Claims for Patent: 12,290,596

Summary for Patent: 12,290,596

Title:	Compositions and methods for the treatment of opioid overdose
Abstract:	Drug products adapted for nasal delivery, comprising a pre-primed device filled with a pharmaceutical composition comprising nalmefene are provided. Methods of treating opioid overdose with the drug products are also provided.
Inventor(s):	Phil Skolnick, Mark Ellison, Roger Crystal
Assignee:	Indivior Inc , Indivior UK Ltd
Application Number:	US17/881,306
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,290,596
Patent Claims:	1. A method of emergency treatment of a known or suspected opioid overdose or a symptom thereof caused by natural or synthetic opioids in an adult human subject in need thereof, comprising nasally administering to the subject a pharmaceutical formulation in an aqueous solution of about 100 μL, comprising: about 3 mg of nalmefene hydrochloride; about 0.87 mg NaCl; about 0.25 mg dodecyl maltoside; about 0.04 mg benzalkonium chloride (50% solution); about 0.2 mg disodium edetate; and water in an amount sufficient to achieve a volume of about 100 μL; wherein said formulation has a pH of 4.1 to 4.9; further wherein upon intranasal administration of said formulation to said adult human subject, median Tmax is less and the Cmax geometric mean is higher than each would have been for intramuscular administration of 1 mg nalmefene hydrochloride; further wherein upon intranasal administration of said formulation to said adult human subject, the time to onset of reversal in said adult human subject of a remifentanil-induced respiratory depression ranges from 2.5 to 5 minutes after said administration in a ventilatory-response to hypercapnia model, and the time to full reversal of remifentanil-induced depression of minute ventilation in said adult human subject ranges from 5 and 15 minutes after said administration in the model; further wherein the plasma concentration versus time curve of the nalmefene in said adult human subject has a Tmax of between 12 and 18 minutes; and wherein the Cmax geometric mean is between 89 ng/ml and 12 ng/ml; thereby treating the opioid overdose or a symptom thereof in the adult human subject. 2. A method of treating a remifentanil-induced respiratory depression in an adult human subject in need thereof, comprising nasally administering to the subject a pharmaceutical formulation in an aqueous solution of about 100 μL, comprising: about 3 mg of nalmefene hydrochloride; about 0.87 mg NaCl; about 0.25 mg dodecyl maltoside; about 0.04 mg benzalkonium chloride (50% solution); about 0.2 mg disodium edetate; and water in an amount sufficient to achieve a volume of about 100 μL; wherein said formulation has a pH of 4.1 to 4.9; further wherein upon intranasal administration of said formulation to said adult human subject, median Tmax is less and the Cmax geometric mean is higher than each would have been for intramuscular administration of 1 mg nalmefene hydrochloride; further wherein upon intranasal administration of said formulation to said adult human subject, the time to onset of reversal in said adult human subject of respiratory depression ranges from 2.5 to 5 minutes after said administration in a ventilatory-response to hypercapnia model, and the time to full reversal of remifentanil-induced depression of minute ventilation in said adult human subject ranges from 5 and 15 minutes after said administration in the model; further wherein the plasma concentration versus time curve of the nalmefene in said adult human subject has a Tmax of between 12 and 18 minutes; and wherein the Cmax geometric mean is between 8 ng/ml and 12 ng/ml; thereby treating the remifentanil-induced respiratory depression in the adult human subject and wherein the remifentanil-induced respiratory depression is created by an initial bolus of 0.5 micrograms/kg dose of remifentanil followed by an infusion of remifentanil for about 15 minutes at an infusion rate of about 0.175 micrograms/kg/min.