SYH2095 for Advanced Malignant Tumors: Phase I Study

Trial statusNot yet recruiting
Trial phaseNot listed
Trial typeObservational
Biological sexAll
Age18+
SponsorCSPC ZhongQi Pharmaceutical Technology Co., Ltd.

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 volunteers

Qualifiers

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

Design model

Cohort

Time perspective

Prospective

Treatments tested in this trial

  • SYH2095

    Drug

    Selective KAT6A/B inhibitor, oral tablet.. Administered orally once daily on an empty stomach, 4 weeks per treatment cycle.

Treatment groups

140 Participants
are divided into 2 treatment groups
Group A: SYH2095 Monotherapy Dose Escalation Cohort (1A)1 intervention
Group B: SYH2095 Monotherapy Expansion Cohort (2A)1 intervention

Trial outcomes

Primary outcomes

1

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.

Time frame
End of Part 1 Dose Escalation and Backfill phase (each cycle is 28 days; all safety data collected through Day 28 of Cycle 1 for every dose-escalation subject)]
2

Maximum Tolerated Dose (MTD) of SYH2095

Determine the MTD of SYH2095 for monotherapy based on DLT and overall safety data.

Time frame
End of Part 1 Dose Escalation and Backfill phase (each cycle is 28 days; all safety data collected through Day 28 of Cycle 1 for every dose-escalation subject)]
3

Maximum Tolerated Dose of SYH2095

Description: Determine the MTD of SYH2095 for monotherapy based on DLT and overall safety data

Time frame
End of Part 1 Dose Escalation phase (each cycle is 28 days; safety data collected through Day 28 of Cycle 1 for all dose-escalation subjects)]
4

Objective Response Rate

Confirmed ORR assessed by investigators per RECIST 1.1 in cohort expansion participants.

Time frame
2 years

Secondary outcomes

1

Time to Maximum concentration (Tmax)

Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A

Time frame
2 years
2

AUC from time zero to time of last measurable concentration (AUClast)

Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A

Time frame
2 years
3

Terminal Elimination half-life (t1/2)

Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A

Time frame
2 years
4

Steady-State Cmax

Pharmacokinetic (PK) assessments for SYH2095 Part 1A and Part 2A

Time frame
2 years

Other outcomes

1

Pharmacodynamic (PD) Changes of H3K23ac

Dynamic changes of peripheral blood H3K23ac level after SYH2095 administration

Time frame
2 years

Sponsors and contacts

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CSPC ZhongQi Pharmaceutical Technology Co., Ltd.

Lead sponsor

Hangzhou Innogate Pharma Co., Ltd

Collaborator

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