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-12029751-B2
Publication Date
2024-07-09
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
A vitamin B12 agent, particularly methylcobalamin, is provided as a therapeutic agent for nervous system diseases, including central nervous system disorders such as cerebral infarction, dementia, and spinal cord injury. The disclosed treatment comprises administering an agent comprising an effective amount of methylcobalamin to a patient having cerebral infarction by continuous intravenous drip infusion administration for a period of time.
The disclosed therapeutic effect is linked to modulation of macrophage/microglia phenotypes. It promotes M2 macrophage/microglia induction and inhibits M1 macrophage/microglia induction, thereby reducing the M1/M2 imbalance.
The methylcobalamin therapeutic agent is further associated with enhanced neuronal survival/apoptosis and nerve regeneration. Supporting outcomes described include changes in M1/M2 marker expression and effects on neuronal injury and regeneration-related measures, including neurite outgrowth and functional recovery in cerebral infarction models and spinal cord injury models.
Claims Coverage
The claim coverage centers on one independent claim for treating cerebral infarction by administering methylcobalamin with continuous intravenous drip infusion for a period of time. The claim set also includes dependent refinements specifying treatment timing and macrophage/microglia phenotype objectives, for a total of four inventive features.
Treating cerebral infarction by continuous intravenous drip infusion of methylcobalamin
A method comprising administering to a patient with the cerebral infarction an agent comprising an effective amount of methylcobalamin by continuous intravenous drip infusion administration for a period of time.
Treatment-start timing for cerebral infarction
Starting administration immediately after onset of the cerebral infarction or within 12 hours of onset.
Methylcobalamin effective amount to shift macrophage/microglia toward M2
An effective amount of methylcobalamin that is an amount effective for promoting M2 macrophage/microglia induction and inhibiting M1 macrophage/microglia induction.
Methylcobalamin effective amount to reduce M1/M2 ratio
An effective amount of methylcobalamin that is an amount effective for reducing the ratio of M1 macrophage/microglia to M2 macrophage/microglia.
Overall, the claims focus on continuous intravenous drip infusion administration of an effective amount of methylcobalamin for cerebral infarction, with dependent refinements that specify early treatment timing and define the intended macrophage/microglia phenotype shift.
Stated Advantages
Promotes M2 macrophage/microglia induction while inhibiting M1 macrophage/microglia induction.
Reduces the M1/M2 imbalance by reducing the ratio of M1 macrophage/microglia to M2 macrophage/microglia.
Enhances neuronal survival/apoptosis and nerve regeneration.
Improves functional outcomes in cerebral infarction models and spinal cord injury models.
Documented Applications
Treating a cerebral infarction in a patient by administering methylcobalamin by continuous intravenous drip infusion administration for a period of time.
Neuroprotective and regenerative use targeting nervous system diseases including central nervous system disorders such as cerebral infarction, dementia, and spinal cord injury.
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