The purpose of this open-label, first-in-human (FIH) trial is to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of DZR123 (Tulmimetostat, CPI-0209), both as monotherapy and in combination with enzalutamide, in patients with advanced solid tumors and lymphomas.
Adults aged ≥18 years with life expectancy ≥12 weeks
ECOG performance status 0-1
Adequate recovery from prior therapy-related toxicities (Grade ≤1, with exceptions)
Adequate bone marrow, renal, and hepatic function per protocol-defined thresholds
Prior solid organ or allogeneic hematopoietic cell transplant
Active or untreated symptomatic CNS metastases (with limited exceptions)
Clinically significant cardiovascular disease, including uncontrolled arrhythmias or prolonged QTc
Active interstitial lung disease or pneumonitis
Parallel
Tulmimetostat
DrugTulmimetostat dosed once per day orally in 28 day cycles
Enzalutamide
DrugEnzalutamide dosed once per day orally in 28 day cycles
10
Treatment groupsSee each treatment group below.
Tulmimetostat Monotherapy Phase 1: Frequency of Dose-limiting toxicities (DLTs)
The maximum tolerated dose (MTD) and/or recommended phase 2 dose (RP2D) of Tulmimetostat as monotherapy in patients with advanced tumors.
Tulmimetostat Monotherapy Phase 2: Overall response rate (ORR)
ORR is defined as the proportion of patients with a best overall response of complete response (CR) or partial response (PR) based on RECIST 1.1 or applicable response criteria
Cohort M8 Part 1: Frequency of Dose-limiting toxicities (DLTs)
The maximum tolerated dose (MTD) and/or recommended phase 2 dose (RP2D) of Tulmimetostat in combination with enzalutamide in patients with castration-resistant prostate cancer (mCRPC) with measurable soft tissue disease.
Cohort M8 Part 2: Prostate-Specific Antigen 50 (PSA50) Response
Prostate-Specific Antigen 50 (PSA50) is defined as a ≥ 50% decrease in PSA levels from baseline at any timepoint, confirmed by a second PSA measurement ≥ 3 weeks without any PSA progression in between
Tulmimetostat Monotherapy (Phase 1 & 2) and Cohort M8 (Parts 1 & 2): Incidence Rate of Adverse Events (AEs)
Number of Participants With Adverse Events (AEs)
Tulmimetostat Monotherapy (Phase 1 & 2), Cohort M7 and Cohort M8 (Parts 1 & 2): Maximum observed plasma concentration (Cmax)
Venous whole blood samples will be collected for pharmacokinetics characterization. Cmax of Tulmimetostat will be listed and summarized using descriptive statistics.
Tulmimetostat Monotherapy (Phase 1 & 2), Cohort M7 and Cohort M8 (Parts 1 & 2): Time of maximum observed plasma concentration (Tmax)
Venous whole blood samples will be collected for pharmacokinetics characterization. Tmax of Tulmimetostat will be listed and summarized using descriptive statistics.
Tulmimetostat Monotherapy (Phase 1 & 2), Cohort M7 and Cohort M8 (Parts 1 & 2): Area under the plasma concentration-time curve from time zero to the last quantifiable time point (AUC0-last)
Venous whole blood samples will be collected for pharmacokinetics characterization. AUC0-last of Tulmimetostat will be listed and summarized using descriptive statistics.
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