NCT03037385 · OUTCOME

Phase 1: Apparent Oral Clearance (CL/F)

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: liters per hour (L/hr)
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: 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. Overall number analyzed is the number of participants with data available for analysis. 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	3
Phase I: Pralsetinib 200 mg	10
Phase I: Pralsetinib 300 mg	9
Phase I: Pralsetinib 400 mg	8
Phase I: Pralsetinib 600 mg	3
Phase I: Pralsetinib 100/100 mg	0
Phase I: Pralsetinib 200/100 mg	0

Reported measurements

Cycle 1 Day 1

Analysis denominator · Participants

Group	Source count
Phase I: Pralsetinib 30 mg	2
Phase I: Pralsetinib 60 mg	5
Phase I: Pralsetinib 100 mg	3
Phase I: Pralsetinib 200 mg	10
Phase I: Pralsetinib 300 mg	5
Phase I: Pralsetinib 400 mg	7
Phase I: Pralsetinib 600 mg	3
Phase I: Pralsetinib 100/100 mg	0
Phase I: Pralsetinib 200/100 mg	0

Values in liters per hour (L/hr) · Interval/dispersion: Geometric Coefficient of Variation
Group	Value	Spread	Lower	Upper	Comment
Phase I: Pralsetinib 30 mg	4.26	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	14.7	42.3	Not reported	Not reported	Not reported
Phase I: Pralsetinib 100 mg	20.6	48.1	Not reported	Not reported	Not reported
Phase I: Pralsetinib 200 mg	27.3	60.3	Not reported	Not reported	Not reported
Phase I: Pralsetinib 300 mg	23.3	40.2	Not reported	Not reported	Not reported
Phase I: Pralsetinib 400 mg	15.2	88.1	Not reported	Not reported	Not reported
Phase I: Pralsetinib 600 mg	11.6	81.3	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	10
Phase I: Pralsetinib 300 mg	9
Phase I: Pralsetinib 400 mg	8
Phase I: Pralsetinib 600 mg	2
Phase I: Pralsetinib 100/100 mg	0
Phase I: Pralsetinib 200/100 mg	0

Values in liters per hour (L/hr) · Interval/dispersion: Geometric Coefficient of Variation
Group	Value	Spread	Lower	Upper	Comment
Phase I: Pralsetinib 30 mg	14.0	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	11.3	51.2	Not reported	Not reported	Not reported
Phase I: Pralsetinib 100 mg	12.0	38.9	Not reported	Not reported	Not reported
Phase I: Pralsetinib 200 mg	31.4	97.8	Not reported	Not reported	Not reported
Phase I: Pralsetinib 300 mg	13.2	33.0	Not reported	Not reported	Not reported
Phase I: Pralsetinib 400 mg	11.1	72.2	Not reported	Not reported	Not reported
Phase I: Pralsetinib 600 mg	8.57	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
4.26
group Id
OG001
spread
42.3
value
14.7
group Id
OG002
spread
48.1
value
20.6
group Id
OG003
spread
60.3
value
27.3
group Id
OG004
spread
40.2
value
23.3
group Id
OG005
spread
88.1
value
15.2
group Id
OG006
spread
81.3
value
11.6
denoms
counts
group Id
OG000
value
2
group Id
OG001
value
5
group Id
OG002
value
3
group Id
OG003
value
10
group Id
OG004
value
5
group Id
OG005
value
7
group Id
OG006
value
3
group Id
OG007
value
0
group Id
OG008
value
0
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
14.0
group Id
OG001
spread
51.2
value
11.3
group Id
OG002
spread
38.9
value
12.0
group Id
OG003
spread
97.8
value
31.4
group Id
OG004
spread
33.0
value
13.2
group Id
OG005
spread
72.2
value
11.1
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
8.57
denoms
counts
group Id
OG000
value
1
group Id
OG001
value
6
group Id
OG002
value
3
group Id
OG003
value
10
group Id
OG004
value
9
group Id
OG005
value
8
group Id
OG006
value
2
group Id
OG007
value
0
group Id
OG008
value
0
units
Participants
title
Cycle 1 Day 15

denoms

counts
group Id
OG000
value
2
group Id
OG001
value
6
group Id
OG002
value
3
group Id
OG003
value
10
group Id
OG004
value
9
group Id
OG005
value
8
group Id
OG006
value
3
group Id
OG007
value
0
group Id
OG008
value
0
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

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. Overall number analyzed is the number of participants with data available for analysis. 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: Apparent Oral Clearance (CL/F)

type

SECONDARY

unit Of Measure

liters per hour (L/hr)

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

Preserved source evidence · Not medical advice