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Synonyms: 1,11-anhydro[L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl- N-methyl-L-valyl-[(2S,3R,4R,6E)-3-hydroxy-4-methyl- 2-(methylamino)nona-6,8-dienoyl][(2S)-2-aminobutanoyl]- N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucine] | E-ISA247 | ISA(TX)247 | ISA-247 | ISA247 | ISATX247 | Lupkynis® | R 1524 | R-1524 | R1524
voclosporin is an approved drug (FDA (2021))
Compound class: Peptide or derivative
Comment: Voclosporin (ISA247, ISATX247) is a cyclic peptide that is a semi-synthetic cyclosporine analogue [1-3,6], but with distinct clinical efficacy and safety profiles . Like cyclosporine, it has immunosuppressive action, and it binds cyclophilin A . Functionally, it acts as a calcineurin inhibitor. Prior to voclosporin, clinically used calcineurin inhibitors were cyclosporine (cyclosporin A), tacrolimus, and pimecrolimus.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Abel MD, Aspeslet LJ, Freitag DG, Naicker S, Trepanier DJ, Kneteman NM, Foster RT, Yatscoff RW. (2001)
ISATX247: a novel calcineurin inhibitor.
J Heart Lung Transplant, 20 (2): 161. [PMID:11250240]
2. Aspeslet L, Freitag D, Trepanier D, Abel M, Naicker S, Kneteman N, Foster R, Yatscoff R. (2001)
ISA(TX)247: a novel calcineurin inhibitor.
Transplant Proc, 33 (1-2): 1048-51. [PMID:11267185]
3. Bîrsan T, Dambrin C, Freitag DG, Yatscoff RW, Morris RE. (2005)
The novel calcineurin inhibitor ISA247: a more potent immunosuppressant than cyclosporine in vitro.
Transpl Int, 17 (12): 767-71. [PMID:15827754]
4. Kuglstatter A, Mueller F, Kusznir E, Gsell B, Stihle M, Thoma R, Benz J, Aspeslet L, Freitag D, Hennig M. (2011)
Structural basis for the cyclophilin A binding affinity and immunosuppressive potency of E-ISA247 (voclosporin).
Acta Crystallogr D Biol Crystallogr, 67 (Pt 2): 119-23. [PMID:21245533]
5. Li Y, Palmisano M, Sun D, Zhou S. (2020)
Pharmacokinetic Disposition Difference Between Cyclosporine and Voclosporin Drives Their Distinct Efficacy and Safety Profiles in Clinical Studies.
Clin Pharmacol, 12: 83-96. [PMID:32669879]
ISA 247: trans-ISA 247, trans-R 1524, ISA(TX)247, ISAtx 247, ISATx247, LX 211, LX211, R 1524, R-1524.
Drugs R D, 8 (2): 103-12. [PMID:17324008]