spesolimab   Click here for help

GtoPdb Ligand ID: 12169

Synonyms: BI-655130 | BI655130 | spesolimab-sbzo | Spevigo®
Approved drug Immunopharmacology Ligand
spesolimab is an approved drug (FDA and EMA (2022))
Compound class: Antibody
Comment: Spesolimab (BI-655130) is a monoclonal antibody that disrupts interleukin-36 (IL-36)/IL-36 receptor signalling. Blocking this pathway is a molecular mechanism with potential to treat inflammatory diseases in skin and other epithelial tissues [2-3,5,7], since IL-36R expression is restricted to epithelial cells that are in direct contact with the environment, including those in the skin. Spesolimab (BI-655130) appears to be related to MAB92 which was reported by Boehringer Ingelheim in 2017 [6], but we have been unable to perform direct sequence matches. The heavy and light chain sequences for spesolimab (from its INN record) are claimed in Boehringer Ingelheim's patent US9023995B2 [4].
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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.

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View interactive charts of activity data across species
References
1. Bachelez H, Choon SE, Marrakchi S, Burden AD, Tsai TF, Morita A, Navarini AA, Zheng M, Xu J, Turki H et al.. (2021)
Trial of Spesolimab for Generalized Pustular Psoriasis.
N Engl J Med, 385 (26): 2431-2440. [PMID:34936739]
2. Bachelez H, Choon SE, Marrakchi S, Burden AD, Tsai TF, Morita A, Turki H, Hall DB, Shear M, Baum P et al.. (2019)
Inhibition of the Interleukin-36 Pathway for the Treatment of Generalized Pustular Psoriasis.
N Engl J Med, 380 (10): 981-983. [PMID:30855749]
3. Baum P, Visvanathan S, Garcet S, Roy J, Schmid R, Bossert S, Lang B, Bachelez H, Bissonnette R, Thoma C et al.. (2022)
Pustular psoriasis: Molecular pathways and effects of spesolimab in generalized pustular psoriasis.
J Allergy Clin Immunol, 149 (4): 1402-1412. [PMID:34678325]
4. Brown SE, Canada K, Chlewicki L, Howell M, Mennerich D, Woska JR. (2015)
Anti IL-36R antibodies.
Patent number: US9023995B2. Assignee: Boehringer Ingelheim International GmbH. Priority date: 16/11/2011. Publication date: 05/05/2015.
5. Ferrante M, Irving PM, Selinger CP, D'Haens G, Kuehbacher T, Seidler U, Gropper S, Haeufel T, Forgia S, Danese S et al.. (2023)
Safety and tolerability of spesolimab in patients with ulcerative colitis.
Expert Opin Drug Saf, 22 (2): 141-152. [PMID:35861588]
6. Ganesan R, Raymond EL, Mennerich D, Woska Jr JR, Caviness G, Grimaldi C, Ahlberg J, Perez R, Roberts S, Yang D et al.. (2017)
Generation and functional characterization of anti-human and anti-mouse IL-36R antagonist monoclonal antibodies.
MAbs, 9 (7): 1143-1154. [PMID:28726542]
7. Hwang J, Rick J, Hsiao J, Shi VY. (2022)
A review of IL-36: an emerging therapeutic target for inflammatory dermatoses.
J Dermatolog Treat, 33 (6): 2711-2722. [PMID:35470744]
8. Maçães CO, Lé AM, Torres T. (2022)
Generalized pustular psoriasis: the new era of treatment with IL-36 receptor inhibitors.
J Dermatolog Treat, 33 (7): 2911-2918. [PMID:35695278]