Urelumab

Urelumab
Monoclonal antibody
Type	Whole antibody
Source	Human
Target	CD137
Clinical data
Other names	BMS-663513
ATC code	none;
Identifiers
CAS Number	934823-49-1 ;
ChemSpider	none;
UNII	230902QLLC;
KEGG	D09984;
Chemical and physical data
Formula	C6502H9972N1712O2030S44
Molar mass	146015.89 g·mol−1
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Urelumab (BMS-663513 or anti-4-1BB antibody) is a fully human, non‐ligand binding, CD137 agonist immunoglobulin‐γ 4 (IgG4) monoclonal antibody.^[1] It was developed utilizing Medarex's UltiMAb(R) technology by Bristol-Myers Squibb for the treatment of cancer and solid tumors.^[2] Urelumab promotes anti-tumor immunity, or an immune response against tumor cells, via CD137 activation.^[2]^[3] The application of Urelumab has been limited due to the fact that it can cause severe liver toxicity.^[4]^[5]^[6]

^ Timmerman J, Herbaux C, Ribrag V, Zelenetz AD, Houot R, Neelapu SS, et al. (May 2020). "Urelumab alone or in combination with rituximab in patients with relapsed or refractory B-cell lymphoma". American Journal of Hematology. 95 (5): 510–520. doi:10.1002/ajh.25757. PMC 7383599. PMID 32052473.
^ ^a ^b "Urelumab Overview".
^ "Urelumab". National Cancer Institute.
^ Ho SK, Xu Z, Thakur A, Fox M, Tan SS, DiGiammarino E, et al. (April 2020). "Epitope and Fc-Mediated Cross-linking, but Not High Affinity, Are Critical for Antitumor Activity of CD137 Agonist Antibody with Reduced Liver Toxicity". Molecular Cancer Therapeutics. 19 (4): 1040–1051. doi:10.1158/1535-7163.MCT-19-0608. PMID 31974274. S2CID 210882192.
^ Qi X, Li F, Wu Y, Cheng C, Han P, Wang J, Yang X (May 2019). "Optimization of 4-1BB antibody for cancer immunotherapy by balancing agonistic strength with FcγR affinity". Nature Communications. 10 (1): 2141. Bibcode:2019NatCo..10.2141Q. doi:10.1038/s41467-019-10088-1. PMC 6526162. PMID 31105267. S2CID 256641802.
^ Etxeberria I, Bolaños E, Teijeira A, Garasa S, Yanguas A, Azpilikueta A, et al. (June 2021). "Antitumor efficacy and reduced toxicity using an anti-CD137 Probody therapeutic". Proceedings of the National Academy of Sciences of the United States of America. 118 (26). Bibcode:2021PNAS..11825930E. doi:10.1073/pnas.2025930118. PMC 8255787. PMID 34172583.

[1] Timmerman J, Herbaux C, Ribrag V, Zelenetz AD, Houot R, Neelapu SS, et al. (May 2020). "Urelumab alone or in combination with rituximab in patients with relapsed or refractory B-cell lymphoma". American Journal of Hematology. 95 (5): 510–520. doi:10.1002/ajh.25757. PMC 7383599. PMID 32052473.

[:0-2] "Urelumab Overview".

[:1-3] "Urelumab". National Cancer Institute.

[:2-4] Ho SK, Xu Z, Thakur A, Fox M, Tan SS, DiGiammarino E, et al. (April 2020). "Epitope and Fc-Mediated Cross-linking, but Not High Affinity, Are Critical for Antitumor Activity of CD137 Agonist Antibody with Reduced Liver Toxicity". Molecular Cancer Therapeutics. 19 (4): 1040–1051. doi:10.1158/1535-7163.MCT-19-0608. PMID 31974274. S2CID 210882192.

[:3-5] Qi X, Li F, Wu Y, Cheng C, Han P, Wang J, Yang X (May 2019). "Optimization of 4-1BB antibody for cancer immunotherapy by balancing agonistic strength with FcγR affinity". Nature Communications. 10 (1): 2141. Bibcode:2019NatCo..10.2141Q. doi:10.1038/s41467-019-10088-1. PMC 6526162. PMID 31105267. S2CID 256641802.

[:4-6] Etxeberria I, Bolaños E, Teijeira A, Garasa S, Yanguas A, Azpilikueta A, et al. (June 2021). "Antitumor efficacy and reduced toxicity using an anti-CD137 Probody therapeutic". Proceedings of the National Academy of Sciences of the United States of America. 118 (26). Bibcode:2021PNAS..11825930E. doi:10.1073/pnas.2025930118. PMC 8255787. PMID 34172583.

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