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The Effect of Tesetaxel on the QTc Interval and the Effect of Food, Itraconazole, and Rifampin on Tesetaxel Pharmacokinetics in Patients With Advanced Solid Tumors

Phase 1
Terminated
Conditions
Advanced Solid Tumors
Interventions
Registration Number
NCT04312282
Lead Sponsor
Odonate Therapeutics, Inc.
Brief Summary

This is a 3-cohort, multicenter, Phase 1 study of the effect of tesetaxel, an investigational, orally administered taxane, on the corrected QT (QTc) interval and the potential effect of food, a cytochrome P450 (CYP) 3A inhibitor (itraconazole), and a CYP3A inducer (rifampin) on tesetaxel pharmacokinetics (PK) in adult patients with advanced solid tumors.

Detailed Description

Cohort 1:

Cohort 1 is a 2-period, 2-sequence, crossover study designed to assess the effect of food on the PK of tesetaxel and tesetaxel metabolites. Patients were randomized in a 1:2 ratio to receive tesetaxel on Day 1 of two 21-day cycles under fed and fasting conditions in one of two opposing sequences (Sequence 1A and Sequence 1B).

Cohort 2:

Cohort 2 is a 2-period, single-sequence, crossover study designed to assess the potential PK drug-drug interaction (DDI) of a strong CYP3A inhibitor (itraconazole) on tesetaxel and tesetaxel metabolites. Patients receive tesetaxel during Cycle 1 followed by a reduced dose of tesetaxel plus itraconazole during Cycle 2.

Cohort 3:

Cohort 3 is a 2-period, single-sequence, crossover study designed to assess the potential PK DDI of a strong CYP3A inducer (rifampin) on tesetaxel and tesetaxel metabolites. Patients receive tesetaxel during Cycle 1 followed by tesetaxel plus rifampin during Cycle 2.

Patients in all cohorts also participate in a study designed to assess the effect of tesetaxel and tesetaxel metabolites on cardiac repolarization as measured by the change from baseline in the QTc interval over the first cycle of treatment. Patients who are tolerating and benefitting from treatment with tesetaxel have the opportunity to continue onto an optional treatment extension.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
93
Inclusion Criteria
  • Female or male patients at least 18 years of age
  • Histologically or cytologically confirmed solid tumor
  • Eastern Cooperative Oncology Group (ECOG) performance status 0, 1 or 2
  • Adequate cardiac conduction by ECG
  • Adequate bone marrow, hepatic, and renal function
Exclusion Criteria
  • Presence of risk factors for QTc prolongation

  • Presence of neuropathy Grade > 1

  • Anticancer treatment ≤ 14 days prior to randomization

  • Major surgery ≤ 28 days prior to randomization

  • Less than 2 weeks or 5 plasma half-lives (whichever is greater) since last use of:

    • A moderate or strong inhibitor or inducer of CYP3A
    • A CYP3A substrate with a narrow therapeutic range or that is contraindicated with either itraconazole or rifampin

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Cohort 1, Sequence 1B: Fasted then fedTesetaxelCycle 1: Tesetaxel on Day 1 of a 21-day cycle under fasted conditions Cycle 2: Tesetaxel on Day 1 of a 21-day cycle under fed conditions
Cohort 2: Tesetaxel plus itraconazoleTesetaxelCycle 1: Tesetaxel on Day 1 of a 21-day cycle Cycle 2: Tesetaxel on Day 1 of a 21-day cycle and itraconazole on Day -3 through Day 14 of a 21-day cycle
Cohort 3: Tesetaxel plus rifampinRifampinCycle 1: Tesetaxel on Day 1 of a 21-day cycle Cycle 2: Tesetaxel on Day 1 of a 21-day cycle and rifampin on Day -6 through Day 14 of a 21-day cycle
Cohort 1, Sequence 1A: Fed then fastedTesetaxelCycle 1: Tesetaxel on Day 1 of a 21-day cycle under fed conditions Cycle 2: Tesetaxel on Day 1 of a 21-day cycle under fasted conditions
Cohort 2: Tesetaxel plus itraconazoleItraconazoleCycle 1: Tesetaxel on Day 1 of a 21-day cycle Cycle 2: Tesetaxel on Day 1 of a 21-day cycle and itraconazole on Day -3 through Day 14 of a 21-day cycle
Cohort 3: Tesetaxel plus rifampinTesetaxelCycle 1: Tesetaxel on Day 1 of a 21-day cycle Cycle 2: Tesetaxel on Day 1 of a 21-day cycle and rifampin on Day -6 through Day 14 of a 21-day cycle
Primary Outcome Measures
NameTimeMethod
All Cohorts: The change from baseline in Fridericia's corrected QT (ΔQTcF) intervalApproximately 3 weeks
Cohort 2: AUC from 0 to 336 hours (AUC0-336h) for tesetaxel in the presence and absence of itraconazoleApproximately 6 weeks
Cohort 1, Sequences 1A and 1B: Maximum observed plasma concentration (Cmax) for tesetaxel under fed and fasted conditionsApproximately 6 weeks
Cohort 1, Sequences 1A and 1B: Area under the plasma concentration-time curve from 0 to the last measurable plasma concentration (AUC0-t) for tesetaxel under fed and fasted conditionsApproximately 6 weeks
Cohort 2: Cmax for tesetaxel in the presence and absence of itraconazoleApproximately 6 weeks
Cohort 3: AUC0-336h for tesetaxel in the presence and absence of rifampinApproximately 6 weeks
Cohort 3: Cmax for tesetaxel in the presence and absence of rifampinApproximately 6 weeks
Secondary Outcome Measures
NameTimeMethod
All Cohorts: Cmax for tesetaxel metabolitesApproximately 6 weeks
All Cohorts: Treatment-emergent adverse events (TEAEs), including serious adverse events (SAEs)Baseline through 30 days after last administration of Study treatment
All Cohorts: AUC for tesetaxel metabolitesApproximately 6 weeks

Trial Locations

Locations (3)

NEXT Oncology

🇺🇸

San Antonio, Texas, United States

Mary Crowley Cancer Research

🇺🇸

Dallas, Texas, United States

START Midwest

🇺🇸

Grand Rapids, Michigan, United States

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