mirogabalin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
gabamimetic agents	5491	1138245-13-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: mirogabalin mirogabalin besilate tarlige DS 5565	Mirogabalin, a novel ligand for the alpha2delta subunit of voltage-gated calcium channels, has been approved for the treatment of peripheral neuropathic pain including painful diabetic peripheral neuropathy (DPNP) and postherpetic neuralgia (PHN) in Japan. Mirogabalin showed potent and selective binding affinities for the alpha2delta subunits, and slower dissociation rates for the alpha2delta-1 subunit than for the alpha2delta-2 subunit. It also showed potent and long-lasting analgesic effects in rat models of neuropathic pain, and wider safety margins for the central nervous system side effects. A pharmacological study using mutant mice demonstrated that the analgesic effects of mirogabalin were mediated by binding of the drug to the alpha2delta-1 subunit, not the alpha2delta-2 subunit. Molecular weight: 209.29 Formula: C12H19NO2 CLOGP: -0.34 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 63.32 ALOGS: -2.14 ROTB: 4

Molecule

Description

Molfile Inchi Smiles

Synonyms:

mirogabalin
mirogabalin besilate
tarlige
DS 5565

Mirogabalin, a novel ligand for the alpha2delta subunit of voltage-gated calcium channels, has been approved for the treatment of peripheral neuropathic pain including painful diabetic peripheral neuropathy (DPNP) and postherpetic neuralgia (PHN) in Japan. Mirogabalin showed potent and selective binding affinities for the alpha2delta subunits, and slower dissociation rates for the alpha2delta-1 subunit than for the alpha2delta-2 subunit. It also showed potent and long-lasting analgesic effects in rat models of neuropathic pain, and wider safety margins for the central nervous system side effects. A pharmacological study using mutant mice demonstrated that the analgesic effects of mirogabalin were mediated by binding of the drug to the alpha2delta-1 subunit, not the alpha2delta-2 subunit.

Molecular weight: 209.29
Formula: C12H19NO2
CLOGP: -0.34
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 63.32
ALOGS: -2.14
ROTB: 4

Drug dosage:

Dose	Unit	Route
25	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Aug. 1, 2019	PMDA	DAIICHI SANKYO COMPANY, LIMITED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N02BF03	NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Gabapentinoids

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID
Postherpetic neuralgia	indication	2177002
Peripheral neuropathic pain	indication	279981003
Diabetic peripheral neuropathy	indication	424736006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Voltage-dependent calcium channel subunit alpha-2/delta-1	Ion channel	P54289	CA2D1_HUMAN	MODULATOR	Kd	7.87		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Voltage-dependent calcium channel subunit alpha-2/delta-2	Ion channel	Q9NY47	CA2D2_HUMAN	MODULATOR	Kd	7.64		SCIENTIFIC LITERATURE

External reference:

ID	Source
8X9	PDB_CHEM_ID
CHEMBL3545257	ChEMBL_ID
CHEMBL3545125	ChEMBL_ID
C000598618	MESH_SUPPLEMENTAL_RECORD_UI
8303	IUPHAR_LIGAND_ID
DB11825	DRUGBANK_ID
D10790	KEGG_DRUG
C4043827	UMLSCUI
9767	INN_ID
59509752	PUBCHEM_CID
S7LK2KDM5U	UNII

Pharmaceutical products:

None