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HomeProduct name listMirogabalin besylate

Mirogabalin besylate

  • CAS NO.:1138245-21-2
  • Empirical Formula: C18H25NO5S
  • Molecular Weight: 367.46
  • MDL number: MFCD31631215
  • Update Date: 2024-07-24 13:33:21
Mirogabalin besylate Structural

What is Mirogabalin besylate?

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].

The Uses of Mirogabalin besylate

Mirogabalin besylate is an oral gabapentin analogue for the treatment of peripheral neuralgia (PNP), including diabetic PNP and postherpetic neuralgia. The drug has been approved in Japan for the treatment of PNP and has not yet received FDA approval.

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.

Properties of Mirogabalin besylate

storage temp.  Store at -20°C
solubility  DMSO : 125 mg/mL (340.17 mM)
form  Solid
color  White to off-white
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

Safety information for Mirogabalin besylate

Computed Descriptors for Mirogabalin besylate

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|

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