This study was a outstanding result for R-125489 and its prodrug...

This study was a outstanding result for R-125489 and its prodrug CS-8958 ( inavir )

(Once administered, the prodrug is metabolised in vivo into an active metabolite, a process termed bioactivation.)

Wouldnt it great if BTA mgmt promoted this news for R-125489 (and by direct association Inavir) when the world is so worried about H274Y Tamiflu resistance. Don't hold your breath. Great news anyway.


'Based on results obtained by SMD and the molecular mechanics-Poisson?Boltzmann surface area
method, we predict that R-125489 can be used to treat not only wild-type but also tamiflu-resistant
N294S, H274Y variants of A/H5N1 virus as its binding affinity does not vary much across these systems.'

'Our prediction is qualitatively supported by the experiments of Kiso et al. [19] who have shown that
R-125489 displays almost the same inhibition ability for WT andmutants of VN1203 and HN30408. In fact, using their data on CI50 one obtains DGexp13.11, 11.91 and 12.15 kcal/molfor WT, N294S and H274Y of VN1203, respectively.

This implies that the binding of R-125489 is insensitive to mutations.'


http://info.ifpan.edu.pl/~masli/Publications/Binh_BBRC11.pdf