A Phase 1 interventional study of Tazemetostat and Itraconazole in All Malignancies, Advanced Malignancies and Hematologic Malignancy, sponsored by Epizyme, Inc.. Completed at 10 sites in 2 countries. Open to participants aged 18 Years and older. Per ClinicalTrials.gov, last updated 2025-02-19.
Sponsored by Epizyme, Inc. (part of Ipsen) · Phase 1, Interventional, and Treatment
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.
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.
1,444 studies on the registry are indexed under Hematologic Neoplasms; 420 are open to participants now.
This study's enrollment of 42 is close to the median of 46 across 1,044 interventional studies indexed under Hematologic Neoplasms.
Browse Hematologic Neoplasms studies →Epizyme, Inc. is the lead sponsor of 21 studies on the registry; none are open to participants now.
Of its 12 completed or terminated interventional studies of FDA-regulated products, 9 (75%) have results posted.
First submitted before Epizyme, Inc. became part of Ipsen.
Counted across the registry records on this site, refreshed daily.
Go through the criteria one by one — yes, no or not sure — and take the list to your doctor or the study team. Kept in this browser only.
and/or cytologically confirmed advanced or unresectable solid tumors has progressed after treatment for which there are no standard therapies available OR histologically and/or cytologically confirmed hematologic that have , or refractory disease, following at least 2 standard for which there are no standard therapies available.
Note: Subjects with prior radiotherapy will be included; however, radiotherapy alone will not be considered a separate systemic treatment regimen.
Male subjects must have had a successful vasectomy OR must either practice complete abstinence or agree to use a latex or synthetic condom during sexual contact with a female of childbearing potential (FCBP) during study treatment (including during dose interruptions), and for 3 months after study drug discontinuation.
NOTE: Male subjects must not donate sperm during study treatment (including during dose interruptions), and for 3 months after study drug discontinuation.
EXCLUSION CRITERIA:
Underlined terms in the criteria open these too. Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
A scale of how much an illness limits everyday activity. For people being assessed to join a study, scores run from 0 (fully active) to 4; lower is more active.
Studies most often ask for 0–1 or 0–2. Your doctor gives the score; the WHO scale uses the same steps. The full scale also has 5, which records death.
Before you join, the study team explains what taking part involves — its purpose, what happens, the risks and possible benefits — and answers your questions, so you can decide freely. Consent is usually recorded on a form (the informed consent form, ICF) signed by you or, where the law allows, by someone legally authorised to decide for you.
You can keep asking questions during the study, you are told of new information that matters, and you can choose to leave at any time.
The study doctor’s estimate of how long someone is likely to live. Criteria use it so that people can stay in the study long enough for it to answer its question.
The diagnosis was confirmed by looking at a sample under a microscope: tissue from a biopsy or surgery (histology), or cells from a fluid or needle sample (cytology).
Your pathology report is the document that shows this.
Cancer that has spread from where it began to other parts of the body. “Metastatic” cancer is cancer that has spread this way.
Malignancy means cancer. Criteria about another or earlier malignancy ask whether you have had a different cancer, usually within a set number of years.
Some are commonly allowed, such as treated skin cancers other than melanoma and early cancers removed completely — check the exceptions this study lists.
Relapsed: the illness came back after treatment had worked. Refractory: it did not respond to treatment, or stopped responding while still on it.
A line of therapy is one course of treatment, which may combine several drugs. First-line is the first course given; second-line follows when that stops working or is not tolerated.
“Two prior lines” means two courses that count separately under the study’s rules — not simply two drugs. Ask the study team if you are unsure how yours are counted.
The amount of disease can be tracked with a defined measurement, so the study can see whether it shrinks or grows. It might be a tumour measured on a scan or, in some blood cancers such as myeloma, a marker measured in blood or urine.
The criteria or the study team say which measurement counts — having no tumour visible on a scan does not by itself rule you out.
Judged by the study doctor to matter for your health or for the study. It is a doctor’s decision, so ask the study team if you are unsure whether something counts.
The US National Cancer Institute’s scale of how severe an adverse event is — any unwanted medical event during a study, such as a symptom, an illness or an abnormal test result, whether or not a treatment caused it. Whether it did is judged separately.
“Side effects of earlier treatment resolved to grade 1 or less” means they have settled to mild or gone.
A planned gap after a treatment, so that its effects can lessen before the study treatment or a study assessment. Ask the study team and the doctor who prescribed it before changing any medicine.
Able to become pregnant: from the first period until menopause, unless permanently unable to through surgery (removal of the womb, or of both ovaries or both fallopian tubes).
Criteria for people of childbearing potential usually ask for a negative pregnancy test and for contraception during the study and for a time after it.
Ways of preventing pregnancy. “Highly effective” methods fail less than 1% of the time a year when used correctly — for example an IUD or an implant.
Criteria usually say which methods count and how long to keep using them after the last dose, sometimes for male participants too. Some studies accept a partner’s vasectomy if it was confirmed successful and that person is the participant’s only sexual partner.
On an ECG, the QT interval is the time the heart’s lower chambers take to activate electrically and recover in each beat. QTc is that time adjusted for heart rate (QTcF by Fridericia’s formula, QTcB by Bazett’s). Some medicines lengthen it, and a long QTc can raise the risk of a dangerous heart rhythm.
The study may name a correction formula and a limit in milliseconds, often around 450–480.
Cancer that has spread to the leptomeninges, the thin layers covering the brain and spinal cord, and the fluid between them. It is not the same as brain metastases.
Criteria often treat it separately, and many studies leave it out even where treated brain metastases are allowed.
Cancer deposits in the brain from a cancer that started elsewhere in the body (CNS metastases include the spinal cord).
Studies differ: some leave out any brain metastases, some accept ones treated and stable for some weeks. Check what this study allows.
An allergy, or another reaction of the immune system, to a substance. “Hypersensitivity to the study drug” means a known allergic reaction to it — not every side effect a medicine can have.
A drug or device being studied in a clinical trial.
It may be new, or already approved and being studied for another use, dose or form. Criteria often leave out people who took part in another study of one within a recent period, commonly 30 days or five half-lives.
Hepatitis B is a virus that infects the liver. These are separate tests: HBsAg positive usually means a current infection (a recent vaccination can briefly cause it too); total anti-HBc (HBcAb) positive means an infection now or in the past; HBV DNA measures how much virus is in the blood.
Some studies accept a past infection if HBV DNA is undetectable, sometimes with antiviral medicine during the study. Check what this study allows.
Hepatitis C is a virus that infects the liver. An HCV antibody test can stay positive after an infection has cleared (and is occasionally positive without one); an HCV RNA test shows whether the virus is there now.
After treatment, hepatitis C counts as cured when HCV RNA is still undetectable 12 weeks or more after the treatment ended. Studies often accept people cured this way.
CYP3A is a group of enzymes, mainly CYP3A4, in the liver and gut that break down many medicines. Some medicines, supplements and foods (grapefruit, St John’s wort) slow them down or speed them up, which changes how much of a study drug stays in the body.
Studies list them so they can be avoided or switched; bring a list of everything you take, including supplements.
ECOG performance status
A scale of how much an illness limits everyday activity. For people being assessed to join a study, scores run from 0 (fully active) to 4; lower is more active.
Studies most often ask for 0–1 or 0–2. Your doctor gives the score; the WHO scale uses the same steps. The full scale also has 5, which records death.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Informed consent
Before you join, the study team explains what taking part involves — its purpose, what happens, the risks and possible benefits — and answers your questions, so you can decide freely. Consent is usually recorded on a form (the informed consent form, ICF) signed by you or, where the law allows, by someone legally authorised to decide for you.
You can keep asking questions during the study, you are told of new information that matters, and you can choose to leave at any time.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Life expectancy
The study doctor’s estimate of how long someone is likely to live. Criteria use it so that people can stay in the study long enough for it to answer its question.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Histologically or cytologically confirmed
The diagnosis was confirmed by looking at a sample under a microscope: tissue from a biopsy or surgery (histology), or cells from a fluid or needle sample (cytology).
Your pathology report is the document that shows this.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Metastases
Cancer that has spread from where it began to other parts of the body. “Metastatic” cancer is cancer that has spread this way.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Cancer (malignancy)
Malignancy means cancer. Criteria about another or earlier malignancy ask whether you have had a different cancer, usually within a set number of years.
Some are commonly allowed, such as treated skin cancers other than melanoma and early cancers removed completely — check the exceptions this study lists.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Relapsed and refractory
Relapsed: the illness came back after treatment had worked. Refractory: it did not respond to treatment, or stopped responding while still on it.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Line of therapy
A line of therapy is one course of treatment, which may combine several drugs. First-line is the first course given; second-line follows when that stops working or is not tolerated.
“Two prior lines” means two courses that count separately under the study’s rules — not simply two drugs. Ask the study team if you are unsure how yours are counted.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Measurable disease
The amount of disease can be tracked with a defined measurement, so the study can see whether it shrinks or grows. It might be a tumour measured on a scan or, in some blood cancers such as myeloma, a marker measured in blood or urine.
The criteria or the study team say which measurement counts — having no tumour visible on a scan does not by itself rule you out.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Clinically significant
Judged by the study doctor to matter for your health or for the study. It is a doctor’s decision, so ask the study team if you are unsure whether something counts.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
CTCAE grade
The US National Cancer Institute’s scale of how severe an adverse event is — any unwanted medical event during a study, such as a symptom, an illness or an abnormal test result, whether or not a treatment caused it. Whether it did is judged separately.
“Side effects of earlier treatment resolved to grade 1 or less” means they have settled to mild or gone.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Washout period
A planned gap after a treatment, so that its effects can lessen before the study treatment or a study assessment. Ask the study team and the doctor who prescribed it before changing any medicine.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Childbearing potential
Able to become pregnant: from the first period until menopause, unless permanently unable to through surgery (removal of the womb, or of both ovaries or both fallopian tubes).
Criteria for people of childbearing potential usually ask for a negative pregnancy test and for contraception during the study and for a time after it.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Contraception
Ways of preventing pregnancy. “Highly effective” methods fail less than 1% of the time a year when used correctly — for example an IUD or an implant.
Criteria usually say which methods count and how long to keep using them after the last dose, sometimes for male participants too. Some studies accept a partner’s vasectomy if it was confirmed successful and that person is the participant’s only sexual partner.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
QT and QTc
On an ECG, the QT interval is the time the heart’s lower chambers take to activate electrically and recover in each beat. QTc is that time adjusted for heart rate (QTcF by Fridericia’s formula, QTcB by Bazett’s). Some medicines lengthen it, and a long QTc can raise the risk of a dangerous heart rhythm.
The study may name a correction formula and a limit in milliseconds, often around 450–480.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Leptomeningeal disease
Cancer that has spread to the leptomeninges, the thin layers covering the brain and spinal cord, and the fluid between them. It is not the same as brain metastases.
Criteria often treat it separately, and many studies leave it out even where treated brain metastases are allowed.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Brain metastases
Cancer deposits in the brain from a cancer that started elsewhere in the body (CNS metastases include the spinal cord).
Studies differ: some leave out any brain metastases, some accept ones treated and stable for some weeks. Check what this study allows.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Hypersensitivity
An allergy, or another reaction of the immune system, to a substance. “Hypersensitivity to the study drug” means a known allergic reaction to it — not every side effect a medicine can have.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Investigational drug or device
A drug or device being studied in a clinical trial.
It may be new, or already approved and being studied for another use, dose or form. Criteria often leave out people who took part in another study of one within a recent period, commonly 30 days or five half-lives.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Hepatitis B tests
Hepatitis B is a virus that infects the liver. These are separate tests: HBsAg positive usually means a current infection (a recent vaccination can briefly cause it too); total anti-HBc (HBcAb) positive means an infection now or in the past; HBV DNA measures how much virus is in the blood.
Some studies accept a past infection if HBV DNA is undetectable, sometimes with antiviral medicine during the study. Check what this study allows.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Hepatitis C tests
Hepatitis C is a virus that infects the liver. An HCV antibody test can stay positive after an infection has cleared (and is occasionally positive without one); an HCV RNA test shows whether the virus is there now.
After treatment, hepatitis C counts as cured when HCV RNA is still undetectable 12 weeks or more after the treatment ended. Studies often accept people cured this way.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
CYP3A (CYP3A4) inhibitors and inducers
CYP3A is a group of enzymes, mainly CYP3A4, in the liver and gut that break down many medicines. Some medicines, supplements and foods (grapefruit, St John’s wort) slow them down or speed them up, which changes how much of a study drug stays in the body.
Studies list them so they can be avoided or switched; bring a list of everything you take, including supplements.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Participants in Part 1 of the study will receive a single oral, 400 mg dose of tazemetostat on Day 1, 15, and Day 36. The study participants will receive tazemetostat (oral 400 mg) tablets to be taken twice daily on Days 3 - 14 and Days 21 - 35. In addition, the participants will receive oral 200 mg itraconazole once daily on Days 18 - 38. Study participants may continue tazemetostat from Day 40+ at the recommended therapeutic dose (oral 800 mg twice daily) in 28-day cycles.
Drug: Tazemetostat · Drug: Itraconazole
Participants in Part 2 of the study will receive a single oral, 800 mg dose of tazemetostat on Days 1, 15, and Day 36. The study participants will receive tazemetostat (oral 800 mg dose) tablets to be taken twice daily on Days 3 - 14 and Days 17 - 23. In addition, the participants will receive oral 200 mg rifampin once daily on Days 17 - 25. Study participants may continue tazemetostat from Day 27+ at the recommended therapeutic dose (oral 800 mg twice daily) in 28-day cycles.
Drug: Tazemetostat · Drug: Rifampin
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.
Also known as: EPZ-6438, Tazverik
Oral 200 mg itraconazole once daily on Days 18 - 38
Also known as: Sporanox
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.
Also known as: EPZ-6438, Tazverik
Oral 600 mg rifampin once daily on Days 17 - 25.
Also known as: RIF, Rifampicin, Rifadin, Rimactane
Part 1: Area Under the Plasma Concentration-Time Curve From Time 0 to 12 Hours of Quantifiable Concentration (AUC0-12h) of Tazemetostat
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, and 12 hours post-dose on Cycle 1 Day 1 and Cycle 1 Day 15
Part 1: Maximum Observed Plasma Concentration (Cmax) of Tazemetostat
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, 48, and 72 hours post-dose on Cycle 1 Day 1 and Cycle 1 Day 15
Part 2: AUC0-12h of Tazemetostat
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose on Cycle 1 Day 1 and Cycle 1 Day 15
Part 2: Cmax of Tazemetostat
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, and 48 hours post-dose on Cycle 1 Day 1 and Cycle 1 Day 15
Part 1: AUC0-12h of EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, and 12 hours post-dose on Cycle 1 Day 15
Part 1: AUC0-12h of Tazemetostat and EPZ-6930 After Tazemetostat at Steady-State With Itraconazole
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, and 12 hours post-dose on Cycle 1 Day 36
Part 1: Cmax of EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, and 72 hours post-dose on Cycle 1 Day 15
Part 1: Cmax of Tazemetostat and EPZ-6930 After Tazemetostat at Steady State With Itraconazole
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, and 72 hours post-dose on Cycle 1 Day 36
Part 1: Observed Time at Cmax (Tmax) of Tazemetostat and EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, and 72 hours post-dose on Cycle 1 Day 15
Part 1: Tmax of Tazemetostat and EPZ-6930 After Tazemetostat at Steady-State With Itraconazole
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, and 72 hours post-dose on Cycle 1 Day 36
Part 1: Apparent Terminal Elimination Half-Life (t1/2) of Tazemetostat and EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, and 72 hours post-dose on Cycle 1 Day 15
Part 1: T1/2 of Tazemetostat and EPZ-6930 After Tazemetostat at Steady-State With Itraconazole
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, and 72 hours post-dose on Cycle 1 Day 36
Part 2: AUC0-12h of EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, and 12 hours post-dose on Cycle 1 Day 15
Part 2: AUC0-12h of Tazemetostat and EPZ-6930 After Tazemetostat at Steady-State With Rifampin
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose on Cycle 1 Day 24
Part 2: Cmax of EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, and 48 hours post-dose on Cycle 1 Day 15
Part 2: Cmax of Tazemetostat and EPZ-6930 After Tazemetostat at Steady State With Rifampin
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, and 48 hours post-dose on Cycle 1 Day 24
Part 2: Tmax of Tazemetostat and EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, and 48 hours post-dose on Cycle 1 Day 15
Part 2: Tmax of Tazemetostat and EPZ-6930 After Tazemetostat at Steady-State With Rifampin
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, and 48 hours post-dose on Cycle 1 Day 24
Part 2: T1/2 of Tazemetostat and EPZ-6930 EPZ-6930 After Tazemetostat Alone at Steady-State
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, and 48 hours post-dose on Cycle 1 Day 15
Part 2: T1/2 of Tazemetostat and EPZ-6930 After Tazemetostat at Steady-State With Rifampin
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, and 48 hours post-dose on Cycle 1 Day 24
Part 1: Least Squares Geometric Mean Ratio of Observed Accumulation Ratio of AUC0-12h for Tazemetostat
Blood samples were collected at specified timepoints. AUC0-12h accumulation ratio was assessed using non-compartmental data analysis method. AUC0-12h accumulation ratio was calculated as the ratio of AUC0-12h at steady state (Cycle 1 Day 15) divided by AUC0-12 during the initial dosing interval (Cycle 1 Day 1).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose on Cycle 1 Day 1 and Cycle 1 Day 15
Part 1: Least Squares Geometric Mean Ratio of Cmax Accumulation Ratio for Tazemetostat
Blood samples were collected at specified timepoints. Cmax accumulation ratio was assessed using non-compartmental data analysis method. Cmax accumulation ratio was calculated as the ratio of Cmax at steady state (Cycle 1 Day 15) divided by Cmax during the initial dosing interval (Cycle 1 Day 1).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8,12, 36, 48 post-dose on Cycle 1 Day 1, and 72 hours post-dose on Cycle 1 Day 15
Part 1: Least Squares Geometric Mean Ratio of AUC0-12h After Single Dose of Tazemetostat With Itraconazole
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using analysis of variance (ANOVA).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, and 12 hours post-dose on Cycle 1 Day 1 (without itraconazole) and Cycle 1 Day 21 (with itraconazole)
Part 1: Least Squares Geometric Mean Ratio of Cmax After Single Dose of Tazemetostat With Itraconazole
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, and 48 hours post-dose on Cycle 1 Day 1 (without itraconazole) and Cycle 1 Day 21 (with itraconazole)
Part 1: Least Squares Geometric Mean Ratio of AUC0-12h After Tazemetostat at Steady-State With Itraconazole
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, and 12 hours post-dose on Cycle 1 Day 15 (without itraconazole) and Cycle 1 Day 36 (with itraconazole)
Part 1: Least Squares Geometric Mean Ratio of Cmax After Tazemetostat at Steady-State With Itraconazole
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 36, and 72 hours post-dose on Cycle 1 Day 15 (without itraconazole) and Cycle 1 Day 36 (with itraconazole)
Part 2: Least Squares Geometric Mean Ratio of Observed Accumulation Ratio of AUC0-12h for Tazemetostat
Blood samples were collected at specified timepoints. AUC0-12h accumulation ratio was assessed using non-compartmental data analysis method. AUC0-12h accumulation ratio was calculated as the ratio of AUC0-12h at steady state (Cycle 1 Day 15) divided by AUC0-12h during the initial dosing interval (Cycle 1 Day 1).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8,12, 24, 36, and 48 hours post-dose on Cycle 1 Day 1 and Cycle 1 Day 15
Part 2: Least Squares Geometric Mean Ratio of Cmax Accumulation Ratio for Tazemetostat
Blood samples were collected at specified timepoints. Cmax accumulation ratio was assessed using non-compartmental data analysis method. Cmax accumulation ratio was calculated as the ratio of Cmax at steady state (Cycle 1 Day 15) divided by Cmax during the initial dosing interval (Cycle 1 Day 1).
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8,12, 24, 36, and 48 hours post-dose on Cycle 1 Day 1 and Cycle 1 Day 15
Part 2: Least Squares Geometric Mean Ratio of AUC0-12h After Tazemetostat at Steady State With Rifampin
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours post-dose on Cycle 1 Day 15 (without rifampin) and Cycle 1 Day 24 (with rifampin)
Part 2: Least Squares Geometric Mean Ratio of Cmax After Tazemetostat at Steady State With Rifampin
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
Time frame: Pre-dose (0 hour), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, and 48 hours post-dose on Cycle 1 Day 15 (without rifampin) and Cycle 1 Day 24 (with rifampin)
This Phase 1, 2-part, multi-dose, open-label study was conducted in participants with advanced malignancies from 23 April 2020 to 03 April 2023 at 10 investigational sites in Spain and USA. Part 1 evaluated drug-drug interaction (DDI) between tazemetostat and itraconazole; Part 2 evaluated DDI between tazemetostat and rifampin.
| Milestone | Part 1: Tazemetostat + Itraconazole | Part 2: Tazemetostat + Rifampin |
|---|---|---|
| Started | 21 | 21 |
| Completed | 10 | 16 |
| Not completed | 11 | 5 |
| Withdrew: Death | 3 | 1 |
| Withdrew: Withdrawal by subject | 3 | 1 |
| Withdrew: Other | 4 | 3 |
| Withdrew: Progressive disease | 1 | 0 |
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
| hours*nanogram/milliliter (h*ng/mL) | Part 1: Tazemetostat |
|---|---|
| Cycle 1 Day 1 | 2180 ± 55.3 |
| Cycle 1 Day 15 | 1830 ± 37.6 |
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
| ng/mL | Part 1: Tazemetostat |
|---|---|
| Cycle 1 Day 1 | 704 ± 56.5 |
| Cycle 1 Day 15 | 543 ± 63.3 |
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
| h*ng/mL | Part 2: Tazemetostat |
|---|---|
| Cycle 1 Day 1 | 4420 ± 83.2 |
| Cycle 1 Day 15 | 3610 ± 70.3 |
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
| ng/mL | Part 2: Tazemetostat |
|---|---|
| Cycle 1 Day 1 | 1330 ± 67.4 |
| Cycle 1 Day 15 | 1100 ± 78.7 |
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
| h*ng/mL | Part 1: Tazemetostat |
|---|---|
| Part 1: AUC0-12h of EPZ-6930 After Tazemetostat Alone at Steady-State | 3650 ± 26.4 |
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
| h*ng/mL | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Tazemetostat | 4530 ± 64.5 |
| EPZ-6930 | 5450 ± 46.6 |
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
| ng/mL | Part 1: Tazemetostat |
|---|---|
| Part 1: Cmax of EPZ-6930 After Tazemetostat Alone at Steady-State | 780 ± 38.2 |
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
| ng/mL | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Tazemetostat | 1010 ± 76.3 |
| EPZ-6930 | 792 ± 44.7 |
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
| hour | Part 1: Tazemetostat |
|---|---|
| Tazemetostat | 1.34 ± 72.1 |
| EPZ-6930 | 1.70 ± 51.4 |
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
| hour | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Tazemetostat | 1.55 ± 63.4 |
| EPZ-6930 | 1.82 ± 49.9 |
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
| hour | Part 1: Tazemetostat |
|---|---|
| Tazemetostat | 8.21 (4.67 to 19.8) |
| EPZ-6930 | 15.8 (8.10 to 22.8) |
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
| hour | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Tazemetostat | 12.8 (6.40 to 22.0) |
| EPZ-6930 | 13.9 (7.19 to 21.6) |
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
| h*ng/mL | Part 2: Tazemetostat |
|---|---|
| Part 2: AUC0-12h of EPZ-6930 After Tazemetostat Alone at Steady-State | 7010 ± 72.0 |
Blood samples were collected at specified timepoints. AUC0-12h was assessed using non-compartmental data analysis method. AUC0-12h was estimated by a combination of linear trapezoidal method on concentrations going up and logarithmic trapezoidal method on concentrations going down (Linear up/Log down method).
| h*ng/mL | Part 2: Tazemetostat + Rifampin |
|---|---|
| Tazemetostat | 588 ± 65.2 |
| EPZ-6930 | 3070 ± 34.1 |
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
| ng/mL | Part 2: Tazemetostat |
|---|---|
| Part 2: Cmax of EPZ-6930 After Tazemetostat Alone at Steady-State | 1530 ± 49.5 |
Blood samples were collected at specified timepoints. Cmax was assessed using non-compartmental data analysis method.
| ng/mL | Part 2: Tazemetostat + Rifampin |
|---|---|
| Tazemetostat | 181 ± 71.7 |
| EPZ-6930 | 857 ± 40.5 |
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
| hour | Part 2: Tazemetostat |
|---|---|
| Tazemetostat | 1.25 ± 47.0 |
| EPZ-6930 | 1.47 ± 59.1 |
Blood samples were collected at specified timepoints. Tmax was assessed using non-compartmental data analysis method.
| hour | Part 2: Tazemetostat + Rifampin |
|---|---|
| Tazemetostat | 1.40 ± 1.10 |
| EPZ-6930 | 1.85 ± 0.934 |
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
| hour | Part 2: Tazemetostat |
|---|---|
| Tazemetostat | 7.21 (5.55 to 10.6) |
| EPZ-6930 | 8.38 (6.44 to 13.8) |
Blood samples were collected at specified timepoints. T1/2 was assessed using non-compartmental data analysis method.
| hour | Part 2: Tazemetostat + Rifampin |
|---|---|
| Tazemetostat | 5.24 (2.45 to 8.19) |
| EPZ-6930 | 8.07 (3.70 to 10.3) |
Blood samples were collected at specified timepoints. AUC0-12h accumulation ratio was assessed using non-compartmental data analysis method. AUC0-12h accumulation ratio was calculated as the ratio of AUC0-12h at steady state (Cycle 1 Day 15) divided by AUC0-12 during the initial dosing interval (Cycle 1 Day 1).
| ratio | Part 1: Tazemetostat |
|---|---|
| Part 1: Least Squares Geometric Mean Ratio of Observed Accumulation Ratio of AUC0-12h for Tazemetostat | 0.842 (0.726 to 0.976) |
Blood samples were collected at specified timepoints. Cmax accumulation ratio was assessed using non-compartmental data analysis method. Cmax accumulation ratio was calculated as the ratio of Cmax at steady state (Cycle 1 Day 15) divided by Cmax during the initial dosing interval (Cycle 1 Day 1).
| ratio | Part 1: Tazemetostat |
|---|---|
| Part 1: Least Squares Geometric Mean Ratio of Cmax Accumulation Ratio for Tazemetostat | 0.771 (0.662 to 0.897) |
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using analysis of variance (ANOVA).
| ratio | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Part 1: Least Squares Geometric Mean Ratio of AUC0-12h After Single Dose of Tazemetostat With Itraconazole | 3.12 (2.44 to 3.99) |
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
| ratio | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Part 1: Least Squares Geometric Mean Ratio of Cmax After Single Dose of Tazemetostat With Itraconazole | 2.00 (1.60 to 2.48) |
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
| ratio | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Part 1: Least Squares Geometric Mean Ratio of AUC0-12h After Tazemetostat at Steady-State With Itraconazole | 2.47 (2.02 to 3.02) |
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
| ratio | Part 1: Tazemetostat + Itraconazole |
|---|---|
| Part 1: Least Squares Geometric Mean Ratio of Cmax After Tazemetostat at Steady-State With Itraconazole | 1.86 (1.49 to 2.31) |
Blood samples were collected at specified timepoints. AUC0-12h accumulation ratio was assessed using non-compartmental data analysis method. AUC0-12h accumulation ratio was calculated as the ratio of AUC0-12h at steady state (Cycle 1 Day 15) divided by AUC0-12h during the initial dosing interval (Cycle 1 Day 1).
| ratio | Part 2: Tazemetostat |
|---|---|
| Part 2: Least Squares Geometric Mean Ratio of Observed Accumulation Ratio of AUC0-12h for Tazemetostat | 0.816 (0.638 to 1.04) |
Blood samples were collected at specified timepoints. Cmax accumulation ratio was assessed using non-compartmental data analysis method. Cmax accumulation ratio was calculated as the ratio of Cmax at steady state (Cycle 1 Day 15) divided by Cmax during the initial dosing interval (Cycle 1 Day 1).
| ratio | Part 2: Tazemetostat |
|---|---|
| Part 2: Least Squares Geometric Mean Ratio of Cmax Accumulation Ratio for Tazemetostat | 0.828 (0.635 to 1.08) |
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
| ratio | Part 2: Tazemetostat + Rifampin |
|---|---|
| Part 2: Least Squares Geometric Mean Ratio of AUC0-12h After Tazemetostat at Steady State With Rifampin | 0.163 (0.128 to 0.208) |
Blood samples were collected at specified timepoints. Drug-drug interaction was assessed using ANOVA.
| ratio | Part 2: Tazemetostat + Rifampin |
|---|---|
| Part 2: Least Squares Geometric Mean Ratio of Cmax After Tazemetostat at Steady State With Rifampin | 0.164 (0.122 to 0.219) |
Collected over Treatment-emergent adverse events and all-cause mortality were reported from the first dose of study treatment (Day 1) through 30 days after the end of study treatment (approximately 33 months).. Non-serious events are listed at a 5% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Part 1: Tazemetostat + Itraconazole | 10/21 (47.6%) | 8/21 (38.1%) | 19/21 (90.5%) |
| Part 2: Tazemetostat + Rifampin | 3/21 (14.3%) | 9/21 (42.9%) | 20/21 (95.2%) |
| Event | Part 1: Tazemetostat + Itraconazole | Part 2: Tazemetostat + Rifampin |
|---|---|---|
| Pericardial effusionCardiac disorders | 2/21 | 0/21 |
| SepsisInfections and infestations | 0/21 | 2/21 |
| Acute respiratory failureRespiratory, thoracic and mediastinal disorders | 2/21 | 0/21 |
| ColitisGastrointestinal disorders | 1/21 | 0/21 |
| DiarrhoeaGastrointestinal disorders | 0/21 | 1/21 |
| VomitingGastrointestinal disorders | 0/21 | 1/21 |
| Oedema peripheralGeneral disorders | 0/21 | 1/21 |
| PainGeneral disorders | 0/21 | 1/21 |
| PneumoniaInfections and infestations | 1/21 | 1/21 |
| Abdominal infectionInfections and infestations | 1/21 | 0/21 |
| Event | Part 1: Tazemetostat + Itraconazole | Part 2: Tazemetostat + Rifampin |
|---|---|---|
| FatigueGeneral disorders | 6/21 | 9/21 |
| DiarrhoeaGastrointestinal disorders | 2/21 | 7/21 |
| Decreased appetiteMetabolism and nutrition disorders | 7/21 | 4/21 |
| DyspnoeaRespiratory, thoracic and mediastinal disorders | 7/21 | 2/21 |
| AnaemiaBlood and lymphatic system disorders | 6/21 | 5/21 |
| NauseaGastrointestinal disorders | 6/21 | 5/21 |
| CoughRespiratory, thoracic and mediastinal disorders | 2/21 | 6/21 |
| ConstipationGastrointestinal disorders | 5/21 | 5/21 |
| Abdominal painGastrointestinal disorders | 4/21 | 1/21 |
| Oedema peripheralGeneral disorders | 4/21 | 1/21 |
The Enrolled population included all participants who signed informed consent and met all screening criteria.
| Age, Continuous(years) | Part 1: Tazemetostat + Itraconazole | Part 2: Tazemetostat + Rifampin | Total |
|---|---|---|---|
| Mean | 60.9 ± 13.45 | 60.1 ± 13.05 | 60.5 ± 13.09 |
| Sex: Female, Male(Participants) | Part 1: Tazemetostat + Itraconazole | Part 2: Tazemetostat + Rifampin | Total |
|---|---|---|---|
| Female | 8 | 13 | 21 |
| Male | 13 | 8 | 21 |
| Ethnicity (NIH/OMB)(Participants) | Part 1: Tazemetostat + Itraconazole | Part 2: Tazemetostat + Rifampin | Total |
|---|---|---|---|
| Hispanic or Latino | 0 | 0 | 0 |
| Not Hispanic or Latino | 19 | 18 | 37 |
| Unknown or Not Reported | 2 | 3 | 5 |
| Race/Ethnicity, Customized(Participants) | Part 1: Tazemetostat + Itraconazole | Part 2: Tazemetostat + Rifampin | Total |
|---|---|---|---|
| White | 18 | 12 | 30 |
| Asian | 2 | 3 | 5 |
| Black or African American | 0 | 2 | 2 |
| American Indian or Alaska Native | 0 | 0 | 0 |
| Native Hawaiian or Other Pacific Islander | 0 | 0 | 0 |
| Not reported/Other | 1 | 4 | 5 |
PDFs hosted by the registry, ClinicalTrials.gov.
Plan to share: No
Ran from Apr 2020 to primary completion in Apr 2023, 35 months.
Results were first posted in Aug 2024, 1 year 4 months after primary completion.
Of 95 industry-sponsored phase 1 interventional studies under Hematologic Neoplasms, half reached primary completion within 43 months of starting (the median), counting those still running; a quarter within 30 and three quarters within 78. This study's 35 months is below that.
Counting every sponsor, half of 159 studies reached it within 51 months; a quarter within 28 and three quarters within 78.
How these figures are worked out, and which studies are left out of them.
This study is completed, as verified in Feb 2025. You cannot join it, but the record below documents what was studied.
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Studies of the drugs tested here: Itraconazole · Rifampin