US 2026/0062382 A1Published application

Crystalline forms of trofinetide

AssigneeACADIA Pharmaceuticals Inc.

InventorsMatthew PETERSON, Marlon CARLOS, Martin Bernard Catherine BOUSMANNE, Cecilia BETTI, David T. JONAITIS, Lisa M. MCCRACKEN, Lisa M. GROVE

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Abstract

This disclosure provides crystalline forms of trofinetide and trofinetide hydrate, pharmaceutical compositions comprising crystalline forms of trofinetide and trofinetide hydrate, methods of making crystalline forms of trofinetide or trofinetide hydrate, and methods of treating a disease, condition, or disorder in a subject comprising administering a composition comprising crystalline forms of trofinetide or trofinetide hydrate to the subject.

Claims50

Dependent claims

Crystalline trofinetide·xH2O, wherein x is about 2 to about 4, characterized as having:

(i) a powder x-ray diffraction pattern with a peak in the range of 6.6-6.8, a peak in the range of 11.3-11.6, a peak in the range of 12.5-12.7, and a peak in the range of 13.6-13.8 degrees 2Θ using Cu Kα radiation, wherein the 2Θ values are ±0.2 degrees 2Θ;
or
(ii) a powder x-ray diffraction pattern with d-spacings at 13.1, 7.7, 7.0, 6.4, and 5.3 Å using Cu Kα radiation;
or
(iii) a FT-Raman spectrum with peaks at 2989, 2934, 2883, 1685, 1637, 1459, and 930 cm-1, wherein the cm-1 values are ±4 cm-1;
or
(iv) a low frequency (LF) Raman spectrum with peaks at 13, 24, 67, and 77 cm-1, wherein the cm-1 values are ±4 cm-1;
or
(v) a 13C solid-state nuclear magnetic resonance spectrum with peaks at 179.7, 177.9, 177.5, 177.2, 177.0, 165.3, 164.9, 164.8, 67.8, 67.4, 58.6, 58.2, 46.8, 40.3, 33.3, 25.3, 23.5, and 21.1 ppm, wherein the ppm values are ±3 μm;
or
(vi) a 13C solid-state nuclear magnetic resonance spectrum with 18 peaks, wherein the Δ from the furthest downfield peak to:
(i) the second furthest downfield peak is 1.8 ppm;
(ii) the third furthest downfield peak is 2.2 ppm;
(iii) the fourth furthest downfield peak is 2.5 ppm;
(iv) the fifth furthest downfield peak is 2.7 ppm (v) the sixth furthest downfield peak is 14.4 ppm;
(vi) the seventh furthest downfield peak is 14.8 ppm;
(vii) the eight furthest downfield peak is 14.9 ppm;
(viii) the ninth furthest downfield peak is 111.9 ppm;
(ix) the tenth furthest downfield peak is 112.3 ppm;
(x) the eleventh furthest downfield peak is 121.1 ppm;
(xi) the twelfth furthest downfield peak is 121.5 ppm;
(xii) the thirteenth furthest downfield peak is 133.1 ppm;
(xiii) the fourteenth furthest downfield peak is 139.4 ppm;
(xiv) the fifteenth furthest downfield peak is 146.3 ppm;
(xv) the sixteenth furthest downfield peak is 154.6 ppm;
(xvi) the seventeenth furthest downfield peak is 156.2 ppm;
and/or (xvii) the Δ from the furthest downfield peak to the furthest upfield peak is 158.6 ppm, or any combination thereof;
or
(vii) a melting point with an onset temperature of 71.71° C. and a peak temperature of 72.06° C. based on differential scanning calorimetry;
or
(viii) an infrared (IR) spectrum with peaks at 1678, 1636, 1589, 1525, 1214, and 1196 cm-1, wherein the cm-1 values are ±4 cm-1;
or
(ix) a near-infrared (NIR) spectrum with peaks at 5145, 4630, and 4423 cm-1, wherein the cm-1 values are ±4 cm-1;
or
a combination thereof.

32 more elements

Crystalline trofinetide·xH2O, wherein x is about 2 to about 4, characterized as having:

(i) a powder x-ray diffraction pattern with peaks at 6.8, 11.5, 12.6, 13.8, and 16.8 degrees 2Θ using Cu Kα radiation, wherein the 2Θ values are ±0.2 degrees 2Θ;
and/or
(ii) a powder x-ray diffraction pattern with d-spacings at 13.1, 7.7, 7.0, 6.4, and 5.3 Å using Cu Kα radiation;
and/or
(iii) a FT-Raman spectrum with peaks at 2989, 2934, 2883, 1685, 1637, 1459, and 930 cm−1, wherein the cm−1 values are ±4 cm−1;
and/or
(iv) a low frequency (LF) Raman spectrum with peaks at 13, 24, 67, and 77 cm−1, wherein the cm−1 values are ±4 cm−1;
and/or
(v) a 13C solid-state nuclear magnetic resonance spectrum with peaks at 179.7, 177.9, 177.5, 177.2, 177.0, 165.3, 164.9, 164.8, 67.8, 67.4, 58.6, 58.2, 46.8, 40.3, 33.3, 25.3, 23.5, and 21.1 ppm, wherein the ppm values are ±3 μm;
and/or
(vi) a 13C solid-state nuclear magnetic resonance spectrum with 18 peaks, wherein the Δ from the furthest downfield peak to:
(i) the second furthest downfield peak is 1.8 ppm;
(ii) the third furthest downfield peak is 2.2 ppm;
(iii) the fourth furthest downfield peak is 2.5 ppm;
(iv) the fifth furthest downfield peak is 2.7 ppm (v) the sixth furthest downfield peak is 14.4 ppm;
(vi) the seventh furthest downfield peak is 14.8 ppm;
(vii) the eight furthest downfield peak is 14.9 ppm;
(viii) the ninth furthest downfield peak is 111.9 ppm;
(ix) the tenth furthest downfield peak is 112.3 ppm;
(x) the eleventh furthest downfield peak is 121.1 ppm;
(xi) the twelfth furthest downfield peak is 121.5 ppm;
(xii) the thirteenth furthest downfield peak is 133.1 ppm;
(xiii) the fourteenth furthest downfield peak is 139.4 ppm;
(xiv) the fifteenth furthest downfield peak is 146.3 ppm;
(xv) the sixteenth furthest downfield peak is 154.6 ppm;
(xvi) the seventeenth furthest downfield peak is 156.2 ppm;
and/or (xvii) the Δ from the furthest downfield peak to the furthest upfield peak is 158.6 ppm, or any combination thereof;
and/or
(vii) a melting point with an onset temperature of 71.71° C. and a peak temperature of 72.06° C. based on differential scanning calorimetry;
and/or
(viii) an infrared (IR) spectrum with peaks at 1678, 1636, 1589, 1525, 1214, and 1196 cm−1, wherein the cm−1 values are ±4 cm−1;
and/or
(ix) a near-infrared (NIR) spectrum with peaks at 5145, 4630, and 4423 cm−1, wherein the cm−1 values are ±4 cm−1;
and/or
a combination thereof.

32 more elements

Dependencies are inferred from the claim text.

Facts

Application: 19/384,953Filed 10 Nov 2025
Priority: 12 Jul 2021
Published: 5 Mar 2026
Term ends: Not estimatedThe source records don’t support an estimate.

Classification10 codes

A61P 25/00
Drugs for disorders of the nervous system
C07D 207/16
With hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals,…:…
C07K 5/0806
And aliphatic: the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
A61K 38/00
Medicinal preparations containing peptides

Family

Application63/220,660Us provisional application · filed 12 Jul 2021
Application17/862,865Continuation · filed 12 Jul 2022
Application18/491,057Continuation · filed 20 Oct 2023
Application19/384,953Continuation
US 11,827,600 B2Related patent
US 12,492,167 B2Related patent
US 2023/0023114 A1Published application
US 2025/0019347 A1Published application
US 2026/0062382 A1This patent

From the US filing history. Foreign family members aren’t listed.

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