Safety and Tolerability of Zelquistinel in Normal Human Volunteers

A Phase 1, Single Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of AGN-241751 After Oral Administration in Healthy Volunteers

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT04981561

Enrollment

Registered

2021-07-29

Start date

2016-12-09

Completion date

2017-12-21

Last updated

2026-03-12

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Major Depressive Disorder

Keywords

NMDA receptor, NMDA receptor positive allosteric modulator, pharmacokinetics, biomarker, eeg

Brief summary

To evaluate the safety and tolerability of single ascending doses of zelquistinel in normal human volunteers

Detailed description

Single ascending dose (SAD), double-blind placebo-controlled study in normal human volunteers. Secondary objectives: To evaluate the pharmacokinetics (PK) and eeg biomarker of target engagement of zelquistinel following increasing single doses of zelquistinel. Zelquistinel or Placebo: Dose/Mode of Administration: Single dose; oral

Interventions

DRUGzelquistinel

Single dose of zelquistinel

DRUGPlacebo

Placebo

Study design

Allocation

RANDOMIZED

Intervention model

PARALLEL

Primary purpose

TREATMENT

Masking

TRIPLE (Subject, Investigator, Outcomes Assessor)

Masking description

Triple blind

Intervention model description

Double blind placebo controlled

Eligibility

Sex/Gender

ALL

Age

18 Years to 45 Years

Healthy volunteers

Yes

Inclusion criteria

* Agree to effective method of birth control * If female, negative pregnancy test at screening and Day -1 * Nonsmoking at least 2 years * BMI 18-30 * Supine pulse rate 30-100

Exclusion criteria

* Known hypersensitivity to NMDA receptor drugs * clinically significant disease in any body system * QTcF \> 430 ms in males, \>450 ms in females * positive test for hepatitis B or C * abnormal liver function tests on Day -1 * History of alcohol or other substance abuse during the previous 5 years * Positive drug screen at screening or Day -1 * Taken any medication within the past 14 days

Design outcomes

Primary

Measure	Time frame	Description
Treatment emergent adverse events	28 days	through study completion

Secondary

Measure	Time frame	Description
Pharmacokinetics, maximum plasma concentration	24 hours	maximum plasma concentration
Pharmacokinetics, time to maximum plasma concentration	24 hours	time to maximum plasma concentration
Pharmacokinetics, area under the curve for plasma concentration	72 hours	area under the curve, plasma calculated 0-infinity

Contacts

STUDY_CHAIRAaron Koenig, MD

Syndeio Biosciences

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Mar 13, 2026