Pharmacokinetics of Zelquistinel in Fasted or Fed State

NCT07099989 | Active Not Recruiting Phase 1 FDA Drug

• 1 other identifier: GATE-251-C-110
• Study Type: interventional
• Target: 32
• Locations: 1 country
• Sites: 1

Brief Summary

The primary purpose of this study is to assess the effect of food on the rate and extent of absorption of a single dose of Zelquistinel 3 mg or 10 mg oral tablets tablets in healthy adult volunteers.

Conditions

Healthy Volunteers in Fed and Fasted State

Keywords

GATE-251; zelquistinel; N-methyl-D-aspartate (NMDA) receptor positive allosteric modulator; pharmacokinetics

Outcome Measures

Primary Outcomes (4)

• Pharmacokinetic parameter Maximum Concentration (Cmax) in plasma

  Maximum concentration in plasma

  Hour zero to Hour 24

• Pharmacokinetic parameter Area Under the Curve (AUC) for Concentration in plasma over time

  Area under the curve from time 0 to hour 24

  Hour 0 to hour 24

• Pharmacokinetic parameter Maximum Concentration (Cmax) in cerebrospinal fluid

  Maximum concentration in cerebrospinal fluid in plasma

  Hour 0 to Hour 24

• Pharmacokinetic parameter Area Under the Curve (AUC) for concentration in cerebrospinal fluid over time

  Area under the curve from time 0 to hour 24 in cerebrospinal fluid

  Hour 0 to hour 24

Secondary Outcomes (17)

• Pharmacokinetic parameter Time of Maximum Concentration (Tmax) in plasma

  Hour 0 to hour 24

• Pharmacokinetic parameter Elimination Half-Life (T1/2) in plasma

  Hour 0 to hour 24

• Pharmacokinetic parameter maximum concentration (Tmax) in cerebrospinal fluid

  Hour 0 to hour 24

• Pharmacokinetic parameter Elimination Half-Life (T1/2) in cerebrospinal fluid

  Hour 0 to hour 24

• Safety - Pulse Rate

  Day -1 to Day 10

Study Arms (4)

Zelquistinel, 3 mg Fasted

ACTIVE COMPARATOR

Subjects will be randomized to one of two sequences. Subjects will be dosed with GATE-251, 3 mg oral tablet, during each sequence. Each subject will serve as their own control.

Drug: Zelquistinel 3 mg

Zelquistinel, 3 mg Fed

ACTIVE COMPARATOR

Subjects will be randomized to one of two sequences. Subjects will be dosed with GATE-251, 3 mg oral tablet, during each sequence. Each subject will serve as their own control.

Drug: Zelquistinel 3 mg

Zelquisitinel, 10 mg Fasted

ACTIVE COMPARATOR

Subjects will be randomized to one of two sequences. Subjects will be dosed with GATE-251, 10 mg oral tablet, during each sequence. Each subject will serve as their own control.

Drug: Zelquistinel 10 mg

Zelquistinel, 10 Fed

ACTIVE COMPARATOR

Subjects will be randomized to one of two sequences. Subjects will be dosed with GATE-251, 10 mg oral tablet, during each sequence. Each subject will serve as their own control.

Drug: Zelquistinel 10 mg

Interventions

Zelquistinel 3 mg DRUG

Subjects will receive Zelquistinel 3 mg in fed and fasted state (high fat meal).

Zelquistinel, 3 mg Fasted; Zelquistinel, 3 mg Fed

Zelquistinel 10 mg DRUG

Subjects will receive Zelquistinel 10 mg in fed and fasted state (high fat meal).

Zelquisitinel, 10 mg Fasted; Zelquistinel, 10 Fed

Eligibility Criteria

• Age: 18 Years - 59 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Available for the entire study period; willing and able to comply with the protocol requirements and study restrictions, to remain at the CRU for the required duration of the study, and to return for the Follow-Up Visit
• Male or female participants ≥18 to ≤59 years of age at Screening
• Minimum body weight of at least 50.0 kg at Screening
• Body mass index (BMI) 18.0 to 35.0 kg/m2, inclusive, at Screening
• Able and willing to swallow whole tablets without breaking, cutting, or chewing
• Non- or ex-smokers
• Considered generally healthy in the opinion of an investigator upon completion of medical history, physical examination, vital sign measurements, Screening clinical laboratory test results, and Screening ECG
• Female participants of childbearing potential must use an acceptable method of contraception, including hormonal contraceptives, abstinence from heterosexual intercourse, intrauterine device with or without hormones, or double-barrier method (eg, condom and spermicide) for 30 days before Screening, during the study, and for 30 days after the last administration of study drug
• Female participants of nonchildbearing potential should be surgically sterile (ie, have undergone complete hysterectomy, bilateral salpingectomy, bilateral oophorectomy, or tubal ligation/occlusion) or in a menopausal state (at least 1 year without menses)
• Male participants must agree to use a double-barrier method (condom and spermicide) or remain abstinent from heterosexual intercourse at the time of Screening, during the study, and for 90 days after the last administration of study drug
• Male participants must agree not to donate sperm during the study and for 90 days after the last administration of study drug
• Able to fully consume the required fed meal within 30 minutes without substitutions
• Willing and able to provide written informed consent to participate in the study, is able to understand the procedures and study requirements, and agrees to comply with all required study requests and procedures
• Able to speak, read, and understand English sufficiently to allow completion of all study assessments

You may not qualify if:

• Female participant who is currently pregnant or lactating or is planning to become pregnant during the study
• Positive pregnancy test at Screening or on Day -1
• Positive test results for HIV 1/2 Ag/Ab, hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) at Screening
• Positive urine screen for drugs or alcohol at Screening or on Day -1
• Clinically significant history or evidence of gastrointestinal (excluding cholecystectomy), hepatic, renal, endocrine, pulmonary, neurologic, psychiatric, cardiovascular, hematologic, dermatologic, immunologic, or metabolic disease; or any other condition or organ system disease known to interfere with the absorption, distribution, metabolism, or elimination of drugs that in the opinion of an investigator would jeopardize the safety of the participant or impact validity of study results.
• Current or history of alcohol or substance abuse, with the exception of being fully recovered with no use of alcohol or substances of abuse within the 12 months before Screening
• Any clinically significant illness in the previous 30 days before Screening or Day -1
• Malignancy, a history of malignancy, or has received treatment for a malignancy at any time, with the exception of resected and cured basal cell carcinoma and squamous cell carcinoma of the skin (\>1 year)
• Poor venous access
• Any medical condition(s) considered by an investigator to be clinically significant for study participation
• Supine pulse rate \<60 or ≥100 bpm at Screening or on Day -1
• Donation or significant loss of blood products of 500 mL or more within 56 days before Screening, or donation or loss of plasma within 7 days before Screening
• Suicidal behavior or suicidal ideation of score 4 (active suicidal ideation with some intent to act without specific plan) or score 5 (active suicidal ideation with specific plan and intent) based on the C-SSRS within 12 months before Screening; a history of suicide attempt in the last 6 months; or more than 1 lifetime suicide attempt
• Positive responses on the CADSS or BPRS+ assessments at Screening, indicating evidence of dissociative symptoms or psychosis, as determined by the investigator
• Unable to abstain from consumption of grapefruit or Seville oranges or their juices from 14 days before the first administration of study drug until collection of the final PK sample

Sponsors & Collaborators

• Syndeio Biosciences, Inc: lead
• Dr. Vince Clinical Research: collaborator

Study Sites (1)

Dr. Vince Clinical Research

Overland Park, Kansas, 66212, United States

Location

MeSH Terms

Conditions

Fasting

Condition Hierarchy (Ancestors)

Feeding Behavior; Behavior

Study Officials

• Ronald Burch Burch, MD, PhD

  Syndeio Biosciences, Inc

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 21, 2025
• First Posted: August 1, 2025
• Study Start: July 24, 2025
• Primary Completion: February 5, 2026
• Study Completion (Estimated): July 1, 2026
• Last Updated: March 20, 2026

Record last verified: 2026-03

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)