Compositions and methods for treating or preventing inflammatory bowel disease, familial adenomatous polyposis and colon cancer
Inventors
Assignees
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Publication Number
US-8852649-B2
Publication Date
2014-10-07
Expiration Date
Abstract
Methods for treating colon cancer include administering, to a patient in need thereof, a polymeric proanthocyanidin composition from a Croton species or Calophyllum species in an amount sufficient to treat colon cancer, which composition inhibits COX-2. Methods for treating inflammation locally in the intestines comprise administering, to a patient in need thereof, a polymeric proanthocyanidin composition from a Croton species or Calophyllum species in an amount sufficient to treat inflammation. In one embodiment, the polymeric proanthocyanidin compound is crofelemer.
Core Innovation
The disclosure relates to polymeric proanthocyanidin compositions from Croton or Calophyllum species, including crofelemer, for local intestinal treatment and/or prevention of COX-2-related conditions. Crofelemer is described as selectively inhibiting COX-2 over COX-1, and when orally administered, the composition is not substantially absorbed systemically.
The background problem addressed is COX-2-related conditions, including inflammatory bowel disease such as Crohn’s disease and ulcerative colitis, and also colon cancer and familial adenomatous polyposis (FAP). The disclosed crofelemer compositions are positioned as aiming to avoid cardiovascular side effects associated with other COX-2 inhibitors by local intestinal action and selective COX-2 inhibition.
The disclosure supports the claimed approach by describing crofelemer composition characteristics and formulation concepts for enteric-protected and/or enteric-coated delivery, including delayed release and controlled release. It describes oral administration and also non-oral local routes including suppository and enema.
The disclosure includes a mechanism of action support section, including cytokine/cyclooxygenase assays, describing COX-2 inhibition and inhibition of cytokine release. It also provides examples of enteric-coated dosage forms and an illustrated chemical structure of crofelemer.
Claims Coverage
The partial content provides one independent claim directed to a method of treating colon cancer by administering an isolated crofelemer composition. The provided claim set includes inventive features relating to dosage, oral delivery, enteric protection, enteric-coated forms, and controlled release formulation.
Treating colon cancer with isolated crofelemer
A method of treating colon cancer in a subject comprising administering to a subject having colon cancer an amount of isolated crofelemer effective to treat colon cancer.
Defined daily dosage range of crofelemer
The method includes administering crofelemer at a daily dosage ranging from about 50 mg per day to 2000 mg per day.
Oral administration of crofelemer
The method specifies that crofelemer is administered orally.
Enteric-protected crofelemer
The method is characterized by using an enteric-protected crofelemer.
Enteric-coated tablets, beads, or granules
The method uses an enteric-protected crofelemer formulation in the form of enteric-coated tablets, beads, or granules.
Controlled release crofelemer pharmaceutical composition
The method specifies that crofelemer is formulated as a controlled release pharmaceutical composition.
Across the provided claim set, the core inventive coverage is a colon cancer treatment method using isolated crofelemer, further limited by a specific daily dosage range, oral delivery, enteric-protected and enteric-coated formulation features, and controlled release pharmaceutical composition features.
Stated Advantages
Selectively inhibits COX-2 over COX-1.
Not substantially absorbed systemically when orally administered.
Aims to avoid cardiovascular side effects associated with other COX-2 inhibitors.
Documented Applications
Local intestinal treatment and/or prevention of COX-2-related conditions including inflammatory bowel disease (Crohn’s disease and ulcerative colitis).
Treatment and/or prevention context for colon cancer.
Treatment and/or prevention context for familial adenomatous polyposis (FAP).
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