Table 5.
Relevant patents of Trofinetide.
| Patent/Application Number (Status on 6 May 2023; Applicant; Filing Date; Publication Date) |
Summary |
|---|---|
|
EP0366638A2 (Withdrawn; Kabigen; 24 October 1989; 2 May 1990) |
This patent application disclosed that some peptides, including GPE (gly-pro-glu), are effective as a neuromodulator. These peptides either stimulate or inhibit neural activity within the CNS and affect the electrical properties of neurons. It claimed the use of GPE for medicinal and diagnostic use [47]. |
|
WO9517204A1 (Lapsed; Auckland Uniservices Limited; 20 December 1994; 29 June 1995) |
This patent application revealed GPE’s neuroprotective effects. It claimed a method of treating neural damage with a therapeutically effective amount of GPE [48]. |
|
WO9814202A1 (Lapsed; Auckland Uniservices Limited; 6 October 1997; 9 April 1998) |
This patent application unveiled that administration of GPE augments the concentration of choline acetyltransferase (ChAT), glutamic acid decarboxylase (GAD), and nitric oxide synthase (NOS) in CNS. It claimed a method of treating diseases caused by the enzymes’ imbalanced activity [49]. |
|
WO9965509A1 (Lapsed; Neuronz Limited; 15 June 1999; 23 December 1999) |
This patent application discovered that GPE’s administration could augment the concentration of tyrosine hydroxylase in the brain and may be useful for treating Parkinson’s disease [50]. |
|
US7304029B1 (Expired; Neuren Pharmaceuticals; 3 September 1999; 4 December 2007) |
A method of protecting neurons from degeneration, ischemia, or hypoxia by administering growth hormone or its derivatives, including GPE and IGF-1 [51]. |
|
WO0216408A2 (Withdrawn; Neuronz Limited; 24 August 2001; 28 February 2002) |
This patent application disclosed GPE analogs for treating brain injury and neurodegenerative diseases [52]. |
|
US7041314B2 (Expired; Neuren Pharmaceuticals; 24 May 2002; 9 May 2006) |
This patent generically claims Trofinetide and its pharmaceutical compositions with a pharmaceutically acceptable excipient for administration by different routes (intravenous, subcutaneous, topical, intraspinal, aerosol, etc.). It further claims treatment of neural degeneration by administering the claimed compositions of Trofinetide [53]. |
|
US7605177B2 (Patented case; Neuren Pharmaceuticals; 20 December 2005; 20 October 2009) |
Treating neurological injury caused by traumatic brain injury by administering a therapeutically effective amount of Trofinetide alone or in combination with another anti-apoptotic or neuroprotective agent. It also claims treatment of seizures induced by traumatic brain injury by administering a pharmacologically effective amount of Trofinetide [54]. |
|
US7714020B2 (Patented case; Neuren Pharmaceuticals; 4 April 2006; 11 May 2010) |
A treatment of traumatic brain injury and non-convulsive seizure using Trofinetide (0.01–10 mg/kg/hour) alone or in combination with another therapeutic agent (phenytoin, phenobarbital, diazepam, acetazolamide, dextromethorphan, etc.) [55]. |
|
US7887839B2 (Patented case; Neuren Pharmaceuticals; 15 September 2008; 15 February 2011) |
A pharmaceutical emulsion comprising an oil, a surfactant (polyoxyethylene (20) sorbitan monooleate, and sorbitan monooleate), and Trofinetide. The composition may optionally contain a permeability enhancer (sodium caprate and sodium taurocholate). It also claims a tablet comprising the above-mentioned pharmaceutical composition, a binder, and an enteric coating. The claimed composition can be used for treating neurological disorders [56]. |
|
US8178125B2 (Patented case; Neuren Pharmaceuticals; 14 February 2011; 15 May 2012) |
A pharmaceutical emulsion composition comprising one caprylic triglyceride, a surfactant, and Trofinetide [57]. |
|
US8496963B2 (Patented case; Neuren Pharmaceuticals; 14 May 2012; 30 July 2013) |
An emulsion comprising Trofinetide and a lipid-containing carboxylic acid. It also claims pharmaceutical composition comprising Trofinetide and a peptide conjugating agent (ethyl 2-cyanoacrylate) [58]. |
|
US9708366B2 (Patented case; Neuren Pharmaceuticals; 27 January 2012; 18 July 2017) |
A method for treating Fragile X Syndrome (FXS) using an aqueous solution of Trofinetide (0.001 to 100 mg/Kg) alone or combined with a second therapeutic agent [59]. |
|
US2015224164A1 (Discontinued; Neuren Pharmaceuticals; 9 February 2015; 13 August 2015) |
A method for treating autism spectrum disorder (RTT, FXS, etc.) using Trofinetide alone or combined with another therapeutic agent on a need basis [60]. |
|
US9212204B2 (Patented case; Neuren Pharmaceuticals; 26 January 2015; 15 December 2015) |
This patent claims a method for treating RTT symptoms with an aqueous solution of Trofinetide. The claimed solution may contain a second therapeutic agent, including IGF-I, GPE, selegiline, and fluoxetine [61]. |
|
US11612642B2 (Patented case; Beyond Barriers Therapeutics; 27 April 2020; 28 March 2023) |
A method of treating a CNS disorder using an antioxidant (N-acetylcysteine to increase glutathione level in the brain) intranasally alone or in combination with Trofinetide, progesterone, matrix metallopeptidase 9, or NSAIDs [62]. |
|
US11370755B2 (Patented case; Neuren Pharmaceuticals; 14 June 2021; 28 June 2022) |
The patent relates to the compositions and commercially feasible manufacturing process of Trofinetide. It claims a composition comprising Trofinetide and a side product of Formula II (0.001 to 2 wt%) produced during the manufacturing process of Trofinetide. It also claims a composition comprising about 98 wt% and 100 wt% of Trofinetide on an anhydrous basis [63]. |
|
US2022324799A1 (Under examination; Neuren Pharmaceuticals; 23 June 2022; 13 October 2022) |
The compositions and commercially feasible manufacturing process of Trofinetide. A composition comprising Trofinetide and two side products (Formula II or Formula III in a concentration of 0.001 to 2 wt%) produced during the manufacturing process of Trofinetide. It also claims a kit containing a dosage form comprising Trofinetide, a side product of Formula II (0.001 to 2 wt%) produced during the manufacturing process of Trofinetide, and instructions for administration to a subject in need thereof [64]. |
|
US2023023114A1 (Under examination; Acadia Pharmaceuticals; 12 July 2022; 26 January 2023) |
Crystalline Trofinetide hydrate is characterized by its powder x-ray diffraction pattern, d-spacings, FT-Raman spectrum, low-frequency Raman spectrum, 13C solid-state nuclear magnetic resonance spectrum, melting point (71.71–72.06 °C, infrared spectrum, near-infrared spectrum or a combination thereof. It also claims an aqueous pharmaceutical formulation comprising the crystalline Trofinetide hydrate for treating RTT, FXS, autism spectrum disorder, and other neurodevelopmental disorders [65]. |
|
US2022339138A1 (Under examination; Acadia Pharmaceuticals; 1 February 2022; 27 October 2022) |
A method of treating RTT by administering a pharmaceutical composition of Trofinetide to the patient with MECP2 mutation in a daily amount of (a) 4–10 g if the patient weighs between 8 and 11.9 kg; (b) 10.1–14.0 g if the patient weighs between 12–20 kg; (c) 14.1–18.0 g if the patient weighs between 20.1 and 35 kg; (d) 18.1–22.0 g if the patient weighs between 35.1 and 50 kg; or (e) 22.1–26 g if the patient weighs between 50.1 and 150 kg [66]. |
|
WO2022246277A2 (No national phase entry; Harvard College and Tufts Medical Center; 20 May 2022; 24 November 2022) |
A method of treating RTT and a symptom of CDKL5 deficiency disorder with a therapeutically effective amount of vorinostat, ivermectin, and Bacteroides fragilis or a polysaccharide isolated from Bacteroides fragilis alone or in combination thereof. It further claims a composition comprising (a) two or more of vorinostat, ivermectin, Trofinetide, and Bacteroides fragilis or a polysaccharide isolated from Bacteroides fragilis and (b) a pharmaceutically acceptable excipient [67]. |
|
WO2022165250A1 (No national phase entry; University of Florida; 28 January 2022; 4 August 2022) |
A method of treating a DYRK1A-related disorder (autism spectrum disorder, intellectual disability, microcephaly, and sociability deficits) using IGF-1, Trofinetide, or NNZ-2591. The claimed treatment method improves sociability, decreases microcephaly, increases spine density, and/or improves synaptic function [68]. |