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iscalimab   Click here for help

GtoPdb Ligand ID: 9802

Synonyms: CFZ-533 | CFZ533 | NVP-CFZ533 | OM11-62MF
Immunopharmacology Ligand
Compound class: Antibody
Comment: Iscalimab (CFZ533) is a Fc-silent anti-CD40 monoclonal antibody that is designed exhibit no agonist activity and is non-depleting (no ADCC activity for an improved safety profile, particularly in non-oncologic indications) [1,8]. It is claimed in Novartis' patent WO2012065950 [6] as mAb1 (based on peptide sequence alignments between the INN record for iscalimab and patented sequences retrieved from a BLAST search). Blocking CD40-mediated inflammatory responses is a well advanced mechanism being expoited for potential to treat autoimmune and inflammatory disorders and/or for preventing/reducing graft rejection following organ transplant.
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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. Cordoba F, Wieczorek G, Audet M, Roth L, Schneider MA, Kunkler A, Stuber N, Erard M, Ceci M, Baumgartner R et al.. (2015)
A novel, blocking, Fc-silent anti-CD40 monoclonal antibody prolongs nonhuman primate renal allograft survival in the absence of B cell depletion.
Am J Transplant, 15 (11): 2825-36. [PMID:26139432]
2. Espié P, He Y, Koo P, Sickert D, Dupuy C, Chokoté E, Schuler R, Mergentaler H, Ristov J, Milojevic J et al.. (2020)
First-in-human clinical trial to assess pharmacokinetics, pharmacodynamics, safety, and tolerability of iscalimab, an anti-CD40 monoclonal antibody.
Am J Transplant, 20 (2): 463-473. [PMID:31647605]
3. Fisher BA, Mariette X, Papas A, Grader-Beck T, Bootsma H, Ng WF, van Daele PLA, Finzel S, Noaiseh G, Elgueta S et al.. (2024)
Safety and efficacy of subcutaneous iscalimab (CFZ533) in two distinct populations of patients with Sjögren's disease (TWINSS): week 24 results of a randomised, double-blind, placebo-controlled, phase 2b dose-ranging study.
Lancet, 404 (10452): 540-553. [PMID:39096929]
4. Fisher BA, Szanto A, Ng WF, Bombardieri M, Posch MG, Papas AS, Farag AM, Daikeler T, Bannert B, Kyburz D et al.. (2020)
Assessment of the anti-CD40 antibody iscalimab in patients with primary Sjögren's syndrome: a multicentre, randomised, double-blind, placebo-controlled, proof-of-concept study.
Lancet Rheumatol, 2 (3): e142-e152. [PMID:38263652]
5. GomezMancilla B, Meriggioli MN, Genge A, Roubenoff R, Espié P, Dupuy C, Hartmann N, Pezous N, Kinhikar A, Tichy M et al.. (2024)
Efficacy and safety of iscalimab, a novel anti-CD40 monoclonal antibody, in moderate-to-severe myasthenia gravis: A phase 2 randomized study.
J Clin Neurosci, 119: 76-84. [PMID:37988976]
6. Heusser C, Rush J, Vincent K. (2012)
Silent fc variants of anti-cd40 antibodies.
Patent number: WO2012065950. Assignee: Novartis Ag. Priority date: 15/11/2010. Publication date: 24/05/2012.
7. Kahaly GJ, Stan MN, Frommer L, Gergely P, Colin L, Amer A, Schuhmann I, Espie P, Rush JS, Basson C et al.. (2020)
A Novel Anti-CD40 Monoclonal Antibody, Iscalimab, for Control of Graves Hyperthyroidism-A Proof-of-Concept Trial.
J Clin Endocrinol Metab, 105 (3). [PMID:31512728]
8. Ulrich P, Flandre T, Espie P, Sickert D, Rubic-Schneider T, Shaw DA, Rush JS. (2018)
Nonclinical Safety Assessment of CFZ533, a Fc-Silent Anti-CD40 Antibody, in Cynomolgus Monkeys.
Toxicol Sci, 166 (1): 192-202. [PMID:30099540]