days) of multiple dosing peroid
Secondary Outcome Measures
NameTimeMethod
Incidence of AEs, clinically significant laboratory abnormalities, and electrocardiographic (ECG) changes and vital signsfrom first dose to 30 days after last dose of study treatment
maximum plasma concentration (Cmax)from first dose to day 56 of multiple dosing peroid
Objective response rate (ORR)Every 8 weeks while being treated with HMPL-453 (expected average of 16 weeks)
terminal half-life (t1/2)from first dose to day 56 of multiple dosing peroid
Duration of response (DoR)Every 8 weeks while being treated with HMPL-453 (expected average of 16 weeks)
Disease Control Rate (DCR)Every 8 weeks while being treated with HMPL-453 (expected average of 16 weeks)
Change in tumor sizeEvery 8 weeks while being treated with HMPL-453 (expected average of 16 weeks)

Tumor size is defined as the sum of the lengths of the longest diameters of the RECIST 1.1 target lesions (TLs). Percentage change in tumor size will be determined for patients with measurable disease at baseline and is derived at each visit by the percentage change in the sum of the diameters of TLs compared to baseline.

area under the concentration-time curve (AUC0-t)from first dose to day 56 of multiple dosing peroid
Progression free survival (PFS)Every 8 weeks while being treated with HMPL-453 (expected average of 16 weeks)
time to reach maximum concentration (Tmax)from first dose to day 56 of multiple dosing peroid
apparent clearance (CL/F)from first dose to day 56 of multiple dosing peroid
Serum phosphate level increasesfrom first dose to Day 21 of the last treatment cycle

Trial Locations

Locations (4)

Peninsula and Southeast Oncology

🇦🇺

Frankston, Victoria, Australia

Monash Medical Centre

🇦🇺

Melbourne, Victoria, Australia

St Vincent's Cancer Services

🇦🇺

Sydney, New South Wales, Australia

Chris O'Brien Lifehouse

🇦🇺

Sydney, New South Wales, Australia

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