Literature summary for 2.4.2.12 extracted from

Beauparlant, P.; Bedard, D.; Bernier, C.; Chan, H.; Gilbert, K.; Goulet, D.; Gratton, M.O.; Lavoie, M.; Roulston, A.; Turcotte, E.; Watson, M.
Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777 (2009), Anticancer Drugs, 20, 346-354.

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Application

Application	Comment	Organism
medicine	a dose of 75 mg/kg GMX1777, i.e. 1-[2-(2-(2-(2-methoxyethoxy)-ethoxy)ethoxy)-ethoxy-carbonyloxymethyl]-4-[N'-cyano-N''-(6-(4-chlorophenyl)-hexyl)-N-guanidino]pyridinium chloride, prodrug of GMX1778, administered over a 24 h intravenous infusion causes tumor regression in the IM-9 model, the SHP-77 model, and HCT-116 model. A 72 h continuous intravenous infusion is also effective in the IM-9 model, but is associated with smaller therapeutic index	Homo sapiens
medicine	a dose of 75 mg/kg GMX1777, i.e. 1-[2-(2-(2-(2-methoxyethoxy)-ethoxy)ethoxy)-ethoxy-carbonyloxymethyl]-4-[N'-cyano-N''-(6-(4-chlorophenyl)-hexyl)-N-guanidino]pyridinium chloride, prodrug of GMX1778, administered over a 24 h intravenous infusion produces GMX1778 steady-state plasma levels of about 1 microg/ml and causes nicotinamide dinucleotide levels to decrease significnantly in tumors. Nicotinic acid protects mice treated with a lethal dose of GMX1777	Mus musculus

Inhibitors

Inhibitors	Comment	Organism	Structure
GMX1777	i.e. 1-[2-(2-(2-(2-methoxyethoxy)-ethoxy)ethoxy)-ethoxy-carbonyloxymethyl]-4-[N'-cyano-N''-(6-(4-chlorophenyl)-hexyl)-N-guanidino]pyridinium chloride, prodrug of GMX1778. A dose of 75 mg/kg administered over a 24 h intravenous infusion causes tumor regression in the IM-9 model, the SHP-77 model, and HCT-116 model. A 72 h continuous intravenous infusion is also effective in the IM-9 model, but is associated with smaller therapeutic index	Homo sapiens
GMX1777	i.e. 1-[2-(2-(2-(2-methoxyethoxy)-ethoxy)ethoxy)-ethoxy-carbonyloxymethyl]-4-[N'-cyano-N''-(6-(4-chlorophenyl)-hexyl)-N-guanidino]pyridinium chloride, prodrug of GMX1778. A dose of 75 mg/kg administered over a 24 h intravenous infusion produces GMX1778 steady-state plasma levels of about 1 microg/ml and causes nicotinamide dinucleotide levels to decrease significnantly in tumors. Nicotinic acid protects mice treated with a lethal dose of GMX1777	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Mus musculus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
HCT-116 cell	-	Homo sapiens	-
IM-9 cell	-	Homo sapiens	-
SHP-77 cell	-	Homo sapiens	-

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Release 2023.1 (January 2023)