A Phase I Clinical Study Evaluating the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Oral Dose Escalation of GS1-144 Tablets and the Effects of Food on the Pharmacokinetics of GS1-144 in a Chinese Population

NCT06385158 | Completed Phase 1

• 1 other identifier: GenSci074-101
• Study Type: interventional
• Target: 110
• Locations: 1 country
• Sites: 1

Brief Summary

A Phase I clinical study evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral dose escalation of GS1-144 tablets and the effects of food on the pharmacokinetics of GS1-144 in a Chinese population

Conditions

Vasomotor System; Labile; Healthy Volunteer

Outcome Measures

Primary Outcomes (3)

• Part 1:Number of Participants With Treatment -Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

  Number of participants with TEAEs and SAEs will be reported

  Up to Day 4

• Part 2: Number of Participants With Treatment -Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs).

  Number of participants with TEAEs and SAEs will be reported.

  Up to Day 9;

• Part 3: Number of Participants With TEAEs and SAEs

  Number of female post-menopausal participants with TEAEs and SAEs will be reported.

  Up to Day 12

Secondary Outcomes (16)

• Part1,Part2 and Part3 AUC0-t- Area Under the Drug Concentration-time Curve From Time 0 to the Last Sample Collection Time t for GS1-144

  Part 1 Day 1- pre-dose and up to 72 hour post-dose; Part 2 Days 1 and 6-pre-dose and up to 72 hour post-dose, Part 3 Days 1 and 7-pre-dose and up to 72 hour post-dose,

• Part 1 , Part2 and Part 3: AUC0-infinity- Area Under the Drug Concentration-time Curve From 0 to Infinity for GS1-144

  Part 1 Day 1- pre-dose and up to 72 hour post-dose; Part 2 Days 1 and 6-pre-dose and up to 72 hour post-dose, Part 3 Days 1 and 7-pre-dose and up to 72 hour post-dose,

• Part 1, Part2 and Part 3: Cmax- Maximum Observed Plasma Concentration for GS1-144

  Part 1 Day 1- pre-dose and up to 72 hour post-dose; Part 2 Days 1 and 6-pre-dose and up to 72 hour post-dose, Part 3 Days 1 and 7-pre-dose and up to 72 hour post-dose,

• Part 1 Part2 and Part 3: Tmax- Time to Reach the Maximum Plasma Concentration (Cmax) for GS1-144

  Part 1 Day 1- pre-dose and up to 24 hour post-dose; Part 2 Days 1 and 7-pre-dose and up to 30 hour post-dose

• Part 1 Part2 and Part 3:: T1/2- Terminal Half-life for GS1-144

  Time Frame: Part 1 Day 1- pre-dose and up to 72 hour post-dose; Part 2 Days 1 and 6-pre-dose and up to 72 hour post-dose, Part 3 Days 1 and 7-pre-dose and up to 72 hour post-dose

Study Arms (2)

GS1-144 tablet

EXPERIMENTAL

Drug: GS1-144 tablet

placebo controlled study

PLACEBO COMPARATOR

Drug: GS1-144 tablet

Interventions

GS1-144 tablet DRUG

GS1-144 tablet is an NK3R antagonist.

GS1-144 tablet; placebo controlled study

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• At the time of signing the informed consent form (ICF):
• Part 1and Part 2 only: healthy male and female subjects aged between 18 and 45 years inclusive; Part 3 only: healthy women aged between 40 and 65 years inclusive who have undergone natural menopause (natural menopause is defined as surgically sterile (hysterectomy, bilateral salpingectomy, tubal ligation or bilateral oophorectomy - verbal confirmation through medical history review acceptable) or postmenopausal (no menses for 12 months and confirmed by FSH level ≥40 mlU/mL);
• Body weight ≥ 50 kg (male), ≥ 45 kg (female) with a body mass index between 19.0 and 27.9 kg/m2 inclusive at screening
• From signing the ICF to 1 month (female subjects) /3 months (male subjects and their female partners) after the end of the study, no family planning and egg/sperm donation plans, and effective contraceptive methods (such as IUD, bilateral tubal/vasectomy, condom and safe period calculation, etc.) (applicable to Parts 1 and 2)' ' ● Volunteer to sign ICF and be able to understand and comply with the requirements of this study

You may not qualify if:

• Any known allergy to the components or analogues of the investigational product, or those with an allergic constitution (such as allergy to two or more drugs or foods)；
• A history of currently suffering from any other cardiovascular, gastrointestinal, endocrine, hematological, hepatic, immunological, metabolic, urinary, pulmonary, neurological, dermatological, psychiatric, renal and/or other major diseases deemed clinically significant by the investigator;
• Known/confirmed history of malignancy；
• A history of epileptic seizure or increased risk of epileptic seizure, or subjects with a recent history (within six months prior to screening) of head trauma leading to loss of consciousness or concussion;
• A history of currently suffering from hypothalamic dysfunction;
• Significant acute/chronic infections within two weeks prior to dosing;
• Undergone major surgical procedures (such as coronary artery bypass grafting, organ resection, gynecological surgery, etc.) within six months prior to screening or plan to undergo any surgery during the trial;
• Participated in other clinical trials (except those who have not received any intervention) within 3 months prior to dosing, Or are participating in other clinical trials.
• Have lost or donated more than 400 mL of blood within 3 months prior to screening;
• Have taken any prescription/over-the-counter drugs or dietary supplements ,within 7 days prior to dosing or within 5 half-lives of the drug (whichever is longer);
• Clinically significant abnormalities on physical examination or genitourinary ultrasound at the time of screening;
• Clinically significant abnormalities in vital signs, where the criteria for clinically significant blood pressure abnormalities are defined as systolic blood pressure ≥ 140 mmHg or \< 90 mmHg, and diastolic blood pressure ≥ 90 mmHg or \< 60 mmHg;
• Prolonged QTcF interval in 12-lead ECG results (\> 450 ms for males, \> 470 ms for females) or clinically significant abnormalities in other 12-lead ECG parameters at screening;
• Alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma-glutamyltransferase (GGT), total bilirubin (TBIL), blood creatinine (CRE), blood urea nitrogen (BUN), or international normalized ratio (INR) higher than the upper limit of normal (ULN) at screening, that are considered as clinically significant abnormalities by the investigator;
• Part 3 only: abnormal sex hormone levels at screening that are considered clinically significant by the investigator;

Sponsors & Collaborators

• Changchun GeneScience Pharmaceutical Co., Ltd.: lead

Study Sites (1)

Huashan Hospital, Fudan University

Shanghai, Shanghai Municipality, 200040, China

Location

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: April 11, 2024
• First Posted: April 25, 2024
• Study Start: January 3, 2024
• Primary Completion: January 6, 2024
• Study Completion: November 5, 2024
• Last Updated: May 8, 2025

Record last verified: 2025-05

Locations

CN (1)