Palovarotene

Palovarotene
Systematic (IUPAC) name

4-[(E)-2-[5,5,8,8-tetramethyl-3-(1H-pyrazol-1-ylmethyl)-5,6,7,8-tetrahydronaphthalen-2-yl]ethenyl]benzoic acid
Clinical data
Legal status	Investigational
Routes of administration	Oral
Identifiers
ATC code	None
PubChem	CID 10295295
ChemSpider	8470763
Chemical data
Formula	C₂₇H₃₀N₂O₂
Molecular mass	414.5393 g/mol
SMILES CC1(CCC(C2=C1C=C(C(=C2)/C=C/C3=CC=C(C=C3)C(=O)O)CN4C=CC=N4)(C)C)C
InChI InChI=1S/C27H30N2O2/c1-26(2)12-13-27(3,4)24-17-22(18-29-15-5-14-28-29)21(16-23(24)26)11-8-19-6-9-20(10-7-19)25(30)31/h5-11,14-17H,12-13,18H2,1-4H3,(H,30,31)/b11-8+ Key:YTFHCXIPDIHOIA-DHZHZOJOSA-N

Palovarotene (R-667, RO-3300074) is a highly selective retinoic acid receptor gamma (RAR-γ) agonist that is under investigation as a potential treatment for emphysema.^[1] It is being developed by Roche. One such clinical trial found that palovarotene failed to produce any significant improvement in those with α₁-antitrypsin deficiency-induced emphysema over a period of a year.^[2]

Reference list

↑ Hind, M; Stinchcombe, S (November 2009). "Palovarotene, a novel retinoic acid receptor gamma agonist for the treatment of emphysema". Current Opinion in Investigation Drugs 10 (11): 1243–1250. PMID 19876792.
↑ Stolk, J; Stockley, RA; Stoel, BC; Cooper, BG; Piitulainen, E; Seersholm, N; Chapman, KR; Burdon, JG; Decramer, M; Abboud, RT; Mannes, GP; Wouters, EF; Garrett, JE; Barros-Tizon, JC; Russi, EW; Lomas, DA; MacNee, WA; Rames, A (August 2012). "Randomised controlled trial for emphysema with a selective agonist of the c-type retinoic acid receptor". European Respiratory Journal 40 (2): 306–312. doi:10.1183/09031936.00161911. PMID 22282548.