Injectable, sustained-release microsphere formulations containing rapamycin and/or rapamycin analogs and methods of making and using the formulations

Abstract

A microsphere formulation is provided, as well as a pharmaceutical composition including the microsphere formulation, a kit for forming the pharmaceutical composition and a therapeutic regimen including administering the pharmaceutical composition to a subject to treat an immune-mediated disease. The microsphere formulation includes polymer microspheres, wherein each polymer microsphere includes: an active pharmaceutical ingredient consisting of rapamycin, a rapamycin analog, a pharmaceutically acceptable salt of rapamycin, and/or a pharmaceutically acceptable salt of the rapamycin analog; and a biodegradable polymer, wherein each polymer microsphere comprises a drug load of the active pharmaceutical ingredient that is between 20 and 40 percent by weight of the polymer microsphere, and wherein the polymer microspheres have a median particle size of about 15 micrometers to about 30 micrometers.

Dependencies are inferred from the claim text.