A Study To Evaluate The Effect Of Rifampicin Or Ltraconazole On Pharmacokinetics Of Ensartinib In Healthy Volunteers

NCT06492525 | Not Yet Recruiting Phase 1

• 1 other identifier: BTP-42319
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to estimate the effect of rifampicin or itraconazole on the single dose PK of ensartinib.

Conditions

Healthy

Outcome Measures

Primary Outcomes (6)

• Plasma AUC0-t for Ensartinib Given Alone and With Rifampicin

  AUC0-t is the plasma area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration (Clast).

  Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours post-dose on Day 1 after Ensartinib 225 mg administration in Period 1, and at the same time points on Day 18 after Ensartinib 225 mg with rifampin administration in Period 2.

• Plasma AUC0-t for Ensartinib Given Alone and With Itraconazole

  AUC0-t is the plasma area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration (Clast).

  Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post-dose on Day 1 after Ensartinib 100 mg administration in Period 1, and at the same time points on Day 12 after Ensartinib 100 mg with Itraconazole administration in Period 2.

• Plasma AUC0-∞ for Ensartinib Given Alone and With Rifampicin

  AUC0-∞ is the plasma area under the plasma concentration-time profile from time 0 extrapolated to infinite time.

  Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours post-dose on Day 1 after Ensartinib 225 mg administration in Period 1, and at the same time points on Day 18 after Ensartinib 225 mg with rifampin administration in Period 2.

• Plasma AUC0-∞ for Ensartinib Given Alone and With Itraconazole

  AUC0-∞ is the plasma area under the plasma concentration-time profile from time 0 extrapolated to infinite time.

  Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post-dose on Day 1 after Ensartinib 100 mg administration in Period 1, and at the same time points on Day 12 after Ensartinib 100 mg with Itraconazole administration in Period 2.

• Plasma Cmax for Ensartinib Given Alone and With Rifampicin

  Maximum plasma concentration

  Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours post-dose on Day 1 after Ensartinib 225 mg administration in Period 1, and at the same time points on Day 18 after Ensartinib 225 mg with rifampin administration in Period 2.

• Plasma Cmax for Ensartinib Given Alone and With Itraconazole

  Maximum plasma concentration

  Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post-dose on Day 1 after Ensartinib 100 mg administration in Period 1, and at the same time points on Day 12 after Ensartinib 100 mg with Itraconazole administration in Period 2.

Study Arms (2)

Cohort 1

EXPERIMENTAL

All subjects in this cohort will receive the same dose of Ensartinib in both periods. Subjects will receive Ensartinib Alone in Period 1 followed by Ensartinib with Rifampicin in Period 2.

Drug: Ensartinib; Drug: Rifampicin

Cohort 2

EXPERIMENTAL

All subjects in this cohort will receive the same dose of Ensartinib in both periods. Subjects will receive Ensartinib Alone in Period 1 followed by Ensartinib with Itraconazole in Period 2.

Drug: Itraconazole; Drug: Ensartinib

Interventions

Ensartinib DRUG

225 mg oral dose on day 1 in period 1 and on day 18 in period 2

Cohort 1

Rifampicin DRUG

600 mg QD from day 9 to day 22 in period 2

Cohort 1

Itraconazole DRUG

200 mg QD from day 9 to day 19 in period 2

Cohort 2

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male body weight ≥ 50kg, female body weight ≥ 45kg, body mass index (BMI) within the range of 19 \~ 26kg /m2;
• Clinical laboratory evaluations within the reference range for the test laboratory, unless deemed not clinically significant by the Investigator;
• The subjects should took effective contraceptive measures voluntarily from informed consent until 3 months after Study Completion；
• Able to comprehend and willing to sign an informed consent form.

You may not qualify if:

• Those with a history of chronic systemic or serious diseases such as cardiovascular, liver, kidney, lung, gastrointestinal, nervous, musculoskeletal, hematopoietic or metabolic diseases, especially surgical conditions or conditions that may affect drug absorption, distribution, metabolism and excretion；
• Family history or presence of long QTc syndrome; History or presence of an abnormal ECG；
• Hepatitis B virus surface antigen (HBsAg), hepatitis C virus antibody (HCV-Ab), treponema pallidum antibody or human immunodeficiency virus antigen/antibody (HIV-Ag/Ab) is positive；
• Use of any medications (prescription drugs, over-the-counter drugs, Chinese herbal medicines, health products, moderate or strong CYP3A inhibitors or inducers, etc) within 14 days prior to the first administration；
• Those who have special dietary requirements (habitual consumption of grapefruit juice or excessive tea, coffee and/or caffeinated beverages) and are unable to withdraw during the trial；
• Drug abusers, smokers or alcoholics；
• Those with a history of fear of needles and hemophobia, difficulty in blood collection or inability to tolerate venipuncture blood collection;
• Donation of blood ≥ 400 mL or receipt of blood products within 3 months before enrollment;
• Receive any vaccine within 1 months before enrollment；
• Participation in any other investigational drug study within 3 months before enrollment；
• History of significant hypersensitivity to any drug compound or food；
• Other conditions that, in the opinion of the investigator, are not suitable for the subject to participate in this study.

Sponsors & Collaborators

• Betta Pharmaceuticals Co., Ltd.: lead

Study Sites (1)

The Second Affiliated hospital of Zhejiang University School of Medicine

Hangzhou, Zhejiang, 310009, China

Location

MeSH Terms

Interventions

ensartinib; Rifampin; Itraconazole

Intervention Hierarchy (Ancestors)

Rifamycins; Heterocyclic Compounds, 4 or More Rings; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Lactams, Macrocyclic; Macrocyclic Compounds; Polycyclic Compounds; Triazoles; Azoles; Heterocyclic Compounds, 1-Ring; Piperazines

Central Study Contacts

Bo Jiang, Ph.D

CONTACT

0571-87783759; jiangbo@zju.edu.cn

Study Design

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

Study Record Dates

• First Submitted: July 1, 2024
• First Posted: July 9, 2024
• Study Start: July 1, 2024
• Primary Completion: October 1, 2024
• Study Completion: December 1, 2024
• Last Updated: July 9, 2024

Record last verified: 2024-07

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)