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Chemical Compound Review

Apricitabine     4-amino-1-[(2R,4R)-2- (hydroxymethyl)-1,3...

Synonyms: AVX-754, BCH-270, SPD-754, AVX754, SPD754, ...
 
 
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Disease relevance of trans-Oxathiolan-C

 

High impact information on trans-Oxathiolan-C

 

Chemical compound and disease context of trans-Oxathiolan-C

 

Biological context of trans-Oxathiolan-C

 

Anatomical context of trans-Oxathiolan-C

 

Associations of trans-Oxathiolan-C with other chemical compounds

  • The mean 50% inhibitory concentration of dOTC for drug-naive isolates was 1.76 microM, rising to only 2.53 and 2.5 microM for viruses resistant to 3TC and viruses resistant to 3TC and AZT, respectively [10].
  • Intracellular metabolism studies showed that dOTC is phosphorylated within cells via the deoxycytidine kinase pathway and that approximately 2 to 5% of dOTC is converted into the racemic triphosphate derivatives, which had measurable half-lives (2 to 3 hours) within cells [10].
  • In contrast, virus resistant to dOTC and (-)dOTC took longer to appear (15-20 passages), with a methionine (ATG) to valine (GTG) amino acid change at position 184 identified in both cases [7].
 

Analytical, diagnostic and therapeutic context of trans-Oxathiolan-C

  • Subjects received single oral doses of 100, 200, 400, 800, and 1,600 mg of racemic dOTC in a placebo-controlled, dose-rising, incomplete crossover study design, and the pharmacokinetics of both (+)dOTC and (-)dOTC were determined [8].

References

  1. Selection and characterization of HIV-1 variants resistant to the (+) and (-) enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine (dOTC). Richar, N., Quan, Y., Salomon, H., Hsu, M., Bedard, J., Harrigan, P.R., Rando, R., Mansour, T., Bowlin, T.L., Wainberg, M.A. Antivir. Ther. (Lond.) (1999) [Pubmed]
  2. Efficacy and tolerability of 10-day monotherapy with apricitabine in antiretroviral-naive, HIV-infected patients. Cahn, P., Cassetti, I., Wood, R., Phanuphak, P., Shiveley, L., Bethell, R.C., Sawyer, J. AIDS (2006) [Pubmed]
  3. Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. Mansour, T.S., Jin, H., Wang, W., Hooker, E.U., Ashman, C., Cammack, N., Salomon, H., Belmonte, A.R., Wainberg, M.A. J. Med. Chem. (1995) [Pubmed]
  4. In vitro antiretroviral activity and in vitro toxicity profile of SPD754, a new deoxycytidine nucleoside reverse transcriptase inhibitor for treatment of human immunodeficiency virus infection. Gu, Z., Allard, B., de Muys, J.M., Lippens, J., Rando, R.F., Nguyen-Ba, N., Ren, C., McKenna, P., Taylor, D.L., Bethell, R.C. Antimicrob. Agents Chemother. (2006) [Pubmed]
  5. Antiviral activity of 2'-deoxy-3'-oxa-4'-thiocytidine (BCH-10652) against lamivudine-resistant human immunodeficiency virus type 1 in SCID-hu Thy/Liv mice. Stoddart, C.A., Moreno, M.E., Linquist-Stepps, V.D., Bare, C., Bogan, M.R., Gobbi, A., Buckheit, R.W., Bedard, J., Rando, R.F., McCune, J.M. Antimicrob. Agents Chemother. (2000) [Pubmed]
  6. Selection of resistance-conferring mutations in HIV-1 by the nucleoside reverse transcriptase inhibitors (+/-)dOTC and (+/-)dOTFC. Richard, N., Salomon, H., Oliveira, M., Rando, R., Mansour, T., Gu, Z., Wainberg, M.A. Antivir. Chem. Chemother. (2000) [Pubmed]
  7. Drug resistance and drug combination features of the human immunodeficiency virus inhibitor, BCH-10652 [(+/-)-2'-deoxy-3'-oxa-4'-thiocytidine, dOTC]. Taylor, D.L., Ahmed, P.S., Tyms, A.S., Wood, L.J., Kelly, L.A., Chambers, P., Clarke, J., Bedard, J., Bowlin, T.L., Rando, R.F. Antivir. Chem. Chemother. (2000) [Pubmed]
  8. Safety, tolerability, and pharmacokinetics of single oral doses of BCH-10652 in healthy adult males. Smith, P.F., Forrest, A., Ballow, C.H., Martin, D.E., Proulx, L. Antimicrob. Agents Chemother. (2000) [Pubmed]
  9. Absolute bioavailability and disposition of (-) and (+) 2'-deoxy- 3'-oxa-4'-thiocytidine (dOTC) following single intravenous and oral doses of racemic dOTC in humans. Smith, P.F., Forrest, A., Ballow, C.H., Martin, D.E., Proulx, L. Antimicrob. Agents Chemother. (2000) [Pubmed]
  10. Anti-human immunodeficiency virus type 1 activity, intracellular metabolism, and pharmacokinetic evaluation of 2'-deoxy-3'-oxa-4'-thiocytidine. de Muys, J.M., Gourdeau, H., Nguyen-Ba, N., Taylor, D.L., Ahmed, P.S., Mansour, T., Locas, C., Richard, N., Wainberg, M.A., Rando, R.F. Antimicrob. Agents Chemother. (1999) [Pubmed]
  11. Effect of food on the pharmacokinetics of (-) and (+) dOTC when administered as an oral racemate. Smith, P.F., Forrest, A., Adams, J.M., Ballow, C.H. Journal of clinical pharmacology. (2002) [Pubmed]
 
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