Healthy VolunteersPhase 1NCT05134337

Study of the Effects of Itraconazole and Rifampin on LOXO-305 in Healthy Participants

A Phase 1 study testing LOXO-305, Itraconazole and Rifampin in people with Healthy Volunteers, run by Loxo Oncology, Inc. at 1 site in United States.

Completed

Finished. The study has ended and is not enrolling. Results may be posted on the official record.

Official record

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Trial summary

The main purpose of this study is to learn about how itraconazole and rifampin affect LOXO-305 in healthy participants. Participation could last about 8 weeks. Read more about this study

Who is it for?: Ages 18 to 55 yearsHealthy volunteers can take part
Conditions the study is for: Healthy Volunteers
What is being tested?: LOXO-305, Itraconazole and Rifampin
Type of treatment: Pill or oral medicine
Could I receive a placebo?: No, everyone receives an active treatment
How many people: 27 participants
Where: 1 siteUnited States
Study dates: 12 Feb 2020to 30 Oct 2020
Phase: Phase 1
Are there results?: Yes, posted in the registrySummary in the doctors' view

Key requirements

Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.

Ages 18 to 55 years
All sexes
Healthy volunteers accepted
Adult

Who may be able to join

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 19-night stay for those participating in Part 1 or 24-night stay for those participating in Part 2 at the Clinical Research Unit and follow-up phone call.

Who cannot join

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

Show all 16Show fewer

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).
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) and through end of 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), gastrointestinal (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).

Trial locations and contacts

1 site in 1 country.

United States1 site

Covance Clinical Research Unit
Daytona Beach, Florida, 32117

Other trials in United States

About this study

Official title: A Phase 1, Open Label, Two-part, Fixed-sequence Drug Interaction Study to Investigate the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and CYP3A4 Inducer (Rifampin) on the Pharmacokinetics of LOXO 305 in Healthy Adult Subjects

The main purpose of this study is to learn about how itraconazole and rifampin affect LOXO-305 in healthy participants. Participation could last about 8 weeks.

Conditions: Healthy Volunteers
Being tested: LOXO-305, Itraconazole, Rifampin

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

LOXO-305Drug
Also called Pirtobrutinib
Oral LOXO-305
ItraconazoleDrug
Oral itraconazole
RifampinDrug
Oral rifampin

Study groups in NCT05134337
Study group	Role	What they receive
Part 1 (LOXO-305/Itraconazole)	Experimental	* Day 1: a single oral dose of 200 milligrams (mg) LOXO-305 was administered. * Day 8: oral doses of 200 mg itraconazole was administered twice daily. * Days 9 to 18: single oral dose of 200 mg itraconazole was administered once daily, and on Day 12 it was co-administered with a single oral dose of 200 mg LOXO-305. Receives: Drug: LOXO-305; Drug: Itraconazole
Part 2 (LOXO 305/Rifampin)	Experimental	* Day 1: a single oral dose of 200 mg LOXO-305 was administered. * Days 8 to 23: oral dose of 600 mg rifampin was administered once daily, and on Days 8 \& 17, it was co-administered with a single oral dose of 200 mg LOXO-305. Receives: Drug: LOXO-305; Drug: Rifampin

What is being measured

The primary outcome is the main question the study is designed to answer.

Part 1: Pharmacokinetics (PK): Maximum Observed Plasma Concentration (Cmax) of LOXO-305
Cmax of LOXO-305
Measured: 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 postdose on days 1 and 12
Part 1: PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of LOXO 305
PK: AUC0-t of LOXO 305
Measured: 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 postdose on days 1 and 12
Part 1: PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of LOXO-305
AUC0-inf of LOXO-305
Measured: 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 postdose on days 1 and 12
Part 2: PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305
Cmax of LOXO-305
Measured: 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 postdose on days 1 and 17; Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose on day 8
Part 2: PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of LOXO 305
PK: AUC0-t of LOXO 305
Measured: 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 postdose on days 1 and 17; Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose on day 8
Part 2: PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of LOXO-305
AUC0-inf of LOXO-305
Measured: 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 postdose on days 1 and 17
Part 2: PK: Area Under the Concentration Versus Time Curve From Time Zero to 24 Hours Postdose (AUC0-24) of LOXO-305
AUC0-24 of LOXO-305
Measured: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose on days 1 and 8

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

12 Feb 202030 Oct 2020

First posted24 Nov 2021
Study start12 Feb 2020
Primary completion30 Oct 2020
Study completion30 Oct 2020

Resources

Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
Posted resultsParticipant flow, outcome measures and adverse events reported by the sponsor.
Other trials for Healthy VolunteersStudies of the same condition, open and under way.
What the trial phases meanHow a treatment moves from first tests in people to approval.

More details

For doctors and researchers: how the study is designed, who runs it, and its registry IDs.

Study design

Study type: Interventional
Phase: Phase 1
Primary purpose: Basic science
Allocation: Non-randomised
Intervention model: Sequential
Masking: None (open label)
Enrolment: 27 participants (actual)

IDs, dates and publications

ClinicalTrials.gov ID: NCT05134337
Sponsor's protocol ID: LOXO-BTK-20006
Other IDs: J2N-OX-JZNC
Status last verified: Nov 2024
First submitted: 22 Oct 2021
Last updated: 9 Jan 2025
Results posted: Yes, on ClinicalTrials.gov
Data monitoring committee: No
FDA-regulated drug: Yes
FDA-regulated device: No
Individual data sharing: No

Want to know more?

The sponsor has not listed a contact. The official record may have more details.

Talk to your doctor first and take this page with you. Only the study team can confirm whether you can join.

Questions to ask the study team

What is the study trying to find out?
What would I need to do, and how often would I visit?
Could I receive a placebo instead of the treatment?
What are the possible risks and benefits for me?
Will it cost me anything? Are travel or time paid for?
Can I keep seeing my own doctor during the study?
What happens when the study ends?

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Study at a glance

From the registry record, last updated by the sponsor on 9 Jan 2025. Recruitment status is as the sponsor reported it: confirm with the study team.

Official title: A Phase 1, Open Label, Two-part, Fixed-sequence Drug Interaction Study to Investigate the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and CYP3A4 Inducer (Rifampin) on the Pharmacokinetics of LOXO 305 in Healthy Adult Subjects
ClinicalTrials.gov ID: NCT05134337
Acronym / sponsor ID: LOXO-BTK-20006
Conditions: Healthy Volunteers
Phase: Phase 1
Study type: Interventional
Recruitment status: Completed
Enrolment: 27 participants (actual)
Lead sponsor: Loxo Oncology, Inc.Industry (pharma, biotech, devices)
Study start: 12 Feb 2020 (actual)
Primary completion: 30 Oct 2020 (actual)
Study completion: 30 Oct 2020 (actual)
First posted: 24 Nov 2021 (actual)
Results: Posted 9 Jan 2025

Clinical summary

The research question as the sponsor registered it. This describes what the study plans to test, not what it found.

The main purpose of this study is to learn about how itraconazole and rifampin affect LOXO-305 in healthy participants. Participation could last about 8 weeks.

Study design

Primary purpose: Basic science
Allocation: Non-randomised
Intervention model: Sequential
Masking: None (open label)
Number of arms: 2

Arm	Type	Receives
Part 1 (LOXO-305/Itraconazole)	Experimental	Drug: LOXO-305, Drug: Itraconazole* Day 1: a single oral dose of 200 milligrams (mg) LOXO-305 was administered. * Day 8: oral doses of 200 mg itraconazole was administered twice daily. * Days 9 to 18: single oral dose of 200 mg itraconazole was administered once daily, and on Day 12 it was co-administered with a single oral dose of 200 mg LOXO-305.
Part 2 (LOXO 305/Rifampin)	Experimental	Drug: LOXO-305, Drug: Rifampin* Day 1: a single oral dose of 200 mg LOXO-305 was administered. * Days 8 to 23: oral dose of 600 mg rifampin was administered once daily, and on Days 8 \& 17, it was co-administered with a single oral dose of 200 mg LOXO-305.

Who may qualify

Ages: 18 to 55 years
Sex: All
Healthy volunteers: Accepted
Age groups: Adult

Key inclusion criteria (4 listed)

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 19-night stay for those participating in Part 1 or 24-night stay for those participating in Part 2 at the Clinical Research Unit and follow-up phone call.

Key exclusion criteria (16 listed)

History or presence of any of the following, deemed clinically significant by the Investigator (or designee), and/or Sponsor:
Participants with out-of-range, at-rest vital signs.
Abnormal laboratory values determined to be clinically significant by the Investigator (or designee).
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).

Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.

Interventions

Intervention	Type	Arms
LOXO-305Also: PirtobrutinibOral LOXO-305	Drug	Part 1 (LOXO-305/Itraconazole), Part 2 (LOXO 305/Rifampin)
ItraconazoleOral itraconazole	Drug	Part 1 (LOXO-305/Itraconazole)
RifampinOral rifampin	Drug	Part 2 (LOXO 305/Rifampin)

Primary outcome

Part 1: Pharmacokinetics (PK): Maximum Observed Plasma Concentration (Cmax) of LOXO-305
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 postdose on days 1 and 12
Cmax of LOXO-305
Part 1: PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of LOXO 305
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 postdose on days 1 and 12
PK: AUC0-t of LOXO 305
Part 1: PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of LOXO-305
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 postdose on days 1 and 12
AUC0-inf of LOXO-305
Part 2: PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305
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 postdose on days 1 and 17; Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose on day 8
Cmax of LOXO-305
Part 2: PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of LOXO 305
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 postdose on days 1 and 17; Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose on day 8
PK: AUC0-t of LOXO 305
Part 2: PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of LOXO-305
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 postdose on days 1 and 17
AUC0-inf of LOXO-305
Part 2: PK: Area Under the Concentration Versus Time Curve From Time Zero to 24 Hours Postdose (AUC0-24) of LOXO-305
Time frame: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose on days 1 and 8
AUC0-24 of LOXO-305

Results and safety

Results posted to the registry on 9 Jan 2025, as reported by the sponsor. Figures are copied from the record, not re-analysed. Full results on ClinicalTrials.gov.

Participant flow

Group	Started	Completed
Part 1 (LOXO-305/Itraconazole)	15	12
Part 2 (LOXO 305/Rifampin)	12	12

Primary outcome: Part 1: Pharmacokinetics (PK): Maximum Observed Plasma Concentration (Cmax) of LOXO-305

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 postdose on days 1 and 12. Geometric mean (Geometric Coefficient of Variation). Unit: nanogram per milliliter (ng/mL)

Measure	Part 1 (LOXO-305/Itraconazole) n = 15
Day 1	4000 (23.5)
Day 12	4100 (17.2)

Population analysed: All part 1 participants who received a dose of LOXO-305 on day 1, itraconazole with LOXO-305 on day 12, had at least one quantifiable plasma concentration of LOXO-305, and had at least one PK parameter computed for the specified timepoints. Participants were excluded from the analysis if they experienced an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).

Primary outcome: Part 1: PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of LOXO 305

Measure	Part 1 (LOXO-305/Itraconazole) n = 15
Day 1	80000 (23.4)
Day 12	122000 (22.7)

Primary outcome: Part 1: PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of LOXO-305

Measure	Part 1 (LOXO-305/Itraconazole) n = 15
Day 1	80800 (23.4)
Day 12	123000 (23.4)

Primary outcome: Part 2: PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305

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 postdose on days 1 and 17; Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose on day 8. Geometric mean (Geometric Coefficient of Variation). Unit: nanogram per milliliter (ng/mL)

Measure	Part 2 (LOXO 305/Rifampin) n = 12
Day 1	4480 (20.4)
Day 8	4170 (15.6)
Day 17	2580 (22.4)

Population analysed: All part 2 participants who received a dose of LOXO-305 on day 1, rifampin with LOXO-305 on day 8 and day 17, had at least one quantifiable plasma concentration of LOXO-305, and had at least one PK parameter computed for the specified timepoints. Participants were excluded from the analysis if they experienced an AE of vomiting that occurred at or before 2 times the median Tmax.

Adverse events

Time frame: Baseline to Follow-up (up to day 28 for Part 1; up to day 33 for Part 2). Other adverse events reported at 5% frequency or more

Group	Serious adverse events	Other adverse events	Deaths
Part 1: 200 mg LOXO-305 Alone	0 of 15 (0%)	0 of 15 (0%)	0 of 15
Part 1: 200 mg Itraconazole Alone	0 of 12 (0%)	2 of 12 (16.7%)	0 of 12
Part 1: 200 mg LOXO-305 + 200 mg Itraconazole	0 of 12 (0%)	1 of 12 (8.3%)	0 of 12
Part 2: 200 mg LOXO-305 Alone	0 of 12 (0%)	0 of 12 (0%)	0 of 12
Part 2: 200 mg LOXO-305 (Day 8) + 600 mg Rifampin	0 of 12 (0%)	0 of 12 (0%)	0 of 12
Part 2: 200 mg LOXO-305 (Day 17) + 600 mg Rifampin	0 of 12 (0%)	1 of 12 (8.3%)	0 of 12

Loading the posted results from ClinicalTrials.gov…

Research links

Official record on ClinicalTrials.govLast updated by the sponsor 9 Jan 2025.
Posted resultsParticipant flow, baseline, all outcome measures and adverse events.
Individual participant dataSharing planned: No

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Referral and contact

AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.

Renée Ward, MD, PhD study director

Loxo Oncology, Inc.

1 site in 1 country: see every site and its status.

Questions about this trial

What is this clinical trial studying?

A Phase 1 study testing LOXO-305, Itraconazole and Rifampin in people with Healthy Volunteers, run by Loxo Oncology, Inc. at 1 site in United States.

The full registered description is in the About this study section and the official record.

Who may be eligible to take part?

The sponsor lists 4 inclusion and 16 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.

Is this clinical trial currently recruiting?

The record says: finished, as of the sponsor's last update on 9 Jan 2025. Status can change between updates, so confirm with the study contact before making plans.

Where is the study taking place?

The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.

What are the possible benefits and risks?

They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

What does this phase mean?

Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.

Not every study follows the same path, and some studies (observational studies, device studies) have no phase.

Are results available for this study?

Yes. Results are posted in the registry (first posted 9 Jan 2025). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.

How can a doctor refer a patient or contact the research team?

The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.

What does the primary outcome measure?

Part 1: Pharmacokinetics (PK): Maximum Observed Plasma Concentration (Cmax) of LOXO-305 (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 postdose on days 1 and 12). The study lists 7 primary outcomes in all. It is what the study was designed to measure, not a finding.

Where can I read the original study information?

On the ClinicalTrials.gov record for NCT05134337.

Does a listing mean the treatment is approved or proven to work?

No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.

How often is this information updated?

AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 9 Jan 2025.