Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

DMP-851 (4R,5S,6S,7R)-1-[(3-amino-1H- indazol-5...

Synonyms: CHEMBL413332, XQ-443, AG-E-37857, SureCN1046061, DMP 851, ...

Rodgers, J.D. et al., Aungst, B.J. et al.

Rodgers, Lam, Johnson, Wang, Li, Ru, Ko, Seitz, Trainor, Anderson, Klabe, Bacheler, Cordova, Garber, Reid, Wright, Chang, Erickson-Viitanen, Aungst, Nguyen, Bulgarelli, Oates-Lenz,

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Disease relevance of DMP 851

As DMP 850 and DMP 851 provide plasma levels of free drug that are sufficient to inhibit wild-type HIV and several mutant forms of HIV, they could show improved ability to decrease viral load for clinically significant time periods [1].

High impact information on DMP 851

The ultimate success of DMP 850 and DMP 851 in clinical trials might depend on achieving or exceeding the oral bioavailability seen in dog [1].
The cyclic ureas, DMP 450, DMP 850, and DMP 851, have Caco-2 permeabilities suggestive of moderate-to-high oral absorption potential in humans [2].

References

Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors. Rodgers, J.D., Lam, P.Y., Johnson, B.L., Wang, H., Li, R., Ru, Y., Ko, S.S., Seitz, S.P., Trainor, G.L., Anderson, P.S., Klabe, R.M., Bacheler, L.T., Cordova, B., Garber, S., Reid, C., Wright, M.R., Chang, C.H., Erickson-Viitanen, S. Chem. Biol. (1998) [Pubmed]
The influence of donor and reservoir additives on Caco-2 permeability and secretory transport of HIV protease inhibitors and other lipophilic compounds. Aungst, B.J., Nguyen, N.H., Bulgarelli, J.P., Oates-Lenz, K. Pharm. Res. (2000) [Pubmed]

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