Methods for treatment of oncological disorders using epimetabolic shifters, multidimensional intracellular molecules, or environmental influencers
Inventors
Narain, Niven Rajin • McCook, John Patrick • Sarangarajan, Rangaprasad
Assignees
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Publication Number
US-10519504-B2
Publication Date
2019-12-31
Expiration Date
Abstract
Methods and formulations for treating oncological disorders in humans using epimetabolic shifters, multidimensional intracellular molecules or environmental influencers are described.
Core Innovation
The patent describes treating an oncological disorder in a mammal by administering a composition comprising Coenzyme Q10 in the oxidized form, together with one or more pharmaceutically acceptable carriers. The composition contains 0.001% to 30% w/w oxidized Coenzyme Q10 with a purity between 95% and 100%, and the oncological disorder is not melanoma.
The patent further discloses exposing a cancer cell to a therapeutically effective amount of a composition comprising oxidized Coenzyme Q10 to block anaerobic use of glucose (glycolysis) or augment mitochondrial oxidative phosphorylation. In this context, the cancer cell is not a melanoma cell, and the composition includes 0.001% to 30% w/w oxidized Coenzyme Q10 having purity between 95% and 100% with pharmaceutically acceptable carriers.
The described mechanistic basis links oxidized Coenzyme Q10 to apoptosis in cancer cells and to maintained oxidized form after entering cells. The patent also describes modulation of pathways related to apoptosis and metabolism, including glycolysis/anaerobic glucose use and mitochondrial oxidative phosphorylation, as well as modulation of gene/protein pathways including transport and signaling.
The document discusses diagnostic and biomarker identification using molecular marker panels and measuring glycolysis/oxidative phosphorylation together with assessment of mitochondrial Q10 form. It also frames the approach in terms of environmental influencers including multidimensional intracellular molecules and epimetabolic shifters, with oxidized Coenzyme Q10 treated as an environmental influencer.
Claims Coverage
The partial content provides two independent claims, each anchored on exposure to oxidized Coenzyme Q10 with defined purity and concentration ranges while excluding melanoma. Across these independent claims, the inventive features emphasize therapeutic administration for non-melanoma oncological disorder treatment and cancer-cell metabolic modulation by blocking anaerobic glucose use and augmenting mitochondrial oxidative phosphorylation.
Non-melanoma oncological disorder treatment with oxidized Coenzyme Q10 composition
Administering to a mammal a therapeutically effective amount of a composition consisting of 0.001% to 30% w/w Coenzyme Q10 and one or more pharmaceutically acceptable carriers, wherein the Coenzyme Q10 is in the oxidized form and has a purity between 95% and 100%, thereby treating the oncological disorder, wherein the oncological disorder is not melanoma.
Blocking anaerobic glucose use or augmenting mitochondrial oxidative phosphorylation with oxidized Coenzyme Q10
Exposing a cancer cell to a therapeutically effective amount of a composition consisting of 0.001% to 30% w/w Coenzyme Q10 and one or more pharmaceutically acceptable carriers, wherein the Coenzyme Q10 is supplied in the oxidized form and has a purity between 95% and 100%, to thereby block anaerobic use of glucose (glycolysis) or to augment mitochondrial oxidative phosphorylation in said cancer cell, wherein the cancer cell is not a melanoma cell.
Claim coverage is centered on oxidized Coenzyme Q10 (0.001% to 30% w/w; purity 95% to 100%) used for non-melanoma settings, either as a method for treating an oncological disorder in a mammal or as a method to block anaerobic glucose use and augment mitochondrial oxidative phosphorylation in a cancer cell.
Stated Advantages
Treating an oncological disorder, wherein the oncological disorder is not melanoma.
Blocking anaerobic use of glucose (glycolysis) in a cancer cell.
Augmenting mitochondrial oxidative phosphorylation in a cancer cell.
Improved outcomes when combined with doxorubicin in an in vivo pancreatic cancer rat study.
Dose-dependent survival benefit in the in vivo pancreatic cancer rat study.
Shifts cancer-cell metabolism toward normalized glycolysis-to-mitochondrial OXPHOS coupling.
Provides a cancer-relevant “epi-shifter”/metabolic modulator effect associated with apoptosis-linked and mitochondrial-associated gene/protein regulation.
Shows relative efficacy of CoQ10 with greater effects in more aggressive cancer cell types than in normal cells, with a noted supportive effect in some normal cells.
Enables topical delivery of CoQ10 via formulated creams, with documented skin penetration results and evaluation in SCCIS and superficial BCC topical studies.
Includes documented systemic exposure and distribution/clearance signals from a radiolabeled topical CoQ10 pharmacokinetic study.
Documented Applications
Treating an oncological disorder in a mammal using a composition comprising oxidized Coenzyme Q10 and pharmaceutically acceptable carriers, excluding melanoma.
Exposing a cancer cell, not a melanoma cell, to block anaerobic use of glucose (glycolysis) or to augment mitochondrial oxidative phosphorylation.
Pancreatic cancer rat use in an in vivo study, including combination with doxorubicin and reporting dose-dependent survival benefit at 28 days.
Diabetes-model gene expression modulation context under hyperglycemia using CoQ10 with gene expression arrays including HK-2 and HASMC and selected diabetes and mitochondrial gene lists.
Topical treatment evaluation of tumors in a murine melanoma model.
In vitro cancer cell line screening and mechanistic evaluation of CoQ10 as an epi-shifter, including apoptosis induction/readouts and mitochondrial-associated marker changes.
Topical treatment study in SCCIS with histology-defined complete/partial responses and tolerability grading.
Topical treatment study in superficial BCC using a randomized double-blind vehicle-controlled design with biopsy-based response assessment at about 8 weeks.
Mouse pharmacokinetic evaluation of topical CoQ10 cream using radiolabeled API, assessing organ accumulation and excretion signals.
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