| Identification | Back Directory | [Name]
Mirogabalin besylate | [CAS]
1138245-21-2 | [Synonyms]
Mirogabalin besylat
Mirogabalin Besilate
Mirogabalin besylate
Mirogabalin Besylate 10928
MIROGABALIN BENZENESULFONIC ACID
Mirogabalin besylate (DS 5565 besylate)
[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0] hept-3-en-6-yl]acetic acid benzenesulfonate
((1R,5S,6S)-6-(carboxymethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)methanaminium benzenesulfonate
2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid compound with benzenesulfonic acid (1:1) | [Molecular Formula]
C18H25NO5S | [MDL Number]
MFCD31631215 | [MOL File]
1138245-21-2.mol | [Molecular Weight]
367.46 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (340.17 mM) | [InChI]
InChI=1/C12H19NO2.C6H6O3S/c1-2-8-3-9-5-12(7-13,6-11(14)15)10(9)4-8;7-10(8,9)6-4-2-1-3-5-6/h4,9-10H,2-3,5-7,13H2,1H3,(H,14,15);1-5H,(H,7,8,9)/t9-,10-,12-;/s3 | [InChIKey]
OKJXJRVWXYRSAN-QWGAVYBYNA-N | [SMILES]
S(C1C=CC=CC=1)(O)(=O)=O.C([C@]1(C[C@@]2([H])CC(CC)=C[C@@]12[H])CN)C(=O)O |&1:11,13,20,r| |
| Hazard Information | Back Directory | [Description]
Mirogabalin besylate (mirogabalin, Tarlige) is a gabapentinoid therapy developed by Daiichi Sankyo, which is approved in Japan for the treatment of postherpetic neuralgia and painful diabetic peripheral neuropathy. Mirogabalin has a potent pain-modulating effect with a unique high affinity and prolonged dissociation rate for the a2delta-1 subunit of voltage-gated calcium (Ca2+) channels (VGCCs) on the dorsal root ganglion resulting in more sustained analgesia compared with traditional gabapentinoids[1].
| [Side effects]
Mirogabalin has a superior adverse events (AEs) profile due to a rapid dissociation from the a2delta-2 subunit of VGCCs potentially implicated in central nervous system-specific AEs. The most common AEs for mirogabalin are dizziness (approximately 8-16%), somnolence (approximately 6-24%) and headache (approximately 6-14%), with a lower incidence of constipation, nausea, diarrhea, vomiting, edema, fatigue and weight gain[1]. | [References]
[1] J Burgess. “Mirogabalin besylate in the treatment of neuropathic pain.” Drugs of today 56 2 (2020): 135–149.
|
|
|