Phase 1
Completed N=37
A Study of Effect of Selpercatinib (LY3527723) in Participants With Normal and Impaired Renal Function
Healthy · Renal Insufficiency
Source: ClinicalTrials.gov NCT05469100 ↗
Enrolled (actual)
37
Serious AEs
0.0%
Results posted
Sep 2025
Primary outcomePrimary: Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib in Plasma — 19770; 23440; 29270; 20640 nanogram*hour per milliliter (ng*hr/mL)
Summary
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib in Plasma |
19770; 23440; 29270; 20640 | — |
| PRIMARY PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib in Plasma |
19870; 23510; 29470; 21000 | — |
| PRIMARY PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib.in Plasma |
0.4856; 0.2988; 0.6738; 1.706 | — |
| PRIMARY PK: Maximum Observed Concentration (Cmax) of Selpercatinib in Plasma |
1399; 2247; 1742; 1006 | — |
| PRIMARY PK: Time to Maximum Observed Plasma Concentration (Tmax) of Selpercatinib in Plasma |
1.500; 1.500; 1.500; 1.000 | — |
| PRIMARY PK: Apparent First Order Terminal Elimination Rate Constant (Kel) of Selpercatinib in Plasma |
0.02853; 0.03434; 0.02662; 0.02204 | — |
| PRIMARY PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib in Plasma |
24.854; 22.632; 27.139; 33.828 | — |
| PRIMARY PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib in Plasma |
8.976; 7.188; 5.581; 9.184 | — |
| PRIMARY PK: Apparent Volume of Distribution During the Terminal Elimination Phase After Oral (Extravascular) Administration (Vz/F) of Selpercatinib in Plasma |
334.5; 227.9; 219.4; 444.7 | — |
| PRIMARY PK: Unbound AUC0-t (AUC0-t,u) of Selpercatinib in Plasma |
533.1; 659.7; 856.3; 709.9 | — |
| PRIMARY PK: Unbound AUC0-inf (AUC0-inf,u) of Selpercatinib in Plasma |
535.7; 661.6; 862.1; 722.3 | — |
| PRIMARY PK: Unbound Cmax (Cmax,u) of Selpercatinib in Plasma |
37.72; 63.23; 50.95; 34.60 | — |
| PRIMARY PK: Unbound CL/F (CL/F,u) of Selpercatinib in Plasma |
337.9; 247.9; 191.6; 300.6 | — |
| PRIMARY PK: Unbound Vz/F (Vz/F,u) of Selpercatinib in Plasma |
12700; 8214; 7697; 14340 | — |
| PRIMARY PK: Cumulative Amount of Selpercatinib Excreted (CumAe) in Urine |
16.14; 14.54; 13.94; 7.652 | — |
| PRIMARY PK: Cumulative Percentage of Administered Selpercatinib Dose (Cum%Dose) Excreted in Urine |
10.09; 9.087; 8.713; 4.782 | — |
| PRIMARY PK: Renal Clearance (CLr) of Selpercatinib in Urine |
735.9; 641.6; 480.4; 314.6 | — |
Eligibility Criteria
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
Data sourced from ClinicalTrials.gov (NCT05469100). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.