DGIdb - PEMBROLIZUMAB Drug Record

PEMBROLIZUMAB chembl:CHEMBL3137343 ApprovedAntineoplastic

Alternate Names:

KEYLYNK-010 COMPONENT PEMBROLIZUMAB
SCH-900475
PEMBROLIZUMAB
PEMBROLIZUMAB COMPONENT OF KEYLYNK-010
KEYTRUDA
MK-3475
LAMBROLIZUMAB
rxcui:1547545
pubchem.compound:254741536
chembl:CHEMBL3137343
chemidplus:1374853-91-4
pubchem.substance:254741536
drugbank:09037

Drug Info:

FDA Approval	Classical Hodgkin lymphoma, Melanoma, Non-small cell lung cancer (PD-L1+), Head and neck squamous cell carcinoma
Drug Class	Therapeutic Antibodies

(8 More Sources)

Publications:

Zaretsky et al., 2016, Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma., N. Engl. J. Med.
Peng et al., 2016, Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy., Cancer Discov
McDermott et al., 2015, Pembrolizumab: PD-1 inhibition as a therapeutic strategy in cancer., Drugs Today
Dong et al., 2017, Potential Predictive Value of TP53 and KRAS Mutation Status for Response to PD-1 Blockade Immunotherapy in Lung Adenocarcinoma., Clin. Cancer Res.
Shin et al., 2017, Primary Resistance to PD-1 Blockade Mediated by JAK1/2 Mutations., Cancer Discov
Gainor et al., 2016, EGFR Mutations and ALK Rearrangements Are Associated with Low Response Rates to PD-1 Pathway Blockade in Non-Small Cell Lung Cancer: A Retrospective Analysis., Clin. Cancer Res.
Skoulidis F et al., 2018, <i>STK11/LKB1</i> Mutations and PD-1 Inhibitor Resistance in <i>KRAS</i>-Mutant Lung Adenocarcinoma., Cancer Discov
Mehnert et al., 2016, Immune activation and response to pembrolizumab in POLE-mutant endometrial cancer., J. Clin. Invest.
Johanns et al., 2016, Immunogenomics of Hypermutated Glioblastoma: A Patient with Germline POLE Deficiency Treated with Checkpoint Blockade Immunotherapy., Cancer Discov
Gong J et al., 2017, Response to PD-1 Blockade in Microsatellite Stable Metastatic Colorectal Cancer Harboring a <i>POLE</i> Mutation., J Natl Compr Canc Netw
Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
Hastings K et al., 2019, EGFR mutation subtypes and response to immune checkpoint blockade treatment in non-small-cell lung cancer., Ann Oncol
Zhao J et al., 2019, Immune and genomic correlates of response to anti-PD-1 immunotherapy in glioblastoma., Nat Med
Chen et al., 2017, KRAS mutation-induced upregulation of PD-L1 mediates immune escape in human lung adenocarcinoma., Cancer Immunol. Immunother.
Garon et al., 2015, Pembrolizumab for the treatment of non-small-cell lung cancer., N. Engl. J. Med.
Aguiar et al., 2017, PD-L1 expression as a predictive biomarker in advanced non-small-cell lung cancer: updated survival data., Immunotherapy
Reck et al., 2016, Pembrolizumab versus Chemotherapy for PD-L1-Positive Non-Small-Cell Lung Cancer., N. Engl. J. Med.
Passiglia et al., 2016, PD-L1 expression as predictive biomarker in patients with NSCLC: a pooled analysis., Oncotarget
Carbognin et al., 2015, Differential Activity of Nivolumab, Pembrolizumab and MPDL3280A according to the Tumor Expression of Programmed Death-Ligand-1 (PD-L1): Sensitivity Analysis of Trials in Melanoma, Lung and Genitourinary Cancers., PLoS ONE
Johnson et al., 2016, Melanoma-specific MHC-II expression represents a tumour-autonomous phenotype and predicts response to anti-PD-1/PD-L1 therapy., Nat Commun
Kato et al., 2017, Hyperprogressors after Immunotherapy: Analysis of Genomic Alterations Associated with Accelerated Growth Rate., Clin. Cancer Res.
Yearley JH et al., 2017, PD-L2 Expression in Human Tumors: Relevance to Anti-PD-1 Therapy in Cancer., Clin Cancer Res
Miao D et al., 2018, Genomic correlates of response to immune checkpoint therapies in clear cell renal cell carcinoma., Science
Shen J et al., 2018, ARID1A deficiency promotes mutability and potentiates therapeutic antitumor immunity unleashed by immune checkpoint blockade., Nat Med

PEMBROLIZUMAB PDCD1LG2

Interaction Score: 2.81

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28619999

Sources:
CIViC
PEMBROLIZUMAB POLE

Interaction Score: 2.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27159395 27683556 28188185

Sources:
CIViC
PEMBROLIZUMAB B2M

Interaction Score: 1.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27433843

Sources:
CIViC
PEMBROLIZUMAB CD274

Interaction Score: 1.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25891174 28472902 27718847 26918451 26086854

Sources:
CIViC PharmGKB FDA
PEMBROLIZUMAB ARID1A

Interaction Score: 1.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29736026

Sources:
CIViC
PEMBROLIZUMAB MDM4

Interaction Score: 1.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28351930

Sources:
CIViC
PEMBROLIZUMAB HLA-DRA

Interaction Score: 0.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26822383

Sources:
CIViC
PEMBROLIZUMAB PDCD1

Interaction Score: 0.8

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Programmed cell death protein 1 inhibitor

Direct Interaction yes

PMIDs:
25685857

Sources:
MyCancerGenome ChemblInteractions TTD
PEMBROLIZUMAB PBRM1

Interaction Score: 0.62

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29301960

Sources:
CIViC
PEMBROLIZUMAB JAK1

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27433843 27903500

Sources:
COSMIC CIViC
PEMBROLIZUMAB MDM2

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28351930

Sources:
CIViC
PEMBROLIZUMAB CDK12

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
OncoKB
PEMBROLIZUMAB STK11

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29773717

Sources:
CIViC
PEMBROLIZUMAB ALK

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type decreased response

Approval Status Clinical Study

PMIDs:
27225694

Sources:
JAX-CKB PharmGKB FDA
PEMBROLIZUMAB JAK2

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type predicted – resistant

Approval Status Clinical Study

PMIDs:
27433843

Sources:
JAX-CKB COSMIC CIViC
PEMBROLIZUMAB NRAS

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pembrolizumab + Trametinib

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
28514312

Sources:
JAX-CKB
PEMBROLIZUMAB PTEN

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Clinical Study

PMIDs:
26645196 30742119

Sources:
JAX-CKB CIViC
PEMBROLIZUMAB BRAF

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type no benefit

Approval Status Preclinical

PMIDs:
26645196

Sources:
JAX-CKB PharmGKB FDA
PEMBROLIZUMAB EGFR

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type decreased response

Approval Status Clinical Study

PMIDs:
27225694 31086949

Sources:
JAX-CKB CIViC PharmGKB FDA
PEMBROLIZUMAB KIT

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pembrolizumab + Trametinib

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
28514312

Sources:
JAX-CKB
PEMBROLIZUMAB KRAS

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
28039262 28451792

Sources:
JAX-CKB CIViC
PEMBROLIZUMAB TP53

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
28039262

Sources:
JAX-CKB

MyCancerGenome: MK-3475
- Version: 20-Jun-2017
Alternate Names:

MK-3475 Development Name

Drug Info:

Drug Class Therapeutic Antibodies

Publications:
MyCancerGenome: PEMBROLIZUMAB
- Version: 20-Jun-2017
Alternate Names:

KEYTRUDA Trade Name

Drug Info:

Drug Class Therapeutic Antibodies

FDA Approval Classical Hodgkin lymphoma, Melanoma, Non-small cell lung cancer (PD-L1+), Head and neck squamous cell carcinoma

Publications:

JAX-CKB: Pembrolizumab

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Zaretsky et al., 2016, Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma., N. Engl. J. Med.

Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)

Dong et al., 2017, Potential Predictive Value of TP53 and KRAS Mutation Status for Response to PD-1 Blockade Immunotherapy in Lung Adenocarcinoma., Clin. Cancer Res.

PharmGKB: pembrolizumab

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Carbognin et al., 2015, Differential Activity of Nivolumab, Pembrolizumab and MPDL3280A according to the Tumor Expression of Programmed Death-Ligand-1 (PD-L1): Sensitivity Analysis of Trials in Melanoma, Lung and Genitourinary Cancers., PLoS ONE

CIViC: PEMBROLIZUMAB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Hastings K et al., 2019, EGFR mutation subtypes and response to immune checkpoint blockade treatment in non-small-cell lung cancer., Ann Oncol

Passiglia et al., 2016, PD-L1 expression as predictive biomarker in patients with NSCLC: a pooled analysis., Oncotarget

Carbognin et al., 2015, Differential Activity of Nivolumab, Pembrolizumab and MPDL3280A according to the Tumor Expression of Programmed Death-Ligand-1 (PD-L1): Sensitivity Analysis of Trials in Melanoma, Lung and Genitourinary Cancers., PLoS ONE

TTD: MK-3475
- Version: 2020.06.01
Alternate Names:

D07DMY TTD Drug ID

Drug Info:

Publications:
TTD: Pembrolizumab
- Version: 2020.06.01
Alternate Names:

D08ANZ TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3137343
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Pembrolizumab
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
OncoKB: Pembrolizumab
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3137343
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
COSMIC: Pembrolizumab
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Programmed cell death protein 1 inhibitor
Direct Interaction	yes

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	decreased response
Approval Status	Clinical Study

Indication/Tumor Type	melanoma
Response Type	predicted – resistant
Approval Status	Clinical Study

combination therapy	Pembrolizumab + Trametinib
Indication/Tumor Type	melanoma
Response Type	no benefit

antibody (inhibitory)
antagonist (inhibitory)
inhibitor (inhibitory)

PEMBROLIZUMAB Drug Record

PEMBROLIZUMAB chembl:CHEMBL3137343 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28619999

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27159395 27683556 28188185

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27433843

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25891174 28472902 27718847 26918451 26086854

Sources: CIViC PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29736026

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28351930

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26822383

Sources: CIViC

Interaction Types & Directionality: antibody (inhibitory) antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Programmed cell death protein 1 inhibitor Direct Interaction yes

PMIDs: 25685857

Sources: MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29301960

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27433843 27903500

Sources: COSMIC CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28351930

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29773717

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type decreased response Approval Status Clinical Study

PMIDs: 27225694

Sources: JAX-CKB PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type predicted – resistant Approval Status Clinical Study

PMIDs: 27433843

Sources: JAX-CKB COSMIC CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Pembrolizumab + Trametinib Indication/Tumor Type melanoma Response Type no benefit

PMIDs: 28514312

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type sensitive Approval Status Clinical Study

PMIDs: 26645196 30742119

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type no benefit Approval Status Preclinical

PMIDs: 26645196

Sources: JAX-CKB PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type decreased response Approval Status Clinical Study

PMIDs: 27225694 31086949

Interaction Types & Directionality:

n/a

PMIDs:
28619999

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
27159395 27683556 28188185

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
27433843

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
25891174 28472902 27718847 26918451 26086854

Sources:
CIViC PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
29736026

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28351930

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
26822383

Sources:
CIViC

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Programmed cell death protein 1 inhibitor

Direct Interaction yes

PMIDs:
25685857

Sources:
MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality:

n/a

PMIDs:
29301960

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
27433843 27903500

Sources:
COSMIC CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28351930

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
29773717

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type decreased response

Approval Status Clinical Study

PMIDs:
27225694

Sources:
JAX-CKB PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type predicted – resistant

Approval Status Clinical Study

PMIDs:
27433843

Sources:
JAX-CKB COSMIC CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pembrolizumab + Trametinib

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
28514312

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Clinical Study

PMIDs:
26645196 30742119

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type no benefit

Approval Status Preclinical

PMIDs:
26645196

Sources:
JAX-CKB PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type decreased response

Approval Status Clinical Study

PMIDs:
27225694 31086949

Sources:
JAX-CKB CIViC PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pembrolizumab + Trametinib

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
28514312

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
28039262 28451792

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
28039262

Sources:
JAX-CKB

Alternate Names:

MK-3475 Development Name

Drug Info:

Drug Class Therapeutic Antibodies

Alternate Names:

KEYTRUDA Trade Name

Drug Info:

Drug Class Therapeutic Antibodies

FDA Approval Classical Hodgkin lymphoma, Melanoma, Non-small cell lung cancer (PD-L1+), Head and neck squamous cell carcinoma