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

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Chemical Compound Review:

CHEMBL313113 4-[2-[4-[(E)-3-ethoxyprop-1- enyl]phenyl]-5...

Synonyms: SureCN3826448, ONT 093, AC1O52DR, OC 144-093, 216227-54-2

Chi, K.N. et al., Mistry, P. et al., Kuppens, I.E. et al.

Mistry, Folkes, Kuppens, Bosch, van Maanen, Rosing, Fitzpatrick, Beijnen, Schellens, Chi, Chia, Dixon, Newman, Wacher, Sikic, Gelmon,

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Disease relevance of ONT 093

Phase I trials of ONT-093 in normal human volunteers showed no dose-limiting toxicities at serum concentrations associated with biologic activity achieved with doses ranging from 300 to 500 mg [1].
Four of 6 patients receiving 500 mg doses of ONT-093 and paclitaxel at 175 mg/m(2) (dose level 4) had higher-grade neutropenia with cycle 2, with 1 patient experiencing febrile neutropenia [1].

High impact information on ONT 093

A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer [1].
Oral bioavailability of docetaxel in combination with OC144-093 (ONT-093) [2].

Biological context of ONT 093

In pre-clinical studies, ONT-093 could inhibit P-gp and reverse multidrug resistance at nM concentrations with no effect on paclitaxel pharmacokinetics [1].

Analytical, diagnostic and therapeutic context of ONT 093

Ontogen is developing ONT-093 (formerly OC-144-093), a P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy [3].

References

A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Chi, K.N., Chia, S.K., Dixon, R., Newman, M.J., Wacher, V.J., Sikic, B., Gelmon, K.A. Investigational new drugs. (2005) [Pubmed]
Oral bioavailability of docetaxel in combination with OC144-093 (ONT-093). Kuppens, I.E., Bosch, T.M., van Maanen, M.J., Rosing, H., Fitzpatrick, A., Beijnen, J.H., Schellens, J.H. Cancer Chemother. Pharmacol. (2005) [Pubmed]
ONT-093 (Ontogen). Mistry, P., Folkes, A. Current opinion in investigational drugs (London, England : 2000) (2002) [Pubmed]

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