NCT03037385 · OUTCOME

Phase 1: Maximum Plasma Concentration (Cmax)

Phase 1/2 Study of the Highly-selective RET Inhibitor, Pralsetinib (BLU-667), in Participants With Thyroid Cancer, Non-Small Cell Lung Cancer, and Other Advanced Solid Tumors · Source last updated 2025-05-31

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

Measure: GEOMETRIC_MEAN
Unit: nanograms per milliliters (ng/mL)
Interval / dispersion: Geometric Coefficient of Variation
Time frame: Predose on 0.5, 1, 2, 4, 6, 8 and 24 hours postdose on Days 1 and 15 of Cycle 1 (1 cycle = 28 days)

What was measured

Number of participants in each arm of this OM is based on the actual treatment received. 1 participant originally assigned to the 200/100 mg arm received the 100/100 mg treatment and hence, was counted under the 100/100 mg arm for this OM.

Analysis population: Pharmacokinetic (PK)-evaluable population included all participants who received at least one dose of pralsetinib and from whom at least one post dose PK sample was collected. Number analyzed is the number of participants with data available for analysis at the specified timepoint.

Groups in this outcome

Phase I: Pralsetinib 30 mg

Participants received pralsetinib 30 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 60 mg

Participants received pralsetinib 60 mg orally, QD until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 100 mg

Participants received pralsetinib 100 mg orally, QD until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 200 mg

Participants received pralsetinib 200 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 300 mg

Participants received pralsetinib 300 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 400 mg

Participants received pralsetinib 400 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 600 mg

Participants received pralsetinib 600 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 100/100 mg

Participants received pralsetinib 100 mg, orally, BID until discontinuation due to toxicity, disease progression, or other reasons.

Phase I: Pralsetinib 200/100 mg

Participants received pralsetinib 200 mg in the morning and then 100 mg in the evening orally until discontinuation due to toxicity, disease progression, or other reasons.

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
Phase I: Pralsetinib 30 mg	2
Phase I: Pralsetinib 60 mg	6
Phase I: Pralsetinib 100 mg	5
Phase I: Pralsetinib 200 mg	13
Phase I: Pralsetinib 300 mg	11
Phase I: Pralsetinib 400 mg	12
Phase I: Pralsetinib 600 mg	4
Phase I: Pralsetinib 100/100 mg	6
Phase I: Pralsetinib 200/100 mg	3

Reported measurements

Cycle 1 Day 1

Analysis denominator · Participants

Group	Source count
Phase I: Pralsetinib 30 mg	2
Phase I: Pralsetinib 60 mg	6
Phase I: Pralsetinib 100 mg	5
Phase I: Pralsetinib 200 mg	13
Phase I: Pralsetinib 300 mg	11
Phase I: Pralsetinib 400 mg	12
Phase I: Pralsetinib 600 mg	4
Phase I: Pralsetinib 100/100 mg	6
Phase I: Pralsetinib 200/100 mg	3

Values in nanograms per milliliters (ng/mL) · Interval/dispersion: Geometric Coefficient of Variation
Group	Value	Spread	Lower	Upper	Comment
Phase I: Pralsetinib 30 mg	346	NA	Not reported	Not reported	Values were LTR for 1 participant. Since data was evaluable only for 1 participant geometric co-efficient of variation was not evaluable.
Phase I: Pralsetinib 60 mg	335	52.8	Not reported	Not reported	Not reported
Phase I: Pralsetinib 100 mg	198	99.8	Not reported	Not reported	Not reported
Phase I: Pralsetinib 200 mg	459	52.3	Not reported	Not reported	Not reported
Phase I: Pralsetinib 300 mg	688	53.3	Not reported	Not reported	Not reported
Phase I: Pralsetinib 400 mg	1210	85.3	Not reported	Not reported	Not reported
Phase I: Pralsetinib 600 mg	1820	63.8	Not reported	Not reported	Not reported
Phase I: Pralsetinib 100/100 mg	569	42.0	Not reported	Not reported	Not reported
Phase I: Pralsetinib 200/100 mg	715	64.1	Not reported	Not reported	Not reported

Cycle 1 Day 15

Analysis denominator · Participants

Group	Source count
Phase I: Pralsetinib 30 mg	1
Phase I: Pralsetinib 60 mg	6
Phase I: Pralsetinib 100 mg	3
Phase I: Pralsetinib 200 mg	12
Phase I: Pralsetinib 300 mg	9
Phase I: Pralsetinib 400 mg	10
Phase I: Pralsetinib 600 mg	2
Phase I: Pralsetinib 100/100 mg	5
Phase I: Pralsetinib 200/100 mg	2

Values in nanograms per milliliters (ng/mL) · Interval/dispersion: Geometric Coefficient of Variation
Group	Value	Spread	Lower	Upper	Comment
Phase I: Pralsetinib 30 mg	130	NA	Not reported	Not reported	Since data was available only for 1 participant geometric co-efficient of variation was not evaluable.
Phase I: Pralsetinib 60 mg	420	56.9	Not reported	Not reported	Not reported
Phase I: Pralsetinib 100 mg	586	47.8	Not reported	Not reported	Not reported
Phase I: Pralsetinib 200 mg	525	72.5	Not reported	Not reported	Not reported
Phase I: Pralsetinib 300 mg	1390	35.3	Not reported	Not reported	Not reported
Phase I: Pralsetinib 400 mg	1930	66.7	Not reported	Not reported	Not reported
Phase I: Pralsetinib 600 mg	4330	NA	Not reported	Not reported	Values were LTR for 1 participant. Since data was evaluable only for 1 participant geometric co-efficient of variation was not evaluable.
Phase I: Pralsetinib 100/100 mg	1080	43.8	Not reported	Not reported	Not reported
Phase I: Pralsetinib 200/100 mg	1780	NA	Not reported	Not reported	Values were LTR for 1 participant. Since data was evaluable only for 1 participant geometric co-efficient of variation was not evaluable.

Complete source fields

classes

categories
measurements
comment
Values were LTR for 1 participant. Since data was evaluable only for 1 participant geometric co-efficient of variation was not evaluable.
group Id
OG000
spread
NA
value
346
group Id
OG001
spread
52.8
value
335
group Id
OG002
spread
99.8
value
198
group Id
OG003
spread
52.3
value
459
group Id
OG004
spread
53.3
value
688
group Id
OG005
spread
85.3
value
1210
group Id
OG006
spread
63.8
value
1820
group Id
OG007
spread
42.0
value
569
group Id
OG008
spread
64.1
value
715
denoms
counts
group Id
OG000
value
2
group Id
OG001
value
6
group Id
OG002
value
5
group Id
OG003
value
13
group Id
OG004
value
11
group Id
OG005
value
12
group Id
OG006
value
4
group Id
OG007
value
6
group Id
OG008
value
3
units
Participants
title
Cycle 1 Day 1
categories
measurements
comment
Since data was available only for 1 participant geometric co-efficient of variation was not evaluable.
group Id
OG000
spread
NA
value
130
group Id
OG001
spread
56.9
value
420
group Id
OG002
spread
47.8
value
586
group Id
OG003
spread
72.5
value
525
group Id
OG004
spread
35.3
value
1390
group Id
OG005
spread
66.7
value
1930
comment
Values were LTR for 1 participant. Since data was evaluable only for 1 participant geometric co-efficient of variation was not evaluable.
group Id
OG006
spread
NA
value
4330
group Id
OG007
spread
43.8
value
1080
comment
Values were LTR for 1 participant. Since data was evaluable only for 1 participant geometric co-efficient of variation was not evaluable.
group Id
OG008
spread
NA
value
1780
denoms
counts
group Id
OG000
value
1
group Id
OG001
value
6
group Id
OG002
value
3
group Id
OG003
value
12
group Id
OG004
value
9
group Id
OG005
value
10
group Id
OG006
value
2
group Id
OG007
value
5
group Id
OG008
value
2
units
Participants
title
Cycle 1 Day 15

denoms

counts
group Id
OG000
value
2
group Id
OG001
value
6
group Id
OG002
value
5
group Id
OG003
value
13
group Id
OG004
value
11
group Id
OG005
value
12
group Id
OG006
value
4
group Id
OG007
value
6
group Id
OG008
value
3
units
Participants

description

dispersion Type

Geometric Coefficient of Variation

groups

description
Participants received pralsetinib 30 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.
id
OG000
title
Phase I: Pralsetinib 30 mg
description
Participants received pralsetinib 60 mg orally, QD until discontinuation due to toxicity, disease progression, or other reasons.
id
OG001
title
Phase I: Pralsetinib 60 mg
description
Participants received pralsetinib 100 mg orally, QD until discontinuation due to toxicity, disease progression, or other reasons.
id
OG002
title
Phase I: Pralsetinib 100 mg
description
Participants received pralsetinib 200 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.
id
OG003
title
Phase I: Pralsetinib 200 mg
description
Participants received pralsetinib 300 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.
id
OG004
title
Phase I: Pralsetinib 300 mg
description
Participants received pralsetinib 400 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.
id
OG005
title
Phase I: Pralsetinib 400 mg
description
Participants received pralsetinib 600 mg, orally, QD until discontinuation due to toxicity, disease progression, or other reasons.
id
OG006
title
Phase I: Pralsetinib 600 mg
description
Participants received pralsetinib 100 mg, orally, BID until discontinuation due to toxicity, disease progression, or other reasons.
id
OG007
title
Phase I: Pralsetinib 100/100 mg
description
Participants received pralsetinib 200 mg in the morning and then 100 mg in the evening orally until discontinuation due to toxicity, disease progression, or other reasons.
id
OG008
title
Phase I: Pralsetinib 200/100 mg

param Type

GEOMETRIC_MEAN

population Description

Pharmacokinetic (PK)-evaluable population included all participants who received at least one dose of pralsetinib and from whom at least one post dose PK sample was collected. Number analyzed is the number of participants with data available for analysis at the specified timepoint.

reporting Status

POSTED

time Frame

Predose on 0.5, 1, 2, 4, 6, 8 and 24 hours postdose on Days 1 and 15 of Cycle 1 (1 cycle = 28 days)

title

Phase 1: Maximum Plasma Concentration (Cmax)

type

SECONDARY

unit Of Measure

nanograms per milliliters (ng/mL)

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

Preserved source evidence · Not medical advice