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CompletedNCT05134350Updated Jan 10, 2025Results posted

Study of the Effect of Food and a Proton Pump Inhibitor (PPI; Omeprazole) on LOXO-305 in Healthy Participants

A Phase 1 interventional study of LOXO-305 and Omeprazole in Healthy Volunteers, sponsored by Loxo Oncology, Inc.. Completed at 1 site in United States. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2025-01-10.

Sponsored by Loxo Oncology, Inc. · Phase 1, Interventional, and Basic science

From the registry’s dates

  • Registered 1 year 8 months after the study started (first participant enrolled Feb 2020, registered Oct 2021).
Phase
Phase 1
Study type
Interventional
Enrollment
10
Allocation
Randomized
Ages
18 Years to 55 Years
Sex
All
01

Study summary

The main purpose of this study is to learn about how food and a PPI (omeprazole) affect LOXO-305 in healthy participants. Participation could last about nine weeks.

02

Conditions studied

  • Healthy Volunteers
03

In context

Lead sponsor

Loxo Oncology, Inc. is the lead sponsor of 17 studies on the registry; 2 are open to participants now.

Of its 8 completed or terminated interventional studies of FDA-regulated products, 7 (88%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years to 55 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

Inclusion criteria

  • Males and females of non-childbearing potential.
  • Within body mass index (BMI) range 18.0 to 32.0 kilograms per square meter (kg/m²).
  • Participants will be in good general health, based on medical history, physical examination findings, vital signs, 12 lead electrocardiogram (ECG), or clinical laboratory tests, as determined by the Investigator (or designee).
  • Able to comply with all study procedures, including the 25-night stay at the Clinical Research Unit and follow-up phone call.

Exclusion criteria

Exclusion Criteria:

  • History or presence of any of the following, deemed clinically significant by the Investigator (or designee), and/or Sponsor:

    • liver disease
    • pancreatitis
    • peptic ulcer disease
    • intestinal malabsorption
    • gastric reduction surgery
    • history or presence of clinically significant cardiovascular disease.
  • Participants with out-of-range, at-rest vital signs.
  • Abnormal laboratory values determined to be clinically significant by the Investigator (or designee), and Sponsor.
  • Clinically significant abnormality, as determined by the Investigator (or designee), from physical examination.
  • Participation in any other investigational study drug trial involving administration of any investigational drug in the past 30 days or 5 half-lives, whichever was longer, prior to the first dose administration (Day 1).
  • Use or intention to use any prescription or over-the-counter medications within 14 days prior to the first dose administration (Day 1) through the end of the trial.
  • History or presence, upon clinical evaluation, of any illness that, in the opinion of the Investigator, would interfere with the ability to provide informed consent or comply with study instructions, or that might confound the interpretation of the study results, or put the participant at undue risk.
  • Donation of blood from 56 days prior to Screening, plasma or platelets from 4 weeks prior to Screening.
  • Receipt of blood products within 2 months prior to Check-in (Day -1).
  • Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, biliary, renal, hematological, pulmonary, cardiovascular (including any prior history of cardiomyopathy or cardiac failure), GI, neurological, or psychiatric disorder (as determined by the Investigator), or cancer within the past 5 years (except localized basal cell, squamous, or in situ cancer of the skin).
05

Study design

Phase
Phase 1
Primary purpose
Basic science
Allocation
Randomized
Intervention model
Crossover assignment
Masking
None (open label)
Enrollment
10 participants (actual)

Study arms

  • Experimental
    Treatment Sequence 1: ABC

    * Period 1: Single oral dose of 200 milligram (mg) LOXO-305 (Fasted state) on Day 1 (Treatment A) * Period 2: Single oral dose of 200 mg LOXO-305 (Fed state) on Day 8 (Treatment B) * Period 3: Single oral dose of 40 mg Omeprazole (Fasted state) on Day 15 to 17 and single oral dose of 200 mg LOXO-305 + 40 mg Omeprazole (Fasted state) on Day 18 (Treatment C) A washout period of 7 days was maintained between each treatment period.

    Drug: LOXO-305 · Drug: Omeprazole

  • Experimental
    Treatment Sequence 2: BAC

    * Period 1: Single oral dose of 200 mg LOXO-305 (Fed state) on Day 1 (Treatment B) * Period 2: Single oral dose of 200 mg LOXO-305 (Fasted state) on Day 8 (Treatment A) * Period 3: Single oral dose of 40 mg Omeprazole (Fasted state) on Day 15 to 17 and single oral dose of 200 mg LOXO-305 + 40 mg Omeprazole (Fasted state) on Day 18 (Treatment C) A washout period of 7 days was maintained between each treatment period.

    Drug: LOXO-305 · Drug: Omeprazole

Interventions

  • DrugLOXO-305

    LOXO-305 orally.

  • DrugOmeprazole

    Omeprazole Orally.

06

What researchers measure

Primary outcomes

  1. Pharmacokinetics (PK): Area Under the Concentration-time Curve From Hour 0 to 24 (AUC [0-24]) Hours of LOXO-305

    PK: AUC(0-24) hours of LOXO-305 is reported. AUC(0-24) was calculated by the linear trapezoidal method.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post LOXO-305 dose

  2. PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC[0-t]) of LOXO-305

    PK: AUC(0-t) of LOXO-305 is reported. AUC(0-t) was calculated by linear trapezoidal method.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose

  3. PK: Area Under the Concentration-time Curve Extrapolated to Infinity (AUC[0-Inf]) of LOXO-305

    PK: AUC(0-inf) of LOXO-305 is reported. AUC(0-inf) was calculated using the formula: AUC(0-inf) = AUC(0-t) + Ct/λZ; where Ct is the last measurable concentration and λZ is the apparent terminal elimination rate constant.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose

  4. PK: Percentage Extrapolation for AUC0-Inf (%AUCextrap) of LOXO-305

    PK: %AUCextrap of LOXO-305 is reported.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose

  5. PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305

    PK: Cmax of LOXO-305 is reported.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose

  6. PK: Time to Maximum Observed Plasma Concentration (Tmax) of LOXO-305

    PK: tmax of LOXO-305 is reported.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose

  7. PK: Apparent Terminal Elimination Half-life (t½) of LOXO-305

    PK: t½ of LOXO-305 is reported.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose

  8. PK: Apparent Systemic Clearance (CL/F) of LOXO-305

    PK: CL/F of LOXO-305 is reported.

    Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose

07

Results

Posted Jan 10, 2025

Participant flow

Participants were randomized to 2 treatment sequences (ABC and BAC), with each sequence having 3 periods where participants were crossed over between the periods in each sequence. A washout period of 7 days was maintained between each treatment period.

Period 1
Participant flow — Period 1
MilestoneTreatment Sequence 1: ABCTreatment Sequence 2: BAC
Started55
Received at least 1 dose of study drug55
Completed55
Not completed00
Period 2
Participant flow — Period 2
MilestoneTreatment Sequence 1: ABCTreatment Sequence 2: BAC
Started55
Completed55
Not completed00
Period 3
Participant flow — Period 3
MilestoneTreatment Sequence 1: ABCTreatment Sequence 2: BAC
Started55
Completed55
Not completed00

Outcome measures

PrimaryPharmacokinetics (PK): Area Under the Concentration-time Curve From Hour 0 to 24 (AUC [0-24]) Hours of LOXO-305

PK: AUC(0-24) hours of LOXO-305 is reported. AUC(0-24) was calculated by the linear trapezoidal method.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post LOXO-305 dose
Reported as:
Geometric mean · hour*nanograms per milliliter
Pharmacokinetics (PK): Area Under the Concentration-time Curve From Hour 0 to 24 (AUC [0-24]) Hours of LOXO-305
hour*nanograms per milliliterTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
Pharmacokinetics (PK): Area Under the Concentration-time Curve From Hour 0 to 24 (AUC [0-24]) Hours of LOXO-30555100 ± 17.551900 ± 12.859900 ± 15.5
PrimaryPK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC[0-t]) of LOXO-305

PK: AUC(0-t) of LOXO-305 is reported. AUC(0-t) was calculated by linear trapezoidal method.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose
Reported as:
Geometric mean · hour*nanograms per milliliter
PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC[0-t]) of LOXO-305
hour*nanograms per milliliterTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC[0-t]) of LOXO-30589400 ± 17.885100 ± 19.399600 ± 17.1
PrimaryPK: Area Under the Concentration-time Curve Extrapolated to Infinity (AUC[0-Inf]) of LOXO-305

PK: AUC(0-inf) of LOXO-305 is reported. AUC(0-inf) was calculated using the formula: AUC(0-inf) = AUC(0-t) + Ct/λZ; where Ct is the last measurable concentration and λZ is the apparent terminal elimination rate constant.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose
Reported as:
Geometric mean · hour*nanograms per milliliter
PK: Area Under the Concentration-time Curve Extrapolated to Infinity (AUC[0-Inf]) of LOXO-305
hour*nanograms per milliliterTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
PK: Area Under the Concentration-time Curve Extrapolated to Infinity (AUC[0-Inf]) of LOXO-30590200 ± 17.686100 ± 18.9101000 ± 16.8
PrimaryPK: Percentage Extrapolation for AUC0-Inf (%AUCextrap) of LOXO-305

PK: %AUCextrap of LOXO-305 is reported.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose
Reported as:
Geometric mean · percentage of extrapolation
PK: Percentage Extrapolation for AUC0-Inf (%AUCextrap) of LOXO-305
percentage of extrapolationTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
PK: Percentage Extrapolation for AUC0-Inf (%AUCextrap) of LOXO-3050.911 ± 27.21.12 ± 42.60.893 ± 34.5
PrimaryPK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305

PK: Cmax of LOXO-305 is reported.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose
Reported as:
Geometric mean · nanograms per milliliter
PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305
nanograms per milliliterTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-3055450 ± 31.74340 ± 16.65490 ± 16.7
PrimaryPK: Time to Maximum Observed Plasma Concentration (Tmax) of LOXO-305

PK: tmax of LOXO-305 is reported.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose
Reported as:
Median · hours
PK: Time to Maximum Observed Plasma Concentration (Tmax) of LOXO-305
hoursTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
PK: Time to Maximum Observed Plasma Concentration (Tmax) of LOXO-3052.50 (1.50 to 4.00)3.00 (1.00 to 4.00)2.25 (1.50 to 3.00)
PrimaryPK: Apparent Terminal Elimination Half-life (t½) of LOXO-305

PK: t½ of LOXO-305 is reported.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose
Reported as:
Mean · hours
PK: Apparent Terminal Elimination Half-life (t½) of LOXO-305
hoursTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
PK: Apparent Terminal Elimination Half-life (t½) of LOXO-30520.2 ± 4.2421.5 ± 5.7519.7 ± 2.87
PrimaryPK: Apparent Systemic Clearance (CL/F) of LOXO-305

PK: CL/F of LOXO-305 is reported.

Time frame:
Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post LOXO-305 dose
Reported as:
Geometric mean · Liter per Hours (L/h)
PK: Apparent Systemic Clearance (CL/F) of LOXO-305
Liter per Hours (L/h)Treatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)
PK: Apparent Systemic Clearance (CL/F) of LOXO-3052.22 ± 17.62.32 ± 18.91.99 ± 16.8

Adverse events

Collected over Day 1 up to Day 32. Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Treatment A: 200 mg LOXO-305 (Fasted)0/10 (0%)0/10 (0%)0/10 (0%)
Treatment B: 200 mg LOXO-305 (Fed)0/10 (0%)0/10 (0%)1/10 (10%)
Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)0/10 (0%)0/10 (0%)0/10 (0%)
Treatment C: 40 mg Omeprazole (Fasted)0/10 (0%)0/10 (0%)0/10 (0%)
Most frequent other events
Most frequent other events
EventTreatment A: 200 mg LOXO-305 (Fasted)Treatment B: 200 mg LOXO-305 (Fed)Treatment C: 200 mg LOXO-305 + 40 mg Omeprazole (Fasted)Treatment C: 40 mg Omeprazole (Fasted)
NauseaGastrointestinal disorders0/101/100/100/10
VomitingGastrointestinal disorders0/101/100/100/10
HeadacheNervous system disorders0/101/100/100/10

Baseline characteristics

All participants who received at least one dose of study drug.

Age, Continuous
Age, Continuous(years)Treatment Sequence 1: ABCTreatment Sequence 2: BACTotal
Mean43.2 ± 10.6635.2 ± 4.8739.2 ± 8.88
Sex: Female, Male
Sex: Female, Male(Participants)Treatment Sequence 1: ABCTreatment Sequence 2: BACTotal
Female123
Male437
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)Treatment Sequence 1: ABCTreatment Sequence 2: BACTotal
Hispanic or Latino336
Not Hispanic or Latino224
Unknown or Not Reported000
Race (NIH/OMB)
Race (NIH/OMB)(Participants)Treatment Sequence 1: ABCTreatment Sequence 2: BACTotal
American Indian or Alaska Native000
Asian000
Native Hawaiian or Other Pacific Islander000
Black or African American112
White448
More than one race000
Unknown or Not Reported000
Region of Enrollment
Region of Enrollment(Participants)Treatment Sequence 1: ABCTreatment Sequence 2: BACTotal
United States5510
08

Study locations

1 site
  • Covance Clinical Research Unit
    Daytona Beach, Florida 32117, United States
09

References and documents

Study documents

  • Study protocol · Jan 29, 2020
  • Statistical analysis plan · May 21, 2020

Documents are hosted by the registry — open the source record to download them.

Individual participant data

Plan to share: No

10

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jan 10, 2025, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
11

Registry details

Key details

Study ID
NCT05134350
Lead sponsor
Loxo Oncology, Inc.
Responsible party
Sponsor
First posted
Nov 24, 2021
Start date
Feb 6, 2020
Primary completion
Mar 23, 2020
Completion
Mar 23, 2020
Results posted
Jan 10, 2025
Last update
Jan 10, 2025

Study contacts

Renée Ward, MD, PhD
study director · Loxo Oncology, Inc.

Oversight

Data monitoring committee
No
FDA-regulated drug
Yes
FDA-regulated device
No
View the source record on ClinicalTrials.gov ↗

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This study is completed, as verified in Nov 2024. You cannot join it, but the record below documents what was studied.

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