Delving into the Latest Updates on Rafigrelide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

PDE3

Mechanism

PDE3 inhibitors(Phosphodiesterase 3 inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Thrombosis

Originator Organization

Shire Plc

Active Organization-

Inactive Organization

Shire Pharmaceuticals Services Ltd.

Shire Plc

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC12H11Cl2N3O

InChIKeyIGMDPBNGNRHCRW-UHFFFAOYSA-N

CAS Registry1029711-88-3

SummaryPlatelets play a central role in atherothrombotic events. We investigated the effect of a novel platelet-lowering agent, rafigrelide, on thrombus formation and characteristics. In this phase 1, open-label, non-randomised, single-sequence, crossover study, healthy male volunteers received rafigrelide for 14 days (Period 1). Following a ≥6-week washout period, they then received rafigrelide + acetylsalicylic acid (ASA) for 14 days (Period 2). Thrombus formation was assessed ex vivo using the Badimon perfusion chamber, and thrombus characteristics were assessed using thromboelastography. A total of 15 volunteers were enrolled in the study and were assigned to Panel A or Panel B, which had different schedules of assessments. In Panel A, after treatment with rafigrelide alone (Period 1), mean (± standard deviation) platelet count was reduced from 283 (± 17) × 109/l at Day 1, to 125 (± 47) × 109/l at Day 14 (n=6) and thrombus area reduced under high and low shear conditions. Reductions in thrombus area under high shear conditions correlated with reductions in platelet count (r2=0.11, p=0.022; n=12). Rafigrelide treatment prolonged clot formation time and reduced clot strength. The addition of ASA to rafigrelide (Period 2) had no additional effect on platelet count or thrombus area under high or low shear conditions. Similar results were seen in Panel B for all parameters. The most common adverse events (≥3 participants per period) were thrombocytopenia and headache. While confirming the platelet-lowering effects of rafigrelide, this early phase study also indicates that rafigrelide has antithrombotic properties under both high and low shear conditions.

100 Deals associated with Rafigrelide

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