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LY3039478 Formulation

Phase 1

Healthy | Small molecule | Other |Eli Lilly and Company|Last Updated: Aug 12, 2025

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
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Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
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Trial Design
RandomizedDouble-BlindPLACEBO_CONTROLLEDBiomarker
Total Trials3
Total Enrollment47
FDA Designations
No designations recorded
Clinical Trials (3)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT02906618Study of LY3039478 in Healthy ParticipantsPHASE1 COMPLETED 12Oct 4, 2016Nov 11, 2016Jul 9, 20251 United Kingdom
NCT02917733A Study of the Absorption, Distribution, Metabolism and Excretion of LY3039478 in Healthy ParticipantsPHASE1 COMPLETED 6Sep 1, 2016Nov 1, 2016Jul 28, 20251 United States
NCT02659865A Study of LY3039478 in Healthy ParticipantsPHASE1 COMPLETED 29Jan 1, 2016Jun 1, 2016Aug 12, 20251 United States
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Study Endpoints
Primary Endpoints
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of LY3039478 and 13C 15N 2H-LY3039478
Predose, 0.5, 1, 1.5, 2, 2.5, 3.5, 4, 6, 8, 12, 24, 36, 48 Hours Postdose

Pharmacokinetics (PK) is the area under the concentration versus time curve (AUC) from time zero to the last time point with a measurable concentration (AUC\[0-tlast\]) of LY3039478 and 13C 15N 2H-LY3039478.

PK: AUC From Zero to Infinity (AUC[0 - Inf]) of LY3039478 and 13C 15N 2H-LY3039478
Predose, 0.5, 1, 1.5, 2, 2.5, 3.5, 4, 6, 8, 12, 24, 36, 48 Hours Postdose

PK is AUC from zero to infinity (AUC\[0 - inf\]) of LY3039478 and 13C 15N 2H-LY3039478.

Urinary and Fecal Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered
Predose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, and 312 hours postdose

To determine the disposition of radioactivity and LY3039478 in healthy participants following oral administration of a single dose 14C-labeled LY3039478.

Pharmacokinetics (PK): Mean Time-Matched Difference in Placebo-Adjusted QTcF Interval With Time Matched Concentrations Between LY3039478 Capsule Formulation (Formulation 3) Part A
Predose, 0.5, 1, 2, 3, 4, 6, 8,12, 24, 36, 48 Hours Postdose

PK: mean time-matched difference in QTcF interval with time-matched concentrations between LY3039478 capsule formulation (formulation 3) compared to placebo. Analyses of QTcF was assessed by the mean change in QTcF as a function of plasma drug concentration. Triplicate measures at each time point was averaged prior to analysis. The primary analysis was based on the time-matched placebo-adjusted QTcF (ΔQTcF) for each time point, which was calculated by subtracting each participant's time-matched placebo QTcF from their QTcF results after receiving LY3039478. The relationship between plasma concentrations of LY3039478 and ΔQTcF was evaluated using a linear mixed-effects modeling approach. The response variable was ΔQTcF, and concentrations was fitted as a fixed effect with participants as a random effect. The regression slope was presented with the unit in "milliseconds per nanogram per milliliter" abbreviated as "ms/ng/mL".

Secondary Endpoints
PK: Maximum Observed Drug Concentration (Cmax) of LY3039478 and 13C 15N 2H-LY3039478 - IV
Predose, 0.5, 1, 1.5, 2, 2.5, 3.5, 4, 6, 8, 12, 24, 36, 48 Hours Postdose
PK: Time of Cmax (Tmax) of LY3039478 and 13C 15N 2H-LY3039478
Predose, 0.5, 1, 1.5, 2, 2.5, 3.5, 4, 6, 8, 12, 24, 36, 48 Hours Postdose
PK: Half Life Associated With The Terminal Rate Constant (t1/2) of LY3039478 and 13C 15N 2H-LY3039478
Predose, 0.5, 1, 1.5, 2, 2.5, 3.5, 4, 6, 8, 12, 24, 36, 48 Hours Postdose
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Study Design & Arms
AllocationNON_RANDOMIZED
MaskingNONE
ModelSINGLE_GROUP
PurposeBASIC_SCIENCE
Treatment Arms
ArmTypeDescription
LY3039478 - OralEXPERIMENTALLY3039478 given once, orally
13C 15N 2H-LY3039478 - IVEXPERIMENTAL13C 15N 2H-LY3039478 given once, IV
Radiolabelled LY3039478EXPERIMENTALSingle dose of radiolabelled LY3039478 administered orally.
Part A: PlaceboPLACEBO_COMPARATORSingle oral dose of placebo administered in one of three study periods
Part A: LY3039478 Capsule Formulation (Formulation 3)EXPERIMENTALEscalating single oral dose of 25 milligram (mg), 50 mg, and 75 mg capsule formulation (formulation 3) LY3039478 administered in two of three study periods
Part B: LY3039478 Drug-In Capsule (Reference, Formulation 1)EXPERIMENTALSingle oral 50 mg dose of drug-in capsule (reference, formulation 1) LY3039478 administered in one of two study periods
Part B: LY3039478 Formulated Capsule (Test, Formulation 3)EXPERIMENTALSingle oral 50 mg dose of formulated capsule (test, formulation 3) LY3039478 administered in one of two study periods
Interventions
NameTypeDescription
LY3039478DRUGAdministered orally
13C 15N 2H-LY3039478 IVDRUGAdministered IV
PlaceboDRUGAdministered orally
LY3039478 Capsule Formulation (Formulation 3)DRUGAdministered orally
LY3039478 Drug-in Capsule (Reference, Formulation 1)DRUGAdministered orally
LY3039478 Formulated Capsule (Test, Formulation 3)DRUGAdministered orally
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Eligibility Criteria
Age Range18 Years — 65 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: \- Have a body mass index (BMI) of 18.5 to 32.0 kilogram per meter square (kg/m²) inclusive Exclusion Criteria: \- Have previously completed or withdrawn from this study or any other study investigating LY3039478, and have previously received the investigational product • Hav...

Countries:United KingdomUnited States
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