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Chemical Compound Review:

ACMC-20mohj 5-chloro-1-[4-fluoro-5...

Synonyms: SureCN11890294, AC1L1TRN, CTK8G6647, AC1Q3H9D, Uridine,5-chloro-2',3'-dideoxy-3'-fluoro-

Riddler, S.A. et al., Daluge, S.M. et al., Balzarini, J. et al., Van Aerschot, A. et al.

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Disease relevance of Fddclurd

5-Halogeno-3'-fluoro-2',3'-dideoxyuridines as inhibitors of human immunodeficiency virus (HIV): potent and selective anti-HIV activity of 3'-fluoro-2',3'-dideoxy-5-chlorouridine [1].
935U83 showed low toxicity [2].
Of these 5-halogenated derivatives, 3'-fluoro-2',3'-dideoxy-5-chlorouridine emerged as the most selective inhibitor of HIV-1 replication [3].

High impact information on Fddclurd

The effect of a high-fat meal on the oral bioavailability of 935U83 was also assessed [4].
Safety and pharmacokinetics of 5-chloro-2',3'-dideoxy-3'-fluorouridine (935U83) following oral administration of escalating single doses in human immunodeficiency virus-infected adults [4].
Systemic exposure to 935U83 at levels exceeding its average in vitro antiretroviral 50% inhibitory concentration (approximately 0.5 microgram/ml or 1.8 microM) can be achieved after a single oral dose [4].
In an in vitro assay for toxicity to a human erythrocyte progenitor, erythroid burst-forming unit (BFU-E), the IC50 for 935U83 (> 400 microM) was more than 1,000-fold those of FLT (0.07 microM) and AZT (0.30 microM) [2].

Biological context of Fddclurd

A phase I study was conducted to evaluate the safety and pharmacokinetics of six escalating single oral doses of 935U83 in 12 HIV-infected adults [4].

Anatomical context of Fddclurd

Mild reversible reductions in erythrocytes and associated parameters were seen in mice dosed orally with 2,000 mg of 935U83 per kg per day for 1 and 6 months [2].

Analytical, diagnostic and therapeutic context of Fddclurd

935U83 was rapidly and well absorbed following oral administration with peak plasma concentrations (Cmax) occurring at 0.8 to 1.3 h postdosing [4].

References

5-Halogeno-3'-fluoro-2',3'-dideoxyuridines as inhibitors of human immunodeficiency virus (HIV): potent and selective anti-HIV activity of 3'-fluoro-2',3'-dideoxy-5-chlorouridine. Balzarini, J., Van Aerschot, A., Pauwels, R., Baba, M., Schols, D., Herdewijn, P., De Clercq, E. Mol. Pharmacol. (1989) [Pubmed]
5-Chloro-2',3'-dideoxy-3'-fluorouridine (935U83), a selective anti-human immunodeficiency virus agent with an improved metabolic and toxicological profile. Daluge, S.M., Purifoy, D.J., Savina, P.M., St Clair, M.H., Parry, N.R., Dev, I.K., Novak, P., Ayers, K.M., Reardon, J.E., Roberts, G.B. Antimicrob. Agents Chemother. (1994) [Pubmed]
3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. Van Aerschot, A., Herdewijn, P., Balzarini, J., Pauwels, R., De Clercq, E. J. Med. Chem. (1989) [Pubmed]
Safety and pharmacokinetics of 5-chloro-2',3'-dideoxy-3'-fluorouridine (935U83) following oral administration of escalating single doses in human immunodeficiency virus-infected adults. Riddler, S.A., Wang, L.H., Bartlett, J.A., Savina, P.M., Packard, M.V., McMahon, D.K., Blum, M.R., Dunn, J.A., Elkins, M.M., Mellors, J.W. Antimicrob. Agents Chemother. (1996) [Pubmed]

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