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durvalumab

别名 anti-B7H1 monoclonal antibody, MEDI4736, MEDI-4736, Imfinzi®
Compound Class Antibody
变动原因 Durvalumab is a monoclonal antibody directed against programmed death-1 ligand-1 (PD-L1, aka CD274), an important immunopharmacological drug discovery target in immuno-oncology.
Peptide sequence and structural information for this antibody are available from its IMGT/mAb-db record. A patent search suggests that the development and use of durvalumab may be covered by patent WO2011066389 , although we cannot verify this by peptide sequence matches as no sequences from this patent are pulled in a protein BLAST with the light or heavy variable regions of durvalumab peptide sequences. An X-ray crystal structure of the PD-L1/durvalumab complex has been submitted to the RCSB PDB (accession 5X8M) .

Summary

是否批准为药物? (FDA (2017), EMA (2018))
IUPAC Name 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
别名 anti-B7H1 monoclonal antibody, MEDI4736, MEDI-4736, Imfinzi®

生物活性

生物活性评价 The affinity value in the table below is that reported in patent WO2011066389.

临床资料

Summary of Clinical Use Durvalumab (MEDI-4736) was 'fast tracked' to Phase 3 clinical trial, then receiving full FDA approval in May 2017 for the treatment of advanced/metastatic bladder cancer (urothelial carcinoma) in patients who have already received platinum-containing chemotherapy. In February 2018 FDA approval was expanded to include treatment of some stage III non-small cell lung cancer (NSCLC) patients. It is hoped that durvalumab may show clinical efficacy against other cancers. Click here to link to ClinicalTrials.gov's list of Phase 2 and 3 studies evaluating MEDI-4736 in additional cancer types.
作用机制与药效学效应 Anti-PD-L1 antibodies interfere with PD-L1 signalling, which results in the activation of tumour-detecting/infiltrating T cells. The drug’s mechanism of action enables the immune cells to detect and destroy tumour cells.

参考文献

1. Queva C, Morrow M, Hammond S, Alimzhanov M, Babcock J, Foltz I, Kang JS, Sekirov L, Boyle M, Chodorge M.  (2011)  Targeted binding agents against b7-h1..  Drugs,  71  (13):  (1755-70).  [PMID:21902297]
2. Lee HT, Lee JY, Lim H, Lee SH, Moon YJ, Pyo HJ, Ryu SE, Shin W, Heo YS.  (2017)  Molecular mechanism of PD-1/PD-L1 blockade via anti-PD-L1 antibodies atezolizumab and durvalumab..  Sci Rep,  (1):  (5532).  [PMID:28717238]

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品牌简介

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