Gabapentin enacarbil

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Gabapentin enacarbil
Clinical data
Trade namesHorizant, Regnite
Other namesXP-13512
AHFS/Drugs.comProfessional Drug Facts
License data
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth
Drug classGabapentinoid
ATC code
  • None
Legal status
Legal status
Pharmacokinetic data
ExcretionKidney
Identifiers
  • (1-{[({(1RS)-1-[isobutyryloxy]ethoxy}carbonyl)
    amino]methyl}cyclohexyl)acetic acid
JSmol)
  • CC(C)C(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O
  • InChI=1S/C16H27NO6/c1-11(2)14(20)22-12(3)23-15(21)17-10-16(9-13(18)19)7-5-4-6-8-16/h11-12H,4-10H2,1-3H3,(H,17,21)(H,18,19) ☒N
  • Key:TZDUHAJSIBHXDL-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Gabapentin enacarbil (Horizant (ER) (U.S.Tooltip United States), Regnite (in Japan)) is an anticonvulsant and analgesic drug of the gabapentinoid class, and a prodrug to gabapentin.[1] It was designed for increased oral bioavailability over gabapentin,[2][3] and human trials showed it to produce extended release of gabapentin with almost twice the overall bioavailability,[4] especially when taken with a fatty meal.[5] Gabapentin enacarbil has passed human clinical trials for the treatment of restless legs syndrome, and initial results have shown it to be well tolerated and reasonably effective.[6][7][8]

Gabapentin enacarbil was denied approval by the U.S. Food and Drug Administration (FDA) in February 2010, citing concerns about possible increased cancer risk shown by some animal studies. Similar concerns had been raised about gabapentin itself in the past, but were felt to be outweighed by its clinical utility as an anticonvulsant, whereas the treatment of restless legs syndrome was not seen to justify the same kind of risk.[9] On April 6, 2011, Xenoport received FDA approval for Horizant (gabapentin enacarbil) for the treatment of moderate-to-severe restless legs syndrome.[10] On June 7, 2012, the FDA approved Horizant for the treatment of postherpetic neuralgia in adults.[11]

References

  1. PMID 19787095
    .
  2. S2CID 1535942
    .
  3. S2CID 25152318
    .
  4. S2CID 23598218
    .
  5. PMID 20137764
    .
  6. PMID 20200691
    .
  7. PMID 20511481
    .
  8. S2CID 27594934
    .
  9. ^ GlaxoSmithKline/XenoPort: FDA setback halts gabapentin reformulations[permanent dead link]
  10. ^ "XenoPort, Inc. > Investors > RSS Content". Archived from the original on 2012-07-13.
  11. ^ Jeffrey, Susan. "FDA Approves Gabapentin Enacarbil for Postherpetic Neuralgia". Medscape.

External links