IP Library Granted Patent US 10,071,100
Granted Patent B2
US 10,071,100 · App. 15/860,881 · Granted Sep 11, 2018

Therapeutic nanoparticles comprising a therapeutic agent and methods of making and using the same

Inventors: Shubha Bagrodia (San Diego, CA); Jennifer Lafontaine (San Diego, CA); Zach Lovatt (Belmont, MA); Eyoung Shin (Marlborough, MA); Young Ho Song (Natick, MA); Greg Troiano (Pembroke, MA); Hong Wang (Newton, MA)
Assignee: Pfizer Inc.
A61K31/5377A61K9/1075A61K9/5153A61K47/12A61K47/28A61K47/34
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Quick Facts
Patent No.
US 10,071,100
App. No.
15/860,881
Granted
Sep 11, 2018
Kind
B2
Abstract

The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid and a therapeutic agent (1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea), or pharmaceutically acceptable salts thereof, and a polymer. Other aspects include methods of making and using such nanoparticles.

Claims (9)

1. A method of treating cancer, wherein said cancer is selected from breast cancer and prostate cancer, in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a therapeutic nanoparticle; wherein said therapeutic nanoparticle comprises:

a therapeutic agent selected from the group consisting of 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyI)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea and pharmaceutically acceptable salt thereof;

a polymer selected from the group consisting of diblock poly(lactic) acid-poly (ethylene)glycol (PLA-PEG) copolymer, diblock poly(lactic acid-co-glycolic acid)-poly (ethylene)glycol (PLGA-PEG) copolymer, and combinations thereof; and

a substantially hydrophobic acid selected from the group consisting of dioctyl sulfosuccinic acid, 1-hydroxy-2-naphthoic acid, dodecylsulfuric acid, naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, pamoic acid, undecanoic acid, and combinations thereof;

wherein the substantially hydrophobic acid and the therapeutic agent form a hydrophobic ion pair that is encapsulated in the therapeutic nanoparticle;

wherein the hydrophobic ion pair is dispersed throughout a polymeric matrix comprising the polymer; and

wherein PLA-PEG-GL is additionally present, wherein targeting ligand GL has the following structure:

2. The method of claim 1 , wherein the cancer is breast cancer.

3. The method of claim 1 , wherein the cancer is prostate cancer.

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →
Continuity (3)
Continuation 14656899 · Mar 13, 2015
Provisional Application 61953628 · Mar 14, 2014
Related Publication 20180125854A1 · May 10, 2018
Cited By (1)
US 12,642,803