IP Library Granted Patent US 11,079,379
Granted Patent B2
US 11,079,379 · App. 16/054,854 · Granted Aug 3, 2021

Methods of treating transthyretin (TTR) mediated amyloidosis

Inventor: Brian Bettencourt (Groton, MA)
Assignee: ALNYLAM PHARMACEUTICALS, INC.
G01N33/566C07D263/57C12N15/113G01N33/50G01N33/53G01N33/567G01N33/6896C07K1/00C12N2310/14
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Quick Facts
Patent No.
US 11,079,379
App. No.
16/054,854
Granted
Aug 3, 2021
Kind
B2
Abstract

Disclosed herein are methods for reducing or arresting an increase in a Neuropathy Impairment Score (NIS) or a modified NIS (mNIS+7) in a human subject by administering an effective amount of a transthyretin (TTR)-inhibiting composition.

Claims (14)

1. A method of treating polyneuropathy in a patient with hereditary transthyretin-mediated amyloidosis (hATTR), the method comprising administering a dose of a TTR siRNA with lipid excipients to the patient,

wherein the TTR siRNA consists of a sense strand consisting of SEQ ID NO:1 and an antisense strand consisting of SEQ ID NO:2; and

the lipid excipients consist of DLin-MC3-DMA ((6Z, 9Z, 28Z, 31Z)-heptatriaconta-6, 9, 28, 31-tetraen-19-yl-4-(dimethylamino) butanoate), DSPC ((1,2-Distearoyl-sn-Glycero-3-Phosphocholine), cholesterol, and PEG 2000 -C-DMG (((R)-methoxy-PEG 2000 -carbamoyl-di-O-myristyl-sn-glyceride) in isotonic phosphate buffered saline;

wherein the dose is 0.3 mg siRNA per kg body weight, and the TTR siRNA with lipid excipients is administered via IV infusion once every three weeks, and the patient receives a premedication before infusion to reduce the risk of infusion-related reactions.

2. The method of claim 1 , wherein the patient receives the premedication on the evening before and the day of infusion.

3. The method of claim 1 , wherein the premedication comprises dexamethasone, acetaminophen, diphenhydramine, and ranitidine.

4. The method of claim 1 , wherein the premedication comprises dexamethasone, acetaminophen, cetirizine, and ranitidine.

5. The method of claim 1 , wherein the premedication comprises dexamethasone, paracetamol (acetaminophen), an H2 blocker and an H1 blocker.

6. The method of claim 5 , wherein the H2 blocker is ranitidine or famotidine.

7. The method of claim 5 , wherein the H1 blocker is cetirizine, hydroxyzine or fexofenadine.

8. The method of claim 1 , wherein the TTR siRNA with lipid excipients is administered via a 70 minute infusion of 1 mL/min for 15 minutes followed by 3 mL/min for 55 minutes.

9. The method of claim 1 , wherein the TTR siRNA with lipid excipients is administered via a 70 minute infusion of 1 mL/min for 15 minutes followed by 3 mL/min for 55 minutes and the premedication comprises dexamethasone, paracetamol (acetaminophen), an H2 blocker and an H1 blocker.

10. The method of claim 1 , wherein the patient has cardiomyopathy.

11. The method of claim 1 , wherein the patient has does not have cardiomyopathy.

Assignments (4)
SECURITY INTEREST Recorded Oct 1, 2025
From: ALNYLAM PHARMACEUTICALS, INC.; SIRNA THERAPEUTICS, INC.
To: BANK OF AMERICA, N.A.
Reel/Frame 072996/0337 →
RELEASE OF SECURITY INTEREST Recorded Sep 19, 2022
From: WILMINGTON TRUST, NATIONAL ASSOCIATION
To: ALNYLAM PHARMACEUTICALS, INC.
Reel/Frame 061141/0059 →
SECURITY INTEREST Recorded Apr 13, 2020
From: ALNYLAM PHARMACEUTICALS, INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 052381/0156 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 30, 2018
From: BETTENCOURT, BRIAN
To: ALNYLAM PHARMACEUTICALS, INC.
Reel/Frame 046759/0720 →
Continuity (4)
Continuation 15507691
Provisional Application 62150596 · Apr 21, 2015
Provisional Application 62044100 · Aug 29, 2014
Related Publication 20190162724A1 · May 30, 2019
Cited By (1)
US 12,227,744