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Identification
NamePembrolizumab
Accession NumberDB09037
TypeBiotech
GroupsApproved
DescriptionPembrolizumab is an antibody drug that targets the cell surface receptor programmed cell death protein 1 (PD-1) found on T cells. By preventing the binding of its ligands (PD-L1 and PD-L2), pembrolizumab induces an antitumor immune response. Upregulation of PD-1 ligands occurs in some tumors and signaling through this pathway can contribute to inhibition of active T-cell immune surveillance of tumors. Its use is indicated for the treatment of patients with unresectable or metastatic melanoma and disease progression following therapy with ipilimumab and, if BRAF V600 mutation positive, a BRAF inhibitor. Due to its success in clinical trials, pembrolizumab was approved early to allow quick patient access and was given breakthrough therapy and orphan drug designation. Pembrolizumab (as Keytruda) was approved by the U.S. Food and Drug Administration to treat advanced cases of the most common type of lung malignancy, non-small cell lung cancer (NSCLC) on Oct. 2, 2015.
Protein structureDb09037
Related Articles
Protein chemical formulaC6504H10004N1716O2036S46
Protein average weight146286.2902 Da
Sequences
>Heavy Chain Sequence
QVQLVQSGVEVKKPGASVKVSCKASGYTFTNYYMYWVRQAPGQGLEWMGGINPSNGGTNF
NEKFKNRVTLTTDSSTTTAYMELKSLQFDDTAVYYCARRDYRFDMGFDYWGQGTTVTVSS
ASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEG
NVFSCSVMHEALHNHYTQKSLSLSLGK
>Light Chain Sequence
EIVLTQSPATLSLSPGERATLSCRASKGVSTSGYSYLHWYQQKPGQAPRLLIYLASYLES
GVPARFSGSGSGTDFTLTISSLEPEDFAVYYCQHSRDLPLTFGGGTKVEIKRTVAAPSVF
IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS
STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
SynonymsNot Available
External Identifiers
  • lambrolizumab
  • MK 3475
  • MK-3475
  • MK3475
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
KeytrudaPowder, for solution50 mgIntravenousMerck Ltd.2015-06-01Not applicableCanada
KeytrudaInjection, solution25 mg/mLIntravenousMerck Sharp & Dohme Limited  2015-01-15Not applicableUs
KeytrudaSolution25 mgIntravenousMerck Ltd.Not applicableNot applicableCanada
KeytrudaInjection, powder, lyophilized, for solution50 mg/2mLIntravenousMerck Sharp & Dohme Limited  2014-09-04Not applicableUs
KeytrudaInjection, powder, for solution50 mgIntravenousMerck Sharp & Dohme Limited  2015-07-17Not applicableEu
KeytrudaInjection, solution, concentrate25 mg/mlIntravenousMerck Sharp & Dohme Limited  2015-07-17Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIDPT0O3T46P
CAS number1374853-91-4
Pharmacology
IndicationFor the treatment of patients with unresectable or metastatic melanoma and disease progression following therapy with ipilimumab and, if BRAF V600 mutation positive, a BRAF inhibitor. It is also for the treatment of patients with metastatic NSCLC (non-small cell lung cancer) whose tumors express PD-L1 (as determined by an approved test) and who have disease progression on or after platinum-containing chemotherapy.
Structured Indications
Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentCancer of the Esophagus / Esophageal Cancers / Neoplasms, Esophageal1
0RecruitingTreatmentEndometrial Cancers / Endometrial Carcinoma / Neoplasms, Endometrial1
0RecruitingTreatmentMalignant Melanoma, Metastatic1
1Active Not RecruitingTreatmentAdvanced Solid Tumors1
1Active Not RecruitingTreatmentNeuroblastomas1
1Active Not RecruitingTreatmentRenal Cell Carcinoma (RCC)1
1Not Yet RecruitingNot AvailableInvasive Bladder Cancer1
1Not Yet RecruitingNot AvailableThoracic Tumours1
1Not Yet RecruitingTreatmentCancer, Breast1
1Not Yet RecruitingTreatmentGastrointestinal Cancer Metastatic1
1Not Yet RecruitingTreatmentMalignant Pleural Mesothelioma (MPM)1
1Not Yet RecruitingTreatmentMelanoma1
1Not Yet RecruitingTreatmentPancreatic Cancers1
1Not Yet RecruitingTreatmentPleural Mesotheliomas1
1Not Yet RecruitingTreatmentStage IV Skin Melanoma1
1Not Yet RecruitingTreatmentTumors, Solid1
1RecruitingTreatmentALK-positive Advanced NSCLC1
1RecruitingTreatmentAdenocarcinomas of the Gastroesophageal Junction / Biliary Tract Cancer / Gastric Adenocarcinoma / Non-Small-Cell Lung Carcinoma (NSCLC) / Transitional Cell Carcinoma1
1RecruitingTreatmentAdvanced Solid Tumors (Part A/B/C/D) / Non-small Cell Lung Cancer (NSCLC) and Melanoma (Part E)1
1RecruitingTreatmentAdvanced Solid Tumors / Endometrial Cancers / Head and Neck Squamous Cell Carcinoma (HNSCC) / Melanoma / Microsatellite Unstable (MSI) Colorectal Cancer / MMR-deficient Tumors / Non-Small-Cell Lung Carcinoma (NSCLC) / Renal Cell Carcinoma (RCC) / Transitional Cell Carcinoma of the Genitourinary Tract / Triple Negative Breast Cancer (TNBC)1
1RecruitingTreatmentAdvanced or Unresectable Melanoma Progressing After PD1 Blockade1
1RecruitingTreatmentBladder Cancers2
1RecruitingTreatmentBone Neoplasms / Neoplasms, Breast1
1RecruitingTreatmentCancer, Breast / Cancer, Ovarian / Carcinoma, Colorectal / Carcinoma, Pancreatic / Melanoma / Non-Small Cell Lung Carcinoma (NSCLC) / Prostate Cancers / Renal Cell Carcinoma (RCC) / Tumors, Solid1
1RecruitingTreatmentCancers1
1RecruitingTreatmentColorectal Cancers1
1RecruitingTreatmentHead and Neck Cancers / Hypopharynx Cancer / Laryngeal Cancer / Larynx Cancer / Oral Cavity Cancer / Oropharynx Cancers / Squamous Cell Carcinoma (SCC)1
1RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC) / Metastatic Renal Cell Cancer / Recurrent Head and Neck Carcinoma / Recurrent Lung Carcinoma / Recurrent Renal Cell Carcinoma / Recurrent Skin Carcinoma / Stage III Renal Cell Cancer / Stage IV Lung Cancer / Stage IV Skin Melanoma1
1RecruitingTreatmentLung Cancers1
1RecruitingTreatmentMalignant Gliomas1
1RecruitingTreatmentMalignant Melanoma / Melanoma / Melanoma Recurrent1
1RecruitingTreatmentMelanoma4
1RecruitingTreatmentMetastatic Cancers1
1RecruitingTreatmentMetastatic Urothelial Carcinoma of the Renal Pelvis and Ureter / Recurrent Bladder Carcinoma / Recurrent Urothelial Carcinoma of the Renal Pelvis and Ureter / Regional Urothelial Carcinoma of the Renal Pelvis and Ureter / Stage III Bladder Urothelial Carcinoma / Stage III Urethral Cancer / Stage IV Bladder Urothelial Carcinoma / Stage IV Urethral Cancer / Urethral Urothelial Carcinoma1
1RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
1RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
1RecruitingTreatmentPancreatic Adenocarcinoma1
1RecruitingTreatmentRectal Cancers1
1RecruitingTreatmentRenal Cell Cancer1
1RecruitingTreatmentRenal Cell Carcinoma (RCC)1
1RecruitingTreatmentStage III Melanoma / Stage IV Melanoma1
1RecruitingTreatmentStage IV Melanoma1
1RecruitingTreatmentStage IV Non-Small Cell Lung Cancer1
1, 2Active Not RecruitingTreatmentAdvanced GI Cancer1
1, 2Active Not RecruitingTreatmentBladder Cancers / Carcinoma, Urothelial1
1, 2Enrolling by InvitationTreatmentGlioblastomas1
1, 2Not Yet RecruitingTreatmentAdvanced Solid Tumors1
1, 2Not Yet RecruitingTreatmentMelanoma2
1, 2Not Yet RecruitingTreatmentRelapsed Acute Myeloid Leukemia1
1, 2Not Yet RecruitingTreatmentRenal Cell Carcinoma (RCC) / Urinary Bladder Neoplasms1
1, 2Not Yet RecruitingTreatmentTumors, Solid1
1, 2RecruitingTreatmentAdenocarcinoma of the Endometrium / Carcinoma, Squamous Cell of Head and Neck / Lymphoma, Large B-Cell, Diffuse / Malignant Solid Tumours / Neoplasms, Ovarian / Non-Small-Cell Lung Carcinoma (NSCLC) / Renal Cell Carcinoma (RCC) / Transitional Cell Carcinoma of Genitourinary Tract / Triple Negative Breast Cancer (TNBC)1
1, 2RecruitingTreatmentAdvanced Liver Cancer / Malignant Neoplasms of Digestive Organs1
1, 2RecruitingTreatmentCD19+ Diffuse Large B-cell Lymphomas / Follicular Lymphoma (FL) / Mantle Cell Lymphomas1
1, 2RecruitingTreatmentCancer, Advanced / Cancer, Breast / Colorectal Cancers / Esophageal Cancers / Gastric Cancers1
1, 2RecruitingTreatmentCancer, Advanced / Cancer, Breast / Ovarian / Pancreatic Cancers / Sarcomas / Small Cell Lung Cancer (SCLC)1
1, 2RecruitingTreatmentCancer, Breast1
1, 2RecruitingTreatmentCancers2
1, 2RecruitingTreatmentCancers / Prostate Cancers1
1, 2RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL)1
1, 2RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL) / Lymphoma, Hodgkins / Multiple Myeloma (MM) / Myelofibrosis / Non-Hodgkin's Lymphoma (NHL) / Richter's Syndrome / Waldenstrom's Macroglobulinemia (WM)1
1, 2RecruitingTreatmentClear Cell Renal Carcinoma1
1, 2RecruitingTreatmentFollicular Lymphoma (Marginal Zone B Cell Lymphoma)1
1, 2RecruitingTreatmentGastric Cancers1
1, 2RecruitingTreatmentHead and Neck Carcinoma1
1, 2RecruitingTreatmentLung Cancers1
1, 2RecruitingTreatmentLung Cancers / Melanoma1
1, 2RecruitingTreatmentLung Cancers / Non-Small-Cell Lung Carcinoma (NSCLC)1
1, 2RecruitingTreatmentMelanoma2
1, 2RecruitingTreatmentMelanoma / Non-Small-Cell Lung Carcinoma (NSCLC)1
1, 2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1, 2RecruitingTreatmentMetastatic Melanoma / Stage III Melanoma / Stage IV Melanoma1
1, 2RecruitingTreatmentMultiple Myeloma (MM)1
1, 2RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
1, 2RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)2
1, 2RecruitingTreatmentPancreatic Cancers1
1, 2RecruitingTreatmentTumors1
1, 2WithdrawnTreatmentAdvanced Triple Negative Breast Cancer / Malignant Melanoma / Mesothelioma / Non Small Cell Lung Cancer (NSCLC) / Small Cell Lung Cancer (SCLC) / Urothelial Cancer1
1, 2WithdrawnTreatmentLymphoma NOS / Lymphoma, Hodgkins / Non-Hodgkin's Lymphoma (NHL)1
2Active Not RecruitingTreatmentColorectal Cancers1
2Active Not RecruitingTreatmentGlioblastomas1
2Active Not RecruitingTreatmentMetastatic Urothelial Carcinoma1
2Active Not RecruitingTreatmentNK-Cell Lymphoma / T-Cell Lymphomas1
2Active Not RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
2Active Not RecruitingTreatmentSarcoma, Bone / Soft Tissue Sarcoma (STS)1
2Active Not RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2CompletedTreatmentMalignant Melanoma1
2Not Yet RecruitingDiagnosticCancers of the Head and Neck / Esophageal Squamous Cell Carcinomas / Non-Small-Cell Lung Carcinoma (NSCLC) / Transitional Cell Carcinoma / Urinary Bladder Neoplasms1
2Not Yet RecruitingTreatmentAcute Myeloid Leukaemias (AML)1
2Not Yet RecruitingTreatmentAdenocarcinoma Esophagus / Esophageal Cancers / Squamous Cell Esophagus Cancer1
2Not Yet RecruitingTreatmentAlveolar Soft Part Sarcoma (ASPS) / Soft Tissue Sarcoma (STS)1
2Not Yet RecruitingTreatmentAnaplastic Meningioma / Atypical Meningioma / Hemangiopericytoma1
2Not Yet RecruitingTreatmentAnaplastic Thyroid Cancers1
2Not Yet RecruitingTreatmentBiliary Cancer1
2Not Yet RecruitingTreatmentBladder Cancers2
2Not Yet RecruitingTreatmentBreast - Female / Male Breast Cancer1
2Not Yet RecruitingTreatmentCancer, Ovarian / Ovarian Cancer Metastatic1
2Not Yet RecruitingTreatmentCentral Nervous System Neoplasms / Neoplasms, Germ Cell and Embryonal / Neoplasms, Ovarian / Neoplasms, Thyroid / Neuroendocrine Carcinomas / Sarcomas1
2Not Yet RecruitingTreatmentCervical Cancers1
2Not Yet RecruitingTreatmentEndometrial Adenocarcinomas / Endometrial Cancers1
2Not Yet RecruitingTreatmentGlioblastomas1
2Not Yet RecruitingTreatmentHead and Neck Cancers1
2Not Yet RecruitingTreatmentHead and Neck Cancers / Squamous Cell Carcinoma of the Head and Neck (SCCHN)1
2Not Yet RecruitingTreatmentHistory of Invasive Oral Cancer / Intra-epithelial Neoplasias / Oral Pre-malignant Lesion(s)1
2Not Yet RecruitingTreatmentInflammatory carcinoma of the breast / Malignant Neoplasm of Breast1
2Not Yet RecruitingTreatmentKidney Cancer1
2Not Yet RecruitingTreatmentMalignant Neoplasms of Digestive Organs / Pancreatic Cancer Metastatic1
2Not Yet RecruitingTreatmentMalignant Peripheral Nerve Sheath Tumour (MPNST)1
2Not Yet RecruitingTreatmentMelanoma1
2Not Yet RecruitingTreatmentMetastatic Colorectal Cancers1
2Not Yet RecruitingTreatmentMetastatic Malignant Melanoma1
2Not Yet RecruitingTreatmentMetastatic Melanoma1
2Not Yet RecruitingTreatmentMetastatic Non Small Cell Lung Cancer1
2Not Yet RecruitingTreatmentMetastatic Squamous Non-small Cell Lung Cancer1
2Not Yet RecruitingTreatmentMetastatic Uveal Melanoma1
2Not Yet RecruitingTreatmentMultiple Myeloma (MM)1
2Not Yet RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
2Not Yet RecruitingTreatmentOsteosarcomas1
2Not Yet RecruitingTreatmentProstatic Neoplasms1
2Not Yet RecruitingTreatmentRectal Cancers / Rectal Neoplasms1
2Not Yet RecruitingTreatmentRecurrent Respiratory Papillomatosis1
2Not Yet RecruitingTreatmentSmall Cell Lung Cancer (SCLC)2
2Not Yet RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2Not Yet RecruitingTreatmentStage IV Non-Small Cell Lung Cancer1
2Not Yet RecruitingTreatmentStage IV Renal Cell Cancer AJCC V71
2Not Yet RecruitingTreatmentThymic Epithelial Tumors1
2RecruitingTreatmentAcute Myeloid Leukemia, in Relapse1
2RecruitingTreatmentAdrenocortical Carcinoma1
2RecruitingTreatmentAdvanced Cancers1
2RecruitingTreatmentAdvanced Melanoma1
2RecruitingTreatmentAdvanced Solid Tumors / Epithelial Ovarian Cancer / Malignant Melanoma / Squamous Cell Cancer of Head and Neck / Triple Negative Breast Cancer (TNBC)1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentAnal Cancer1
2RecruitingTreatmentBladder Cancers / Urothelial Cancer1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentCancer, Breast / Metastatic Triple Negative1
2RecruitingTreatmentCancer, Breast / Neoplasms, Breast / Tumors, Breast1
2RecruitingTreatmentCancer, Breast / Non Small Cell Lung Cancer (NSCLC)1
2RecruitingTreatmentCancer, Ovarian3
2RecruitingTreatmentCancers / Glioblastomas / Tumor, Brain1
2RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck / Recurrent Head and Neck Cancer1
2RecruitingTreatmentDiffuse Large B Cell Lymphoma (DLBCL) / Lymphoma, Hodgkins1
2RecruitingTreatmentEsophageal Cancers / Gastric Cancers1
2RecruitingTreatmentGastric Adenocarcinoma / Gastroesophageal Junction Adenocarcinoma1
2RecruitingTreatmentGenital Neoplasms, Female / Genital Neoplasms, Male / Germ Cell Neoplasms / Mediastinal Neoplasms / Neoplasms, Ovarian / Non Seminomatous Germ Cell Tumors / Testicular Neoplasms1
2RecruitingTreatmentHead and Neck Cancers1
2RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
2RecruitingTreatmentHepatocellular Carcinomas1
2RecruitingTreatmentLymphoma NOS1
2RecruitingTreatmentLymphoma, T-Cell, Peripheral1
2RecruitingTreatmentMSI Negative Colorectal Cancer / MSI Positive Colorectal Cancer / MSI Positive Non-Colorectal Cancers1
2RecruitingTreatmentMelanoma4
2RecruitingTreatmentMelanoma / Metastases, Brain / Non-Small-Cell Lung Carcinoma (NSCLC)1
2RecruitingTreatmentMelanoma / Metastatic Melanoma / Stage III Melanoma / Stage IV Melanoma / Unresectable Malignant Neoplasm1
2RecruitingTreatmentMesothelioma1
2RecruitingTreatmentMetastases, Brain1
2RecruitingTreatmentMetastatic Cholangiocarcinoma / Metastatic Colorectal Cancers / Metastatic Gastric Cancers / Metastatic Hepatocellular Carcinoma / Pancreatic Cancer Metastatic1
2RecruitingTreatmentMetastatic Colorectal Cancers2
2RecruitingTreatmentMetastatic Melanoma2
2RecruitingTreatmentMetastatic Melanoma / Stage IV Melanoma1
2RecruitingTreatmentMultiple Myeloma (MM)2
2RecruitingTreatmentNeoplasms, Breast1
2RecruitingTreatmentNon Small Cell Lung Cancer (NSCLC)1
2RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)3
2RecruitingTreatmentPancreatic Cancers1
2RecruitingTreatmentSarcomas1
2RecruitingTreatmentThymic Carcinoma1
2SuspendedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
3Active Not RecruitingTreatmentNon-Small Cell Lung Carcinoma (NSCLC) / Non-Small-Cell Lung Carcinoma (NSCLC)1
3RecruitingTreatmentMelanoma1
3RecruitingTreatmentOcular Melanoma1
Not AvailableNot Yet RecruitingTreatmentSmoldering Multiple Myeloma (SMM)1
Not AvailableRecruitingNot AvailableMelanoma1
Not AvailableRecruitingTreatmentBrain Cancer1
Not AvailableRecruitingTreatmentGliomas / Recurrent Malignant Gliomas1
PharmacodynamicsNot Available
Mechanism of actionPembrolizumab is an antibody drug that targets the cell surface receptor programmed cell death protein 1 (PD-1) found on T cells. By preventing the binding of its ligands (PD-L1 and PD-L2), pembrolizumab induces an antitumor immune response. Upregulation of PD-1 ligands is a mechanism for tumours to evade antitumor immune response; when PD-1 binds its ligand, the T cell receives an inhibitory signal leading to T cell anergy and blockade of anti tumour immune response. Instead of directly targeting tumor tissue to induce tumor cell death, pembrolizumab acts as a checkpoint inhibitor to stimulate immune responses to eliminate cancer cells.
TargetKindPharmacological actionActionsOrganismUniProt ID
Programmed cell death protein 1Proteinyes
antagonist
antibody
HumanQ15116 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeElimination half life is 28 days.
Clearance

0.22 L/day

ToxicitySince therapy with pembrolizumab induces tumour regression by stimulation of immune responses, side effects may be caused by activating potentially self-reactive T cells. This includes immune-mediated pneumonitis, colitis, hypophysitis, nephritis and renal failure, hyperthyroidism and hypothyroidism, and hepatitis. Other adverse events such as myasthenic syndrome, optic neuritis, uveitis, arthritis, pancreatitis, partial seizures, and rhabdomnyolysis were reported to occur in less than 1% of patients during clinical trials. Female patients are advised to use highly effective contraception during and for 4 months following treatment due to the risk of fetal harm.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Pembrolizumab.Approved
ALT-110The therapeutic efficacy of ALT-110 can be decreased when used in combination with Pembrolizumab.Investigational
AnvirzelAnvirzel may decrease the cardiotoxic activities of Pembrolizumab.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Pembrolizumab is combined with Belimumab.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Pembrolizumab.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Pembrolizumab.Approved
CDX-110The therapeutic efficacy of CDX-110 can be decreased when used in combination with Pembrolizumab.Investigational
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Pembrolizumab.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Pembrolizumab.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Pembrolizumab.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Pembrolizumab.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Pembrolizumab.Approved, Investigational
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Pembrolizumab.Investigational
GI-5005The therapeutic efficacy of GI-5005 can be decreased when used in combination with Pembrolizumab.Investigational
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Pembrolizumab.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Pembrolizumab.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Pembrolizumab.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Pembrolizumab.Approved, Vet Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Pembrolizumab.Approved
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Pembrolizumab.Investigational
TG4010The therapeutic efficacy of TG4010 can be decreased when used in combination with Pembrolizumab.Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Pembrolizumab.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Robert C, Ribas A, Wolchok JD, Hodi FS, Hamid O, Kefford R, Weber JS, Joshua AM, Hwu WJ, Gangadhar TC, Patnaik A, Dronca R, Zarour H, Joseph RW, Boasberg P, Chmielowski B, Mateus C, Postow MA, Gergich K, Elassaiss-Schaap J, Li XN, Iannone R, Ebbinghaus SW, Kang SP, Daud A: Anti-programmed-death-receptor-1 treatment with pembrolizumab in ipilimumab-refractory advanced melanoma: a randomised dose-comparison cohort of a phase 1 trial. Lancet. 2014 Sep 20;384(9948):1109-17. doi: 10.1016/S0140-6736(14)60958-2. Epub 2014 Jul 15. [PubMed:25034862 ]
  2. Hamid O, Robert C, Daud A, Hodi FS, Hwu WJ, Kefford R, Wolchok JD, Hersey P, Joseph RW, Weber JS, Dronca R, Gangadhar TC, Patnaik A, Zarour H, Joshua AM, Gergich K, Elassaiss-Schaap J, Algazi A, Mateus C, Boasberg P, Tumeh PC, Chmielowski B, Ebbinghaus SW, Li XN, Kang SP, Ribas A: Safety and tumor responses with lambrolizumab (anti-PD-1) in melanoma. N Engl J Med. 2013 Jul 11;369(2):134-44. doi: 10.1056/NEJMoa1305133. Epub 2013 Jun 2. [PubMed:23724846 ]
  3. Poole RM: Pembrolizumab: first global approval. Drugs. 2014 Oct;74(16):1973-81. doi: 10.1007/s40265-014-0314-5. [PubMed:25331768 ]
External Links
ATC CodesL01XC18
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (589 KB)
MSDSDownload (134 KB)
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, powder, for solutionIntravenous50 mg
Injection, powder, lyophilized, for solutionIntravenous50 mg/2mL
Injection, solutionIntravenous25 mg/mL
Injection, solution, concentrateIntravenous25 mg/ml
Powder, for solutionIntravenous50 mg
SolutionIntravenous25 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US2012135408 No2012-03-292032-03-29Us
Properties
StateSolid
Experimental PropertiesNot Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonistantibody
General Function:
Signal transducer activity
Specific Function:
Inhibitory cell surface receptor involved in the regulation of T-cell function during immunity and tolerance. Upon ligand binding, inhibits T-cell effector functions in an antigen-specific manner. Possible cell death inducer, in association with other factors.
Gene Name:
PDCD1
Uniprot ID:
Q15116
Molecular Weight:
31646.635 Da
References
  1. McDermott J, Jimeno A: Pembrolizumab: PD-1 inhibition as a therapeutic strategy in cancer. Drugs Today (Barc). 2015 Jan;51(1):7-20. doi: 10.1358/dot.2015.51.1.2250387. [PubMed:25685857 ]
Comments
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Drug created on March 30, 2015 16:49 / Updated on August 17, 2016 12:24