Healthy VolunteersPhase 1NCT04202497

A Study With [18F]MNI-1054 to Determine Lysine -Specific Demethylase 1A (LSD1) Brain Enzyme Occupancy of TAK-418 After Single-Dose Oral Administration in Healthy Participants

A Phase 1 study testing TAK-418 and [18F]MNI-1054 (radiotracer) in people with Healthy Volunteers, run by Takeda at 1 site in United States.

Terminated

Stopped early. The study ended before it was planned to and will not resume.

Official record

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Trial summary

The purpose of this study is to determine brain LSD1 enzyme occupancy and the relationship of occupancy to TAK-418 dose and plasma exposure after single oral dosing of TAK-418 in healthy participants using [18F]MNI-1054 positron emission tomography (PET) imaging. Read more about this study

Who is it for?: Ages 18 to 65 yearsHealthy volunteers can take part
Conditions the study is for: Healthy Volunteers
What is being tested?: TAK-418 and [18F]MNI-1054 (radiotracer)
Type of treatment: Pill or oral medicine, Injection or infusion
Could I receive a placebo?: No, everyone receives an active treatment
How many people: 7 participants
Where: 1 siteUnited States
Study dates: 18 Dec 2019to 19 Mar 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 65 years
All sexes
Healthy volunteers accepted
Adult, Older adult

Who may be able to join

The participant must have a body mass index (BMI) greater than or equal to (>=) 18.5 and less than or equal to (<=) 30.0 kilogram per square meter (kg/m^2) at the screening visit.
The participant must be a current nonsmoker at screening as demonstrated by negative cotinine test.
The participant has adequate circulation to both hands for safe placement of arterial lines (as determined by Allen's test).

Who cannot join

Has a known hypersensitivity to any component of the formulation of TAK-418 or related compounds, including [18F]MNI-1054.
The participant has a positive alcohol or drug screen.
The participant has a history of alcohol consumption exceeding 2 standard drinks per day on average (1 glass is approximately equivalent to the following: beer [354 milliliter (mL)/12 ounce (oz)], wine [118 mL/4 oz], or distilled spirits [29.5 mL/1 oz] per day).
The participant consumes excessive amounts, defined as greater than 6 servings (1 serving is approximately equivalent to 120 mg of caffeine) of coffee, tea, cola, energy drinks, or other caffeinated beverages per day.
The participant has a substance abuse disorder.
The participant cannot tolerate venipuncture or has poor venous access that would cause difficulty in collecting blood samples.

Show all 12Show fewer

The participant has contraindications to undergoing magnetic resonance imaging (MRI) examination including but not limited to implants, such as implanted cardiac pacemakers or defibrillators, insulin pumps, cochlear implants, metallic ocular foreign body, implanted neural stimulators, central nervous system aneurysm clips, and other medical implants that have not been certified for MRI, or history of claustrophobia in MRI.
The participant has clinically significant abnormal findings on brain MRI scan that in the opinion of the investigator may interfere with the interpretation of the PET imaging.
The participant has experienced an acute illness within 10 days before the screening visit.
The participant has a risk of suicide according to the investigator's clinical judgement per the Columbia-Suicide Severity Rating Scale at screening or has made a suicide attempt in the 12 months before screening.
The participant has luteinizing hormone, follicle stimulating hormone (FSH), or estradiol levels that are clinically abnormal.
The participant has existing skin rashes that can be diagnosed as dermatitis.

Trial locations and contacts

1 site in 1 country.

United States1 site

Invicro, A Konica Minolta Company
New Haven, Connecticut, 06510

Other trials in United States

About this study

Official title: A Phase 1, Open-label, Positron Emission Tomography Study With [18F]MNI-1054 to Determine Lysine-Specific Demethylase 1A Brain Enzyme Occupancy of TAK-418 After Single-Dose Oral Administration in Healthy Subjects

Read the detailed description

The drug being tested in this study is called TAK-418. TAK-418 is being tested to determine the relationship between brain LSD1 enzyme occupancy and TAK-418 plasma concentration. This study will utilize the PET radiotracer [18F]MNI-1054 to evaluate the brain LSD1 enzyme occupancy of TAK-418 after single dose oral administration in healthy adult participants.

The study will enroll approximately 16 participants. The TAK-418 starting dose is 1.5 mg, given on Day 1. Each participant will receive one dose of TAK-418 and up to 3 dynamic [18F]MNI-1054 PET scans to assess enzyme occupancy on baseline, Day 1 and Day 2 or 3 post-TAK-418 dosing.

This single center trial will be conducted in the United States. The overall time to participate in this study is 62 days. Participants will be followed up on Day 14 for follow-up safety assessments.

Conditions: Healthy Volunteers
Being tested: TAK-418, [18F]MNI-1054 (radiotracer)
Keywords: Drug Therapy

What participants receive

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

TAK-418Drug
TAK-418 orally.
[18F]MNI-1054 (radiotracer)Drug
[18F]MNI-1054 injection.

Study groups in NCT04202497
Study group	Role	What they receive
TAK-418 1.5 mg	Experimental	TAK-418 1.5 milligram (mg), orally, once on Day 1. Participants will also receive 10 millicurie (mCi) of [18F]MNI-1054 injection intravenously, prior to each PET scans on Day -1, Day 1, and either on Day 2 or 3. Dose levels for subsequent participants may vary based on available review of imaging and pharmacokinetics (PK) data. Receives: Drug: TAK-418; Drug: [18F]MNI-1054 (radiotracer)

What is being measured

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

Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models At Baseline Scan on Day -1
Enzyme binding parameter [Ki] was obtained from irreversible 2-tissue compartment model (mL/cm^3/min). Data is reported for the following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum. Here, mL/cm^3/min signifies 'milliliter per cubic centimeter per minute'.
Measured: Day -1
Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models on Day 1
Enzyme binding parameter [Ki] was obtained from irreversible 2-tissue compartment model (mL/cm^3/min). Data is reported for the following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum. Here, mL/cm^3/min signifies 'milliliter per cubic centimeter per minute'.
Measured: Day 1
Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models on Day 2
Enzyme binding parameter [Ki] was obtained from irreversible 2-tissue compartment model (mL/cm^3/min). Data is reported for the following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum. Here, mL/cm^3/min signifies 'milliliter per cubic centimeter per minute'.
Measured: Day 2
Percent Enzyme Occupancy Based on Quantitative Estimates of Binding for TAK-418 on Day 1
Lysine-Specific Demethylase 1A (LSD1) enzyme occupancy (%) in region of interest (ROI) after a single dose of TAK-418 was obtained from the baseline and postdose Ki values as follows: occupancy (1st postdose) = 100*(Ki [baseline] - Ki [1st postdose]) / Ki (baseline). Data is reported for following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum.
Measured: Day 1
Percent Enzyme Occupancy Based on Quantitative Estimates of Binding for TAK-418 on Day 2
LSD1 enzyme occupancy (%) in ROI after a single dose of TAK-418 was obtained from the baseline and postdose Ki values as follows: occupancy (2nd postdose) = 100*(Ki [baseline] - Ki [2nd postdose]) / Ki (baseline). Data is reported for following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum.
Measured: Day 2
Cmax: Maximum Observed Plasma Concentration for TAK-418
Measured: Day 1: pre-dose and at multiple time points (up to 3 hours) post-dose, immediately before and after the Day 1 PET scan, and within 30 minutes before and 30 minutes after Day 2 or 3 PET scan
AUClast: Area Under the Plasma Concentration-time Curve (AUC) From Time 0 to Time of the Last Quantifiable Concentration for TAK-418
Measured: Day 1: pre-dose and at multiple time points (up to 3 hours) post-dose, immediately before and after the Day 1 PET scan, and within 30 minutes before and 30 minutes after Day 2 or 3 PET scan
AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-418
Measured: Day 1: pre-dose and at multiple time points (up to 3 hours) post-dose, immediately before and after the Day 1 PET scan, and within 30 minutes before and 30 minutes after Day 2 or 3 PET scan

Secondary outcomes (4)

ED50 PET Enzyme Occupancy
The relationship between PET enzyme occupancy and TAK-418 dose level was investigated using an Emax model containing the regression parameters maximal target occupancy (Emax) and dose that gives 50 percent (%) of Emax (ED50). ED50 values are reported for following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum. The data tabulated are the estimated value and confidence intervals of the ED50 value derived from an Emax model fit across all data points from all arms. ED50 is the dose at which 50% enzyme occupancy is expected.
Measured: Days 1 to 2
Number of Participants Reporting One or More Adverse Events (AEs) and Serious Adverse Events (SAEs)
Measured: From first dose of [18F]MNI-1054 radiotracer injection up to Day 14
Number of Participants With Clinically Significant Abnormal Laboratory Values
Measured: From first dose of [18F]MNI-1054 radiotracer injection up to Day 14
Number of Participants With Clinically Significant Abnormal Vital Signs
Measured: From first dose of [18F]MNI-1054 radiotracer injection up to Day 14

Timeline

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

18 Dec 201919 Mar 2020

First posted17 Dec 2019
Study start18 Dec 2019
Primary completion5 Mar 2020
Study completion19 Mar 2020

Why it stopped: Study was prematurely terminated because of administrative reasons.

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.
Publications (2)Papers the sponsor has linked to this study.
Other trials for Healthy VolunteersStudies of the same condition, open and under way.
More trials run by TakedaThe sponsor's other registered studies.
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: Other
Allocation: Not applicable
Intervention model: Single group
Masking: None (open label)
Enrolment: 7 participants (actual)

IDs, dates and publications

ClinicalTrials.gov ID: NCT04202497
Sponsor's protocol ID: TAK-418-0004
Other IDs: U1111-1242-8485
Status last verified: Jul 2021
First submitted: 12 Dec 2019
Last updated: 30 Jul 2021
Results posted: Yes, on ClinicalTrials.gov
Data monitoring committee: No
FDA-regulated drug: Yes
FDA-regulated device: No
Individual data sharing: Yes: Takeda provides access to the de-identified individual participant data (IPD) for eligible studies to aid qualified researchers in addressing legitimate scientific objectives (Takeda's data sharing commitment is available on https://clinicaltrials.takeda.com/takedas-commitment?commitment=5). These IPDs will be provided in a secure research environment following approval of a data sharing request, and under the terms of a data sharing agreement.

Publications

Schwarz AJ, Sandiego CM, Constantinescu C, Takano A, McQuade P, Tauscher J, Daegele N, Marek K, Gunn RN, Madonia J, Russell DS. [18F]MNI-1054, a novel PET ligand for lysine-specific histone demethylase 1 A (LSD1): first-in human validation and enzyme occupancy of the LSD1 inhibitor TAK-418. EJNMMI Res. 2026 Jul 3. doi: 10.1186/s13550-026-01477-x. Online ahead of print.
PubMed 42397656
Matsuda S, Hattori Y, Kimura H. Drug discovery strategy for TAK-418, a specific inhibitor of LSD1 enzyme activity, as a novel therapy for autism. Adv Pharmacol. 2025;102:267-300. doi: 10.1016/bs.apha.2024.10.017. Epub 2024 Oct 29.
PubMed 39929582

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 30 Jul 2021. Recruitment status is as the sponsor reported it: confirm with the study team.

Official title: A Phase 1, Open-label, Positron Emission Tomography Study With [18F]MNI-1054 to Determine Lysine-Specific Demethylase 1A Brain Enzyme Occupancy of TAK-418 After Single-Dose Oral Administration in Healthy Subjects
ClinicalTrials.gov ID: NCT04202497
Acronym / sponsor ID: TAK-418-0004
Conditions: Healthy Volunteers
Keywords: Drug Therapy
Phase: Phase 1
Study type: Interventional
Recruitment status: TerminatedReason stopped: Study was prematurely terminated because of administrative reasons.
Enrolment: 7 participants (actual)
Lead sponsor: TakedaIndustry (pharma, biotech, devices)
Study start: 18 Dec 2019 (actual)
Primary completion: 5 Mar 2020 (actual)
Study completion: 19 Mar 2020 (actual)
First posted: 17 Dec 2019 (actual)
Results: Posted 30 Jul 2021

Clinical summary

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

Detailed description

This single center trial will be conducted in the United States. The overall time to participate in this study is 62 days. Participants will be followed up on Day 14 for follow-up safety assessments.

Study design

Primary purpose: Other
Allocation: Not applicable
Intervention model: Single group
Masking: None (open label)
Number of arms: 1

Arm	Type	Receives
TAK-418 1.5 mg	Experimental	Drug: TAK-418, Drug: [18F]MNI-1054 (radiotracer)TAK-418 1.5 milligram (mg), orally, once on Day 1. Participants will also receive 10 millicurie (mCi) of [18F]MNI-1054 injection intravenously, prior to each PET scans on Day -1, Day 1, and either on Day 2 or 3. Dose levels for subsequent participants may vary based on available review of imaging and pharmacokinetics (PK) data.

Who may qualify

Ages: 18 to 65 years
Sex: All
Healthy volunteers: Accepted
Age groups: Adult, Older adult

Key inclusion criteria (3 listed)

The participant must have a body mass index (BMI) greater than or equal to (>=) 18.5 and less than or equal to (<=) 30.0 kilogram per square meter (kg/m^2) at the screening visit.
The participant must be a current nonsmoker at screening as demonstrated by negative cotinine test.
The participant has adequate circulation to both hands for safe placement of arterial lines (as determined by Allen's test).

Key exclusion criteria (12 listed)

Has a known hypersensitivity to any component of the formulation of TAK-418 or related compounds, including [18F]MNI-1054.
The participant has a positive alcohol or drug screen.
The participant has a history of alcohol consumption exceeding 2 standard drinks per day on average (1 glass is approximately equivalent to the following: beer [354 milliliter (mL)/12 ounce (oz)], wine [118 mL/4 oz], or distilled spirits [29.5 mL/1 oz] per day).
The participant consumes excessive amounts, defined as greater than 6 servings (1 serving is approximately equivalent to 120 mg of caffeine) of coffee, tea, cola, energy drinks, or other caffeinated beverages per day.
The participant has a substance abuse disorder.

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
TAK-418TAK-418 orally.	Drug	TAK-418 1.5 mg
[18F]MNI-1054 (radiotracer)[18F]MNI-1054 injection.	Drug	TAK-418 1.5 mg

Primary outcome

Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models At Baseline Scan on Day -1
Time frame: Day -1
Enzyme binding parameter [Ki] was obtained from irreversible 2-tissue compartment model (mL/cm^3/min). Data is reported for the following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum. Here, mL/cm^3/min signifies 'milliliter per cubic centimeter per minute'.
Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models on Day 1
Time frame: Day 1
Enzyme binding parameter [Ki] was obtained from irreversible 2-tissue compartment model (mL/cm^3/min). Data is reported for the following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum. Here, mL/cm^3/min signifies 'milliliter per cubic centimeter per minute'.
Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models on Day 2
Time frame: Day 2
Enzyme binding parameter [Ki] was obtained from irreversible 2-tissue compartment model (mL/cm^3/min). Data is reported for the following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum. Here, mL/cm^3/min signifies 'milliliter per cubic centimeter per minute'.
Percent Enzyme Occupancy Based on Quantitative Estimates of Binding for TAK-418 on Day 1
Time frame: Day 1
Lysine-Specific Demethylase 1A (LSD1) enzyme occupancy (%) in region of interest (ROI) after a single dose of TAK-418 was obtained from the baseline and postdose Ki values as follows: occupancy (1st postdose) = 100*(Ki [baseline] - Ki [1st postdose]) / Ki (baseline). Data is reported for following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum.
Percent Enzyme Occupancy Based on Quantitative Estimates of Binding for TAK-418 on Day 2
Time frame: Day 2
LSD1 enzyme occupancy (%) in ROI after a single dose of TAK-418 was obtained from the baseline and postdose Ki values as follows: occupancy (2nd postdose) = 100*(Ki [baseline] - Ki [2nd postdose]) / Ki (baseline). Data is reported for following brain regions: cerebellum, frontal lobe, hippocampus, occipital Lobe, pons, and striatum.
Cmax: Maximum Observed Plasma Concentration for TAK-418
Time frame: Day 1: pre-dose and at multiple time points (up to 3 hours) post-dose, immediately before and after the Day 1 PET scan, and within 30 minutes before and 30 minutes after Day 2 or 3 PET scan
AUClast: Area Under the Plasma Concentration-time Curve (AUC) From Time 0 to Time of the Last Quantifiable Concentration for TAK-418
Time frame: Day 1: pre-dose and at multiple time points (up to 3 hours) post-dose, immediately before and after the Day 1 PET scan, and within 30 minutes before and 30 minutes after Day 2 or 3 PET scan
AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-418
Time frame: Day 1: pre-dose and at multiple time points (up to 3 hours) post-dose, immediately before and after the Day 1 PET scan, and within 30 minutes before and 30 minutes after Day 2 or 3 PET scan

4 secondary outcomes

ED50 PET Enzyme Occupancy
Time frame: Days 1 to 2
Number of Participants Reporting One or More Adverse Events (AEs) and Serious Adverse Events (SAEs)
Time frame: From first dose of [18F]MNI-1054 radiotracer injection up to Day 14
Number of Participants With Clinically Significant Abnormal Laboratory Values
Time frame: From first dose of [18F]MNI-1054 radiotracer injection up to Day 14
Number of Participants With Clinically Significant Abnormal Vital Signs
Time frame: From first dose of [18F]MNI-1054 radiotracer injection up to Day 14

Results and safety

Results posted to the registry on 30 Jul 2021, as reported by the sponsor. Figures are copied from the record, not re-analysed. Full results on ClinicalTrials.gov.

Participant flow

Group	Started	Completed
Baseline [18F]MNI-1054	7	6
TAK-418 1.5 mg	0	0
TAK-418 10 mg	0	0
TAK-418 30 mg	0	0

Primary outcome: Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models At Baseline Scan on Day -1

Time frame: Day -1. Mean (Standard Deviation). Unit: mL/cm^3/min

Measure	TAK-418 1.5 mg n = 2	TAK-418 10 mg n = 2	TAK-418 30 mg n = 2
Cerebellum	0.03405 (0.002192)	0.03515 (0.005869)	0.03560 (0.003394)
Frontal Lobe	0.01930 (0.004525)	0.02070 (0.004384)	0.02140 (0.002263)
Hippocampus	0.01900 (0.000141)	0.01935 (0.005303)	0.01960 (0.001414)
Occipital Lobe	0.02140 (0.002404)	0.02225 (0.003606)	0.02365 (0.002616)
Pons	0.01685 (0.000071)	0.01855 (0.004313)	0.01870 (0.004667)
Striatum	0.01575 (0.004031)	0.01930 (0.004950)	0.01995 (0.003323)

Population analysed: The pharmacodynamics (PD) set included all participants who received TAK-418 and have at least 1 analyzable PET Scan following TAK-418.

Primary outcome: Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models on Day 1

Time frame: Day 1. Mean (Standard Deviation). Unit: mL/cm^3/min

Measure	TAK-418 1.5 mg n = 2	TAK-418 10 mg n = 2	TAK-418 30 mg n = 2
Cerebellum	0.01020 (0.003536)	0.00405 (0.000495)	0.00760 (0.000849)
Frontal Lobe	0.01295 (0.001768)	0.00980 (0.001697)	0.01435 (0.002333)
Hippocampus	0.01260 (0.000990)	0.00635 (0.004031)	0.01240 (0.000000)
Occipital Lobe	0.01245 (0.002758)	0.00910 (0.000990)	0.01430 (0.001556)
Pons	0.01265 (0.006718)	0.00970 (0.000707)	0.01515 (0.000212)
Striatum	0.01185 (0.002192)	0.00785 (0.000495)	0.01365 (0.000071)

Population analysed: The PD set included all participants who received TAK-418 and have at least 1 analyzable PET Scan following TAK-418.

Primary outcome: Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models on Day 2

Time frame: Day 2. Mean (Standard Deviation). Unit: mL/cm^3/min

Measure	TAK-418 1.5 mg n = 2	TAK-418 10 mg n = 2	TAK-418 30 mg n = 2
Cerebellum	0.01865 (0.004455)	0.00875 (0.001485)	0.00690 (0.000566)
Frontal Lobe	0.01610 (0.003111)	0.01020 (0.001838)	0.01130 (0.002404)
Hippocampus	0.01650 (0.003960)	0.00865 (0.001061)	0.01015 (0.000919)
Occipital Lobe	0.01665 (0.003889)	0.01045 (0.002192)	0.01180 (0.001980)
Pons	0.01265 (0.004738)	0.01045 (0.002475)	0.00985 (0.000636)
Striatum	0.01410 (0.004667)	0.00915 (0.003182)	0.00965 (0.001344)

Population analysed: The PD set included all participants who received TAK-418 and have at least 1 analyzable PET Scan following TAK-418.

Primary outcome: Percent Enzyme Occupancy Based on Quantitative Estimates of Binding for TAK-418 on Day 1

Time frame: Day 1. Mean (Standard Deviation). Unit: percentage of occupancy

Measure	TAK-418 1.5 mg n = 2	TAK-418 10 mg n = 2	TAK-418 30 mg n = 2
Cerebellum	68.5 (10.61)	87.0 (1.41)	79.5 (2.12)
Frontal Lobe	19.5 (10.61)	44.0 (9.90)	38.0 (9.90)
Hippocampus	33.0 (5.66)	59.5 (26.16)	40.0 (0.00)
Occipital Lobe	37.0 (14.14)	54.5 (4.95)	43.5 (6.36)
Pons	25.0 (39.60)	37.5 (4.95)	31.0 (1.41)
Striatum	8.0 (16.97)	50.5 (3.54)	39.0 (0.00)

Population analysed: The PD set included all participants who received TAK-418 and have at least 1 analyzable PET Scan following TAK-418.

4 secondary outcomes are reported in the full results.

Adverse events

Time frame: Treatment-emergent adverse events are adverse events that started after the first administration of [18F]MNI-1054 radiotracer injection until the Day 14. Other adverse events reported at 0% frequency or more

Group	Serious adverse events	Other adverse events	Deaths
Baseline [18F]MNI-1054	0 of 7 (0%)	1 of 7 (14.3%)	0 of 7
TAK-418 1.5 mg	0 of 2 (0%)	0 of 2 (0%)	0 of 2
TAK-418 10 mg	0 of 2 (0%)	1 of 2 (50%)	0 of 2
TAK-418 30 mg	0 of 2 (0%)	2 of 2 (100%)	0 of 2

Loading the posted results from ClinicalTrials.gov…

Research links

Official record on ClinicalTrials.govLast updated by the sponsor 30 Jul 2021.
Posted resultsParticipant flow, baseline, all outcome measures and adverse events.
Derived from this study: PubMed 42397656Schwarz AJ, Sandiego CM, Constantinescu C, Takano A, McQuade P, Tauscher J, Daegele N, Marek K, Gunn RN, Madonia J, Russell DS. [18F]MNI-1054, a novel PET ligand for lysine-specific histone demethylase 1 A (LSD1): first-in human validation and enzyme occupancy of the LSD1 inhibitor TAK-418. EJNMMI Res. 2026 Jul 3. doi: 10.1186/s13550-026-01477-x. Online ahead of print.
Derived from this study: PubMed 39929582Matsuda S, Hattori Y, Kimura H. Drug discovery strategy for TAK-418, a specific inhibitor of LSD1 enzyme activity, as a novel therapy for autism. Adv Pharmacol. 2025;102:267-300. doi: 10.1016/bs.apha.2024.10.017. Epub 2024 Oct 29.
Individual participant dataSharing planned: Yes. Takeda provides access to the de-identified individual participant data (IPD) for eligible studies to aid qualified researchers in addressing legitimate scientific objectives (Takeda's data sharing commitment is available on https://clinicaltrials.takeda.com/takedas-commitment?commitment=5). These IPDs will be provided in a secure research environment following approval of a data sharing request, and under the terms of a data sharing agreement.

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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.

Medical Director study director

Takeda

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 TAK-418 and [18F]MNI-1054 (radiotracer) in people with Healthy Volunteers, run by Takeda 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 3 inclusion and 12 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: stopped early, as of the sponsor's last update on 30 Jul 2021. 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 30 Jul 2021). 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?

Quantitative Estimates of Binding of [18F]MNI-1054 Based on PET Radiotracer Kinetic Models At Baseline Scan on Day -1 (time frame: Day -1). The study lists 8 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 NCT04202497, which also lists 2 linked publications.

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 30 Jul 2021.