IP Library › Granted Patent US 10,603,290
Granted Patent B2
US 10,603,290 · App. 16/193,812 · Granted Mar 31, 2020

Formulation for inhibiting formation of 5-HT

Inventors: Stephen J. Farr (Orinda, CA); Brooks Boyd (Berkeley, CA)
Assignee: ZOGENIX INTERNATIONAL LIMITED
A61K31/137A61K31/105A61K31/36A61K31/551A61K45/06
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Quick Facts
Patent No.
US 10,603,290
App. No.
16/193,812
Granted
Mar 31, 2020
Kind
B2
Abstract

Drug combinations and their use are disclosed. A first drug is administered in combination with a second drug. The first drug such as fenfluramine is characterized by the formation of a metabolite including 5-HT 2B agonists such as norfenfluramine with known adverse side effects. The second drug is in the form of a CYP inhibitor such as cannabidiol which modulates the formation of metabolite down thereby making the first drug safer.

Claims (19)

1. A method of reducing or ameliorating seizures in a patient, comprising:

administering fenfluramine; and

administering cannabidiol thereby modulating down formation of norfenfluramine, and resulting in higher levels of fenfluramine.

2. The method of claim 1 , wherein the patient is diagnosed with Dravet syndrome.

3. The method of claim 1 , wherein the patient is diagnosed with a form of refractory epilepsy selected from the group consisting of Dravet syndrome, Lennox-Gastaut syndrome, Doose syndrome, and West syndrome.

4. The method of claim 1 , further comprising:

co-administering to the subject an effective amount of a co-therapeutic agent selected from the group consisting of acetazolamide, barbexaclone, beclamide, brivaracetam, buproprion, cinacalet, clobazam, clonazepam, clorazepate, diazepam, divaloprex, eslicarbazepine acetate, ethadione, ethotoin, felbamate, gabapentin, lacosamide, lorazepam, mephenytoin, methazolamide, methsuximide, methylphenobarbitol, midazolam, nimetazepam, nitrazepam, oxcarbazepine, paramethadione, perampanel, piracetam, phenacemide, pheneturide, phensuximide, phenytoin, potassium bromide, pregabalin, primidone, retigabine, rufinamide, selectracetam, sodium valproate, stiripentol, sultiame, temazepam, tiagabine, topiramate, trimethadione, valnoctamide, valpromide, vigabatrin, zonisamide, and pharmaceutically acceptable salts thereof.

5. A method of reducing or ameliorating seizures in a patient diagnosed with a form of refractory epilepsy, comprising:

administering a liquid formulation of fenfluramine to the patient in an amount in the range of 0.2 mg/kg/day to 0.8 mg/kg/day; and

administering cannabidiol in a liquid formulation in an amount of 0.5 mg/kg/day to 25 mg/kg/day thereby modulating down formation of norfenfluramine, and resulting in higher levels of fenfluramine.

6. A method of reducing or ameliorating seizures in a patient diagnosed with a form of refractory epilepsy, comprising:

administering a liquid formulation of fenfluramine to the patient in an amount which is 30% less than an effective amount in the range of 0.2 mg/kg/day to 0.8 mg/kg/day, due to co-administration of cannabidiol in a liquid formulation in an amount of 0.5 mg/kg/day to 25 mg/kg/day thereby modulating down formation of norfenfluramine, and resulting in higher levels of fenfluramine.

7. The method of claim 6 , wherein the fenfluramine is administered in an amount of 70% less than an effective dose of 0.8 mg/kg/day.

8. The method of claim 6 , wherein the fenfluramine is administered in an amount of 0.56 mg/kg/day or less.

9. A method of reducing or ameliorating seizures patient diagnosed with Dravet syndrome, comprising:

administering a liquid formulation of fenfluramine to the patient in an amount in the range of 0.2 mg/kg/day to 0.8 mg/kg/day; and

administering cannabidiol in a liquid formulation in an amount of 0.5 mg/kg/day to 25 mg/kg/day thereby modulating down formation of norfenfluramine, and resulting in higher levels of fenfluramine.

10. A method of reducing or ameliorating seizures in a patient diagnosed with Dravet syndrome, comprising:

administering a liquid formulation of fenfluramine to the patient in an amount which is 40% less than an effective amount in the range of 0.2 mg/kg/day to 0.8 mg/kg/day, due to co-administration of cannabidiol in a liquid formulation in an amount of 0.5 mg/kg/day to 25 mg/kg/day thereby modulating down formation of norfenfluramine, and resulting in higher levels of fenfluramine.

Assignments (2)
CORRECTIVE ASSIGNMENT TO CORRECT THE RECEIVING PARTY DATA PREVIOUSLY RECORDED AT REEL: 48212 FRAME: 910. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jun 6, 2025
From: FARR, STEPHEN J.; BOYD, BROOKS
To: ZOGENIX INTERNATIONAL LIMITED
Reel/Frame 071529/0247 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 31, 2019
From: FARR, STEPHEN J.; BOYD, BROOKS
To: ZOGENIX INTERNATIONAL LIMITED
Reel/Frame 048212/0910 →
Continuity (4)
Continuation 15667112 · Aug 2, 2017
Provisional Application 62379183 · Aug 24, 2016
Provisional Application 62515383 · Jun 5, 2017
Related Publication 20190083424A1 · Mar 21, 2019
Cited By (1)
US 12,734,137