Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study

@inproceedings{Bekker2016CharacterizationOP,
  title={Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study},
  author={P. C. F. Bekker and Daniel J. Dairaghi and Lisa C. Seitz and Manmohan Reddy Leleti and Yu Wang and Linda S. Ertl and Trageen Baumgart and Sarah Shugarts and Lisa K. Lohr and Ton Dang and Shichang Miao and Yibin Zeng and Pingchen Fan and Penglie Zhang and Daniel V. Johnson and Jay P. Powers and Juan A. Ja{\'e}n and Israel Lafayette Charo and Thomas J. Schall},
  booktitle={PloS one},
  year={2016}
}
The complement 5a receptor has been an attractive therapeutic target for many autoimmune and inflammatory disorders. However, development of a selective and potent C5aR antagonist has been challenging. Here we describe the characterization of CCX168 (avacopan), an orally administered selective and potent C5aR inhibitor. CCX168 blocked the C5a binding, C5a-mediated migration, calcium mobilization, and CD11b upregulation in U937 cells as well as in freshly isolated human neutrophils. CCX168… CONTINUE READING

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