Solid forms of emetine

Inventors

KLOPP, John

Assignees

Acer Therapeutics Inc

Abstract

Crystalline forms of emetine dihydrochloride (Compound I dihydrochloride) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms of Compound I dihydrochloride.

Core Innovation

The invention relates to solid-state crystalline and amorphous forms of emetine dihydrochloride, identified as Compound I dihydrochloride. Specific polymorph forms are defined by X-ray powder diffractogram (XRPD) characteristics, including XRPD peak patterns for Forms 1, 2, 3, 4, 5, 6, 7A, 7B, and 8. The disclosure characterizes these forms using thermal analysis including DTA/DSC and thermogravimetric analysis (TGA), and addresses conversion and behavior between forms during crystallization and drying.

Compound I dihydrochloride polymorph Form 7B is described with XRPD-defined peaks, and the material is further characterized using DTA/DSC and TGA. The disclosure includes crystalline forms that are isolated in high yield and purity, and discusses solubility screening and thermodynamic solubility behavior. The forms can be converted during preparation and processing conditions.

Pharmaceutical compositions containing the crystalline forms of Compound I dihydrochloride are described, including compositions that specify high crystallinity thresholds and form-specific percentages. The therapeutic use is described for treating or preventing viral infections, including Zika and coronaviruses such as SARS-CoV-2, MERS-CoV, and SARS-CoV. Treatment regimens emphasize non-hospitalized subjects and reduced severe cytokine release syndrome (CRS) symptoms.

Claims Coverage

Not explicitly described in patent.

Not explicitly described in patent.

Stated Advantages

Documented Applications