Drug intelligence / Profile preview

gabapentin + methylcobalamin

Development stage
Phase 4
Lead developer
Sun Pharmaceutical Industries
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Gabapentin + methylcobalamin is a fixed-dose combination prescription medication primarily indicated for the management of neuropathic pain associated with conditions such as diabetic neuropathy, post-herpetic neuralgia, and peripheral neuropathy. The combination leverages two distinct mechanisms: **gabapentin**, an anticonvulsant, acts as an alpha-2-delta ligand that binds to the α2δ-1 subunit of voltage-gated calcium channels in the central nervous system, thereby reducing the release of excitatory neurotransmitters and modulating abnormal pain signals. **Methylcobalamin**, a neurologically active form of vitamin B12, serves as a cofactor for the enzyme methionine synthase, which is essential for the synthesis of myelin. By promoting myelin sheath regeneration and protecting nerve fibers from further damage, methylcobalamin supports nerve repair and improves nerve conduction velocity. This synergistic approach addresses both the symptomatic transmission of pain and the underlying nerve damage.

Brand names
GabaneuronGabapin MEGabantin MGabamaxGabastar M
Other names
gabapentin and methylcobalamin
02

Targets

Thrombospondin-2 (TSP-2)–Voltage-dependent calcium channel subunit alpha-2/delta-1 (α2δ-1) interactionVoltage-gated calcium channel subunit alpha-2/delta-1–N-methyl-D-aspartate receptor interaction interfaceCACNA2D2 (α2δ-2)GAD1 (Glutamate decarboxylase 1)MTR (Methionine synthase)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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