NCT03157128 · OUTCOME

Phase 1: Pharmacokinetics (PK): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours

A Study of Selpercatinib (LOXO-292) in Participants With Advanced Solid Tumors, RET Fusion-Positive Solid Tumors, and Medullary Thyroid Cancer (LIBRETTO-001) · Source last updated 2026-04-16

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

Measure: GEOMETRIC_MEAN
Unit: nanogram*hour per milliliter (ng*h/mL)
Interval / dispersion: Geometric Coefficient of Variation
Time frame: Cycle 1 Day 8: Predose, 1, 2, 4, 8, 24 hours post dose (cycle length = 28 days)

Analysis population: All Participants who received at least 1 or more doses of selpercatinib and had PK evaluable data for this outcome.

Groups in this outcome

Phase 1: 20 mg Selpercatinib QD

Participants received Selpercatinib 20 milligrams (mg) administered orally once daily (QD), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 20 mg Selpercatinib BID

Participants received Selpercatinib 20 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 40 mg Selpercatinib BID

Participants received Selpercatinib 40 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 60 mg Selpercatinib BID

Participants received Selpercatinib 60 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 160 mg Selpercatinib QD

Participants received Selpercatinib 160 milligrams (mg) administered orally once daily (QD), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 80 mg Selpercatinib BID

Participants received Selpercatinib 80 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 120 mg Selpercatinib BID

Participants received Selpercatinib 120 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 160 mg Selpercatinib BID

Participants received Selpercatinib 160 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 200 mg Selpercatinib BID

Participants received Selpercatinib 200 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.

Phase 1: 240 mg Selpercatinib BID

Participants received Selpercatinib 240 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for 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 1: 20 mg Selpercatinib QD	4
Phase 1: 20 mg Selpercatinib BID	9
Phase 1: 40 mg Selpercatinib BID	12
Phase 1: 60 mg Selpercatinib BID	11
Phase 1: 160 mg Selpercatinib QD	0
Phase 1: 80 mg Selpercatinib BID	15
Phase 1: 120 mg Selpercatinib BID	10
Phase 1: 160 mg Selpercatinib BID	480
Phase 1: 200 mg Selpercatinib BID	2
Phase 1: 240 mg Selpercatinib BID	3

Reported measurements

Source class 1

Values in nanogram*hour per milliliter (ng*h/mL) · Interval/dispersion: Geometric Coefficient of Variation
Group	Value	Spread	Lower	Upper	Comment
Phase 1: 20 mg Selpercatinib QD	2240	36	Not reported	Not reported	Not reported
Phase 1: 20 mg Selpercatinib BID	4570	50	Not reported	Not reported	Not reported
Phase 1: 40 mg Selpercatinib BID	8450	53	Not reported	Not reported	Not reported
Phase 1: 60 mg Selpercatinib BID	17100	46	Not reported	Not reported	Not reported
Phase 1: 80 mg Selpercatinib BID	19400	49	Not reported	Not reported	Not reported
Phase 1: 120 mg Selpercatinib BID	42200	40	Not reported	Not reported	Not reported
Phase 1: 160 mg Selpercatinib BID	53700	53	Not reported	Not reported	Not reported
Phase 1: 200 mg Selpercatinib BID	NA	NA	Not reported	Not reported	Geometric Mean and Geometric Coefficient of Variation could not be calculated as there were only two participants. Individual values reported: 43200 ng\h/mL; 33100 ng\h/mL.
Phase 1: 240 mg Selpercatinib BID	87900	20	Not reported	Not reported	Not reported

Complete source fields

classes

categories
measurements
group Id
OG000
spread
36
value
2240
group Id
OG001
spread
50
value
4570
group Id
OG002
spread
53
value
8450
group Id
OG003
spread
46
value
17100
group Id
OG005
spread
49
value
19400
group Id
OG006
spread
40
value
42200
group Id
OG007
spread
53
value
53700
comment
Geometric Mean and Geometric Coefficient of Variation could not be calculated as there were only two participants. Individual values reported: 43200 ng\*h/mL; 33100 ng\*h/mL.
group Id
OG008
spread
NA
value
NA
group Id
OG009
spread
20
value
87900

denoms

counts
group Id
OG000
value
4
group Id
OG001
value
9
group Id
OG002
value
12
group Id
OG003
value
11
group Id
OG004
value
0
group Id
OG005
value
15
group Id
OG006
value
10
group Id
OG007
value
480
group Id
OG008
value
2
group Id
OG009
value
3
units
Participants

dispersion Type

Geometric Coefficient of Variation

groups

description
Participants received Selpercatinib 20 milligrams (mg) administered orally once daily (QD), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG000
title
Phase 1: 20 mg Selpercatinib QD
description
Participants received Selpercatinib 20 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG001
title
Phase 1: 20 mg Selpercatinib BID
description
Participants received Selpercatinib 40 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG002
title
Phase 1: 40 mg Selpercatinib BID
description
Participants received Selpercatinib 60 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG003
title
Phase 1: 60 mg Selpercatinib BID
description
Participants received Selpercatinib 160 milligrams (mg) administered orally once daily (QD), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG004
title
Phase 1: 160 mg Selpercatinib QD
description
Participants received Selpercatinib 80 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG005
title
Phase 1: 80 mg Selpercatinib BID
description
Participants received Selpercatinib 120 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG006
title
Phase 1: 120 mg Selpercatinib BID
description
Participants received Selpercatinib 160 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG007
title
Phase 1: 160 mg Selpercatinib BID
description
Participants received Selpercatinib 200 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG008
title
Phase 1: 200 mg Selpercatinib BID
description
Participants received Selpercatinib 240 milligrams (mg) administered orally twice daily (BID), in a 28-day treatment cycle. Treatment was continued until disease progression, unacceptable toxicity, or treatment discontinuation for other reasons.
id
OG009
title
Phase 1: 240 mg Selpercatinib BID

param Type

GEOMETRIC_MEAN

population Description

All Participants who received at least 1 or more doses of selpercatinib and had PK evaluable data for this outcome.

reporting Status

POSTED

time Frame

Cycle 1 Day 8: Predose, 1, 2, 4, 8, 24 hours post dose (cycle length = 28 days)

title

Phase 1: Pharmacokinetics (PK): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours

type

SECONDARY

unit Of Measure

nanogram*hour per milliliter (ng*h/mL)

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

Preserved source evidence · Independent clinical review pending · Not medical advice