Rotigotine

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Aderis Pharmaceuticals
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Rotigotine
Clinical data
Trade namesNeupro, Leganto
AHFS/Drugs.comMonograph
MedlinePlusa607059
License data
Pregnancy
category
  • AU: B3
Routes of
administration		Transdermal patch
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class C1 (Other controlled substances)[1]
  • US: ℞-only
  • EU: Rx-only[2]
  • In general: ℞ (Prescription only)
CYP-mediated)
Elimination half-life5–7 hours
ExcretionUrine (71%), Feces (23%)
Identifiers
  • (S)-6-[Propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8- tetrahydronaphthalen-1-ol
JSmol)
  • Oc1cccc3c1CCC(N(CCC)CCc2sccc2)C3
  • InChI=1S/C19H25NOS/c1-2-11-20(12-10-17-6-4-13-22-17)16-8-9-18-15(14-16)5-3-7-19(18)21/h3-7,13,16,21H,2,8-12,14H2,1H3 checkY
  • Key:KFQYTPMOWPVWEJ-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Rotigotine, sold under the brand name Neupro among others, is a dopamine agonist of the non-ergoline class of medications indicated for the treatment of Parkinson's disease and restless legs syndrome.[3][4] It is formulated as a once-daily transdermal patch which provides a slow and constant supply of the drug over the course of 24 hours.[3]

Like other dopamine agonists, rotigotine has been shown to possess antidepressant effects and may be useful in the treatment of depression as well.[5]

History

Initially developed at the University of Groningen in 1985 as N-0437,[6] Aderis Pharmaceuticals acquired rotigotine and continued development toward commercialization.[citation needed] In 1998, Aderis globally out-licensed rotigotine for development and commercialization to Schwarz Pharma,[7] which firm was acquired by UCB S.A. in 2006. Schwarz completed acquisition of full rights to rotigotine from Aderis as of 2005.[8]

The drug was approved by the European Medicines Agency (EMA) for use in Europe in 2006.[2] In 2007, the Neupro patch was approved by the Food and Drug Administration (FDA).[9] It became the first transdermal treatment of Parkinson's disease in the United States.[citation needed] In 2008, Schwarz Pharma recalled all Neupro patches in the United States and some in Europe because of problems with the delivery mechanism. FDA also suspended its marketing authorization after crystal formation was noted in some patches.[10] The patch was reformulated, and was reintroduced in the United States in 2012.[11]

Rotigotine was authorized as a treatment for restless legs syndrome in August 2008.[4]

Side effects

General

pathological gambling.[14] Mild adverse skin reactions at the patch application site may also occur.[3][13]

Pharmacology

Rotigotine acts as a non-selective

pharmacokinetic properties) and pergolide but unlike pramipexole and ropinirole.[15]

binding profile of rotigotine[16]
Receptor Ki (nM)
D1
 83
D2
 13.5
D3
 0.71
D4.2
 3.9
D4.4
 15
D4.7
 5.9
D5
 5.4
α1A 176
α1B 273
α2A 338
α2B 27
α2C 135
5-HT1A 30
5-HT7 86
H1
 330

All affinities listed were assayed using

full agonist (depending on the assay) at all dopamine receptors listed, as an antagonist at the α2B-adrenergic receptor, and as a partial agonist at the 5-HT1A receptor.[16] Though it has affinity for a large number of sites as shown above, at clinical doses rotigotine behaves mostly as a selective
D1-like (D1, D5) and D2-like (D2, D3, D4) receptor agonist, with its α2B-adrenergic and 5-HT1A activity also possibly having some minor relevance.

References

  1. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  2. ^ a b "Neupro EPAR". European Medicines Agency. 17 September 2018. Retrieved 2 March 2020.
  3. ^
    S2CID 40466260
    .
  4. ^
    PMID 19956807
    .
  5. PMID 16959244
    .
  6. S2CID 8847550
    .
  7. ^ Development & Commercialization of rotigotine by Aderis (Aderis Pharmaceuticals making a reference for the commercialization of rotigotine)
  8. ^ "SCHWARZ PHARMA ACQUIRES REMAINING RIGHTS TO ROTIGOTINE FROM ADERIS | FDAnews". www.fdanews.com. Retrieved 11 August 2022.
  9. ^ PubChem. "Rotigotine". pubchem.ncbi.nlm.nih.gov. Retrieved 11 August 2022.
  10. PMID 23936090
    .
  11. ^ "Neupro Patch Re-launches in the US". Archived from the original on 23 March 2016. Retrieved 12 September 2012.
  12. S2CID 34876593
    .
  13. ^
    PMID 14676046
    .
  14. S2CID 23942499
    .
  15. ^
    PMID 25339241
    .
  16. ^
    S2CID 25112443
    .

External links

Wikimedia Commons has media related to Rotigotine.
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