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NCT01915498 · OUTCOME

Phase 1: Time of Minimum Observed Concentration Over 72 Hours Postdose (Tmin) of 2-HG 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
MEDIAN
Unit
hours
Interval / dispersion
Full Range
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). Plasma 2-HG was measured using qualified LC-MS/MS, the LLOQ was 30.0 ng/mL.

Analysis population: Participants who received 1 dose of enasidenib on Day -3 with sufficient data to determine PD 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 mg57
Enasidenib 150 mg8
Enasidenib 200 mg11
Enasidenib 300 mg4
Enasidenib 450 mg2
Enasidenib 650 mg1

Reported measurements

Source class 1
Values in hours · Interval/dispersion: Full Range
GroupValueSpreadLowerUpperComment
Enasidenib 30 mg35.78Not reported24.0072.38Not reported
Enasidenib 50 mg8.00Not reported1.1372.42Not reported
Enasidenib 75 mg23.92Not reported2.9271.42Not reported
Enasidenib 100 mg48.00Not reported0.5073.58Not reported
Enasidenib 150 mg48.20Not reported1.0072.30Not reported
Enasidenib 200 mg48.70Not reported6.0772.45Not reported
Enasidenib 300 mg48.10Not reported24.4272.17Not reported
Enasidenib 450 mg30.79Not reported13.3348.25Not reported
Enasidenib 650 mg8.17Not reported8.178.17Not reported
Complete source fields
classes
  1. categories
    1. measurements
      1. group Id
        OG000
        lower Limit
        24.00
        upper Limit
        72.38
        value
        35.78
      2. group Id
        OG001
        lower Limit
        1.13
        upper Limit
        72.42
        value
        8.00
      3. group Id
        OG002
        lower Limit
        2.92
        upper Limit
        71.42
        value
        23.92
      4. group Id
        OG003
        lower Limit
        0.50
        upper Limit
        73.58
        value
        48.00
      5. group Id
        OG004
        lower Limit
        1.00
        upper Limit
        72.30
        value
        48.20
      6. group Id
        OG005
        lower Limit
        6.07
        upper Limit
        72.45
        value
        48.70
      7. group Id
        OG006
        lower Limit
        24.42
        upper Limit
        72.17
        value
        48.10
      8. group Id
        OG007
        lower Limit
        13.33
        upper Limit
        48.25
        value
        30.79
      9. group Id
        OG008
        lower Limit
        8.17
        upper Limit
        8.17
        value
        8.17
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
      57
    5. group Id
      OG004
      value
      8
    6. group Id
      OG005
      value
      11
    7. group Id
      OG006
      value
      4
    8. group Id
      OG007
      value
      2
    9. group Id
      OG008
      value
      1
    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). Plasma 2-HG was measured using qualified LC-MS/MS, the LLOQ was 30.0 ng/mL.
dispersion Type
Full Range
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
MEDIAN
population Description
Participants who received 1 dose of enasidenib on Day -3 with sufficient data to determine PD 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: Time of Minimum Observed Concentration Over 72 Hours Postdose (Tmin) of 2-HG After a Single Oral Dose of Enasidenib on Day -3
type
SECONDARY
unit Of Measure
hours

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Preserved source evidence · Not medical advice