Efflux inhibitor compositions and methods of treatment using the same
AssigneeIzumi Technology, LLC
InventorsAntonius Martinus Gustave Bunt, Olaf Van Tellingen
Life of this patent
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Abstract
The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).
Claims20
A composition comprising at least about 1% by weight crystalline elacridar nanoparticles having a mean diameter of about 10 nm to about 400 nm and (i) at least about 12% by weight_D-α-Tocopherol polyethylene glycol succinate (TPGS) or (ii) at least about 1% by weight poloxamer 407, wherein said composition achieves one or more of:
- a. a Cmax of elacridar of at least about 500 ng/ml;
- b. bioavailability of elacridar of at least about 0.2:
- c. an AUC(0-48 h) of elacridar of at least about 900 μg/ml*min;
- d. an AUC(0-∞) of elacridar of at least about 1100 μg/ml*min;
- and
- e. an elimination half-life (T½) of elacridar of at least about 10 h;
- when the composition is administered by oral gavage in an aqueous suspension at about 100 mg/kg to fasted, female Sprague-Dawley rats.
Dependencies are inferred from the claim text.