Literature summary for 2.1.1.45 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.

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Application

Application	Comment	Organism
medicine	pharmacological treatment of colorectal cancer	Homo sapiens
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

Inhibitors	Comment	Organism	Structure
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)

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

Organism

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

Source Tissue

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

Substrates and Products (Substrate)

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

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Release 2023.1 (January 2023)