Cabozantinib compositions and methods of use
AssigneeHanda Oncology, LLC
InventorsFang-Yu Liu, K.C. Sung, Yu Zhang, Shang Wei Qin, John Duan, George Kraft
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Abstract
The present invention relates to oral compositions comprising cabozantinib salts and at least one pharmaceutically acceptable excipient and methods of using the oral compositions to increase the oral bioavailability of the cabozantinib and reduce the adverse events associate with the oral administration of cabozantinib. The invention also relates to methods for preparing cabozantinib lauryl sulfate salts.
Claims21
A method for treating a human subject in need of cabozantinib treatment comprising orally administering to the subject a daily dose of about 7.5 mg to about 80 mg of cabozantinib free base in the form of cabozantinib lauryl sulfate salt wherein the administration is once a day and comprises administering one or more capsules wherein the contents of the one or more capsules comprise:
- (i) about 7.5 mg to about 80 mg of cabozantinib free base in the form of cabozantinib lauryl sulfate salt;
- and
- (ii) about 50 wt % to about 90 wt % of one or more polyoxyethylene pharmaceutical acceptable excipients with a hydrophilic-lipophilic balance (HLB) value of about 10 or greater selected from the group consisting of wetting agents, emulsifying agents, solubilizing surfactants and combinations thereof;
- and wherein the once daily administration of the one or more capsules results in a Cmax of at least about 8.0 ng/ml/mg of cabozantinib free base when administered under fasting conditions.
A method for treating a human subject in need of cabozantinib treatment comprising orally administering to the subject a daily dose of about 7.5 mg to about 80 mg of cabozantinib free base in the form of cabozantinib lauryl sulfate salt wherein the administration is once a day and comprises administering one or more capsules wherein the contents of the one or more capsules comprise:
- (i) about 7.5 mg to about 80 mg of cabozantinib free base in the form of cabozantinib lauryl sulfate salt;
- and
- (ii) about 50 wt % to about 90 wt % of one or more polyoxyethylene pharmaceutical acceptable excipients with a hydrophilic-lipophilic balance (HLB) an HLB value of about 10 or greater selected from the group consisting of wetting agents, emulsifying agents, solubilizing surfactants and combinations thereof;
- and wherein the once daily administration of the one or more capsules results in an AUC0-√ of at least 575 ng·hr/mL/mg of cabozantinib free base when administered under fasting conditions.
A method for treating a human subject in need of cabozantinib treatment comprising orally administering to the subject a daily dose of about 7.5 mg to about 80 mg of cabozantinib free base in the form of cabozantinib lauryl sulfate salt wherein the administration is once a day and comprises administering one or more capsules wherein the contents of one or more capsules comprise:
- (i) about 7.5 mg to about 80 mg of cabozantinib free base in the form of cabozantinib lauryl sulfate salt;
- and
- (ii) about 50 wt % to about 90 wt % of one or more polyoxyethylene pharmaceutical acceptable excipients with a hydrophilic-lipophilic balance (HLB) value of about 10 or greater selected from the group consisting of wetting agents, emulsifying agents, solubilizing surfactants and combinations thereof;
- and wherein the once daily administration of the one or more capsules results in a Cmax of at least about 8.0 ng/ml/mg of cabozantinib free base when administered under fasting conditions and an AUC0-√ of at least 575 ng·hr/mL/mg of cabozantinib free base when administered under fasting conditions.
Dependencies are inferred from the claim text.