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Publication Number
US-10370406-B2
Publication Date
2019-08-06
Expiration Date
Abstract
SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.
Core Innovation
The patent describes a method of treating a fungal infection in a patient in need thereof by administering a pharmaceutical composition comprising an effective amount of a pharmaceutically acceptable salt of compound 1. The pharmaceutically acceptable salt is selected from citrate, hippurate, mesylate, and fumarate, and the salt used to prepare the pharmaceutical composition is characterized by defined water sorption behavior as determined by DVS.
For citrate salts of compound 1, the citrate crystal forms include at least one of Type A, Type B, Type E, Type F, Type M, Type N, Type O, Type Q, Type R, and Type S. The core concept is that defined crystalline citrate forms of compound 1 salts are selected for use in a pharmaceutical composition to treat fungal infection.
The document further describes solid-form interconversion and stability studies among SCY-078 citrate polymorph/solvate types, including relationships such as Type A ↔ B and conversion to freebase forms through disproportionation. The document supports form identity and stability using XRPD, DSC, TGA, and DVS, and includes solubility characterization and form-related stability behavior.
Claims Coverage
The partial content provides two independent claims. Across them, the inventive features focus on salt/crystal-form selection of compound 1 for antifungal treatment and defined water sorption and/or defined citrate crystal form selection supported by DVS and solid-state characterization.
Antifungal treatment with defined compound 1 salt and DVS water sorption
Administering to the patient a pharmaceutical composition comprising an effective amount of a pharmaceutically acceptable salt of compound 1, wherein the salt is selected from citrate, hippurate, mesylate, and fumarate, and wherein the pharmaceutically acceptable salt of compound 1 used to prepare the pharmaceutical composition has a water sorption of from 2% to 7% at 25° C. and 80% relative humidity as determined by DVS.
Antifungal treatment with citrate salt containing defined citrate crystal forms
Administering to the patient a pharmaceutical composition comprising an effective amount of a citrate salt of compound 1, wherein the citrate salt of compound 1 used to prepare the pharmaceutical composition comprises at least one of Type A, Type B, Type E, Type F, Type M, Type N, Type O, Type Q, Type R, and Type S citrate crystal forms.
The claim coverage centers on using pharmaceutically acceptable salt forms of compound 1—selected from citrate, hippurate, mesylate, and fumarate with a DVS-defined water sorption range, and/or selected citrate crystal forms (Types A, B, E, F, M, N, O, Q, R, and S)—as the active pharmaceutical composition component for treating fungal infection in a patient.
Stated Advantages
Improved kinetic solubility in dextrose buffer, phosphate buffer, SGF, FaSSIF, and FeSSIF.
Controlled hygroscopicity/water sorption measured by DVS.
Stability under humidity/temperature for the identified crystalline forms.
Documented Applications
Antifungal treatment of invasive candidiasis.
Antifungal treatment of invasive aspergillosis.
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