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 invention provides methods for preventing or reducing neurodegeneration in a human who has the huntingtin gene mutation by administering an effective amount of a composition comprising creatine hydrochloride. The document contrasts creatine hydrochloride with creatine monohydrate and emphasizes lower effective doses for neuroprotection while also addressing improved solubility and bioavailability.

The document also provides a method for treating Huntington’s disease in a human by administering an effective amount of creatine hydrochloride. Proposed biological effects are described in terms of mitochondrial stability, including increased spare respiratory capacity and increased total ATP turnover in Huntington’s disease lymphoblast cells following administration.

Further described effects relate to altered lipid and diacylglycerol (DAG) pathway signaling, including a proposed increase in DGAT2 activity, and the belief that increased DGAT1 and DGAT2 raise DAG. The document includes formulation and administration contexts for creatine hydrochloride, including various dosage formats such as pills/tablets/capsules/gel capsules and liquid/gel/powder, and also includes dosing ranges and example measurements.

Claims Coverage

The independent claims cover three method categories: prevention/reduction of neurodegeneration in a human with a huntingtin gene mutation, treatment of Huntington’s disease, and treatment of Huntington’s disease or Parkinson’s disease via daily dosing with creatine hydrochloride compositions. Across these categories, the claim coverage centers on administering creatine hydrochloride compositions as an effective daily dose and, in dependent claim subject matter, on specific mitochondrial and DGAT-related functional changes and compositional/dosage-form constraints.

Overall, the claims focus on using creatine hydrochloride compositions, administered as effective amounts or daily doses, to prevent/reduce neurodegeneration (including in the presence of a huntingtin gene mutation) and to treat Huntington’s disease, with further dependent claim subject matter directed to compositional/dosage-form features and measurable mitochondrial functional improvements and DGAT2/DAG-pathway-related activity changes.

Stated Advantages

Documented Applications