Trials Sponsors Conditions Drugs Pricing

Brief Summary

ZL-82 is an oral janus kinase (JAK) inhibitor. In vitro biological mass spectrometry identification test proves that ZL-82 can selectively and irreversibly inhibit JAK3. It has obvious safety advantages, with a wide therapeutic window and controllable cardiotoxicity. This is also demonstrated from preliminary GLP-conditions of acute toxicity in SD rats and Beagle dogs. Results of 4-week long-term toxicity in Beagle dogs also support this notion. Therefore, ZL-82 has the potential to treat rheumatoid arthritis. It Used to relieve and heal swelling, pain, stiffness, and limited mobility that may be caused by rheumatoid arthritis.The drug is intended to be used in patients with RA to relieve and heal swelling, pain, stiffness, and limited mobility that may be caused by rheumatoid arthritis. Pharmacodynamic studies show that ZL-82 has a strong inhibitory effect on JAK3 with IC50 of 2.8 nM, and has no obvious inhibitory effect on JAK1, JAK2 and TYK2. Compared with the similar drug Tofacitinib, its inhibitory effect on JAK3 subtype is 1nM, but its inhibition IC50 for JAK1 subtype and JAK2 subtype are 112nM and 20nM, respectively.and its selectivity is 100-fold and 20-fold, respectively.Also, the selectivity multiples of ZL-82 were 100-fold and 20-fold than tofacitinib , respectively, which indicates that ZL-82 is more selective than the marketed Tofacitinib.This allows ZL-82 to precisely inhibit JAK kinase and block a series of cytokines in the downstream signaling pathway. And show significant effect on rheumatoid arthritis. The experimental results showed that in DTH and CIA models, 25, 50, 75, and 100 mg/kg of this variety could dose-dependently inhibit joint swelling in mice. Objectives of Study Main Purpose:

1.To evaluate the tolerability, safety and pharmacokinetic characteristics of a single oral dose of ZL-82 tablets in healthy adult subjects;
2.To explore the effect of eating on the PK of oral ZL-82 tablets in healthy adult subjects;
3.To evaluate the tolerability, safety and pharmacokinetics of ZL-82 tablets after multiple oral administration in healthy adult subjects.

Conditions

Inflammatory Bowel Disease - IBD1 Rheumatoid Arthritis (RA)

Outcome Measures

Primary Outcomes (9)

Pharmacokinetics (PK) of ZL-82：Cmax
Estimation of maximum observed plasma concentration
24hours
Pharmacokinetics (PK) of ZL-82：Tmax
Estimation of time to reach Cmax
24hours
Pharmacokinetics (PK) of ZL-82：AUC0-24h
Estimation of AUC from time zero to the last measured time point
24hours
Pharmacokinetics (PK) of ZL-82：AUC0-∞
Estimation of AUC from time zero extrapolated to infinity
24hours
Pharmacokinetics (PK) of ZL-82：Vd
Estimation of apparent volume of distribution
24hours
Pharmacokinetics (PK) of ZL-82：t1/2

Study Arms (2)

ZL-82

EXPERIMENTAL

1 case，The starting dose，Take the medicine once on D1 ，D1 through 7.

Drug: ZL-82 12.5mgDrug: ZL-82 25mgDrug: ZL-82 50mgDrug: ZL-82 100mgDrug: ZL-82 200mgDrug: ZL-82 300mgDrug: ZL-82 450mgDrug: ZL-82 600mg

zL-82 placebo group

PLACEBO COMPARATOR

1 case,The starting dose,Take the medicine once on D1,D1-7.

Interventions

ZL-82 12.5mgDrug

1 case,The starting dose,Take the medicine once on D1,D1-7.

ZL-82

ZL-82 25mgDrug

1 case,The starting dose,Take the medicine once on D1,D1-7.

ZL-82

Eligibility Criteria

Age18 Years - 45 Years

Sexall

Healthy VolunteersYes

Age GroupsAdult (18-64)

You may qualify if:

Healthy subjects, regardless of gender, 18 to 45 years old (including 18 and 45 years old)
The weighing of male subjects ≥ 50kg, female subjects ≥ 45kg, and a body mass index (BMI) between 19 and 25kg/m2 (including boundary values)

Sponsors & Collaborators

Chengdu Zenitar Biomedical Technology Co., Ltd
Industrylead

Study Sites (1)

Affiliated Hospital of Guizhou Medical University

Guizhou, GuiYang, China

MeSH Terms

Conditions

Arthritis, RheumatoidCrohn Disease

Condition Hierarchy (Ancestors)

ArthritisJoint DiseasesMusculoskeletal DiseasesRheumatic DiseasesConnective Tissue DiseasesSkin and Connective Tissue DiseasesAutoimmune DiseasesImmune System DiseasesInflammatory Bowel DiseasesGastroenteritisGastrointestinal DiseasesDigestive System DiseasesIntestinal Diseases

Study Officials

Chen Lijuan, doctor
West China Hospital
STUDY CHAIR

Enrollment

69 participants (actual enrollment reported by the registry).

Study Design

Study Type: interventional
Phase: phase 1
Allocation: RANDOMIZED
Masking: QUADRUPLE
Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
Purpose: OTHER
Intervention Model: SEQUENTIAL
Sponsor Type: INDUSTRY
Responsible Party: SPONSOR

Study Record Dates

First Submitted

September 19, 2023

First Posted

September 26, 2023

Study Start

April 9, 2023

Actual (reported)

You may not qualify if:

Allergic constitution, such as those who are known to be allergic to two or more substances, or those who are known to be allergic to JAK inhibitors or to the excipients contained in the test drug
ALT and/or AST\>1×ULN, TIB\>1×ULN, GGT\>1×ULN; Scr\>1×ULN
Major surgery within the 3 months prior to the trial or planning to undergo surgery during the trial
Acute illness within 2 weeks prior to trial
Have any serious diseases such as cardiovascular system, digestive system, urinary system, respiratory system, nervous system, immune system, endocrine system, malignant tumor, mental illness, etc.
History of dysphagia or any gastrointestinal disease (or gastrointestinal resection, etc.) affecting drug absorption
HIV antibody, Treponema pallidum antibody, hepatitis B surface antigen and hepatitis C antibody test are positive
Positive urine drug screen (including morphine, methamphetamine, ketamine, MDMA, THC)
Systolic blood pressure\>140mmHg or diastolic blood pressure\>90mmHg during the screening period;
Blood donation or blood loss ≥400mL within 3 months, or blood transfusion; blood donation or blood loss ≥200mL within 1 month;
Have special requirements for diet or cannot comply with the unified diet and corresponding regulations of the research center
Alcoholics (alcoholism refers to drinking 60-degree white wine ≥10.5L or red wine ≥3.5L per week for more than 5 years), drinking a lot of coffee-containing beverages (more than 8 cups per day, 1 cup = 250ml) or heavy smoking (average \> 20 sticks/day);
Have used any prescription drugs (JAK inhibitors, etc.) that may have an effect on the test drug within 2 weeks;
weeks (28 days) before enrollment, strong inducers of liver metabolic enzymes was limit. ( such as omeprazole, barbiturates, carbamazepine, aminoglutamine, griseofulvin, carbamazepine, Phenytoin, Gluter, Rifampicin, Sulfinpyrazone, Roxithromycin, etc. )
Participate in clinical trials of other drugs or medical devices as subjects within 3 months
+3 more criteria

Phase I Clinical Study of ZL-82 Tablets

Brief Summary

Registry Overview

Trial Relationships

Study Timeline

Study Start

First Submitted

First Posted

Primary Completion

Study Completion

Conditions

Outcome Measures

Primary Outcomes (9)

Study Arms (2)

ZL-82

zL-82 placebo group

Interventions

Eligibility Criteria

You may qualify if:

Sponsors & Collaborators

Study Sites (1)

MeSH Terms

Conditions

Condition Hierarchy (Ancestors)

Study Officials

Enrollment

Study Design

Study Record Dates

You may not qualify if:

Data Sharing

Source record

Locations

Phase I Clinical Study of ZL-82 Tablets

Brief Summary

Registry Overview

Trial Relationships

Related Scientific Literature

Study Timeline

Study Start

First Submitted

First Posted

Primary Completion

Study Completion

Conditions

Outcome Measures

Primary Outcomes (9)

Study Arms (2)

ZL-82

zL-82 placebo group

Interventions

Eligibility Criteria

You may qualify if:

Sponsors & Collaborators

Study Sites (1)

MeSH Terms

Conditions

Condition Hierarchy (Ancestors)

Study Officials

Enrollment

Study Design

Study Record Dates

You may not qualify if:

Data Sharing

Source record

Locations