PZ-128 (also known as P1pal7 ) is a cell-penetrating pepducin inhibitor of PAR1 that targets the receptor-G-protein interface on the inside surface of platelets. In preclinical studies, PZ-128 suppresses PAR1 aggregation and arterial thrombosis in guinea pigs and baboons and strongly synergized with oral clopidogrel. PZ-128 shows potent anti-metastatic and anti-angiogenic activity in Breast, Ovarian, and Lung Cancer preclinical studies. In clinical trials, PZ-128 shows a promising antiplatelet activity that provides rapid, specific, dose-dependent, and reversible inhibition of platelet protease-activated receptor-1 through a novel intracellular mechanism.

Entospletinib (GS-9973) is an adenosine triphosphate competitive inhibitor of Syk that disrupts kinase activity, which is currently in clinical trials for multiple B-cell malignancies. The most common treatment-emergent serious adverse events included dyspnea, pneumonia, febrile neutropenia, dehydration, and pyrexia.

Remeglurant is a selective antagonist of subtype 5 metabotropic glutamate receptors (mGluR5). mGluR5 antagonists have a modulatory role in the control of glutamatergic neurotransmission. This drug was developed for treatment in drug-induced dyskinesia (an involuntary movement disorder). A phase 1 trial was conducted but no further development has been reported since 2016.