Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Clamp, A.R.; Schoeffski, P.; Valle, J.W.; Wilson, R.H.; Marreaud, S.; Govaerts, A.S.; Debois, M.; Lacombe, D.; Twelves, C.; Chick, J.; Jayson, G.C.; Jayson, G.C.
    A phase I and pharmacokinetic study of OSI-7904L, a liposomal thymidylate synthase inhibitor in combination with oxaliplatin in patients with advanced colorectal cancer (2008), Cancer Chemother. Pharmacol., 61, 579-585.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.1.45 medicine pharmacological treatment of colorectal cancer Homo sapiens
2.1.1.45 medicine treatment of patients with advanced colorectal carcinoma with liposomal inhibitor OSI-7904L, in combination with oxaliplatin. At the highest dose level of OSI-7904L 9 mg/m2, oxaliplatin 130 mg/m2, one of nine patients experienced dose-limiting toxicity of grade 3 oral mucositis with cycle 1 and five further patients required dose reductions. The toxicity profile of stomatitis, diarrhea, nausea, fatigue, sensory neuropathy and skin rash was consistent with that expected for a thymidylate synthase inhibitor/oxaliplatin combination regimen. High interpatient variability with no detectable interaction between OSI-7904L and oxaliplatin Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.45 OSI-7904L a liposomal thymidylate synthase inhibitor, a liposomal formulation of OSI-7904 (S)-2-(5-((1,2-dihydro-3-methyl-1-oxobenzo(f)quinazolin-9-yl)methyl)amino-1-oxo-2-isoindolynl)-glutaric acid, administered in combination with oxaliplatin every 21 days in patients with advanced colorectal carcinoma; treatment of patients with advanced colorectal carcinoma, in combination with oxaliplatin. At the highest dose level of OSI-7904L 9 mg/m2, oxaliplatin 130 mg/m2, one of nine patients experienced dose-limiting toxicity of grade 3 oral mucositis with cycle 1 and five further patients required dose reductions. The toxicity profile of stomatitis, diarrhea, nausea, fatigue, sensory neuropathy and skin rash was consistent with that expected for a thymidylate synthase inhibitor/oxaliplatin combination regimen. High interpatient variability with no detectable interaction between OSI-7904L and oxaliplatin Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Homo sapiens
-
 7,8-dihydrofolate + dTMP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.45 Homo sapiens
-
-
-
2.1.1.45 Homo sapiens
-
 patients with advanced colorectal carcinoma
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.45 colorectal cancer cell advanced colorectal cancer Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Homo sapiens 7,8-dihydrofolate + dTMP
-
 ?