pembrolizumab   Click here for help

GtoPdb Ligand ID: 7499

Synonyms: Keytruda® | lambrolizumab | MK-3475
Approved drug Immunopharmacology Ligand
pembrolizumab is an approved drug (FDA (2014), EMA (2015))
Compound class: Antibody
Comment: Pembrolizumab is the first-in-class, anti-PD-1 antibody to be approved by the US FDA.
Full peptide sequence and disulphide bond information is available from the IMGT/mAb-DB entry for this antibody.

Pembrolizumab is the first immuno-oncology therapeutic to be approved for use in cancers of any tissue type, so long as they express a specific genetic biomarker (i.e. high microsatellite instability (MSI-H) or mismatch repair deficient (dMMR) tumours). This is an important breakthrough, since up until this point FDA approvals, including earlier approvals for pembrolizumab, had always been restricted to certain tissue-specific cancers.
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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. Carven GJ, Van Eenennaam H, Dulos GJ. (2010)
Antibodies to human programmed death receptor PD-1.
Patent number: US20100266617. Assignee: Organon NV. Priority date: 13/06/2008. Publication date: 21/10/2010.
2. FDA. 
FDA approves pembrolizumab for treatment of relapsed or refractory PMBCL.
Accessed on 18/06/2018. Modified on 18/06/2018. FDA.gov, https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm610670.htm?utm_campaign=Oncology%206%2F13%2F2018&utm_medium=email&utm_source=Eloqua&elqTrackId=ce3e8cb7b99142cba3cc1d7c54d4ca4b&elq=7a1e38bda6884f40bcc462e71a154a89&elqaid=3898&elqat=1&elqCampaignId=3025
3. FDA. 
FDA approves pembrolizumab plus axitinib for advanced renal cell carcinoma.
Accessed on 23/04/2019. Modified on 23/04/2019. fda.gov, https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm636395.htm
4. Greaves P, Gribben JG. (2013)
The role of B7 family molecules in hematologic malignancy.
Blood, 121 (5): 734-44. [PMID:23223433]
5. Hamid O, Robert C, Daud A, Hodi FS, Hwu WJ, Kefford R, Wolchok JD, Hersey P, Joseph RW, Weber JS et al.. (2013)
Safety and tumor responses with lambrolizumab (anti-PD-1) in melanoma.
N Engl J Med, 369 (2): 134-44. [PMID:23724846]
6. Janakiram M, Abadi YM, Sparano JA, Zang X. (2012)
T cell coinhibition and immunotherapy in human breast cancer.
Discov Med, 14 (77): 229-36. [PMID:23114578]
7. Kelley RK, Ueno M, Yoo C, Finn RS, Furuse J, Ren Z, Yau T, Klümpen H-J, Chan SL, Ozaka M et al.. (2023)
Pembrolizumab in combination with gemcitabine and cisplatin compared with gemcitabine and cisplatin alone for patients with advanced biliary tract cancer (KEYNOTE-966): a randomised, double-blind, placebo-controlled, phase 3 trial.
The Lancet, Epub ahead of print. DOI: 10.1016/S0140-6736(23)00727-4
8. Nghiem PT, Bhatia S, Lipson EJ, Kudchadkar RR, Miller NJ, Annamalai L, Berry S, Chartash EK, Daud A, Fling SP et al.. (2016)
PD-1 Blockade with Pembrolizumab in Advanced Merkel-Cell Carcinoma.
N Engl J Med, 374 (26): 2542-52. [PMID:27093365]
9. Paz-Ares L, Luft A, Vicente D, Tafreshi A, Gümüş M, Mazières J, Hermes B, Çay Şenler F, Csőszi T, Fülöp A et al.. (2018)
Pembrolizumab plus Chemotherapy for Squamous Non-Small-Cell Lung Cancer.
N Engl J Med, 379 (21): 2040-2051. [PMID:30280635]
10. Rini BI, Plimack ER, Stus V, Gafanov R, Hawkins R, Nosov D, Pouliot F, Alekseev B, Soulières D, Melichar B et al.. (2019)
Pembrolizumab plus Axitinib versus Sunitinib for Advanced Renal-Cell Carcinoma.
N Engl J Med, 380 (12): 1116-1127. [PMID:30779529]
11. Saada-Bouzid E, Peyrade F, Guigay J. (2019)
Immunotherapy in recurrent and or metastatic squamous cell carcinoma of the head and neck.
Curr Opin Oncol, 31 (3): 146-151. [PMID:30893146]
12. Tang PA, Heng DY. (2013)
Programmed death 1 pathway inhibition in metastatic renal cell cancer and prostate cancer.
Curr Oncol Rep, 15 (2): 98-104. [PMID:23263823]