Next Generation Integrase Inhibitors

The field is now poised to move into a new phase that will address opportunities for improvement on the profiles of RAL and EVG. These next generation drugs will need to deliver notable advantages in resistance profile along with having a high genetic barrier to resistance [51,52]. 

The recent disclosure of 21 (S/GSK1349572) as a next generation INI has been supported by preclinical data showing this compound to be a potent antiviral (PBMC IC50 = 0.15 ng/mL) with a low clearance and good oral bioavailability Cl, (%F) across species (rat 0.2mL/min/kg, (35%), dog 2.2, (35%), cyno 2.1, (25%)) [56]. The protein-binding-adjusted 

Squires, R. Asfour, D. Richman, J. Chen, A. Saah, R. Leavitt, D. Hazuda, and 

Nguyen, Abstract 161, 12th Conference of Retroviruses and Opportunistic Infections, Boston, MA, February, 2005. 

Schaller, R. G. Sherrill, T. Yoshinaga, M. Kobayashi, C. Wakasa-Morimoto, S. Miki, 

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