Fanapanel Explained

Fanapanel (INN, code name ZK-200775), also known as MPQX, is a quinoxalinedione derivative drug which acts as a competitive antagonist of the AMPA receptor.^[1] It was under development by Schering AG for the treatment of cerebral ischemia associated with stroke and trauma, but clinical trials were halted for safety reasons related to possible glial cell toxicity and due to intolerable side effects such as excessive sedation, reduction in consciousness (consisting of stupor and coma), and transient neurological deterioration.^{[2] [3]} The drug was also observed to produce visual alteration and impairment, including blurred vision, strongly impaired color perception, and reduced visual acuity and dark vision, side effects thought to be caused by blockade of AMPA receptors in the retina.^[4]

Notes and References

1. Turski L, Huth A, Sheardown M, McDonald F, Neuhaus R, Schneider HH, Dirnagl U, Wiegand F, Jacobsen P, Ottow E . 6 . ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma . Proceedings of the National Academy of Sciences of the United States of America . 95 . 18 . 10960–10965 . September 1998 . 9724812 . 28003 . 10.1073/pnas.95.18.10960 . free . 1998PNAS...9510960T .
2. Walters MR, Kaste M, Lees KR, Diener HC, Hommel M, De Keyser J, Steiner H, Versavel M . 6 . The AMPA antagonist ZK 200775 in patients with acute ischaemic stroke: a double-blind, multicentre, placebo-controlled safety and tolerability study . Cerebrovascular Diseases . 20 . 5 . 304–309 . 2005 . 16131799 . 10.1159/000087929 . 25034903 .
3. Elting JW, Sulter GA, Kaste M, Lees KR, Diener HC, Hommel M, Versavel M, Teelken AW, De Keyser J . 6 . AMPA antagonist ZK200775 in patients with acute ischemic stroke: possible glial cell toxicity detected by monitoring of S-100B serum levels . Stroke . 33 . 12 . 2813–2818 . December 2002 . 12468775 . 10.1161/01.str.0000043823.37955.fb . free .
4. Bergholz R, Staks T, Rüther K . Effects of the AMPA antagonist ZK 200775 on visual function: a randomized controlled trial . PLOS ONE . 5 . 8 . e12111 . August 2010 . 20711429 . 2920815 . 10.1371/journal.pone.0012111 . free . 2010PLoSO...512111B .