Synonyms: GB-002 | Gb002 | PK-10571 | PK10571 | structure 2a [WO2014110200A1]
Compound class:
Synthetic organic
Comment: Seralutinib (PK10571; Structure 2a; GB002) is a small molecule inhibitor of platelet-derived growth factor receptors A and B (PDGFRα, PDGFRβ; receptor tyrosine kinases) [1]. It was developed to target the PDGF pathway as a therepuetic modality for the treatment of pulmonary arterial hypertension (PAH). PK10571 is being progressed for PAH by Gossamer Bio in collaboration with Pulmokine. Inhibition of PDGFRα/β is predicted to stop and/or reverse the vascular remodeling associated with PAH and thereby improve cardiopulmonary hemodynamics in these patients.
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Bioactivity Comments |
PK10571 (GB002) has demonstrated preclinical efficacy in the rat SU5416 hypoxia model of PAH. |
Selectivity at catalytic receptors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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