vicagrel / Jiangsu Vcare Pharma, China Pharmaceutical University - LARVOL DELTA

Promising clopidogrel analogs may overcome clopidogrel resistance: 2025 update. (PubMed, Biochem Pharmacol) - "The same strategies as those for prasugrel and vicagrel were used to design new compounds, such as tipidogrel, compound 6b, PLD-301, and W-1. All these new compounds in the pipeline are promising antiplatelet drugs, and superior to clopidogrel. DT-678 and evategrel are considered the best clopidogrel analogs that may overcome clopidogrel resistance due to their superior efficacy and safety profiles over clopidogrel."

Journal • Review

Pharmacokinetic/Pharmacodynamic Study of Vicagrel Capsules and Clopidogrel Tablets in Healthy CYP2C19 Normal Metabolizers (clinicaltrials.gov) - P1 | N=18 | Completed | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD | Not yet recruiting ➔ Completed

Trial completion • Acute Coronary Syndrome • Cardiovascular

Pharmacokinetic/Pharmacodynamic Study of Vicagrel Capsules and Clopidogrel Tablets in Healthy CYP2C19 Normal Metabolizers (clinicaltrials.gov) - P1 | N=18 | Not yet recruiting | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD

New P1 trial • Acute Coronary Syndrome • Cardiovascular

Sex differences in the metabolic activation of and platelet response to vicagrel in mice: Androgen as a key player. (PubMed, Biochem Pharmacol) - "SB202190 reversed DHT-induced changes observed in ORX mice. We concluded that sex differences exist in metabolic activation of and platelet response to vicagrel in mice through elevation of p38 phosphorylation by androgen, suggesting sex-based vicagrel dosage adjustments for patient care."

Journal • Preclinical • AADAC

VCP1-III-01: Efficacy and Safety Study of Vicagrel in Patients With Acute Coronary Syndrome (ACS) Undergoing Percutaneous Coronary Intervention (PCI) (clinicaltrials.gov) - P3 | N=1000 | Recruiting | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD | Not yet recruiting ➔ Recruiting

Enrollment open • Acute Coronary Syndrome • Cardiovascular

Efficacy and Safety Study of Vicagrel in Patients With Acute Coronary Syndrome (ACS) Undergoing Percutaneous Coronary Intervention (PCI) (clinicaltrials.gov) - P3 | N=1000 | Not yet recruiting | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD

New P3 trial • Acute Coronary Syndrome • Cardiovascular

The metabolic activation of and platelet response to vicagrel vary with P-glycoprotein deficiency, rather than P-glycoprotein inhibition, in mice. (PubMed, Xenobiotica) - "Moreover, WT mice were administered vicagrel alone or in combination with elacridar (a potent P-gp inhibitor) to determine drug-drug interactions.Compared with WT mice, P-gp KO mice exhibited significant increases in the systemic exposure of H4, the protein expression levels of intestinal Aadac and Ces2, and inhibition of ADP-induced platelet aggregation by vicagrel. However, the H4 exposure was positively correlated with intestinal Aadac protein expression levels but did not vary with short-term inhibition of P-gp efflux activity by elacridar.P-gp-deficient mice, rather than elacridar-treated mice, exhibited significant upregulation of intestinal Aadac and Ces2 and thus, enhanced metabolic activation of and platelet response to vicagrel, suggesting that the metabolic activation of vicagrel may vary with P-gp deficiency, not P-gp inhibition, in mice."

Journal • Preclinical • AADAC

Effects of the thiol methyltransferase inhibitor DCMB on the pharmacokinetics and metabolism of vicagrel in rats. (PubMed, Drug Metab Dispos) - "Overall, the present study found that DCMB did not significantly affect the total exposure, metabolic pathways, metabolite profiles, or total excretion rates of vicagrel-related metabolites in rats, but led to C max decrease, T max delay, and slower excretion rate within 48 h. Significance Statement This study used LC-MS/MS combined with radiolabeling technology to investigate the effects of the TMT inhibitor DCMB on the absorption, metabolism and excretion of vicagrel in rats. This work helps to better understand the in vivo metabolism of active thiol metabolites of P2Y12 inhibitors such as clopidogrel and vicagrel, etc."

Journal • PK/PD data • Preclinical

PK/PD Study of Vicagrel and Clopidogrel in Healthy Subjects With Different CYP2C19 Metabolizers (clinicaltrials.gov) - P1 | N=128 | Completed | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD | Active, not recruiting ➔ Completed

Trial completion • Acute Coronary Syndrome • Cardiovascular • CYP2C19

PK/PD Study of Vicagrel and Clopidogrel in Healthy Subjects With Different CYP2C19 Metabolizers (clinicaltrials.gov) - P1 | N=128 | Active, not recruiting | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD | Recruiting ➔ Active, not recruiting

Enrollment closed • Acute Coronary Syndrome • Cardiovascular • CYP2C19

Assessment of the Effect of Omeprazole on Vicagrel in Healthy Subjects (clinicaltrials.gov) - P1 | N=20 | Recruiting | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD | Trial completion date: Jan 2023 ➔ Apr 2023

Trial completion date

Vicagrel is hydrolyzed by Raf kinase inhibitor protein (RKIP) in human intestine. (PubMed, Biopharm Drug Dispos) - "As an analog of clopidogrel and prasugrel, vicagrel is completely hydrolyzed to intermediate thiolactone metabolite 2-oxo-clopidogrel (also the precursor of active thiol metabolite H4) in human intestine predominantly by AADAC and CES2; however, other unknown vicagrel hydrolases remain to be identified...In addition to locostatin, eserine and vinblastine strongly suppressed vicagrel hydrolysis in HIM...In addition to locostatin, eserine and vinblastine strongly suppressed vicagrel hydrolysis in HIM. It is concluded that RKIP can catalyze the hydrolysis of vicagrel in the human intestine, and that vicagrel can be hydrolyzed by multiple hydrolases, such as RKIP, AADAC, and CES2, concomitantly."

Journal • PEBP1

Assessment of the Effect of Omeprazole on Vicagrel in Healthy Subjects (clinicaltrials.gov) - P1 | N=20 | Recruiting | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD

New P1 trial

Semi-mechanistic Population Pharmacokinetics Analysis Reveals Distinct CYP2C19 Dependency in the Bioactivation of Vicagrel and Clopidogrel to Active Metabolite M15-2. (PubMed, Eur J Pharm Sci) - No abstract available

Journal • PK/PD data • CYP2C19

PK/PD Study of Vicagrel and Clopidogrel in Healthy Subjects With Different CYP2C19 Metabolizers (clinicaltrials.gov) - P1 | N=128 | Recruiting | Sponsor: Jiangsu vcare pharmaceutical technology co., LTD | Not yet recruiting ➔ Recruiting | Trial completion date: Dec 2022 ➔ Apr 2023

Enrollment open • Trial completion date • Acute Coronary Syndrome • Cardiovascular • CYP2C19

Antiplatelet effect, safety, and pharmacokinetics of vicagrel in patients with coronary artery disease undergoing percutaneous coronary intervention. (PubMed, Eur Heart J Cardiovasc Pharmacother) - "Vicagrel had comparable antiplatelet effect and safety to clopidogrel in patients with CAD undergoing PCI."

Clinical • Journal • PK/PD data • Cardiovascular • Coronary Artery Disease • Myocardial Infarction • CYP2C19

Pharmacokinetic/Pharmacodynamic Study of Vicagrel and Clopidogrel in Healthy Subjects With Different CYP2C19 Metabolizers (clinicaltrials.gov) - P1; N=160; Not yet recruiting; Sponsor: Jiangsu vcare pharmaceutical technology co., LTD

Clinical • New P1 trial • Acute Coronary Syndrome • Cardiovascular

Inhibition of cytochrome P450 enzymes and uridine 5'-diphospho-glucuronosyltransferases by vicagrel in human liver microsomes: A prediction of potential drug-drug interactions. (PubMed, Chem Biol Interact) - "Our study provides inhibitory constants for future DDI prediction between vicagrel and drug substrates of CYP2B6, CYP2C19 and UGT1A6. In addition, our simulation suggests the lack of clinically important DDI between vicagrel and bupropion or S-mephenytoin."

Journal • CYP2C19 • CYP2C8 • CYP2C9 • CYP3A4 • UGT1A1 • UGT1A9

A Clinical Trial to Evaluate the Effect of Food on PK and PD of Vicagrel Capsules in Healthy Adult Subjects (clinicaltrials.gov) - P1; N=24; Completed; Sponsor: Jiangsu vcare pharmaceutical technology co., LTD; Not yet recruiting ➔ Completed

Clinical • Trial completion • Acute Coronary Syndrome • Cardiovascular

A Clinical Trial to Evaluate the Effect of Food on PK and PD of Vicagrel Capsules in Healthy Adult Subjects (clinicaltrials.gov) - P1; N=24; Not yet recruiting; Sponsor: Jiangsu vcare pharmaceutical technology co., LTD

Clinical • New P1 trial • Acute Coronary Syndrome • Cardiovascular