Setipiprant

Setipiprant
Clinical data
Routes of
administration		 Oral
ATC code none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number 866460-33-5
PubChem (CID) 49843471
ChemSpider 29738718
UNII BHF20LA2GM
KEGG D10326
Chemical and physical data
Formula C24H19FN2O3
Molar mass 402.417 g/mol
3D model (Jmol) Interactive image

Setipiprant (INN) (developmental code names ACT-129,968, KYTH-105) is a drug originally developed by Actelion which acts as a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2).[1] It was initially researched as a treatment for allergies and inflammatory disorders, particularly asthma, but despite being well tolerated in clinical trials and showing reasonable efficacy against allergen-induced airway responses in asthmatic patients,[2][3] it failed to show sufficient advantages over existing drugs and was discontinued from further development in this application.[4]

However, following the discovery in 2012 that the prostaglandin D2 receptor (DP/PGD2) is expressed at high levels in the scalp of men affected by male pattern baldness,[5] the rights to setipiprant were acquired by Kythera with a view to potentially developing this drug as a novel treatment for baldness, with a previously unexploited mechanism of action.[6] While it is too early to tell whether setipiprant will be an effective treatment for this condition, the favorable pharmacokinetics and relative lack of side effects seen in earlier clinical trials mean that fresh clinical trials for this new application can be conducted fairly quickly.[7]

See also

References

  1. ↑ Fretz H, Valdenaire A, Pothier J, Hilpert K, Gnerre C, Peter O, Leroy X, Riederer MA. Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist. J Med Chem. 2013 Jun 27;56(12):4899-911. doi: 10.1021/jm400122f PMID 23721423
  2. ↑ Sidharta PN, Diamant Z, Dingemanse J. Single- and multiple-dose tolerability and pharmacokinetics of the CRTH2 antagonist setipiprant in healthy male subjects. Fundam Clin Pharmacol. 2014 Dec;28(6):690-9. doi: 10.1111/fcp.12079 PMID 24734908
  3. ↑ Diamant Z, Sidharta PN, Singh D, O'Connor BJ, Zuiker R, Leaker BR, Silkey M, Dingemanse J. Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52. doi: 10.1111/cea.12357 PMID 24964348
  4. ↑ Norman P. Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs. Expert Opin Investig Drugs. 2014 Jan;23(1):55-66. doi: 10.1517/13543784.2013.839658 PMID 24073896
  5. ↑ Garza LA, et al. Prostaglandin D2 inhibits hair growth and is elevated in bald scalp of men with androgenetic alopecia. Science Translational Medicine, 21 March 2012; 4(126):126ra34. doi: 10.1126/scitranslmed.3003122
  6. ↑ George Cotsarelis, Garret Fitzgerald, Luis Garza. Compositions and methods for regulating hair growth. US Patent application 2015/0072963
  7. ↑ Pipeline KYTH-105 (setipiprant)
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