Compstatin is a cyclic tridecapeptide that inhibits a key step in the activation of the human complement system[1]. It binds C3, inhibiting proteolytic cleavage by C3 convertase and activation of classical and alternative pathways[2][3]. Compstatin has been found to be highly potent and selective, with an IC50 of 28 μM[2], and has potential to prevent complement activation during and after clinical cardiac surgery[4].

Compstatins are a third-generation complement inhibitor, and AMY-101 is a selective peptidic compstatin analogue developed by AMYNDAS[1]. Clinical trials have been conducted to assess the efficacy of compstatin analogues in treating age-related macular degeneration[2], severe COVID-19[3], and other conditions[4]. Reviews have also been published on the dawn of clinical C3-targeted complement inhibition[5]. In a recent study published by Science Advances, complement C3 activation contributes to COVID-19 pathology and C3 targeting has emerged as a promising therapeutic strategy.

Reference

1
clinicaltrials.gov
2
nih.gov
3
science.org
4
sciencedirect.com
5
amyndas.com