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NCT01915498 · OUTCOME

Phase 1: Apparent Terminal Phase Half-life (t½) of AGI-16903 After a Single Oral Dose of Enasidenib on Day -3

Phase 1/2 Study of Enasidenib (AG-221) in Adults With Advanced Hematologic Malignancies With an Isocitrate Dehydrogenase Isoform 2 (IDH2) Mutation · Source last updated 2024-10-22

Results reported by the registry submitting party. Population, time horizon, units and missing values must be read together.

Measure
GEOMETRIC_MEAN
Unit
hours
Interval / dispersion
Geometric Coefficient of Variation
Time frame
Day -3 prior to the single dose of enasidenib and at 0.5, 1, 2, 3, 4, 6, 8, 10, 24, 48, and 72 hours post-dose.

What was measured

The first 3 participants enrolled in each cohort of the dose escalation phase and the first 15 participants enrolled in each arm of Phase 1 Expansion received a single dose of enasidenib three days prior to starting the 28-day dosing regimen (Day -3). AGI-16903 is a primary metabolite of enasidenib. Plasma AGI-16903 was measured using validated liquid chromatography-mass spectrometry methods (LC-MS/MS). The lower limit of quantification (LLOQ) in plasma was 1.00 ng/mL. t1/2 was not calculated when the terminal elimination rate constant (λz) was not estimable.

Analysis population: Participants who received 1 dose of enasidenib on Day -3 with sufficient data to determine PK parameters. Participants who received 2 doses on Day -3 or who received the incorrect dose were excluded. Participants in the Phase 1 Escalation BID and QD cohorts and Phase 1 Expansion cohorts were were grouped by dose for Day -3 analyses.

Groups in this outcome

Enasidenib 30 mg

Participants received a single oral dose of enasidenib 30 mg on Day -3.

Enasidenib 50 mg

Participants received a single oral dose of enasidenib 50 mg on Day -3.

Enasidenib 75 mg

Participants received a single oral dose of enasidenib 75 mg on Day -3.

Enasidenib 100 mg

Participants received a single oral dose of enasidenib 100 mg on Day -3.

Enasidenib 150 mg

Participants received a single oral dose of enasidenib 150 mg on Day -3.

Enasidenib 200 mg

Participants received a single oral dose of enasidenib 200 mg on Day -3.

Enasidenib 300 mg

Participants received a single oral dose of enasidenib 300 mg on Day -3.

Enasidenib 450 mg

Participants received a single oral dose of enasidenib 450 mg on Day -3.

Enasidenib 650 mg

Participants received a single oral dose of enasidenib 650 mg on Day -3.

Group identifiers and denominators belong to this outcome only. They may differ in another outcome or in safety reporting.

Analysis denominator · Participants

GroupSource count
Enasidenib 30 mg1
Enasidenib 50 mg4
Enasidenib 75 mg2
Enasidenib 100 mg7
Enasidenib 150 mg1
Enasidenib 200 mg0
Enasidenib 300 mg0
Enasidenib 450 mg0
Enasidenib 650 mg0

Reported measurements

Source class 1
Values in hours · Interval/dispersion: Geometric Coefficient of Variation
GroupValueSpreadLowerUpperComment
Enasidenib 30 mg18.9NANot reportedNot reportedPercent coefficient of variation could not be calculated due to small sample size
Enasidenib 50 mg46.9125.7Not reportedNot reportedNot reported
Enasidenib 75 mg29.0NANot reportedNot reportedPercent coefficient of variation could not be calculated due to small sample size
Enasidenib 100 mg69.2161.0Not reportedNot reportedNot reported
Enasidenib 150 mg106.4NANot reportedNot reportedPercent coefficient of variation could not be calculated due to small sample size
Complete source fields
classes
  1. categories
    1. measurements
      1. comment
        Percent coefficient of variation could not be calculated due to small sample size
        group Id
        OG000
        spread
        NA
        value
        18.9
      2. group Id
        OG001
        spread
        125.7
        value
        46.9
      3. comment
        Percent coefficient of variation could not be calculated due to small sample size
        group Id
        OG002
        spread
        NA
        value
        29.0
      4. group Id
        OG003
        spread
        161.0
        value
        69.2
      5. comment
        Percent coefficient of variation could not be calculated due to small sample size
        group Id
        OG004
        spread
        NA
        value
        106.4
denoms
  1. counts
    1. group Id
      OG000
      value
      1
    2. group Id
      OG001
      value
      4
    3. group Id
      OG002
      value
      2
    4. group Id
      OG003
      value
      7
    5. group Id
      OG004
      value
      1
    6. group Id
      OG005
      value
      0
    7. group Id
      OG006
      value
      0
    8. group Id
      OG007
      value
      0
    9. group Id
      OG008
      value
      0
    units
    Participants
description
The first 3 participants enrolled in each cohort of the dose escalation phase and the first 15 participants enrolled in each arm of Phase 1 Expansion received a single dose of enasidenib three days prior to starting the 28-day dosing regimen (Day -3). AGI-16903 is a primary metabolite of enasidenib. Plasma AGI-16903 was measured using validated liquid chromatography-mass spectrometry methods (LC-MS/MS). The lower limit of quantification (LLOQ) in plasma was 1.00 ng/mL. t1/2 was not calculated when the terminal elimination rate constant (λz) was not estimable.
dispersion Type
Geometric Coefficient of Variation
groups
  1. description
    Participants received a single oral dose of enasidenib 30 mg on Day -3.
    id
    OG000
    title
    Enasidenib 30 mg
  2. description
    Participants received a single oral dose of enasidenib 50 mg on Day -3.
    id
    OG001
    title
    Enasidenib 50 mg
  3. description
    Participants received a single oral dose of enasidenib 75 mg on Day -3.
    id
    OG002
    title
    Enasidenib 75 mg
  4. description
    Participants received a single oral dose of enasidenib 100 mg on Day -3.
    id
    OG003
    title
    Enasidenib 100 mg
  5. description
    Participants received a single oral dose of enasidenib 150 mg on Day -3.
    id
    OG004
    title
    Enasidenib 150 mg
  6. description
    Participants received a single oral dose of enasidenib 200 mg on Day -3.
    id
    OG005
    title
    Enasidenib 200 mg
  7. description
    Participants received a single oral dose of enasidenib 300 mg on Day -3.
    id
    OG006
    title
    Enasidenib 300 mg
  8. description
    Participants received a single oral dose of enasidenib 450 mg on Day -3.
    id
    OG007
    title
    Enasidenib 450 mg
  9. description
    Participants received a single oral dose of enasidenib 650 mg on Day -3.
    id
    OG008
    title
    Enasidenib 650 mg
param Type
GEOMETRIC_MEAN
population Description
Participants who received 1 dose of enasidenib on Day -3 with sufficient data to determine PK parameters. Participants who received 2 doses on Day -3 or who received the incorrect dose were excluded. Participants in the Phase 1 Escalation BID and QD cohorts and Phase 1 Expansion cohorts were were grouped by dose for Day -3 analyses.
reporting Status
POSTED
time Frame
Day -3 prior to the single dose of enasidenib and at 0.5, 1, 2, 3, 4, 6, 8, 10, 24, 48, and 72 hours post-dose.
title
Phase 1: Apparent Terminal Phase Half-life (t½) of AGI-16903 After a Single Oral Dose of Enasidenib on Day -3
type
SECONDARY
unit Of Measure
hours

Download exact source JSON → · Snapshot ctgov-results-191f4516d4760045304b24a0

Preserved source evidence · Not medical advice