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AssigneeXenoPort, Inc.
InventorsNoa Zerangue, Kenneth C. Cundy, Mark A. Gallop
Estimating the term…
Methods of modifying therapeutic compounds such as drugs to be substrates for active transporters expressed in epithelial cells lining the lumen of the human colon are disclosed. The transporters expressed in the human colon include the sodium dependent multi-vitamin transporter (SMVT), and monocarboxylate transporters 1 and 4 (MCT 1 and MCT 4). The modified compounds can themselves be pharmacologically active, or upon cleavage of a chemical moiety after uptake from the colon, can be metabolized to form a compound that is pharmacologically active (e.g., a prodrug). The modified compounds disclosed herein are suitable for use in extended release oral dosage forms, particularly those that release drug over periods of greater than about 2-4 hours following administration.
A pharmaceutical composition comprising an agent linked to a conjugate moiety to form a conjugate, formulated with a pharmaceutical carrier for sustained or delayed release of the conjugate, wherein the conjugate has a higher Vmax for a transporter expressed in plasma membranes of epithelial cells lining a human colon than the agent alone.
A pharmaceutical composition comprising a therapeutic agent linked to a conjugate moiety to form a conjugate, formulated with a pharmaceutical carrier in an oral dosage form which upon oral administration to a human releases at least a portion of the conjugate within the colon of the human, wherein the conjugate has a higher Vmax for a transporter selected from MCT1, MCT4 and SMVT than the agent alone.
A method of formulating an agent, comprising:
A method of delivering an agent, comprising
A method of screening agents, conjugates or conjugate moieties for oral delivery, comprising
A method of delivering an agent, comprising
Dependencies are inferred from the claim text.