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| ID | Type | Description | Link |
|---|---|---|---|
| J2G-OX-JZJE | Other Identifier | Eli Lilly and Company | |
| LOXO-RET-18023 | Other Identifier | Loxo Oncology, Inc. |
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| Name | Class |
|---|---|
| Loxo Oncology, Inc. | INDUSTRY |
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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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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Selpercatinib (Control; Normal Renal Function) | Experimental | Participants with normal renal function (estimated glomerular filtration rate greater than or equal to [eGFR ≥ 90 milliliters per minute (mL/min) per 1.73 square meters (m²)] received a single 160 milligrams (mg) oral dose of Selpercatinib on Day 1, administered in a fasted state. |
|
| Selpercatinib (Mild Renal Impairment) | Experimental | Participants with mild renal impairment (eGFR between 60 and 90 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
|
| Selpercatinib (Moderate Renal Impairment) | Experimental | Participants with moderate renal impairment (eGFR between 30 and 60 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
|
| Selpercatinib (Severe Renal Impairment) | Experimental | Participants with severe renal impairment (eGFR less than (<) 30 mL/min/1.73 m² and not requiring hemodialysis) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Selpercatinib | Drug | Administered orally |
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib in Plasma | PK: AUC0-t of Selpercatinib | 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: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib in Plasma | PK: AUC0-inf of Selpercatinib | 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 (AUC%Extrap) of Selpercatinib.in Plasma | PK: Percentage of AUC0-inf extrapolated was calculated as (1 - AUC0-t/AUC0-inf) * 100. | 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: Maximum Observed Concentration (Cmax) of Selpercatinib in Plasma | PK: Cmax of Selpercatinib | 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: Time to Maximum Observed Plasma Concentration (Tmax) of Selpercatinib in Plasma | PK: Tmax of Selpercatinib | 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 First Order Terminal Elimination Rate Constant (Kel) of Selpercatinib in Plasma | 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). |
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Inclusion Criteria:
For all participants:
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:
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:
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| Name | Affiliation | Role |
|---|---|---|
| Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST) | Eli Lilly and Company | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Anaheim Regional Center | Anaheim | California | 92801 | United States | ||
| Stanford Health Care, Valley Care Program |
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| ID | Title | Description |
|---|---|---|
| FG000 | Selpercatinib (Control; Normal Renal Function) | Participants with normal renal function (estimated glomerular filtration rate greater than or equal to [eGFR ≥ 90 milliliters per minute (mL/min) per 1.73 square meters (m²)] received a single 160 milligrams (mg) oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| FG001 | Selpercatinib (Mild Renal Impairment) | Participants with mild renal impairment (eGFR between 60 and 90 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| FG002 | Selpercatinib (Moderate Renal Impairment) | Participants with moderate renal impairment (eGFR between 30 and 60 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| FG003 | Selpercatinib (Severe Renal Impairment) | Participants with severe renal impairment (eGFR less than (<) 30 mL/min/1.73 m² and not requiring hemodialysis) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| Title | Milestones | Reasons Not Completed | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
All enrolled participants.
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| ID | Title | Description |
|---|---|---|
| BG000 | Selpercatinib (Control; Normal Renal Function) | Participants with normal renal function (eGFR ≥ 90 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| BG001 | Selpercatinib (Mild Renal Impairment) |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | |||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 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 | PK: AUC0-t of Selpercatinib | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax). | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram*hour per milliliter (ng*hr/mL) | 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 |
|
Baseline up to 15 days
All enrolled participants who received at least one dose of Selpercatinib.
Not provided
| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Selpercatinib (Control; Normal Renal Function) | Participants with normal renal function (eGFR ≥ 90 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Abdominal distension | Gastrointestinal disorders | MedDRA 21.1 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Chief Medical Officer | Eli Lilly and Company | 800-545-5979 | ClinicalTrials.gov@lilly.com |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | May 14, 2019 | Aug 29, 2025 | Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Jun 3, 2019 | Aug 29, 2025 | SAP_001.pdf |
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| ID | Term |
|---|---|
| D051437 | Renal Insufficiency |
| ID | Term |
|---|---|
| D007674 | Kidney Diseases |
| D014570 | Urologic Diseases |
| D052776 | Female Urogenital Diseases |
| D005261 | Female Urogenital Diseases and Pregnancy Complications |
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| ID | Term |
|---|---|
| C000656166 | selpercatinib |
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|
| 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 First-order Terminal Elimination Half-life (t½) of Selpercatinib in Plasma | PK: t½ of Selpercatinib. | 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 Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib in Plasma | PK: CL/F of Selpercatinib | 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 Volume of Distribution During the Terminal Elimination Phase After Oral (Extravascular) Administration (Vz/F) of Selpercatinib in Plasma | PK: Vz/F of Selpercatinib | 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: Unbound AUC0-t (AUC0-t,u) of Selpercatinib in Plasma | 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. | 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: Unbound AUC0-inf (AUC0-inf,u) of Selpercatinib in Plasma | 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. | 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: Unbound Cmax (Cmax,u) of Selpercatinib in Plasma | 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. | 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: Unbound CL/F (CL/F,u) of Selpercatinib in Plasma | 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. | 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: Unbound Vz/F (Vz/F,u) of Selpercatinib in Plasma | 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. | 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: Cumulative Amount of Selpercatinib Excreted (CumAe) in Urine | PK: CumAe was reported. The urine sampling time points from pre-dose through 168 hours post-dose were used to assess this outcome. | Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose |
| PK: Cumulative Percentage of Administered Selpercatinib Dose (Cum%Dose) Excreted in Urine | PK: Cum%Dose was reported. The urine sampling time points from pre-dose through 168 hours post-dose were used to assess this outcome. | Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose |
| PK: Renal Clearance (CLr) of Selpercatinib in Urine | 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. | Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose |
| Pleasanton |
| California |
| 94588 |
| United States |
| Orange County Research Center | Tustin | California | 92780 | United States |
| Riverside Clinical Research | Edgewater | Florida | 32132 | United States |
| Clinical Pharmacology of Miami | Miami | Florida | 33014 | United States |
| Orlando Clinical Research Center | Orlando | Florida | 32809 | United States |
Participants with mild renal impairment (eGFR between 60 and 90 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| BG002 | Selpercatinib (Moderate Renal Impairment) | Participants with moderate renal impairment (eGFR between 30 and 60 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| BG003 | Selpercatinib (Severe Renal Impairment) | Participants with severe renal impairment (eGFR < 30 mL/min/1.73 m² and not requiring hemodialysis) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| BG004 | Total | Total of all reporting groups |
| years |
|
| Sex: Female, Male | Count of Participants | Participants | No |
|
| Ethnicity (NIH/OMB) | Count of Participants | Participants | No |
|
| Race (NIH/OMB) | Count of Participants | Participants | No |
|
| Region of Enrollment | Count of Participants | Participants | No |
|
| OG001 | Selpercatinib (Mild Renal Impairment) | Participants with mild renal impairment (eGFR between 60 and 90 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| OG002 | Selpercatinib (Moderate Renal Impairment) | Participants with moderate renal impairment (eGFR between 30 and 60 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
| OG003 | Selpercatinib (Severe Renal Impairment) | Participants with severe renal impairment (eGFR < 30 mL/min/1.73 m² and not requiring hemodialysis) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. |
|
|
| Primary | PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib in Plasma | PK: AUC0-inf of Selpercatinib | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram*hour per milliliter (ng*hr/mL) | 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 |
|
|
|
| Primary | PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib.in Plasma | PK: Percentage of AUC0-inf extrapolated was calculated as (1 - AUC0-t/AUC0-inf) * 100. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | percentage of AUCextrap | 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 |
|
|
|
| Primary | PK: Maximum Observed Concentration (Cmax) of Selpercatinib in Plasma | PK: Cmax of Selpercatinib | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram per milliliter (ng/mL) | 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 |
|
|
|
| Primary | PK: Time to Maximum Observed Plasma Concentration (Tmax) of Selpercatinib in Plasma | PK: Tmax of Selpercatinib | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Median | Full Range | hours (hr) | 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 |
|
|
|
| Primary | PK: Apparent First Order Terminal Elimination Rate Constant (Kel) of Selpercatinib in Plasma | 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). | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | One per hour (1/hour) | 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 |
|
|
|
| Primary | PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib in Plasma | PK: t½ of Selpercatinib. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | hours (hr) | 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 |
|
|
|
| Primary | PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib in Plasma | PK: CL/F of Selpercatinib | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | Liters per Hour (L/h) | 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 |
|
|
|
| Primary | PK: Apparent Volume of Distribution During the Terminal Elimination Phase After Oral (Extravascular) Administration (Vz/F) of Selpercatinib in Plasma | PK: Vz/F of Selpercatinib | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | Liter | 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 |
|
|
|
| Primary | PK: Unbound AUC0-t (AUC0-t,u) of Selpercatinib in Plasma | 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. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax). | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram*hour per milliliter (ng*hr/mL) | 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 |
|
|
|
| Primary | PK: Unbound AUC0-inf (AUC0-inf,u) of Selpercatinib in Plasma | 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. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram*hour per milliliter (ng*hr/mL) | 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 |
|
|
|
| Primary | PK: Unbound Cmax (Cmax,u) of Selpercatinib in Plasma | 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. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanogram per milliliter (ng/mL) | 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 |
|
|
|
| Primary | PK: Unbound CL/F (CL/F,u) of Selpercatinib in Plasma | 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. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | Liters per Hour (L/h) | 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 |
|
|
|
| Primary | PK: Unbound Vz/F (Vz/F,u) of Selpercatinib in Plasma | 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. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | Liter (L) | 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 |
|
|
|
| Primary | PK: Cumulative Amount of Selpercatinib Excreted (CumAe) in Urine | PK: CumAe was reported. The urine sampling time points from pre-dose through 168 hours post-dose were used to assess this outcome. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | milligram (mg) | Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose |
|
|
|
| Primary | PK: Cumulative Percentage of Administered Selpercatinib Dose (Cum%Dose) Excreted in Urine | PK: Cum%Dose was reported. The urine sampling time points from pre-dose through 168 hours post-dose were used to assess this outcome. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | percentage of dose excreted | Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose |
|
|
|
| Primary | PK: Renal Clearance (CLr) of Selpercatinib in Urine | 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. | All enrolled participants who received at least one dose of the study drug and had evaluable PK data. Participants were excluded from the analysis if they experienced emesis (vomiting) that occurred at or before 2 times the median Tmax. | Posted | Mean | Standard Deviation | milliliter per hour (mL/hr) | Predose (spot collection), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours postdose |
|
|
|
| 0 |
| 13 |
| 0 |
| 13 |
| 2 |
| 13 |
| EG001 | Selpercatinib (Mild Renal Impairment) | Participants with mild renal impairment (eGFR between 60 and 90 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. | 0 | 9 | 0 | 9 | 3 | 9 |
| EG002 | Selpercatinib (Moderate Renal Impairment) | Participants with moderate renal impairment (eGFR between 30 and 60 mL/min/1.73 m²) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. | 0 | 8 | 0 | 8 | 3 | 8 |
| EG003 | Selpercatinib (Severe Renal Impairment) | Participants with severe renal impairment (eGFR < 30 mL/min/1.73 m² and not requiring hemodialysis) received a single 160 mg oral dose of Selpercatinib on Day 1, administered in a fasted state. | 0 | 7 | 0 | 7 | 3 | 7 |
| Constipation | Gastrointestinal disorders | MedDRA 21.1 | Systematic Assessment |
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| Diarrhoea | Gastrointestinal disorders | MedDRA 21.1 | Systematic Assessment |
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| Dry mouth | Gastrointestinal disorders | MedDRA 21.1 | Systematic Assessment |
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| Nausea | Gastrointestinal disorders | MedDRA 21.1 | Systematic Assessment |
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| Vomiting | Gastrointestinal disorders | MedDRA 21.1 | Systematic Assessment |
|
| Muscle spasms | Musculoskeletal and connective tissue disorders | MedDRA 21.1 | Systematic Assessment |
|
| Dizziness | Nervous system disorders | MedDRA 21.1 | Systematic Assessment |
|
| Head discomfort | Nervous system disorders | MedDRA 21.1 | Systematic Assessment |
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| Headache | Nervous system disorders | MedDRA 21.1 | Systematic Assessment |
|
| Somnolence | Nervous system disorders | MedDRA 21.1 | Systematic Assessment |
|
| Dyspnoea | Respiratory, thoracic and mediastinal disorders | MedDRA 21.1 | Systematic Assessment |
|
Not provided
| D000091642 | Urogenital Diseases |
| D052801 | Male Urogenital Diseases |