Therapeutic agent for nervous system disease
Inventors
Tanaka, Hiroyuki • Yoshikawa, Hideki • Mochizuki, Hideki • Murase, Tsuyoshi • Sasaki, Tsutomu • Baba, Kousuke • Iwahashi, Toru • Naiki, Mitsuru
Assignees
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Publication Number
US-11679122-B2
Publication Date
2023-06-20
Expiration Date
Abstract
An object is to provide a drug which is useful in treating a nervous system disease. A drug containing vitamin B12 as an active ingredient according to the present invention has an M2 macrophage/microglia induction promoting effect, an M1 macrophage/microglia induction inhibiting effect, a nerve regeneration promoting effect, and the like and is very useful as a therapeutic agent for a nervous system disease, and particularly useful as a therapeutic agent for a central nervous system disease such as cerebral infarction, dementia, or spinal cord injury.
Core Innovation
The invention provides a method for promoting M2 macrophage/microglia induction and inhibiting M1 macrophage/microglia induction, and/or reducing the ratio of M1 macrophage/microglia to M2 macrophage/microglia, in a patient in need thereof. The method comprises administering an agent comprising an effective amount of vitamin B12 to the patient to achieve the immunomodulatory effects on macrophage/microglia phenotypes.
The agent comprises vitamin B12, with cobalamin species and salts including methylcobalamin, cyanocobalamin, hydroxocobalamin, sulfitocobalamin, and adenosylcobalamin. In some embodiments, vitamin B12 is methylcobalamin, and the method includes continuous administration over a period of time and intravenous drip infusion.
The disclosed use is directed to nervous system diseases and injuries, including cerebral infarction, dementia, and spinal cord injury. The disclosed functional outcomes include inhibiting apoptosis and necrosis, promoting nerve/axon regeneration, and functional recovery in the described disease models.
Claims Coverage
The document includes one independent claim reciting a patient method using an agent comprising an effective amount of vitamin B12 to promote M2 macrophage/microglia induction, inhibit M1 macrophage/microglia induction, and/or reduce the M1 macrophage/microglia to M2 macrophage/microglia ratio. Dependent claims further refine the vitamin B12 selection and narrow administration regimens including continuous administration and intravenous drip infusion.
Administering vitamin B12 for M2 promotion and M1 inhibition
Administering an agent comprising an effective amount of vitamin B12 to a patient to promote M2 macrophage/microglia induction, inhibit M1 macrophage/microglia induction, and/or reduce the ratio of M1 macrophage/microglia to M2 macrophage/microglia.
Selected cobalamin species or salts
The method further specifies vitamin B12 selected from methylcobalamin, cyanocobalamin, hydroxocobalamin, sulfitocobalamin, adenosylcobalamin, or salts thereof.
Methylcobalamin embodiment
The method is carried out using vitamin B12 in the form of methylcobalamin.
Continuous administration regimen
The method further includes continuously administering the agent to the patient for a period of time.
Intravenous drip infusion administration
The method further specifies administering the agent to a patient using intravenous drip infusion.
Overall, the claim coverage centers on a vitamin B12-based method that shifts macrophage/microglia balance toward M2 induction and away from M1 induction by reducing the M1/M2 ratio, with dependent claim refinements specifying particular cobalamin forms and narrowing delivery to continuous administration or intravenous drip infusion.
Stated Advantages
Promoting M2 macrophage/microglia induction.
Inhibiting M1 macrophage/microglia induction.
Reducing the ratio of M1 macrophage/microglia to M2 macrophage/microglia.
Inhibiting apoptosis and necrosis.
Promoting nerve/axon regeneration.
Functional recovery in the described nervous system disease models.
Documented Applications
Treating or improving outcomes in central nervous system diseases and injuries including cerebral infarction and dementia.
Treating or improving outcomes in spinal cord injury.
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