Therapeutic Monoclonal Antibody Antagonizing Endothelin Receptor A For Pulmonary Arterial Hypertension
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS(2019)
摘要
Endothelin receptor A (ETA) is a G protein-coupled receptor and a major therapeutic target for pulmonary arterial hypertension (PAH). We took a novel approach and developed an antagonistic monoclonal antibody, getagozumab, specifically against ETA. Getagozumab displayed a K-d value of 8.7 nM and an IC50 value of 37.9 nM in the cell-based assays. Getagozumab could significantly lower pulmonary arterial pressure in both hypoxia-induced and monocrotaline (MCT)induced PAH monkey models and further attenuate the pulmonary arterial and right ventricular hypertrophy in MCT-induced PAH monkeys. The preclinical studies demonstrated that getagozumab is safe, long lasting, and efficacious. Getagozumab may provide a new and effective treatment for PAH patients.
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关键词
antibodies,pharmacodynamics,pulmonary hypertension
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