Peptidomimetic macrocycles and formulations thereof
AssigneeAileron Therapeutics, Inc.
InventorsDavid Allen Annis, Krzysztof Darlak, Chris Rhodes, Sonoko Kanai, Joerg Hoernschemeyer, Michaela Grass
Life of this patent
Estimating the term…
Abstract
Aqueous pharmaceutical formulations, for parenteral administration, comprising peptidomimetic macrocycle or a pharmaceutically acceptable salt thereof wherein the peptidomimetic macrocycle binds to MDM2 and/or MDMX proteins are disclosed. Also disclosed are methods of treating diseases and disorders using the aqueous pharmaceutical formulations disclosed herein.
Claims38
-293. (canceled)
An aqueous pharmaceutical formulation comprising:
- (i) a peptidomimetic macrocycle or a pharmaceutically acceptable salt thereof, wherein the amount of the peptidomimetic macrocycle in the aqueous pharmaceutical formulation is equal to or greater than 15 mg/mL;
- (ii) a buffering agent;
- (iii) a stabilizing agent;
- and
- (iv) a tonicity agent
- wherein the molar ratio of the peptidomimetic macrocycle to the buffering agent is in the range of 0.01-2.5.
A method modulating the activity of p53 and/or MDM2 and/or MDMX in a subject comprising administering to the subject a stable aqueous pharmaceutical formulation comprising a peptidomimetic macrocycle capable of binding to the MDM2 and/or MDMX proteins, wherein the amount of the peptidomimetic macrocycle in the aqueous pharmaceutical formulation is greater than 15 mg/mL and wherein the aqueous pharmaceutical formulation contains less than 2% w/v of any micelle forming agent.
A method of making an aqueous pharmaceutical formulation comprising adding greater than 15 mg/mL of a peptidomimetic macrocycle or a pharmaceutically acceptable salt thereof to water or an aqueous solution, wherein the aqueous pharmaceutical formulation comprises less than 2% w/v of any micelle forming agent.
Dependencies are inferred from the claim text.