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 Targeted therapeutic delivery of vitamin D compounds

Details
Inventors: Mazess, Richard B.; Bishop, Charles W.;
Assignee: Bone Care International, Inc. (Madison, WI)
Primary Examiner: Chan; Christina
Assistant Examiner: Huynh; Phuong
Attorney, Agent or Firm: Michael Best & Friedrich LLP, Welch; Teresa J., Hartwig; Gregory J.

The present invention is directed to a conjugate which includes at least one vitamin D moiety thereof and at least one targeting molecule moiety to pharmaceutical compositions of the conjugate, and to methods for using the conjugate for target-specific delivery of vitamin D or analogs thereof to tissues in need thereof. When a particularly preferred form is administered to a patient, the targeting molecule component of the conjugate of this invention seeks out and binds to a tissue of interest, such as bone or tumor tissue, where the vitamin D has a therapeutic effect.

DETAILED DESCRIPTION The present invention provides conjugates of vitamin D compounds or analogs and a targeting molecule, having an ability for site-specific delivery of the vitamin D.
Specific conjugates include a bone-therapeutic conjugate and an anti-tumor conjugate.
The present invention also provides pharmaceutical formulations of such a conjugate, and methods of site-specific delivery of a vitamin D moiety of the conjugate to a tissue of interest in a patient.
The present invention provides surprisingly useful means for delivery of vitamin D compounds, analogs or derivatives to tissues of interest (i.
e.
, to target tissue).
The conjugates of the present invention comprises at least one vitamin D moiety associated with a target molecule moiety having an affinity for the target tissue.
In one embodiment of the invention, the conjugate includes at least one vitamin D moiety associated with the target molecule moiety via at least one connecting group, such as a bond between the vitamin D moiety and the target molecule moiety, a bifunctional connector, or other connectors such as a biotin-avidin linkage.
In another embodiment, the conjugate includes a target molecule moiety having an affinity for the tissue of interest, associated with at least one vitamin D moiety and with a second therapeutic agent other than vitamin D.
The pharmaceutical compositions of the present invention include a conjugate of at least one vitamin D moiety associated with at least one target molecule moiety, and a suitable pharmaceutically acceptable carrier.
In another embodiment, the present invention provides a method for site-specific delivery of vitamin D or an analog of vitamin D, a method which includes administering to a patient a therapeutically effective dose of a conjugate in a pharmaceutically acceptable carrier, wherein the conjugate has at least one vitamin D moiety associated with at least one target molecule via a connector, and wherein the target molecule has an affinity for a tissue of interest



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