This is a first-in-human clinical study of PEP08, a novel cancer therapy being evaluated both as monotherapy and in combination with other treatments in patients with advanced or metastatic solid tumors harboring MTAP deletion. The study will be conducted in three parts, with Part 1 currently open for enrollment. The primary objectives of the study are to: * Evaluate the safety and tolerability of PEP08, PK and PD * Determine the maximum tolerated dose (MTD) and/or recommended Phase 2 dose (RP2D) * Assess preliminary signs of anti-tumor activity of PEP08 Key study questions include: * What is the recommended dose of PEP08 for further development? * Wht is the tolerable dose of PEP08 when administered alone or in combination? * Does PEP08 show early evidence of clinical activity in patients with MTAP-deleted tumors? Participants in the study will: * Receive PEP08 alone or in combination with another anti-cancer agent, depending on the study part * Attend regular clinic visits for treatment administration, laboratory assessments, and tumor evaluations * Be enrolled in one of the following study phases over time: * \- Part 1: Monotherapy dose escalation (currently enrolling). * \- Parts 2 and 3 (monotherapy extension and combination therapy) will be activated in future protocol amendments.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
40
PEP08 is an oral, potent, MTA-cooperative PRMT5 inhibitor.
Westmead Hospital
Wentworthville, New South Wales, Australia
RECRUITINGChina Medical University Hospital
Taichung, Taiwan
RECRUITINGNational Taiwan University Hospital
Taipei, Taiwan
RECRUITINGTaipei Veterans General Hospital
Taipei, Taiwan
RECRUITINGNumber of Participants Experiencing Adverse Events (AE)
Time frame: Up to 2 years
Number of Participants Experiencing Serious Adverse Events (SAE)
Time frame: Up to 2 years
Number of Patients who Experience Dose-Limiting Toxicity
Time frame: 21 days
Area under the plasma concentration versus time curve (AUC)
Time frame: Up to 6 days
Maximum observed plasma concentration (Cmax)
Time frame: Up to 6 days
Maximum observed plasma concentration (Cmin)
Time frame: Up to 6 days
Time to achieve maximal plasma concentration (Tmax)
Time frame: Up to 6 days
Terminal elimination half-life (t1/2)
Time frame: Up to 6 days
Objective Response Rate (ORR) per RECIST v1.1
Time frame: Up to 2 years
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