About this trial
This is an open-label, multicenter Phase 1 first-in-human trial of SYH2095, a selective KAT6A/B inhibitor. The trail contains two segments: Part 1A dose escalation and Part 2A cohort expansion. Part 1A uses the BOIN dose-escalation design, enrolling patients with advanced malignant tumors with no effective standard treatment. Its primary goals are to assess safety and tolerability, define dose-limiting toxicity (DLT) and maximum tolerated dose (MTD), and establish the recommended expansion dose (RDE). Part 2A is an expansion cohort using the RDE identified in Part 1A,. All participants receive oral SYH2095 once daily in 4-week treatment cycles. Safety evaluations, tumor imaging, pharmacokinetic (PK), pharmacodynamic (PD) and biomarker analyses will be performed at scheduled time points throughout treatment.
Eligibility criteria
This trial does not accept healthy volunteersQualifiers
Fully understand this clinical trial, and voluntarily sign a written informed consent form (ICF);
Age ≥ 18 years (at the time of informed consent), male or female;
Eastern Cooperative Oncology Group Performance Status (ECOG PS) score 0-1;
Estimated life expectancy ≥ 3 months;
Disqualifiers
Presence of known active Central Nervous System (CNS) metastases and/or carcinomatous meningitis. Participants with prior locoregional treatment for brain metastases may be enrolled only if medically stable for ≥ 4 weeks prior to the first dose. Medically stable is defined as the following conditions: no clinical symptoms attributable to CNS metastases within 4 weeks prior to the first dose (e.g., progressive or new neurological deficit, epileptic seizure, increased intracranial pressure, vomiting, papilledema, or headache); no evidence of CNS neoplasm relapse/progression on imaging assessments within 4 weeks prior to the first dose; no glucocorticoid therapy (>10 mg/day prednisone or equivalent) for ≥4 weeks prior to the first dose;
Participants with uncontrolled third interstitial effusions (e.g., pericardial effusion, pleural effusion, ascites) that cannot be controlled by repeated drainage or other interventions, and who are not suitable for enrollment by the investigator;
Participants with history of severe cardiovascular disease within 6 months prior to the first dose, including any of the following: (1) Congestive heart failure (New York Heart Association (NYHA) class > grade Ⅱ); (2) Severe/unstable angina, or new-onset angina pectoris within 3 months before the first dose; (3) Participants with myocardial ischaemia requiring long-term pharmacologic control, or heart failure (NYHA class Ⅲ-Ⅳ); (4) History of acute myocardial infarction; (5) Any grade ≥2 supraventricular or ventricular arrhythmia requiring treatment or intervention; (6) History of atrial fibrillation, coronary/peripheral artery bypass grafting, or transient ischaemic attack (TIA) with cerebrovascular symptoms; (7) Uncontrolled hypertension at screening (despite pharmacotherapy: diastolic blood pressure ≥ 100 mmHg and/or systolic blood pressure ≥ 160 mmHg);(8) QTcF≥ 470 ms on 12-lead (ECGs) performed in triplicate;
Participants with factors affecting oral administration (e.g., dysphagia, intestinal obstruction); or active gastrointestinal diseases or other conditions that may significantly alter drug absorption, distribution, metabolism, or excretion (including active inflammatory bowel disease, chronic diarrhea, frequent vomiting, enterocolitis, etc.);
Trial population
Study population: Patients diagnosed with malignant tumors for whom no established standard therapeutic regimen is available.
Trial design
Cohort
Prospective
Treatments tested in this trial
SYH2095
DrugSelective KAT6A/B inhibitor, oral tablet.. Administered orally once daily on an empty stomach, 4 weeks per treatment cycle.
Treatment groups
Trial outcomes
Primary outcomes
Incidence of Dose-Limiting Toxicity
Proportion of participants with DLT during the first 28-day treatment cycle (DLT observation period), assessed per NCI-CTCAE 6.0.
Maximum Tolerated Dose (MTD) of SYH2095
Determine the MTD of SYH2095 for monotherapy based on DLT and overall safety data.
Maximum Tolerated Dose of SYH2095
Description: Determine the MTD of SYH2095 for monotherapy based on DLT and overall safety data
Objective Response Rate
Confirmed ORR assessed by investigators per RECIST 1.1 in cohort expansion participants.
Secondary outcomes
Time to Maximum concentration (Tmax)
Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A
AUC from time zero to time of last measurable concentration (AUClast)
Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A
Terminal Elimination half-life (t1/2)
Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A
Steady-State Cmax
Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A
Other outcomes
Pharmacodynamic (PD) Changes of H3K23ac
Dynamic changes of peripheral blood H3K23ac level after SYH2095 administration
Sponsors and contacts
Click on the lead sponsor to view all of their trials.
CSPC ZhongQi Pharmaceutical Technology Co., Ltd.
Lead sponsor
Hangzhou Innogate Pharma Co., Ltd
Collaborator
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