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Completed

NCT Number: NCT05469100

A Study of Effect of Selpercatinib (LY3527723) in Participants With Normal and Impaired Renal Function

The main purpose of this study is to assess the amount of study drug that reaches the bloodstream and the time it takes for the body to get rid of it when given to participants with renal (kidney) impairment compared to healthy participants. The study will last up to 9 days, excluding screening.

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Key information

Conditions

Healthy Female Urogenital Diseases Female Urogenital Diseases and Pregnancy Complications Kidney Diseases Male Urogenital Diseases Renal Insufficiency Urogenital Diseases Urologic Diseases

Age range

18 year–70 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Anaheim Regional Center, Anaheim, California, United States

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Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

For all participants:

  • Body mass index (BMI) ≥ 18.0 and ≤ 40.0 kilograms per meter squared (kg/m²) and had a minimum weight of at least 50 kg at screening
  • Have normal blood pressure, pulse rate, electrocardiogram (ECG), and blood and urine laboratory test results that are acceptable for the study
  • Female of non childbearing potential: must have undergone sterilization procedures at least 6 months prior to the Screening
  • Males who are capable of fathering a child must agree to use contraception from the time of the dose administration through 6 months after the last dose

For renal participants:

  • Participant has stable renal disease status and function at least 1 month prior to LOXO-292 administration.
  • Participant is not currently or has not previously being on hemodialysis
  • Baseline estimated glomerular filtration rate (eGFR) based on the Modification of Diet in Renal Disease (MDRD) equation at screening as follows:
  • Severe Renal Impairment (RI): < 30 milliliter per minute (mL/min)/1.73m²
  • Moderate RI: ≥ 30 and < 60 mL/min/1.73m²
  • Mild RI: ≥ 60 and < 90 mL/min/1.73m²

The MDRD equation is as follows (for females multiply result by 0.742, if African American multiply result by 1.212):

eGFR = 175 x [serum creatinine in milligrams per deciliter (mg/dL) measured with a standardized assay]^-1.154 x (Age)^-0.203

Exclusion criteria

For renal participants:

  • Has rapidly fluctuating renal function, as determined by historical measurements; or has demonstrated or suspected renal artery stenosis. Rapidly fluctuating renal function is defined as creatinine clearance or eGFR that differs by more than 20% within at least 3 months of the screening creatinine clearance or eGFR. If historical measurements are not available, then the 2 screening measurements will be used to demonstrate stability.
  • Participants who have had a renal transplant, a nephrectomy, or participants with a known history of nephrotic syndrome.
  • Participants who have required new medication for renal disease within 30 days prior to Check-in

Treatment and study plan

Selpercatinib

Drug

Administered orally

Other names: LY3527723, LOXO-292

Primary outcomes

  1. Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUC0-t of Selpercatinib

  2. PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUC0-inf of Selpercatinib

  3. PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib.in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Percentage of AUC0-inf extrapolated was calculated as (1 - AUC0-t/AUC0-inf) * 100.

  4. PK: Maximum Observed Concentration (Cmax) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Cmax of Selpercatinib

  5. PK: Time to Maximum Observed Plasma Concentration (Tmax) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Tmax of Selpercatinib

  6. PK: Apparent First Order Terminal Elimination Rate Constant (Kel) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Apparent terminal elimination rate constant; represents the fraction of drug eliminated per unit time calculated by linear least squares regression analysis using the maximum number of points in the terminal log linear phase (e.g., three or more non zero plasma concentrations).

  7. PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: t½ of Selpercatinib.

  8. PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: CL/F of Selpercatinib

  9. PK: Apparent Volume of Distribution During the Terminal Elimination Phase After Oral (Extravascular) Administration (Vz/F) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Vz/F of Selpercatinib

  10. PK: Unbound AUC0-t (AUC0-t,u) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    AUC0-t,u was calculated by multiplying AUC0-t by Fu (i.e., AUC0-t*Fu). Fu represented the unbound fraction of Selpercatinib in plasma, that is, the portion of the drug not bound to plasma proteins.

  11. PK: Unbound AUC0-inf (AUC0-inf,u) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    AUC0-inf,u was calculated by multiplying AUC0-inf by Fu (i.e., AUC0-inf*Fu). Fu represented the unbound fraction of Selpercatinib in plasma, that is, the portion of the drug not bound to plasma proteins.

  12. PK: Unbound Cmax (Cmax,u) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    Cmax,u was calculated by multiplying Cmax by Fu (i.e., Cmax*Fu). Fu represented the unbound fraction of Selpercatinib in plasma, that is, the portion of the drug not bound to plasma proteins.

  13. PK: Unbound CL/F (CL/F,u) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    CL/F,u was calculated by multiplying CL/F by Fu (i.e., CL/F*Fu). Fu represented the unbound fraction of Selpercatinib in plasma, that is, the portion of the drug not bound to plasma proteins.

  14. PK: Unbound Vz/F (Vz/F,u) of Selpercatinib in Plasma

    Time frame: Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

    Vz/F,u was calculated by multiplying Vz/F by Fu (i.e., Vz/F*Fu). Fu represented the unbound fraction of Selpercatinib in plasma, that is, the portion of the drug not bound to plasma proteins.

  15. PK: Cumulative Amount of Selpercatinib Excreted (CumAe) in Urine

    Time frame: Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose

    PK: CumAe was reported. The urine sampling time points from pre-dose through 168 hours post-dose were used to assess this outcome.

  16. PK: Cumulative Percentage of Administered Selpercatinib Dose (Cum%Dose) Excreted in Urine

    Time frame: Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose

    PK: Cum%Dose was reported. The urine sampling time points from pre-dose through 168 hours post-dose were used to assess this outcome.

  17. PK: Renal Clearance (CLr) of Selpercatinib in Urine

    Time frame: Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose

    PK: CLr of Selpercatinib was reported.The urine sampling time points from pre-dose through 168 hours post-dose were used to assess this outcome.

Sponsors and collaborators

Lead sponsor

Eli Lilly and Company

Industry

Collaborators

  • Loxo Oncology, Inc.

Registry information

Official study title

A Phase 1, Open-Label, Parallel-Cohort, Single-Dose Study to Evaluate the Effect of Renal Impairment on the Pharmacokinetics of LOXO-292

Important dates

Study start
2018
Primary completion
2019
Study completion
2019
First posted
Jul 21, 2022
Registry last updated
Sep 18, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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