APG-1252 is a highly potent Bcl-2 family protein inhibitor, a promising drug candidate which shown high binding affinities to Bcl-2, Bcl-xL and Bcl-w. The preclinical studies have shown that APG-1252 alone achieves complete and persistent tumor regression in multiple tumor xenograft models with a twice weekly or weekly dose-schedule, including SCLC, colon, breast and ALL cancer xenografts; achieves strong synergy with the chemotherapeutic agents, indicating that APG-1252 may have a broad therapeutic potential for the treatment of human cancer as a single agent and in combination with other classes of anticancer drugs. APG-1252 is intended for the treatment of patients with neuroendocrine tumors. The purpose of the phase 1b study to establish the maximum tolerated dose (MTD), and/or recommended phase 2 dose (RP2D). Preliminary efficacy and pharmacokinetic properties will be aslo evaluated.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
2
Multiple dose cohorts, 30 minute IV infusion, once a week, 28 days as a cycle
The First Affiliated Hospital of Sun Yat-Sen University
Guangzhou, Guangdong, China
Sun Yat-sen University Cancer Center
Guangzhou, Guangdong, China
Fudan University Shanghai Cancer Center
Shanghai, Shanghai Municipality, China
Maximum tolerated dose (MTD) determination
If ≥ 2/6 patients develop a DLT at any dose level, then the MTD will be assumed to have been exceeded. The dose level immediately below will then be expanded to 6 patients and, if no more than 1/6 patients develop DLT, then this dose will be declared the MTD.
Time frame: 28 days
Safety data
Incidence of adverse events (AEs)
Time frame: 24 months
Preliminary Efficacy
Objective response rate (ORR) assessed by RECIST 1.1
Time frame: 24 months
Preliminary Efficacy
Progress free survival (PFS) assessed by RECIST 1.1
Time frame: 24 months
Preliminary Efficacy
Disease control rate assessed (DCR) by RECIST 1.1
Time frame: 24 months
Pharmacokinetic
Peak plasma concentration (Cmax)
Time frame: 28 days
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