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.
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.
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.
Parallel
CG-0255 Besylate for Injection
DrugCalculate 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.
CG-0255 Besylate Capsule
DrugOrally administered as LD or MD with approximately 240 mL of water.
Clopidogrel
DrugOrally administered as LD or MD with approximately 240 mL of water.
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)
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)
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.
The inhibition of platelet reactivity unit (PRU) based on VerifyNow assay, the inhibition of maximum platelet aggregation (MPA) based on Light Transmittance Aggregometry (LTA) assay.
To evaluate the Cmax of CG-0255 when administered CG-0255 Besylate as LD and MD in healthy participants.
Peak Plasma Concentration (Cmax)
To evaluate the safety and tolerability of CG-0255 Besylate and Plavix® when administered as LD and MD in healthy participants.
Number of Participants with Abnormal Laboratory Values and/or Adverse Events That Are Related to Treatment.
To evaluate the AUC of CG-0255 when administered CG-0255 Besylate as LD and MD in healthy participants.
Area under the plasma concentration-time curve from time 0 to the last quantifiable measurement time-point (AUClast)
To explore the effect of CYP2C19 genetic polymorphism on the PK of CG-0236 following CG-0255 Besylate and Plavix® administration.
Comparisons of plasma AUC of CG-0236 stratified by CYP2C19 genotypes: normal, intermediate and poor metabolizers
To explore the effect of CYP2C19 genetic polymorphism on the PD following CG-0255 Besylate and Plavix® administration.
Comparison of platelet reactivity unit (PRU) and/or maximal platelet aggregation (MPA) inhibition stratified by CYP2C19 genotypes: normal, intermediate and poor metabolizers.
To explore the effect of CYP2C19 genetic polymorphism on the PK of CG-0236 following CG-0255 Besylate and Plavix® administration.
Comparisons of plasma Cmax of CG-0236 stratified by CYP2C19 genotypes: normal, intermediate and poor metabolizers.
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