Compositions and methods for neuroprotection and treatment of neurodegeneration

Inventors

Faulkner, Mark C. • Miller, Donald W. • Hatch, Grant M.

Assignees

Vireo Systems Inc

Abstract

Compositions for neuroprotection and treatment of neurodegeneration and methods of administering same. In particular, the present invention relates to compositions and methods for preventing or reducing neurodegeneration, such as neurodegeneration caused by Huntington's disease, including administering a daily dose of a composition including an effective amount of creatine hydrochloride to a patient in need thereof. The methods of the present invention allow for lower dosages of supplementation as compared to creatine monohydrate while retaining all of the desired biological effects of creatine supplementation.

Core Innovation

The disclosure describes compositions comprising creatine hydrochloride and methods for preventing or reducing neurodegeneration in a human having the huntingtin gene mutation and for treating Huntington's disease. The approach administers an effective amount of a composition wherein the effective amount comprises a daily dose of creatine hydrochloride of about 2 grams to about 12 grams. The disclosure emphasizes that creatine hydrochloride enables preserving desired biological effects while permitting a lower effective daily supplementation compared to creatine monohydrate.

The disclosure further relates the creatine hydrochloride compositions to much higher aqueous solubility and higher relative bioavailability. It also describes creatine hydrochloride being provided in compositions at at least about 50 wt% or at least about 75 wt% and optionally at higher thresholds. The compositions are contemplated in dosage forms including pill, tablet, capsule, gel capsule, liquid, and powder, including use as nutritional supplements and functional foods.

Biological findings are described in lymphoblast cells from HD patients, including increases in mitochondrial spare respiratory capacity and increases in total ATP turnover after creatine hydrochloride exposure. The disclosure also reports an increase in diacylglycerol acyltransferase 2 (DGAT2) activity. A clinical-style example is described for early-stage HD gene mutation carriers taking creatine hydrochloride over a multi-year period, where no detected progression is reported on clinical assessment and MRI.

Claims Coverage

The independent claims cover methods of preventing or reducing neurodegeneration in humans with a huntingtin gene mutation and methods of treating Huntington's disease, including an additional independent claim extending treatment to Huntington's disease or Parkinson's disease. Across these independent claims, the inventive features focus on administering creatine hydrochloride at daily doses of about 2 grams to about 12 grams in the human subject.

Overall, the claim coverage centers on use of creatine hydrochloride compositions administered to humans with specified neurodegenerative disease contexts, using daily creatine hydrochloride dosing in the range of about 2 grams to about 12 grams.

Stated Advantages

Documented Applications