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Vilon

KE, L-Lys-L-Glu, lysylglutamic acid

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Studies 40
Trials 100
Completed PHASE1 INTERVENTIONAL NCT05526313

Study of Purinostat Mesylate for Injection in the Treatment of Relapsed or Refractory B Cell-related Tumor-predominant

View on ClinicalTrials.gov Updated Dec 15, 2025

Brief Summary

Purinostat mesylate for injection (PM) was the novel and highly potent Class I a and IIb HDAC-selective inhibitors. The results of regular blood sampling analysis of the mouse B-cell lymphoma model induced by ighmyc transgenic mice showed that the treatment of PM in each group reduced the proportion of peripheral blood tumor cells in mice. Therefore, PM has the potential to treat diffuse large B cell lymphoma. The results of in vitro enzymatic activity screening showed that PM has high inhibitory activity on HDAC tumors (including HDAC1, 2, 3, 8 subtypes) and type II HDACs (including HDAC6, 10 isoforms), which are closely related to tumors in the HDAC family. Therefore, the results of in vitro enzyme activity screening showed that the IC50 values of PM for inhibiting HDAC1, HDAC2, HDAC3, HDAC8, HDAC6, and HDAC10 subtypes of HDAC class I and HDAC class IIb were 0.81, 1.4, 1.7, 3.8, 11.5, and 11 nM, respectively. However, the inhibitory activity of HDAC IIa and HDAC IV enzymes was low, and its IC50 values for HDAC4, HDAC5, HDAC7, HDAC9, and HDAC11 subtypes of HDAC IIa and HDAC IV were 1072, 426, 590, 622, and 3349 nM, respectively. These data means PM exist high selectivity for tumor-associated HDAC class I and HDAC IIb. Compared with the blank control group, the body weight of the tumor-bearing animals in each dose of PM group did not decrease seriously during the treatment process, and the animals were in good condition during the whole experiment, indicating that the PM is efficacy and safe. During the course of the experiment, the tumor cell population (GFP+, B220+) in the blood of the animals basically regressed after treatment with Prilistat hydrochloride. Research purposes: Main purpose: Observation of patients with relapsed or refractory hematological tumors (including but not limited to after standard therapy) mainly in patients with relapsed or refractory B cell-related tumors. Tolerability and safety of B-cell lymphoma, multiple myeloma, B-cell acute leukemia, T-cell lymphoma, T-cell acute leukemia) with disease progression or ineligible for standard therapy. To observe the dose-limiting toxicity (DLT) in patients with relapsed or refractory B cell-related tumors and hematological tumors, and determine its maximum tolerated dose (MTD), which is the maximum tolerated dose (MTD). Phase II clinical dosing schedule provides the basis. Secondary Purpose: To evaluate the pharmacokinetic parameters of patients with relapsed or refractory B-cell-related tumors and hematological tumors after single and multiple intravenous infusions of priinostat mesylate for injection. To evaluate the pharmacodynamics of patients with relapsed or refractory B cell-related tumors and hematological tumors after single and multiple intravenous infusions of priinostat mesylate for injection. To preliminarily observe the efficacy of Priinostat mesylate for injection in the treatment of patients with relapsed or refractory hematological tumors, mainly patients with B cell-related tumors.

Interventions

Name: Purinostat Mesylate 1.2mg/m^2
Type: DRUG
Description: 1 case,The starting dose,Take the medicine once on D1, D8, D11, D15.
Name: Purinostat Mesylate 2.4mg/m^2
Type: DRUG
Description: Take the medicine once on D1, D8, D11, D15.
Name: Purinostat Mesylate 4.0mg/m^2
Type: DRUG
Description: Take the medicine once on D1, D8, D11, D15.
Name: Purinostat Mesylate 6.0mg/m^2
Type: DRUG
Description: Take the medicine once on D1, D8, D11, D15.
Name: Purinostat Mesylate 8.4mg/m^2
Type: DRUG
Description: Take the medicine once on D1, D8, D11, D15.
Name: Purinostat Mesylate 11.2mg/m^2
Type: DRUG
Description: Take the medicine once on D1, D8, D11, D15.
Name: Purinostat Mesylate 15mg/m^2
Type: DRUG
Description: Take the medicine once on D1, D8, D11, D15.

Primary Outcomes

Measure: Purinostat Mesylate Pharmacokinetics (PK):Cmax
TimeFrame: 72hours
Description: Estimation of maximum observed plasma concentration
Measure: Purinostat Mesylate Pharmacokinetics (PK):Tmax
TimeFrame: 72hours
Description: Estimation of time to reach Cmax
Measure: Purinostat Mesylate Pharmacokinetics (PK):AUC0-72h
TimeFrame: 72hours
Description: Estimation of AUC from time zero to the last measured time point
Measure: Purinostat Mesylate Pharmacokinetics (PK):AUC0-∞
TimeFrame: 72hours
Description: Estimation of AUC from time zero extrapolated to infinity
Measure: Purinostat Mesylate Pharmacokinetics (PK):MRT
TimeFrame: 72hours
Description: Estimation of mean residence time
Measure: Purinostat Mesylate Pharmacokinetics (PK):Vd
TimeFrame: 72hours
Description: Estimation of apparent volume of distribution
Measure: Purinostat Mesylate Pharmacokinetics (PK):t1/2
TimeFrame: 72hours
Description: Estimation of terminal elimination half-life
Measure: Purinostat Mesylate Pharmacokinetics (PK):CLz/F
TimeFrame: 72hours
Description: Estimation of clearance when dosed orally
Measure: Purinostat Mesylate Pharmacokinetics (PK):Vz/F
TimeFrame: 72hours
Description: Estimation of apparent volume of distribution when dosed orally
Measure: Purinostat Mesylate Pharmacokinetics (PK):Ke
TimeFrame: 72hours
Description: Estimation of the elimination rate constant of a drug in the body

Trial Information

NCT ID

NCT05526313

Status

Completed

Study Type

INTERVENTIONAL

Phases

PHASE1

Sponsor

Chengdu Zenitar Biomedical Technology Co., Ltd

Last Updated

December 15, 2025