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

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

Study Overview

• Status: Completed
• Conditions: Major Depressive Disorder
• Intervention / Treatment: Drug: Placebo; Drug: zelquistinel

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

• Study Type: Interventional
• Enrollment (Actual): 68
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Triple

Number of Arms

10

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo; Placebo tablet, PO, Single Dose with 28 day follow up	Drug: Placebo; Placebo
Experimental: 100 microgram zelquistinel; zelquistinel, 100 microgram tablet, PO, Single Dose with 28 day follow up	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 1 mg zelquistinel; zelquistinel, 1 mg tablet, PO, Single Dose with 28 day follow up	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 3 mg zelquistinel; zelquistinel, 3 mg tablet, PO, Single Dose with 28 day follow up	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 10 mg zelquistinel; zelquistinel, 10 mg tablet, PO, Single Dose with 28 day follow up	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 25 mg zelquistinel; zelquistinel, 25 mg tablet, PO, Single Dose with 28 day follow up	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 50 mg zelquistinel; zelquistinel, 50 mg tablet, PO, Single Dose with 28 day follow up	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 100 mg zelquistinel; zelquistinel, 100 mg tablet, PO, Single Dose with 28 day follow up	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 1 mg zelquistinel with CSF collection; zelquistinel, 1 mg tablet, PO, Single Dose with 28 day follow up, with CSF collection	Drug: zelquistinel; Single dose of zelquistinel
Experimental: 10 mg zelquistinel with CSF collection; zelquistinel, 10 mg tablet, PO, Single Dose with 28 day follow up, with CSF collection	Drug: zelquistinel; Single dose of zelquistinel

What is the study measuring?

Primary Outcome Measures

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

Secondary Outcome Measures

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

Collaborators and Investigators

• Sponsor: Syndeio Biosciences, Inc
• Investigators: Study Chair: Aaron Koenig, MD, Syndeio Biosciences

Study record dates

Study Major Dates

• Study Start (Actual): December 9, 2016
• Primary Completion (Actual): December 21, 2017
• Study Completion (Actual): December 21, 2017

Study Registration Dates

• First Submitted: July 18, 2021
• First Submitted That Met QC Criteria: July 28, 2021
• First Posted (Actual): July 29, 2021

Study Record Updates

• Last Update Posted (Actual): March 12, 2026
• Last Update Submitted That Met QC Criteria: March 10, 2026
• Last Verified: July 1, 2021

More Information

Terms related to this study

• Keywords: biomarker; pharmacokinetics; NMDA receptor; eeg; NMDA receptor positive allosteric modulator
• Additional Relevant MeSH Terms: Mental Disorders; Mood Disorders; Depressive Disorder; Depressive Disorder, Major
• Other Study ID Numbers: 3125-101-009

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No