NCT04537715

Effects of Itraconazole and Rifampin on the Blood Tazemetostat Levels

A Phase I, Open-label Multi-dose Two-part Study to Characterize the Effects of a Strong CYP3A4 Inhibitor and a Strong CYP3A4 Inducer on the Steady-State Pharmacokinetics of Tazemetostat (EPZ-6438) in Subjects With Advanced Malignancies

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 42 (actual)
• Sponsor: Epizyme, Inc. · Industry
• Sex: All
• Age: 18 Years
• Healthy volunteers: Not accepted

Summary

The participants of this study will have advanced malignancies (also known as advanced cancer). The main aim of this trial will be to study the blood levels (known as pharmacokinetics) of the tazemtostat (the study drug) when administered in combination with another drug. Part 1 of the study will evaluate the interaction between the drugs tazemetostat and itraconazole. Part 2 of the study will evaluate the interaction between the drugs tazemetostat and rifampin For both Parts 1 and 2, safety and the level that effects of the study drug can be tolerated (known as tolerability) will be assessed throughout.

Detailed description

This two-part study is designed to characterize the steady-state PK of oral tazemetostat and its metabolite EPZ 6930 when administered as a single and twice daily dose in subjects with advanced malignancies while taken alone or in combination with either itraconazole or rifampin. Part 1: tazemetostat and Itraconazole Drug Interaction Part 1 of the study will evaluate the drug-drug interaction between tazemetostat and itraconazole in an open-label, fixed sequential cross over design. Part 2: tazemetostat and Rifampin Drug Interaction Part 2 of the study will evaluate the drug-drug interaction between tazemetostat and rifampin in an open-label, fixed sequential cross over design. For both Parts 1 and 2, safety and tolerability will be assessed throughout the subject's participation. Subjects must have an end of study visit after 30 days of the last dose of tazemetostat for safety assessment.

Conditions

• All Malignancies
• Advanced Malignancies
• Hematologic Malignancy
• Solid Tumor
• Follicular Lymphoma (FL)
• Non-Hodgkin Lymphoma (NHL)
• Diffuse Large B-Cell Lymphoma (DLBCL)
• Epithelioid Sarcoma (ES)
• Synovial Sarcoma
• Renal Medullary Carcinoma
• Mesothelioma
• Rhabdoid Tumor

Interventions

Type	Name	Description
DRUG	Tazemetostat	A single, oral, 400 mg dose of tazemetostat on Day 1, Day 15, and Day 36; and tazemetostat (oral 400 mg) tablets twice daily on Days 3 - 14 and Days 21 - 35.
DRUG	Itraconazole	Oral 200 mg itraconazole once daily on Days 18 - 38
DRUG	Tazemetostat	A single, oral, 800 mg dose of tazemetostat on Days 1, 15, and Day 24 ; and tazemetostat (oral 800 mg) twice daily on Days 3 - 14 and on Days 17 - 23.
DRUG	Rifampin	Oral 600 mg rifampin once daily on Days 17 - 25.

Timeline

• Start date: 2020-04-23
• Primary completion: 2023-04-03
• Completion: 2023-04-03
• First posted: 2020-09-03
• Last updated: 2025-02-19
• Results posted: 2024-08-26

Locations

10 sites across 2 countries: United States, Spain

Regulatory

• FDA-regulated drug study