NCT02294461 · OUTCOME
Observed Plasma Concentration in Predose Samples Obtained During Multiple-dose Administration of Minimum Concentration (Plasma Concentration at Pre Dose) (Cmin) Enzalutamide, M1,M2 and Enzalutamide Plus M2
An Asian Study to Evaluate Efficacy and Safety of Oral Enzalutamide in Progressive Metastatic Prostate Cancer Participants · Source last updated 2025-10-24
Results reported by the registry submitting party. Population, time horizon, units and missing values must be read together.
- Measure
- MEAN
- Unit
- μg/mL
- Interval / dispersion
- Standard Deviation
- Time frame
- From the date of randomization up to Days 2, 3, 8, 22, 29, 43, 57, 85, 86, 113, 141 and 169
What was measured
N is the number of participants with available data at this time point.
Analysis population: The Pharmacokinetic Analysis Set (PKAS) population consisted of all participants who received at least 1 dose of study drug and who provided blood samples for drug concentrations at least 1 time point.
Groups in this outcome
Enzalutamide
Participants received 160 mg of enzalutamide orally once a day during double blind period until PSA progression and radiographic disease progression were centrally confirmed and 1 of the following 2 events became applicable to the participants: (1) initiation of cytotoxic chemotherapy or (2) initiation of an investigational agent for treatment of prostate cancer (up to 29.4 months). Eligible participants who received enzalutamide during double blind and who provided consent to take part in open-label period continued to receive 160 mg of enzalutamide in open-label period orally once a day until PSA progression and radiographic disease progression were centrally confirmed and 1 of the following 2 events became applicable to the participants: (1) initiation of cytotoxic chemotherapy or (2) initiation of an investigational agent for treatment of prostate cancer (up to 54.3 months).
M1- Carboxylic Acid Metabolite
Inactive metabolite.
M2- N-Desmethyl Enzalutamide
N-desmethyl enzalutamide (active metabolite).
Enzalutamide Plus M2
Active metabolite.
Group identifiers and denominators belong to this outcome only. They may differ in another outcome or in safety reporting.
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 12 |
|---|
| M1- Carboxylic Acid Metabolite | 12 |
|---|
| M2- N-Desmethyl Enzalutamide | 12 |
|---|
| Enzalutamide Plus M2 | 12 |
|---|
Reported measurements
Day 2 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 12 |
|---|
| M1- Carboxylic Acid Metabolite | 12 |
|---|
| M2- N-Desmethyl Enzalutamide | 12 |
|---|
| Enzalutamide Plus M2 | 12 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 1.65 | 0.343 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 0.111 | 0.0801 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 0.164 | 0.0942 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 1.82 | 0.363 | Not reported | Not reported | Not reported |
|---|
Day 3 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 12 |
|---|
| M1- Carboxylic Acid Metabolite | 12 |
|---|
| M2- N-Desmethyl Enzalutamide | 12 |
|---|
| Enzalutamide Plus M2 | 12 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 3.29 | 1.16 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 0.302 | 0.256 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 0.367 | 0.188 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 3.66 | 1.24 | Not reported | Not reported | Not reported |
|---|
Day 8 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 12 |
|---|
| M1- Carboxylic Acid Metabolite | 12 |
|---|
| M2- N-Desmethyl Enzalutamide | 12 |
|---|
| Enzalutamide Plus M2 | 12 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 9.39 | 2.07 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 1.21 | 0.923 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 1.94 | 0.983 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 11.3 | 2.62 | Not reported | Not reported | Not reported |
|---|
Day 22 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 11 |
|---|
| M1- Carboxylic Acid Metabolite | 11 |
|---|
| M2- N-Desmethyl Enzalutamide | 11 |
|---|
| Enzalutamide Plus M2 | 11 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.6 | 2.37 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 6.09 | 8.26 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 8.34 | 2.74 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 25.9 | 3.25 | Not reported | Not reported | Not reported |
|---|
Day 29 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 12 |
|---|
| M1- Carboxylic Acid Metabolite | 12 |
|---|
| M2- N-Desmethyl Enzalutamide | 12 |
|---|
| Enzalutamide Plus M2 | 12 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 19.6 | 4.00 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 8.16 | 12.5 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 10.9 | 3.72 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 30.5 | 5.47 | Not reported | Not reported | Not reported |
|---|
Day 43 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 11 |
|---|
| M1- Carboxylic Acid Metabolite | 11 |
|---|
| M2- N-Desmethyl Enzalutamide | 11 |
|---|
| Enzalutamide Plus M2 | 11 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.0 | 4.13 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 12.5 | 22.1 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 14.0 | 3.99 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 31.0 | 5.82 | Not reported | Not reported | Not reported |
|---|
Day 57 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 11 |
|---|
| M1- Carboxylic Acid Metabolite | 11 |
|---|
| M2- N-Desmethyl Enzalutamide | 11 |
|---|
| Enzalutamide Plus M2 | 11 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.8 | 3.09 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 18.4 | 28.2 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 14.7 | 3.88 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 32.5 | 4.57 | Not reported | Not reported | Not reported |
|---|
Day 85 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 11 |
|---|
| M1- Carboxylic Acid Metabolite | 11 |
|---|
| M2- N-Desmethyl Enzalutamide | 11 |
|---|
| Enzalutamide Plus M2 | 11 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.9 | 3.19 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 6.33 | 2.95 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 14.9 | 3.67 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 32.8 | 5.10 | Not reported | Not reported | Not reported |
|---|
Day 86 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 10 |
|---|
| M1- Carboxylic Acid Metabolite | 10 |
|---|
| M2- N-Desmethyl Enzalutamide | 10 |
|---|
| Enzalutamide Plus M2 | 10 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.6 | 3.09 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 6.09 | 3.07 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 13.7 | 2.91 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 31.2 | 4.00 | Not reported | Not reported | Not reported |
|---|
Day 113 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 7 |
|---|
| M1- Carboxylic Acid Metabolite | 7 |
|---|
| M2- N-Desmethyl Enzalutamide | 7 |
|---|
| Enzalutamide Plus M2 | 7 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.5 | 4.14 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 17.5 | 33.1 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 15.0 | 3.21 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 32.5 | 3.72 | Not reported | Not reported | Not reported |
|---|
Day 141 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 6 |
|---|
| M1- Carboxylic Acid Metabolite | 6 |
|---|
| M2- N-Desmethyl Enzalutamide | 6 |
|---|
| Enzalutamide Plus M2 | 6 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.3 | 3.73 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 5.52 | 2.10 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 14.3 | 3.90 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 31.6 | 4.70 | Not reported | Not reported | Not reported |
|---|
Day 169 predose
Analysis denominator · Participants
| Group | Source count |
|---|
| Enzalutamide | 4 |
|---|
| M1- Carboxylic Acid Metabolite | 4 |
|---|
| M2- N-Desmethyl Enzalutamide | 4 |
|---|
| Enzalutamide Plus M2 | 4 |
|---|
Values in μg/mL · Interval/dispersion: Standard Deviation| Group | Value | Spread | Lower | Upper | Comment |
|---|
| Enzalutamide | 17.2 | 5.55 | Not reported | Not reported | Not reported |
|---|
| M1- Carboxylic Acid Metabolite | 5.09 | 2.27 | Not reported | Not reported | Not reported |
|---|
| M2- N-Desmethyl Enzalutamide | 14.0 | 4.80 | Not reported | Not reported | Not reported |
|---|
| Enzalutamide Plus M2 | 31.2 | 5.02 | Not reported | Not reported | Not reported |
|---|
Complete source fields
- classes
- categories
- measurements
- group Id
- OG000
- spread
- 0.343
- value
- 1.65
- group Id
- OG001
- spread
- 0.0801
- value
- 0.111
- group Id
- OG002
- spread
- 0.0942
- value
- 0.164
- group Id
- OG003
- spread
- 0.363
- value
- 1.82
- denoms
- counts
- group Id
- OG000
- value
- 12
- group Id
- OG001
- value
- 12
- group Id
- OG002
- value
- 12
- group Id
- OG003
- value
- 12
- units
- Participants
- title
- Day 2 predose
- categories
- measurements
- group Id
- OG000
- spread
- 1.16
- value
- 3.29
- group Id
- OG001
- spread
- 0.256
- value
- 0.302
- group Id
- OG002
- spread
- 0.188
- value
- 0.367
- group Id
- OG003
- spread
- 1.24
- value
- 3.66
- denoms
- counts
- group Id
- OG000
- value
- 12
- group Id
- OG001
- value
- 12
- group Id
- OG002
- value
- 12
- group Id
- OG003
- value
- 12
- units
- Participants
- title
- Day 3 predose
- categories
- measurements
- group Id
- OG000
- spread
- 2.07
- value
- 9.39
- group Id
- OG001
- spread
- 0.923
- value
- 1.21
- group Id
- OG002
- spread
- 0.983
- value
- 1.94
- group Id
- OG003
- spread
- 2.62
- value
- 11.3
- denoms
- counts
- group Id
- OG000
- value
- 12
- group Id
- OG001
- value
- 12
- group Id
- OG002
- value
- 12
- group Id
- OG003
- value
- 12
- units
- Participants
- title
- Day 8 predose
- categories
- measurements
- group Id
- OG000
- spread
- 2.37
- value
- 17.6
- group Id
- OG001
- spread
- 8.26
- value
- 6.09
- group Id
- OG002
- spread
- 2.74
- value
- 8.34
- group Id
- OG003
- spread
- 3.25
- value
- 25.9
- denoms
- counts
- group Id
- OG000
- value
- 11
- group Id
- OG001
- value
- 11
- group Id
- OG002
- value
- 11
- group Id
- OG003
- value
- 11
- units
- Participants
- title
- Day 22 predose
- categories
- measurements
- group Id
- OG000
- spread
- 4.00
- value
- 19.6
- group Id
- OG001
- spread
- 12.5
- value
- 8.16
- group Id
- OG002
- spread
- 3.72
- value
- 10.9
- group Id
- OG003
- spread
- 5.47
- value
- 30.5
- denoms
- counts
- group Id
- OG000
- value
- 12
- group Id
- OG001
- value
- 12
- group Id
- OG002
- value
- 12
- group Id
- OG003
- value
- 12
- units
- Participants
- title
- Day 29 predose
- categories
- measurements
- group Id
- OG000
- spread
- 4.13
- value
- 17.0
- group Id
- OG001
- spread
- 22.1
- value
- 12.5
- group Id
- OG002
- spread
- 3.99
- value
- 14.0
- group Id
- OG003
- spread
- 5.82
- value
- 31.0
- denoms
- counts
- group Id
- OG000
- value
- 11
- group Id
- OG001
- value
- 11
- group Id
- OG002
- value
- 11
- group Id
- OG003
- value
- 11
- units
- Participants
- title
- Day 43 predose
- categories
- measurements
- group Id
- OG000
- spread
- 3.09
- value
- 17.8
- group Id
- OG001
- spread
- 28.2
- value
- 18.4
- group Id
- OG002
- spread
- 3.88
- value
- 14.7
- group Id
- OG003
- spread
- 4.57
- value
- 32.5
- denoms
- counts
- group Id
- OG000
- value
- 11
- group Id
- OG001
- value
- 11
- group Id
- OG002
- value
- 11
- group Id
- OG003
- value
- 11
- units
- Participants
- title
- Day 57 predose
- categories
- measurements
- group Id
- OG000
- spread
- 3.19
- value
- 17.9
- group Id
- OG001
- spread
- 2.95
- value
- 6.33
- group Id
- OG002
- spread
- 3.67
- value
- 14.9
- group Id
- OG003
- spread
- 5.10
- value
- 32.8
- denoms
- counts
- group Id
- OG000
- value
- 11
- group Id
- OG001
- value
- 11
- group Id
- OG002
- value
- 11
- group Id
- OG003
- value
- 11
- units
- Participants
- title
- Day 85 predose
- categories
- measurements
- group Id
- OG000
- spread
- 3.09
- value
- 17.6
- group Id
- OG001
- spread
- 3.07
- value
- 6.09
- group Id
- OG002
- spread
- 2.91
- value
- 13.7
- group Id
- OG003
- spread
- 4.00
- value
- 31.2
- denoms
- counts
- group Id
- OG000
- value
- 10
- group Id
- OG001
- value
- 10
- group Id
- OG002
- value
- 10
- group Id
- OG003
- value
- 10
- units
- Participants
- title
- Day 86 predose
- categories
- measurements
- group Id
- OG000
- spread
- 4.14
- value
- 17.5
- group Id
- OG001
- spread
- 33.1
- value
- 17.5
- group Id
- OG002
- spread
- 3.21
- value
- 15.0
- group Id
- OG003
- spread
- 3.72
- value
- 32.5
- denoms
- counts
- group Id
- OG000
- value
- 7
- group Id
- OG001
- value
- 7
- group Id
- OG002
- value
- 7
- group Id
- OG003
- value
- 7
- units
- Participants
- title
- Day 113 predose
- categories
- measurements
- group Id
- OG000
- spread
- 3.73
- value
- 17.3
- group Id
- OG001
- spread
- 2.10
- value
- 5.52
- group Id
- OG002
- spread
- 3.90
- value
- 14.3
- group Id
- OG003
- spread
- 4.70
- value
- 31.6
- denoms
- counts
- group Id
- OG000
- value
- 6
- group Id
- OG001
- value
- 6
- group Id
- OG002
- value
- 6
- group Id
- OG003
- value
- 6
- units
- Participants
- title
- Day 141 predose
- categories
- measurements
- group Id
- OG000
- spread
- 5.55
- value
- 17.2
- group Id
- OG001
- spread
- 2.27
- value
- 5.09
- group Id
- OG002
- spread
- 4.80
- value
- 14.0
- group Id
- OG003
- spread
- 5.02
- value
- 31.2
- denoms
- counts
- group Id
- OG000
- value
- 4
- group Id
- OG001
- value
- 4
- group Id
- OG002
- value
- 4
- group Id
- OG003
- value
- 4
- units
- Participants
- title
- Day 169 predose
- denoms
- counts
- group Id
- OG000
- value
- 12
- group Id
- OG001
- value
- 12
- group Id
- OG002
- value
- 12
- group Id
- OG003
- value
- 12
- units
- Participants
- description
- N is the number of participants with available data at this time point.
- dispersion Type
- Standard Deviation
- groups
- description
- Participants received 160 mg of enzalutamide orally once a day during double blind period until PSA progression and radiographic disease progression were centrally confirmed and 1 of the following 2 events became applicable to the participants: (1) initiation of cytotoxic chemotherapy or (2) initiation of an investigational agent for treatment of prostate cancer (up to 29.4 months). Eligible participants who received enzalutamide during double blind and who provided consent to take part in open-label period continued to receive 160 mg of enzalutamide in open-label period orally once a day until PSA progression and radiographic disease progression were centrally confirmed and 1 of the following 2 events became applicable to the participants: (1) initiation of cytotoxic chemotherapy or (2) initiation of an investigational agent for treatment of prostate cancer (up to 54.3 months).
- id
- OG000
- title
- Enzalutamide
- description
- Inactive metabolite.
- id
- OG001
- title
- M1- Carboxylic Acid Metabolite
- description
- N-desmethyl enzalutamide (active metabolite).
- id
- OG002
- title
- M2- N-Desmethyl Enzalutamide
- description
- Active metabolite.
- id
- OG003
- title
- Enzalutamide Plus M2
- param Type
- MEAN
- population Description
- The Pharmacokinetic Analysis Set (PKAS) population consisted of all participants who received at least 1 dose of study drug and who provided blood samples for drug concentrations at least 1 time point.
- reporting Status
- POSTED
- time Frame
- From the date of randomization up to Days 2, 3, 8, 22, 29, 43, 57, 85, 86, 113, 141 and 169
- title
- Observed Plasma Concentration in Predose Samples Obtained During Multiple-dose Administration of Minimum Concentration (Plasma Concentration at Pre Dose) (Cmin) Enzalutamide, M1,M2 and Enzalutamide Plus M2
- type
- SECONDARY
- unit Of Measure
- μg/mL
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Preserved source evidence · Not medical advice
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