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Chemical Compound Review

Icofungipen     (1R,2S)-2-amino-4- methylidene-cyclopentane...

Synonyms: AHMA, PLD-118, PLD118, CHEMBL343803, SureCN117349, ...
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Disease relevance of PLD 118

  • All except two in vitro-resistant mutants were pathogenic in a murine candidiasis model, and BAY 10-8888 failed to cure the infection [1].
  • This was demonstrated in a lethal model of C. albicans infection in mice and rats in which icofungipen showed dose-dependent protection at oral doses of 10 to 20 mg/kg of body weight per day in mice and 2 to 10 mg/kg/day in rats [2].

High impact information on PLD 118

  • Icofungipen shows nearly complete oral bioavailability in a variety of species, and its in vivo efficacy indicates its potential for the oral treatment of yeast infections [2].
  • The efficacy of icofungipen in mice and rats was not influenced by concomitant administration of equimolar amounts of L-isoleucine, which was shown to antagonize its antifungal activity in vitro [2].
  • Pharmacokinetics of icofungipen in plasma approximated a dose-dependent relationship of the maximum concentration of drug in serum and the area under the concentration-time curve [3].
  • We investigated the efficacy, plasma pharmacokinetics, and safety of icofungipen in escalating dosages for the treatment of experimental subacute disseminated candidiasis in persistently neutropenic rabbits [3].
  • PLD-118- and DAMB-treated animals showed a significant dosage-dependent clearance of C. albicans from the tongue, oropharynx, and esophagus in comparison to untreated controls (P </= 0.05, P </= 0.01, P </= 0.001, respectively), while FLC had no significant activity [4].

Chemical compound and disease context of PLD 118

  • Study groups consisted of untreated controls; animals receiving PLD-118 at 4, 10, 25, or 50 mg/kg of body weight/day via intravenous (i.v.) twice daily (BID) injections; animals receiving FLC at 2 mg/kg/day via i.v. BID injections; and animals receiving desoxycholate amphotericin B (DAMB) i.v. at 0.5 mg/kg/day [4].

Biological context of PLD 118

  • BAY 10-8888 inhibited isoleucyl-tRNA synthetase with the same concentration dependency as protein biosynthesis in intact cells assuming 200-fold accumulation [5].
  • Inside the cell BAY 10-8888 inhibited specifically isoleucyl-tRNA synthetase, resulting in inhibition of protein synthesis and cell growth [5].

Anatomical context of PLD 118


Associations of PLD 118 with other chemical compounds

  • PLD-118 (10 and 100 microM) incubated for 0-60 min with S9 fractions and NADPH was determined by HPLC, using the Waters AccQ.Tag method after derivatization of amino acids to stable, fluorescent derivatives [6].

Analytical, diagnostic and therapeutic context of PLD 118


  1. Decreased accumulation or increased isoleucyl-tRNA synthetase activity confers resistance to the cyclic beta-amino acid BAY 10-8888 in Candida albicans and Candida tropicalis. Ziegelbauer, K. Antimicrob. Agents Chemother. (1998) [Pubmed]
  2. In vitro activity and in vivo efficacy of icofungipen (PLD-118), a novel oral antifungal agent, against the pathogenic yeast Candida albicans. Hasenoehrl, A., Galic, T., Ergovic, G., Marsic, N., Skerlev, M., Mittendorf, J., Geschke, U., Schmidt, A., Schoenfeld, W. Antimicrob. Agents Chemother. (2006) [Pubmed]
  3. Efficacy, plasma pharmacokinetics, and safety of icofungipen, an inhibitor of Candida isoleucyl-tRNA synthetase, in treatment of experimental disseminated candidiasis in persistently neutropenic rabbits. Petraitiene, R., Petraitis, V., Kelaher, A.M., Sarafandi, A.A., Mickiene, D., Groll, A.H., Sein, T., Bacher, J., Walsh, T.J. Antimicrob. Agents Chemother. (2005) [Pubmed]
  4. Efficacy of PLD-118, a novel inhibitor of candida isoleucyl-tRNA synthetase, against experimental oropharyngeal and esophageal candidiasis caused by fluconazole-resistant C. albicans. Petraitis, V., Petraitiene, R., Kelaher, A.M., Sarafandi, A.A., Sein, T., Mickiene, D., Bacher, J., Groll, A.H., Walsh, T.J. Antimicrob. Agents Chemother. (2004) [Pubmed]
  5. Molecular mode of action of the antifungal beta-amino acid BAY 10-8888. Ziegelbauer, K., Babczinski, P., Schönfeld, W. Antimicrob. Agents Chemother. (1998) [Pubmed]
  6. The novel antifungal agent PLD-118 is neither metabolized by liver microsomes nor inhibits cytochrome P450 in vitro. Parnham, M.J., Bogaards, J.J., Schrander, F., Schut, M.W., Oresković, K., Mildner, B. Biopharmaceutics & drug disposition. (2005) [Pubmed]
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