Immune Response Modifier Formulations And Methods
An aqueous parenteral pharmaceutical formulation of the IRM drug compound N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide dissolved in water, buffer selected from citric acid, acetic acid, lactic acid, succinic acid, and tartaric acid, and optionally a tonicity adjuster, preferably selected from sorbitol and mannitol, wherein the pH is no greater than 6 and the formulation is sterile and preferably substantially free of sodium chloride.
1 . An aqueous pharmaceutical formulation suitable for injection, comprising:
the drug compound N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide fully dissolved in the formulation;
water;
buffer selected from the group consisting of citric acid, acetic acid, lactic acid, succinic acid, and tartaric acid; and
optionally a tonicity adjuster;
wherein the pH is no greater than 6 and the formulation is sterile.
2 . The formulation of claim 1 , wherein the N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide is present at a concentration of at least 1 mg/ml.
3 . The formulation of claim 1 , wherein the N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide is present at a concentration of at least 2 mg/ml.
4 . The formulation of claim 1 , wherein the N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide is present at a concentration of at least 5 mg/ml.
5 . The formulation of claim 1 , wherein the N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide is present at a concentration of at least mg/ml.
6 . The formulation of any preceding claim wherein the buffer is selected from the group consisting of citric acid and acetic acid.
7 . The formulation of claim 6 , wherein the buffer is citric acid.
8 . The formulation of any preceding claim, wherein the pH is 5.
9 . A method of delivering the drug compound N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide by injecting into a subject a formulation comprising:
N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide fully dissolved in the formulation;
water;
buffer selected from the group consisting of citric acid, acetic acid, lactic acid, succinic acid, and tartaric acid; and
optionally a tonicity adjuster;
wherein the pH is no greater than 6 and the formulation is sterile.
10 . The method of claim 9 , wherein the formulation is injected intravenously.
11 . The method of claim 9 , wherein the formulation is injected subcutaneously.
12 . The method of claim 9 , wherein the formulation is injected into a tumor mass.
13 . A method of treating a disease by injecting into a subject in need of treatment of the disease a formulation comprising:
N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide fully dissolved in the formulation;
water;
buffer selected from the group consisting of citric acid, acetic acid, lactic acid, succinic acid, and tartaric acid; and
optionally a tonicity adjuster;
wherein the pH is no greater than 6 and the formulation is sterile.
14 . The method of claim 13 , wherein the injection is subcutaneous.
15 . The method of claim 13 , wherein the injection is intraveneous.
16 . The method of claim 13 , wherein the injection is directly into a tumor mass.
17 . The method of claim 13 , wherein the disease is metastatic melanoma.
18 . The formulation or method of any preceding claim, wherein the formulation includes a tonicity adjuster selected from the group consisting of sorbitol and mannitol.
19 . The formulation or method of claim 18 , wherein the tonicity adjuster is mannitol.
20 . The formulation or method of any preceding claim, wherein the formulation is substantially free of sodium chloride.