Kezar Life Sciences

Onyx Therapeutics, Inc.

Evan Lewis

Sean Dalziel

Dustin L McMinn

Henry Johnson

Mouhannad Jumaa

Peter Shwonek

Mark Nguyen Ho

Fabiana N Fonseca

Dustin Mcminn

Provided herein are pharmaceutical formulations comprising KZR-616 or a salt thereof, and a sugar, wherein the formulations are lyophilized, methods of preparing said formulations, methods of treating immune-related diseases, and methods of treating inflammation.

Immunoproteasome inhibitor formulations

Provided herein is a peptide epoxyketone immunoproteasome inhibitor, crystal forms, salts, and processes for making the same, and formulations thereof.

Crystalline salts of peptide epoxyketone immunoproteasome inhibitor

Provided herein is a peptide epoxyketone immunoproteasome inhibitor having a structure: Formula (I) wherein X&#x2014; is a counterion, crystal forms, salts, and processes for making the same, and formulations thereof. 

This disclosure provides methods for formulating compositions comprising one or more peptide proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin. As well as cyclodextrin complexation methods of formulating a peptide proteasome inhibitor (e.g., a compound of formula (1)-(5) or a pharmaceutically acceptable salt thereof) with one or more cyclodextrins. Such methods substantially increase the solubility and stability of these proteasome inhibitors and facilitate both their manufacture and administration. For example, homogenous solutions of a compound of formula (5) (carfilzomib) can be obtained at a pharmaceutically useful pH (e.g., about 3.5) and at higher concentrations (e.g., about 5 mg/mL) than could be obtained without one or more cyclodextrins and the processes of complexation between the compound and one or more cyclodextrins provided herein. 

Cyclodextrin complexation methods for formulating peptide proteasome inhibitors

Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed.

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Pacifica, CA, United States of America

Evan Lewis