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Chemical Compound Review:

Loveride 2-(2,6-dichlorophenyl)-2-[(2- ethanoyl-5...

Synonyms: loviride, CHEMBL37624, SureCN247781, AG-J-83476, CHEBI:156070, ...

Witvrouw, M. et al., Schmit, J.C. et al., Quiñones-Mateu, M.E. et al., Jonckheere, H. et al., Miller, V. et al., et al.

Miller, de Béthune, Kober, Stürmer, Hertogs, Pauwels, Stoffels, Staszewski,

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Disease relevance of R 89439

The IC50 of the alpha-APA derivative R 89439 for HIV-1 cytopathicity in MT-4 cells was 13 nM [1].
Patterns of resistance and cross-resistance to human immunodeficiency virus type 1 reverse transcriptase inhibitors in patients treated with the nonnucleoside reverse transcriptase inhibitor loviride [2].

High impact information on R 89439

OBJECTIVE: To investigate whether, in addition to HIV-1, different strains of HIV-2 (ROD and EHO) and SIV (mac251, agm3 and mndGB1) are sensitive to a selection of NNRTI i.e. delavirdine, the HEPT derivative I-EBU (MKC-442), 8-chloro-TIBO (tivirapine), alpha-APA (loviride), nevirapine and the pyridinone derivative L-697,661 [3].
We have determined the structures of the unliganded form of the Lys103Asn mutant HIV-1 RT and in complexes with loviride and HBY 097 [4].
A human immunodeficiency virus type 1 (HIV-1)-seropositive patient was treated sequentially with the dideoxynucleoside (ddN) analogues zidovudine, didanosine, zalcitabine, stavudine, and lamivudine and the nonnucleoside HIV-1-specific reverse transcriptase inhibitor (NNRTI) loviride (alpha-APA) [5].
While the RT of the BH10 isolate was sensitive to nevirapine and loviride (IC50 ranged from 0.16 to 8.2 microM, depending on the substrates used), the enzyme of the Spanish HIV-1 group O isolate showed high-level resistance to those compounds (IC50 > 200 microM) [6].
We compared the development of resistance toward BI-RG-587 (nevirapine) and alpha-APA R89439 (loviride) starting from the wild-type HIV-1 strain IIIB and the 3TC-resistant HIV-1 strain containing the M184V mutation [7].

References

Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of alpha-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase. Pauwels, R., Andries, K., Debyser, Z., Van Daele, P., Schols, D., Stoffels, P., De Vreese, K., Woestenborghs, R., Vandamme, A.M., Janssen, C.G. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
Patterns of resistance and cross-resistance to human immunodeficiency virus type 1 reverse transcriptase inhibitors in patients treated with the nonnucleoside reverse transcriptase inhibitor loviride. Miller, V., de Béthune, M.P., Kober, A., Stürmer, M., Hertogs, K., Pauwels, R., Stoffels, P., Staszewski, S. Antimicrob. Agents Chemother. (1998) [Pubmed]
Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV. Witvrouw, M., Pannecouque, C., Van Laethem, K., Desmyter, J., De Clercq, E., Vandamme, A.M. AIDS (1999) [Pubmed]
The Lys103Asn mutation of HIV-1 RT: a novel mechanism of drug resistance. Hsiou, Y., Ding, J., Das, K., Clark, A.D., Boyer, P.L., Lewi, P., Janssen, P.A., Kleim, J.P., Rösner, M., Hughes, S.H., Arnold, E. J. Mol. Biol. (2001) [Pubmed]
Multiple drug resistance to nucleoside analogues and nonnucleoside reverse transcriptase inhibitors in an efficiently replicating human immunodeficiency virus type 1 patient strain. Schmit, J.C., Cogniaux, J., Hermans, P., Van Vaeck, C., Sprecher, S., Van Remoortel, B., Witvrouw, M., Balzarini, J., Desmyter, J., De Clercq, E., Vandamme, A.M. J. Infect. Dis. (1996) [Pubmed]
Characterization of the reverse transcriptase of a human immunodeficiency virus type 1 group O isolate. Quiñones-Mateu, M.E., Soriano, V., Domingo, E., Menéndez-Arias, L. Virology (1997) [Pubmed]
Lamivudine resistance of HIV type 1 does not delay development of resistance to nonnucleoside HIV type 1-specific reverse transcriptase inhibitors as compared with wild-type HIV type 1. Jonckheere, H., Witvrouw, M., De Clercq, E., Anné, J. AIDS Res. Hum. Retroviruses (1998) [Pubmed]

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