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NCT01915498 · OUTCOME

Phase 1: AUC From Time Zero to 24 Hours Postdose (AUC0-24) 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
ng*h/mL
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, and 24 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. Area under the plasma concentration-time curve from time 0 to 24 hours post-dose (AUC0-24) was calculated using the linear trapezoidal rule.

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 mg4
Enasidenib 50 mg9
Enasidenib 75 mg9
Enasidenib 100 mg53
Enasidenib 150 mg8
Enasidenib 200 mg11
Enasidenib 300 mg6
Enasidenib 450 mg2
Enasidenib 650 mg0

Reported measurements

Source class 1
Values in ng*h/mL · Interval/dispersion: Geometric Coefficient of Variation
GroupValueSpreadLowerUpperComment
Enasidenib 30 mg47480.4Not reportedNot reportedNot reported
Enasidenib 50 mg777111.7Not reportedNot reportedNot reported
Enasidenib 75 mg123854.4Not reportedNot reportedNot reported
Enasidenib 100 mg122271.4Not reportedNot reportedNot reported
Enasidenib 150 mg212854.2Not reportedNot reportedNot reported
Enasidenib 200 mg215975.4Not reportedNot reportedNot reported
Enasidenib 300 mg247751.5Not reportedNot reportedNot reported
Enasidenib 450 mg2274NANot reportedNot reportedPercent coefficient of variation could not be calculated due to small sample size
Complete source fields
classes
  1. categories
    1. measurements
      1. group Id
        OG000
        spread
        80.4
        value
        474
      2. group Id
        OG001
        spread
        111.7
        value
        777
      3. group Id
        OG002
        spread
        54.4
        value
        1238
      4. group Id
        OG003
        spread
        71.4
        value
        1222
      5. group Id
        OG004
        spread
        54.2
        value
        2128
      6. group Id
        OG005
        spread
        75.4
        value
        2159
      7. group Id
        OG006
        spread
        51.5
        value
        2477
      8. comment
        Percent coefficient of variation could not be calculated due to small sample size
        group Id
        OG007
        spread
        NA
        value
        2274
denoms
  1. counts
    1. group Id
      OG000
      value
      4
    2. group Id
      OG001
      value
      9
    3. group Id
      OG002
      value
      9
    4. group Id
      OG003
      value
      53
    5. group Id
      OG004
      value
      8
    6. group Id
      OG005
      value
      11
    7. group Id
      OG006
      value
      6
    8. group Id
      OG007
      value
      2
    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. Area under the plasma concentration-time curve from time 0 to 24 hours post-dose (AUC0-24) was calculated using the linear trapezoidal rule.
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, and 24 hours post-dose.
title
Phase 1: AUC From Time Zero to 24 Hours Postdose (AUC0-24) of AGI-16903 After a Single Oral Dose of Enasidenib on Day -3
type
SECONDARY
unit Of Measure
ng*h/mL

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Preserved source evidence · Not medical advice