Cabozantinib dosage form and use in the treatment of cancer
Inventors
Assignees
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Publication Number
US-11564915-B2
Publication Date
2023-01-31
Expiration Date
Abstract
This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer.
Core Innovation
The disclosure relates to treating cancer using Compound 1, cabozantinib (XL184), in the form of malate salt forms, including L-malate. It centers on crystalline malate salt forms, including crystalline N-1 forms of (S)-malate and (R)-malate, and specifically describes the use of an L-malate salt in a pharmaceutical dosage.
A key aspect of the disclosure is a cabozantinib dosage-form and administration regimen in tablet form. The disclosure describes once daily oral dosing regimens of 60 mg, 40 mg, or 20 mg of Compound 1 as the L-malate salt, with formulation-related discussion for tablet and capsule presentations.
The formulation described includes a tablet composition comprising Compound 1 and excipients including microcrystalline cellulose, lactose anhydrous, hydroxypropyl cellulose, croscarmellose sodium, colloidal silicon dioxide, and magnesium stearate. The disclosure also addresses treatment evaluation and response using serological and radiographic assessments, including PSA response and RECIST 1.1, bone scan, CT, NaF, and FDG-PET, along with adverse events and dose adjustment considerations.
Claims Coverage
The provided claim set contains three independent claims, each covering endometrial cancer treatment by once-daily administration of a specified mg amount of Compound 1 as the L-malate salt, formulated as a tablet with specified ingredient percentages. Across the three claims, the inventive features are the same in kind, differing primarily by the dose level (60 mg, 40 mg, or 20 mg).
Once-daily 60 mg L-malate tablet treatment of endometrial cancer
A method of treating endometrial cancer comprising administering once daily to a patient in need thereof a pharmaceutical dosage comprising 60 mg of compound 1 as the L-malate salt, wherein the L-malate salt is administered as a tablet.
Once-daily 40 mg L-malate tablet treatment of endometrial cancer
A method of treating endometrial cancer comprising administering once daily to a patient in need thereof a pharmaceutical dosage comprising 40 mg of compound 1 as the L-malate salt, wherein the L-malate salt is administered as a tablet.
Once-daily 20 mg L-malate tablet treatment of endometrial cancer
A method of treating endometrial cancer comprising administering once daily to a patient in need thereof a pharmaceutical dosage comprising 20 mg of compound 1 as the L-malate salt, wherein the L-malate salt is administered as a tablet.
All independent claims require once daily treatment of endometrial cancer using Compound 1 as the L-malate salt, with tablet administration and specified dosing levels (60 mg, 40 mg, or 20 mg) for the pharmaceutical dosage.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treating endometrial cancer in a patient in need of such treatment.
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