Pharmacokinetics of Olverembatinib in Participants With Hepatic Impairment

NCT07282093 | Recruiting Phase 1

• 1 other identifier: HQP1351XC107
• Study Type: interventional
• Target: 48
• Locations: 1 country
• Sites: 1

Brief Summary

This is a non-randomized, open-label, parallel, single-dose study to evaluate the pharmacokinetic profile of olverembatinib in participants with normal or impaired liver function.

Conditions

Pharmacokinetic; Olverembatinib

Keywords

olverembatinib

Outcome Measures

Primary Outcomes (8)

• Maximum observed plasma concentration C(max)

  The C(max) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated and compared.

  Day 1 to Day 9

• Time to C(max) [ t(max) ]

  The t(max) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

  Day 1 to Day 9

• Apparent terminal elimination half-life (t½)

  The t½ of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

  Day 1 to Day 9

• Area under the concentration-time curve from time zero to last time of quantifiable concentration [AUC(last)]

  The AUC(last) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated and compared.

  Day 1 to Day 9

• Area under the concentration-time curve from time zero to 192h AUC(0-192h)

  The AUC(0-192h) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated and compared.

  Day 1 to Day 9

• Apparent Clearance (CL/F)

  The CL/F of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

  Day 1 to Day 9

• Apparent Volume of distribution (Vz/F)

  The Vz/F of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

  Day 1 to Day 9

• Unbound Fraction (fu)

  The unbound fraction (fu) of a single dose of olverembatinib in participants with impaired hepatic function and controls with normal hepatic function will be evaluated.

  Day 1 to Day 9

Secondary Outcomes (1)

• Safety evaluation endpoints

  Day1-Day21

Study Arms (6)

Group 1: 6-8 participants with mild hepatic impairment.

EXPERIMENTAL

Drug: Olverembatinib 20mg

Group 2: 6-8 participants with normal hepatic function matched to Group 1

EXPERIMENTAL

Drug: Olverembatinib 20mg

Group 3: 6-8 participants with moderate hepatic impairment

EXPERIMENTAL

Drug: Olverembatinib 20mg

Group 4: 6-8 participants with normal hepatic function matched to Group 3

EXPERIMENTAL

Drug: Olverembatinib 20mg

Group 5: 6-8 participants with severe hepatic impairment

EXPERIMENTAL

Drug: Olverembatinib 20mg

Group 6: 6-8 participants with normal hepatic function matched to Group 5

EXPERIMENTAL

Drug: Olverembatinib 20mg

Interventions

Olverembatinib 20mg DRUG

orally after meal, single dose

Group 1: 6-8 participants with mild hepatic impairment.; Group 2: 6-8 participants with normal hepatic function matched to Group 1; Group 3: 6-8 participants with moderate hepatic impairment; Group 4: 6-8 participants with normal hepatic function matched to Group 3; Group 5: 6-8 participants with severe hepatic impairment; Group 6: 6-8 participants with normal hepatic function matched to Group 5

Eligibility Criteria

• Age: 18 Years - 75 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• The participant voluntarily joins the study, signs the Informed Consent Form, and demonstrates good compliance.
• Body Mass Index (BMI) between 18 and 30 kg/m² (inclusive), with male weight ≥ 50 kg and female weight ≥ 45 kg.
• The investigator judges the participant suitable to participate in this study based on physical examination, vital signs, laboratory tests, and 12-lead electrocardiogram (ECG) examination.
• Female participants of childbearing potential must agree to use effective contraception during the study and for 3 months after the study ends; must have a negative serum pregnancy test within 7 days prior to study enrollment; and must not be breastfeeding. Male participants must agree to use effective contraception during the study and for 3 months after the study ends.
• Additional Criteria for Participants with hepatic impairment Only:
• \. Chronic hepatic impairment due to viral hepatitis, alcoholic liver disease, autoimmune hepatitis, or other causes.
• \. Hepatic impairment classified as Child-Pugh Class A, B, or C. 3. Coagulation function: INR ≤ 2.5 without intervention with procoagulant drugs (after a 2-week washout period). Hematology: Neutrophils ≥ 1.0 × 10⁹/L, Hemoglobin ≥ 70 g/L, Platelets ≥ 30 × 10⁹/L. Liver function: Alanine Aminotransferase (ALT) and Aspartate Aminotransferase (AST) ≤ 5 times the Upper Limit of Normal (ULN); Total Bilirubin ≤ 5 × ULN.
• \. Stable treatment for hepatic impairment, complications, and other concomitant diseases prior to study drug administration, with no need for dosage adjustment. Treatment for hepatic impairment must have been stable for at least 4 weeks.

You may not qualify if:

• Drug-induced liver injury.
• Any of the following conditions: history of liver transplantation; presence of acute or worsening liver injury due to any cause; liver failure; concurrent Grade 3/4 hepatic encephalopathy; active hepatocellular carcinoma lesions; severe esophageal or gastric varices or history of rupture and bleeding; severe/late-stage ascites or pleural effusion requiring paracentesis/thoracentesis and albumin supplementation; hepatorenal syndrome; or any other condition deemed by the investigator as unsuitable for study participation.
• History of cholestasis, biliary tract infection, or other diseases affecting bile excretion within 3 months prior to screening.
• Esophageal or gastric variceal bleeding due to portal hypertension within 3 months prior to screening, or history of portosystemic shunt surgery (including Transjugular Intrahepatic Portosystemic Shunt - TIPS) within 6 months prior to screening.
• History of significant allergy or intolerance to any drug, food, or other substance.
• History of any clinically significant disease in the neurological, cardiovascular, digestive, respiratory, urinary, endocrine, hematological, immune systems, or any other disease or condition that the investigator believes may affect the trial results.
• History of surgery that may affect drug absorption, distribution, metabolism, or excretion, or plans for surgery or other reasons requiring hospitalization during the expected study period.
• Uncontrolled bacterial, viral, parasitic, or fungal infection requiring treatment at the time of screening (except Hepatitis B), or history of severe active infection within 1 month prior to screening.
• Positive Human Immunodeficiency Virus (HIV) antigen/antibody test at screening. For participants with normal hepatic function: Positive Treponema pallidum antibody. For hepatically impaired participants: Active syphilis.
• Use of systemic medications with known potential hepatotoxicity for 7 consecutive days or more within 14 days prior to study drug administration.
• Use of traditional Chinese medicine (herbal medicines, proprietary Chinese medicines), dietary supplements, or vitamins within 14 days prior to study drug administration.
• Systemic use of moderate or potent CYP3A4 inhibitors (e.g., itraconazole, fluconazole) or moderate or potent CYP3A4 inducers within 14 days prior to study drug administration.
• Positive urine drug screen or alcohol breath test at screening.
• Excessive alcohol intake (averaging more than 14 units of alcohol per week) within 3 months prior to screening, or inability to abstain from alcohol during the trial period.
• Consumption of grapefruit/juice, foods or beverages rich in methylxanthines, engagement in strenuous exercise, or presence of other factors affecting drug absorption, distribution, metabolism, or excretion within 7 days prior to study drug administration, and inability to abstain from these during the hospitalization period.

Sponsors & Collaborators

• Ascentage Pharma Group Inc.: lead
• Guangzhou Healthquest Pharma Co., Ltd: collaborator

Study Sites (1)

The First Affiliated Hospital of Suzhou Medical University

Suzhou, Jiangsu, 215006, China

RECRUITING

MeSH Terms

Interventions

olverembatinib

Study Officials

• Liyan Miao, M.D.,Ph.D.

  M.D.,Ph.D.

  PRINCIPAL INVESTIGATOR

• Weifeng Zhao, M.D.,Ph.D.

  The First Affiliated Hospital of Suzhou Medical University

  PRINCIPAL INVESTIGATOR

Central Study Contacts

Yifan Zhai, M.D., Ph.D.

CONTACT

18998334688; yzhai@ascentagepharma.com

Xiang Xu, M.D.

CONTACT

Xiang.Xu@ascentage.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: November 19, 2025
• First Posted: December 15, 2025
• Study Start: November 11, 2025
• Primary Completion (Estimated): June 30, 2026
• Study Completion (Estimated): October 31, 2026
• Last Updated: December 23, 2025

Record last verified: 2025-12

Locations

CN (1)