The Pharmacokinetics and Pharmacodynamics Study of CG-0255 Besylate and Plavix® in Healthy Participants

NCT07619885 | Recruiting Phase 1 FDA Drug

• 1 other identifier: Shanghai CureGene Pharmaceutic
• Study Type: interventional
• Target: 136
• Locations: 1 country
• Sites: 1

Brief Summary

CG-0255 is a novel investigational prodrug of the active metabolite of Plavix®， but with different active metabolite conversion routes. This is a randomized, open-label and Plavix®-controlled study to compare the PK and PD of CG-0255 Besylate and Plavix® in healthy participants.

Conditions

Acute Coronary Syndromes (ACS); Recent Myocardial Infarction; Recent Stroke; Peripheral Arterial Disease

Outcome Measures

Primary Outcomes (2)

• To compare the PK of the active metabolite CG-0236 of CG-0255 Besylate and of Plavix® when they are administered as loading dose (LD) and maintenance dose (MD) in healthy participants.

  Area under the plasma concentration-time curve from time 0 to the last quantifiable measurement time-point (AUClast)

  Day 1 (LD) and Day 7 (MD)

• To compare the PK of the active metabolite CG-0236 of CG-0255 Besylate and of Plavix® when they are administered as loading dose (LD) and maintenance dose (MD) in healthy participants.

  Peak Plasma Concentration (Cmax)

  Day 1 (LD) and Day 7 (MD)

Secondary Outcomes (4)

• To compare the PD of the active metabolite CG-0236 of CG-0255 Besylate and of Plavix® when administered as LD and MD in healthy participants.

  Day 1 (LD) and Day 7 (MD)

• To evaluate the Cmax of CG-0255 when administered CG-0255 Besylate as LD and MD in healthy participants.

  Day 1 (LD) and Day 7 (MD)

• To evaluate the safety and tolerability of CG-0255 Besylate and Plavix® when administered as LD and MD in healthy participants.

  Day 1-13

• To evaluate the AUC of CG-0255 when administered CG-0255 Besylate as LD and MD in healthy participants.

  Day 1 (LD) and Day 7 (MD)

Other Outcomes (3)

• To explore the effect of CYP2C19 genetic polymorphism on the PK of CG-0236 following CG-0255 Besylate and Plavix® administration.

  Day 1 (LD) and Day 7 (MD)

• To explore the effect of CYP2C19 genetic polymorphism on the PD following CG-0255 Besylate and Plavix® administration.

  Day 1 (LD) and Day 7 (MD)

• To explore the effect of CYP2C19 genetic polymorphism on the PK of CG-0236 following CG-0255 Besylate and Plavix® administration.

  Day 1 (LD) and Day 7 (MD)

Study Arms (4)

Treatment A: CG-0255 oral for both Loading Dose (LD) and Maintenance Dose (MD)

EXPERIMENTAL

For Treatment A, participants will be administered with 3 mg CG-0255 Besylate capsules on Day 1. Subsequently, they will receive 0.75 mg CG-0255 Besylate capsules once daily from Days 2 to 7.

Drug: CG-0255 Besylate Capsule

Treatment B: CG-0255 iv for LD and oral for MD

EXPERIMENTAL

For Treatment B, participants will be administered with 0.05 mg/kg CG-0255 Besylate for IV infusion within 30 minutes on Day 1. Subsequently, they will receive 0.75 mg CG-0255 Besylate capsules once daily from Days 2 to 7.

Drug: CG-0255 Besylate for Injection; Drug: CG-0255 Besylate Capsule

Treatment C: Plavix® 300mg for LD and 75mg for MD

ACTIVE COMPARATOR

For Treatment C, participants will be administered with 300 mg Plavix® on Day 1 as 4 x 75 mg Plavix® tablets. Subsequently, they will receive 75 mg Plavix® once daily from Days 2 to 7.

Drug: Clopidogrel

Treatment D: Plavix® 600mg for LD and 75mg for MD

ACTIVE COMPARATOR

For Treatment D, participants will be administered with 600 mg Plavix® on Day 1 as 8 x 75 mg Plavix® tablets. Subsequently, they will receive 75 mg Plavix® once daily from Days 2 to 7.

Drug: Clopidogrel

Interventions

CG-0255 Besylate for Injection DRUG

Calculate the dosage and number of vials required for a participant according to body weight. Reconstitute with 5 mL of sterile water for each 5 mg/vial to get clear solution for injection in 1 mg/mL (as CG-0255). The reconstituted CG-0255 Besylate for injection (1 mg/mL), must be further diluted in 100 mL normal saline infusion bag, following the instruction in the pharmacy manual.

Treatment B: CG-0255 iv for LD and oral for MD

CG-0255 Besylate Capsule DRUG

Orally administered as LD or MD with approximately 240 mL of water.

Treatment A: CG-0255 oral for both Loading Dose (LD) and Maintenance Dose (MD); Treatment B: CG-0255 iv for LD and oral for MD

Clopidogrel DRUG

Orally administered as LD or MD with approximately 240 mL of water.

Treatment C: Plavix® 300mg for LD and 75mg for MD; Treatment D: Plavix® 600mg for LD and 75mg for MD

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants must be fully informed about the study, willing to participate, and sign the informed consent document prior to any procedure.
• Healthy male and female participants, aged 18 to 55 years (inclusive) at time of signing informed consent form.
• Body mass index (BMI) between 18 and 32 kg/m2 (inclusive) at screening and body weight between 45 and 120 kg (inclusive).
• Smoking \< 10 cigarettes (10-20 mg of nicotine/month) or equivalent amount of nicotine products per month within 6 months prior to screening and agree to abstain from tobacco and/or nicotine products during the study.
• Generally normal health, or abnormalities deemed non-clinically significant by the Investigator or designee based on medical history, physical examination, vital signs, 12-lead ECG, and clinical laboratory tests at the screening and at the admission.
• For female participants,
• Woman of child-bearing potential (WOCBP) must be non-pregnant and non-lactating, and must agree to use highly effective contraceptive methods and abstain from egg collection or donation from the screening period to 3 months after the last dose of the study treatment (CG-0255 Besylate or Plavix®). The male partner of a female participant also needs to use condoms during this period.
• Woman of non-childbearing potential (WONCBP) must be post menopausal (spontaneous amenorrhea for at least 12 consecutive months prior to dosing) with confirmation by documented FSH levels ≥40 mIU/mL; or surgically sterile (bilateral oophorectomy, bilateral salpingectomy, hysterectomy, or bilateral tubal ligation) at least 3 months prior to dosing.
• Male participants considered fertile must agree to not plan to father a child, not donate sperm and take effective contraceptive methods from the screening period to 3 months after the last dose of the study treatment. The female partner of a male participant also needs to use a highly effective contraceptive method during this period.
• Male participants (including men who have had a vasectomy) with a pregnant partner must agree to use a condom from the screening period to 3 months after the last dose of the study treatment.
• Participants must be able to communicate well with the Investigator or designee, as well as understand and adhere to the study's requirements.

You may not qualify if:

• Difficulty with venous blood collection or a history of fainting upon seeing blood or needles.
• Clinically relevant drug intolerance or allergy or known or suspected hypersensitivity to any component of CG-0255 Besylate or Plavix®, or other related drugs.
• Participation in a clinical research study involving the administration of an investigational or marketed drug or device within 30 days (or 5 times half-life, whichever is longer) prior to the first dosing, administration of a biological product in the context of a clinical research study within 90 days (or 5 times half-life, whichever is longer) prior to the first dosing, or concomitant participation in an investigational study involving no drug or device administration.
• Current or unresolved digestive tract diseases (dyspepsia, gastroesophageal reflux, gastro-hemorrhage, or digestive tract ulcer disease) within the past 6 months, or frequent (\> 1 time/week) digestive tract symptoms including dysphagia, abdominal pain, abdominal distension, acid regurgitation, belching, hematemesis, bloody stool, anorexia, nausea, heartburn, and other symptoms that may increase the risk of bleeding, as determined by the Investigator or designee.
• Any clinically significant diseases including but not limited to pulmonary, cardiovascular, gastrointestinal, hematological, endocrinological, immunological, dermatological, malignant diseases, mental and nervous systems, and other related diseases or any other condition at the discretion of the Investigator or designee.
• Hemoglobin \<120 g/L for males and \<110 g/L for females at screening.
• Medication history of NSAIDs (including Aspirin) or other drugs that may affect coagulation function (e.g, oral anticoagulants) within 4 weeks before the screening.
• Platelet count \< 120 × 10\^9/L at screening.
• Laboratory measures with values above the 1.5 × upper limits of normal (ULN) and deemed clinically significant by the Investigator or designee for the alanine aminotransferase (ALT), alkaline phosphatase (ALP), aspartate aminotransferase (AST).
• Clinically significant ECG abnormalities (QTcF interval ≥ 450 ms for male, ≥ 470 ms for female (Fridericia's Correction)) or vital signs abnormalities (systolic BP lower than 90 or over 140 mmHg, diastolic BP lower than 50 or over 90mmHg, HR less than 50 or over 100 bpm, or RR less than 10 or over 22 bpm) at screening.
• Major surgery within 3 months prior to the first dose of study treatment or plans for surgery during the study.
• Use of prescription, nonprescription or dietary supplements (e.g. food supplements and herbal supplements) within 14 days or 5 times the half life (whichever is longer) prior to the first dose of study treatment (excluding drug products without significant systemic absorption at the discretion of the Investigator or designee), or depot injection or implant within 3 months prior to first dosing, with the exception of the occasional use of acetaminophen (up to 2 g daily).
• Vaccinated within 14 days prior to the first dose of study treatment or planned to be vaccinated during the study.
• Consuming quinine containing products, including quinine water, tonic water bitter lemon, jello shots, any quinine preparations or Cinchona tree bark reparations (e.g., herbal medications containing Cinchona tree bark), and grapefruit or products containing grapefruit, or participants have engaged strenuous exercise or any other factors affecting drug absorption, distribution, metabolism and excretion within 7 days before the first dose of study treatment.
• History of drug abuse within 1 year before screening, or recreational use of soft drugs (such as marijuana) within 1 month or hard drugs (such as cocaine, phencyclidine \[PCP\], crack, opioid derivatives including heroin, and amphetamine derivatives) within 3 months prior to screening.

Sponsors & Collaborators

• Shanghai CureGene Pharmaceutical Co., Ltd.: lead

Study Sites (1)

Syneos Health

Miami, Florida, 33101, United States

RECRUITING

MeSH Terms

Conditions

Acute Coronary Syndrome; Peripheral Arterial Disease

Interventions

Injections; Clopidogrel

Condition Hierarchy (Ancestors)

Myocardial Ischemia; Heart Diseases; Cardiovascular Diseases; Vascular Diseases; Atherosclerosis; Arteriosclerosis; Arterial Occlusive Diseases; Peripheral Vascular Diseases

Intervention Hierarchy (Ancestors)

Drug Administration Routes; Drug Therapy; Therapeutics; Ticlopidine; Thienopyridines; Thiophenes; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Central Study Contacts

Isabel Pino

CONTACT

305-547-5813; Isabel.pino@syneoshealth.com

Study Design

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

Study Record Dates

• First Submitted: May 11, 2026
• First Posted: June 2, 2026
• Study Start: June 1, 2026
• Primary Completion (Estimated): October 1, 2026
• Study Completion (Estimated): December 1, 2026
• Last Updated: June 5, 2026

Record last verified: 2026-06

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)