pembrolizumab Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
humanized origin 4924 1374853-91-4

Description:

MoleculeDescription

Synonyms:

  • pembrolizumab
  • keytruda
  • lambrolizumab
  • SCH-900475
  • MK-3475
  • pembrolizumab (genetical recombination)
A humanized monoclonal immunoglobulin (Ig) G4 antibody directed against human cell surface receptor PD-1 (programmed death-1 or programmed cell death-1) with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, pembrolizumab binds to PD-1, an inhibitory signaling receptor expressed on the surface of activated T cells, and blocks the binding to and activation of PD-1 by its ligands, which results in the activation of T-cell-mediated immune responses against tumor cells. The ligands for PD-1 include programmed cell death ligand 1 (PD-L1), overexpressed on certain cancer cells, and programmed cell death ligand 2 (PD-L2), which is primarily expressed on APCs. Activated PD-1 negatively regulates T-cell activation and plays a key role in in tumor evasion from host immunity.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 28, 2016 PMDA MSD K.K.
July 17, 2015 EMA Merck Sharp & Dohme Limited
Sept. 4, 2014 FDA MERCK SHARP DOHME

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 1916.13 15.97 803 20570 70738 53256955
Product use in unapproved indication 635.16 15.97 450 20923 111839 53215854
Immune-mediated adverse reaction 495.24 15.97 86 21287 164 53327529
Immune-mediated lung disease 283.10 15.97 56 21317 273 53327420
Pneumonitis 280.53 15.97 167 21206 30721 53296972
Immune-mediated hepatitis 239.73 15.97 58 21315 802 53326891
Immune-mediated enterocolitis 218.19 15.97 55 21318 909 53326784
Colitis 216.94 15.97 159 21214 41393 53286300
Hypothyroidism 206.40 15.97 146 21227 35961 53291732
Tumour pseudoprogression 192.48 15.97 38 21335 183 53327510
Tubulointerstitial nephritis 181.17 15.97 101 21272 16403 53311290
Hepatitis 179.84 15.97 131 21242 33763 53293930
Myocarditis 173.21 15.97 79 21294 8389 53319304
Hypophysitis 149.95 15.97 46 21327 1601 53326092
Immune-mediated hypothyroidism 148.16 15.97 24 21349 22 53327671
Death 146.54 15.97 391 20982 356841 52970852
Autoimmune colitis 130.84 15.97 32 21341 464 53327229
Immune-mediated hepatic disorder 130.27 15.97 24 21349 73 53327620
Type 1 diabetes mellitus 125.47 15.97 48 21325 3275 53324418
Thyroiditis 124.06 15.97 41 21332 1821 53325872
Immune-mediated myocarditis 117.73 15.97 21 21352 50 53327643
Autoimmune hypothyroidism 112.65 15.97 22 21351 99 53327594
Vitiligo 109.96 15.97 34 21339 1215 53326478
Off label use 108.67 15.97 424 20949 471788 52855905
Lichenoid keratosis 107.78 15.97 35 21338 1470 53326223
Adverse event 106.27 15.97 105 21268 40956 53286737
Adrenal insufficiency 103.79 15.97 68 21305 14761 53312932
Fulminant type 1 diabetes mellitus 96.50 15.97 23 21350 297 53327396
Immune-mediated thyroiditis 95.75 15.97 17 21356 39 53327654
Immune-mediated dermatitis 91.96 15.97 15 21358 15 53327678
Hyperthyroidism 91.62 15.97 60 21313 13013 53314680
Adrenocorticotropic hormone deficiency 89.45 15.97 21 21352 253 53327440
Product use issue 89.07 15.97 182 21191 139402 53188291
Autoimmune hepatitis 88.80 15.97 50 21323 8268 53319425
Nephritis 87.53 15.97 33 21340 2162 53325531
Therapy partial responder 85.25 15.97 44 21329 6119 53321574
Immune-mediated arthritis 83.96 15.97 14 21359 18 53327675
Immune-mediated pancreatitis 80.37 15.97 15 21358 50 53327643
Autoimmune thyroiditis 77.64 15.97 34 21339 3277 53324416
Myasthenia gravis 75.30 15.97 35 21338 3878 53323815
Myositis 72.12 15.97 44 21329 8439 53319254
Drug hypersensitivity 66.15 15.97 13 21360 265229 53062464
Metastatic malignant melanoma 64.80 15.97 24 21349 1496 53326197
Inappropriate schedule of product administration 61.78 15.97 109 21264 74769 53252924
Immune-mediated gastritis 61.41 15.97 9 21364 0 53327693
Rheumatoid arthritis 56.12 15.97 28 21345 314503 53013190
Drug ineffective 55.71 15.97 157 21216 817088 52510605
Cholestasis 52.36 15.97 61 21312 28634 53299059
Diabetic ketoacidosis 51.63 15.97 51 21322 19864 53307829
Fall 51.46 15.97 41 21332 358399 52969294
Neoplasm progression 50.30 15.97 61 21312 29858 53297835
Renal tubular necrosis 49.18 15.97 39 21334 11380 53316313
Hepatic function abnormal 49.10 15.97 67 21306 36832 53290861
Immune-mediated nephritis 48.94 15.97 10 21363 59 53327634
Autoimmune arthritis 48.22 15.97 9 21364 30 53327663
Immune-mediated endocrinopathy 47.76 15.97 7 21366 0 53327693
Secondary adrenocortical insufficiency 46.76 15.97 18 21355 1248 53326445
Nasopharyngitis 46.73 15.97 10 21363 192285 53135408
Joint swelling 46.39 15.97 18 21355 234620 53093073
Immune-mediated hyperthyroidism 46.14 15.97 8 21365 15 53327678
Uveitis 46.02 15.97 35 21338 9609 53318084
Metastases to central nervous system 45.24 15.97 38 21335 12019 53315674
Drug effective for unapproved indication 44.87 15.97 20 21353 2010 53325683
Lichen planus 44.46 15.97 20 21353 2054 53325639
Hypopituitarism 44.32 15.97 16 21357 927 53326766
Hepatotoxicity 43.89 15.97 55 21318 27825 53299868
Interstitial lung disease 42.85 15.97 81 21292 58541 53269152
Lymphocytic hypophysitis 42.80 15.97 11 21362 197 53327496
Polymyalgia rheumatica 41.95 15.97 21 21352 2738 53324955
Pemphigoid 41.34 15.97 28 21345 6416 53321277
Dizziness 40.49 15.97 54 21319 372205 52955488
Sinusitis 40.47 15.97 9 21364 168555 53159138
Autoimmune pancreatitis 39.83 15.97 11 21362 262 53327431
Hepatocellular injury 39.22 15.97 54 21319 29932 53297761
Blood thyroid stimulating hormone increased 38.95 15.97 27 21346 6425 53321268
Abdominal discomfort 38.91 15.97 20 21353 221042 53106651
Subacute cutaneous lupus erythematosus 38.90 15.97 19 21354 2349 53325344
Exposure during pregnancy 38.63 15.97 3 21370 124857 53202836
Immune-mediated myositis 38.28 15.97 15 21358 1091 53326602
Pyrexia 37.57 15.97 283 21090 402910 52924783
Autoimmune nephritis 37.22 15.97 11 21362 336 53327357
Drug intolerance 37.06 15.97 18 21355 205475 53122218
Hypersensitivity 34.28 15.97 21 21352 210644 53117049
Skin toxicity 34.20 15.97 21 21352 4072 53323621
Hepatitis toxic 33.84 15.97 19 21354 3122 53324571
Tumour hyperprogression 33.80 15.97 8 21365 100 53327593
Eosinophilic fasciitis 33.51 15.97 8 21365 104 53327589
Condition aggravated 33.42 15.97 42 21331 297092 53030601
Transaminases increased 33.16 15.97 50 21323 30082 53297611
Headache 32.94 15.97 108 21265 536713 52790980
Autoimmune myocarditis 32.86 15.97 7 21366 52 53327641
Immune-mediated neuropathy 31.77 15.97 5 21368 3 53327690
Drug interaction 31.54 15.97 25 21348 219304 53108389
Myasthenic syndrome 31.48 15.97 9 21364 244 53327449
Swelling 31.16 15.97 19 21354 191086 53136607
Eastern Cooperative Oncology Group performance status worsened 30.67 15.97 11 21362 625 53327068
Neurofibrosarcoma 30.58 15.97 8 21365 154 53327539
Cholangitis sclerosing 30.44 15.97 13 21360 1178 53326515
Amputation stump pain 30.04 15.97 6 21367 31 53327662
Rash maculo-papular 29.44 15.97 47 21326 29702 53297991
Toxic epidermal necrolysis 28.69 15.97 41 21332 23509 53304184
Immune-mediated hypophysitis 28.30 15.97 5 21368 11 53327682
Polyglandular autoimmune syndrome type II 28.23 15.97 6 21367 44 53327649
Acute kidney injury 28.15 15.97 186 21187 253682 53074011
Tumour associated fever 27.91 15.97 8 21365 219 53327474
Therapeutic product effect decreased 27.67 15.97 8 21365 125647 53202046
Autoimmune dermatitis 27.56 15.97 6 21367 50 53327643
Maternal exposure during pregnancy 27.50 15.97 14 21359 155625 53172068
Overdose 27.42 15.97 5 21368 107731 53219962
Autoimmune endocrine disorder 27.29 15.97 4 21369 0 53327693
Glossodynia 26.98 15.97 4 21369 100287 53227406
Glucocorticoid deficiency 26.96 15.97 8 21365 248 53327445
Pain 26.86 15.97 133 21240 588265 52739428
Alopecia 26.53 15.97 33 21340 234550 53093143
Immune-mediated encephalitis 26.14 15.97 6 21367 65 53327628
Arthropathy 26.09 15.97 12 21361 141441 53186252
Immune-mediated cholangitis 26.08 15.97 5 21368 20 53327673
Thyroid hormones increased 25.84 15.97 8 21365 287 53327406
Oligodipsia 25.34 15.97 5 21368 24 53327669
Metastases to adrenals 25.31 15.97 10 21363 743 53326950
Cytokine release syndrome 25.23 15.97 23 21350 8106 53319587
Neutropenia 25.05 15.97 128 21245 159057 53168636
Bronchitis 24.86 15.97 7 21366 111892 53215801
Rash pruritic 24.79 15.97 59 21314 49951 53277742
Decreased appetite 24.73 15.97 159 21214 214815 53112878
Duodenitis 24.36 15.97 16 21357 3483 53324210
Cutaneous sarcoidosis 23.89 15.97 8 21365 370 53327323
Asthma 23.88 15.97 7 21366 108965 53218728
Aspartate aminotransferase increased 23.84 15.97 81 21292 83948 53243745
Neonatal respiratory depression 23.58 15.97 6 21367 103 53327590
Synovitis 23.51 15.97 7 21366 107886 53219807
Pulmonary embolism 23.12 15.97 99 21274 114343 53213350
Discomfort 23.10 15.97 5 21368 95467 53232226
Pericardial effusion 22.85 15.97 40 21333 27238 53300455
Liver disorder 22.81 15.97 50 21323 40105 53287588
Diarrhoea 22.78 15.97 364 21009 625182 52702511
Radiation pneumonitis 22.76 15.97 11 21362 1329 53326364
BRAF V600E mutation positive 22.24 15.97 5 21368 49 53327644
Thyroid disorder 21.88 15.97 27 21346 13446 53314247
Wound 21.74 15.97 5 21368 91552 53236141
Toxicity to various agents 21.72 15.97 34 21339 219564 53108129
Thrombocytopenia 21.43 15.97 111 21262 138616 53189077
Pleural effusion 21.38 15.97 81 21292 88498 53239195
Antinuclear antibody 21.35 15.97 8 21365 515 53327178
Cholangitis 21.32 15.97 17 21356 4996 53322697
Autoimmune uveitis 21.07 15.97 4 21369 15 53327678
Meningitis aseptic 21.01 15.97 16 21357 4399 53323294
Adenocarcinoma 21.00 15.97 13 21360 2556 53325137
Silent thyroiditis 20.74 15.97 5 21368 68 53327625
Loss of consciousness 20.58 15.97 10 21363 114202 53213491
Rash morbilliform 20.51 15.97 14 21359 3249 53324444
Parathyroid tumour malignant 20.48 15.97 4 21369 18 53327675
Vesical fistula 20.47 15.97 5 21368 72 53327621
Depression 20.43 15.97 26 21347 183026 53144667
Pulmonary sarcoidosis 20.28 15.97 9 21364 895 53326798
Encephalitis 19.95 15.97 20 21353 7924 53319769
Weight increased 19.92 15.97 32 21341 204535 53123158
Palmar-plantar erythrodysaesthesia syndrome 19.83 15.97 33 21340 21573 53306120
Serous retinal detachment 19.83 15.97 6 21367 199 53327494
Alanine aminotransferase increased 19.78 15.97 83 21290 95012 53232681
Tumour pain 19.55 15.97 10 21363 1364 53326329
Contusion 19.49 15.97 10 21363 110722 53216971
Melanoma recurrent 19.33 15.97 5 21368 92 53327601
Stevens-Johnson syndrome 19.25 15.97 35 21338 24547 53303146
Neuropathy peripheral 19.12 15.97 87 21286 103100 53224593
No adverse event 19.11 15.97 46 21327 39219 53288474
EGFR gene mutation 18.83 15.97 6 21367 237 53327456
Blood pressure abnormal 18.72 15.97 25 21348 13458 53314235
Loss of personal independence in daily activities 18.29 15.97 3 21370 69812 53257881
Blood corticotrophin decreased 18.20 15.97 6 21367 264 53327429
Enterocolitis 18.16 15.97 18 21355 7034 53320659
Posterior reversible encephalopathy syndrome 18.04 15.97 27 21346 16133 53311560
Migraine 17.92 15.97 5 21368 80412 53247281
Sarcoidosis 17.89 15.97 16 21357 5498 53322195
Urogenital fistula 17.80 15.97 5 21368 127 53327566
Ototoxicity 17.78 15.97 9 21364 1201 53326492
Cholecystitis 17.78 15.97 26 21347 15220 53312473
Dermatitis bullous 17.71 15.97 19 21354 8144 53319549
Exposure via body fluid 17.71 15.97 7 21366 521 53327172
Peripheral swelling 17.58 15.97 35 21338 206073 53121620
Immune-mediated encephalopathy 17.53 15.97 3 21370 5 53327688
Insomnia 17.53 15.97 30 21343 187042 53140651
Achromotrichia acquired 17.18 15.97 3 21370 6 53327687
Diabetes mellitus 17.11 15.97 54 21319 53845 53273848
Pneumonia moraxella 16.98 15.97 4 21369 49 53327644
Nephropathy toxic 16.94 15.97 19 21354 8553 53319140
Cardiomyopathy 16.90 15.97 27 21346 17061 53310632
Infection 16.70 15.97 27 21346 172178 53155515
B-cell aplasia 16.69 15.97 4 21369 53 53327640
Vital functions abnormal 16.63 15.97 6 21367 347 53327346
Roseolovirus test positive 16.62 15.97 4 21369 54 53327639
Autoimmune thyroid disorder 16.57 15.97 3 21370 8 53327685
Musculoskeletal stiffness 16.57 15.97 15 21358 123353 53204340
Malignant melanoma 16.50 15.97 21 21352 10781 53316912
Radiation associated pain 16.29 15.97 4 21369 59 53327634
Muscle spasms 16.26 15.97 18 21355 134777 53192916
Influenza 16.22 15.97 9 21364 95370 53232323
Giant cell arteritis 16.19 15.97 10 21363 1959 53325734

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 2251.50 14.14 1194 28659 77302 32406371
Immune-mediated adverse reaction 877.25 14.14 177 29676 325 32483348
Product use in unapproved indication 489.70 14.14 495 29358 86709 32396964
Pneumonitis 460.80 14.14 307 29546 29827 32453846
Interstitial lung disease 337.35 14.14 354 29499 64647 32419026
Immune-mediated lung disease 315.87 14.14 81 29772 582 32483091
Immune-mediated hepatic disorder 296.81 14.14 63 29790 165 32483508
Immune-mediated enterocolitis 294.29 14.14 94 29759 1581 32482092
Immune-mediated myocarditis 290.11 14.14 64 29789 213 32483460
Immune-mediated hepatitis 281.86 14.14 88 29765 1369 32482304
Myasthenia gravis 264.45 14.14 106 29747 3516 32480157
Adverse event 228.18 14.14 158 29695 16314 32467359
Adrenal insufficiency 227.54 14.14 140 29713 11828 32471845
Tumour pseudoprogression 224.81 14.14 57 29796 389 32483284
Hypothyroidism 207.80 14.14 151 29702 16824 32466849
Colitis 194.15 14.14 195 29658 33756 32449917
Type 1 diabetes mellitus 185.36 14.14 85 29768 3938 32479735
Myocarditis 169.54 14.14 115 29738 11475 32472198
Product use issue 166.37 14.14 223 29630 52554 32431119
Off label use 165.50 14.14 635 29218 305685 32177988
Hypophysitis 163.37 14.14 64 29789 1995 32481678
Immune-mediated hypothyroidism 159.32 14.14 31 29822 42 32483631
Autoimmune hepatitis 155.45 14.14 75 29778 3900 32479773
Immune-mediated arthritis 150.00 14.14 28 29825 25 32483648
Therapy partial responder 134.58 14.14 73 29780 4857 32478816
Adrenocorticotropic hormone deficiency 132.18 14.14 40 29813 557 32483116
Myositis 126.36 14.14 95 29758 11140 32472533
Immune-mediated myositis 122.18 14.14 49 29804 1626 32482047
Autoimmune colitis 120.18 14.14 42 29811 942 32482731
Tubulointerstitial nephritis 114.71 14.14 114 29739 19463 32464210
Vitiligo 114.18 14.14 38 29815 731 32482942
Hyperthyroidism 111.63 14.14 82 29771 9280 32474393
Immune-mediated dermatitis 103.25 14.14 20 29833 26 32483647
Pemphigoid 98.58 14.14 73 29780 8363 32475310
Nephritis 87.73 14.14 43 29810 2314 32481359
Drug interaction 87.05 14.14 46 29807 218139 32265534
Inappropriate schedule of product administration 86.80 14.14 153 29700 45672 32438001
Immune-mediated pancreatitis 84.29 14.14 17 29836 31 32483642
Hepatitis 83.74 14.14 106 29747 23587 32460086
Thyroiditis 79.36 14.14 38 29815 1942 32481731
Completed suicide 72.03 14.14 3 29850 92514 32391159
Immune-mediated renal disorder 71.70 14.14 13 29840 8 32483665
Polymyalgia rheumatica 71.11 14.14 31 29822 1272 32482401
Death 68.23 14.14 590 29263 381927 32101746
Immune thrombocytopenia 68.21 14.14 59 29794 8438 32475235
Immune-mediated thyroiditis 66.41 14.14 14 29839 35 32483638
Tumour hyperprogression 64.71 14.14 13 29840 23 32483650
Diabetic ketoacidosis 64.59 14.14 81 29772 17851 32465822
Secondary adrenocortical insufficiency 64.38 14.14 28 29825 1142 32482531
Overdose 61.19 14.14 5 29848 87072 32396601
Fall 60.16 14.14 55 29798 196146 32287527
Neoplasm progression 58.72 14.14 81 29772 19577 32464096
Skin toxicity 56.20 14.14 38 29815 3768 32479905
Organising pneumonia 55.07 14.14 44 29809 5637 32478036
Hypopituitarism 54.75 14.14 29 29824 1838 32481835
Fulminant type 1 diabetes mellitus 54.54 14.14 21 29832 624 32483049
Metastatic malignant melanoma 54.13 14.14 31 29822 2291 32481382
Immune-mediated nephritis 52.51 14.14 14 29839 119 32483554
Eyelid ptosis 51.76 14.14 42 29811 5500 32478173
Cholangitis sclerosing 50.85 14.14 23 29830 1031 32482642
Hepatic function abnormal 50.72 14.14 121 29732 44719 32438954
Autoimmune hypothyroidism 50.47 14.14 11 29842 34 32483639
Autoimmune arthritis 48.47 14.14 11 29842 43 32483630
Autoimmune myocarditis 47.79 14.14 14 29839 173 32483500
Immune-mediated uveitis 47.72 14.14 9 29844 9 32483664
Autoimmune thyroiditis 47.05 14.14 22 29831 1065 32482608
Haemophagocytic lymphohistiocytosis 45.35 14.14 54 29799 11281 32472392
Pneumonia bacterial 42.79 14.14 51 29802 10665 32473008
Encephalitis autoimmune 42.53 14.14 17 29836 559 32483114
Subacute cutaneous lupus erythematosus 40.74 14.14 18 29835 763 32482910
Autoimmune pancreatitis 40.61 14.14 14 29839 301 32483372
Lichenoid keratosis 40.42 14.14 26 29827 2370 32481303
Myasthenic syndrome 40.34 14.14 15 29838 404 32483269
Immune-mediated encephalitis 39.85 14.14 10 29843 65 32483608
Hepatotoxicity 39.77 14.14 67 29786 19270 32464403
Lymphocytic hypophysitis 39.46 14.14 12 29841 170 32483503
Rash 39.28 14.14 327 29526 209006 32274667
Pericarditis malignant 39.18 14.14 8 29845 16 32483657
Immune-mediated hypophysitis 39.18 14.14 8 29845 16 32483657
Headache 38.74 14.14 76 29777 196121 32287552
Diarrhoea 38.20 14.14 506 29347 364296 32119377
Lung disorder 38.07 14.14 91 29762 33663 32450010
Colitis microscopic 37.72 14.14 23 29830 1909 32481764
Immune-mediated gastritis 37.11 14.14 7 29846 7 32483666
Plasma cell myeloma 36.14 14.14 5 29848 57609 32426064
Eosinophilic fasciitis 35.70 14.14 10 29843 104 32483569
Depression 35.04 14.14 23 29830 97037 32386636
Pulmonary toxicity 35.00 14.14 32 29821 4921 32478752
Hepatocellular injury 34.98 14.14 74 29779 25244 32458429
Autoimmune nephritis 34.26 14.14 11 29842 188 32483485
Dizziness 34.23 14.14 90 29763 209528 32274145
Toxic epidermal necrolysis 34.21 14.14 65 29788 20528 32463145
Immune-mediated cholangitis 34.00 14.14 8 29845 38 32483635
Immune-mediated endocrinopathy 33.54 14.14 6 29847 3 32483670
Toxicity to various agents 33.41 14.14 71 29782 177970 32305703
Myelosuppression 33.21 14.14 47 29806 11629 32472044
Pleural effusion 33.10 14.14 152 29701 78840 32404833
Metastases to central nervous system 32.96 14.14 38 29815 7670 32476003
Drug-induced liver injury 32.86 14.14 70 29783 23993 32459680
Primary biliary cholangitis 32.54 14.14 10 29843 147 32483526
Encephalitis 32.28 14.14 36 29817 7008 32476665
Immune-mediated cytopenia 31.81 14.14 6 29847 6 32483667
Hypothalamo-pituitary disorder 31.74 14.14 15 29838 744 32482929
Drug hypersensitivity 31.44 14.14 14 29839 73386 32410287
Mucosal inflammation 31.30 14.14 84 29769 33350 32450323
Thyroid disorder 31.24 14.14 24 29829 2903 32480770
Drug effective for unapproved indication 30.34 14.14 18 29835 1421 32482252
Melanoma recurrent 29.50 14.14 9 29844 129 32483544
Anxiety 29.27 14.14 27 29826 95978 32387695
Eastern Cooperative Oncology Group performance status worsened 28.80 14.14 13 29840 580 32483093
Radiation pneumonitis 28.62 14.14 21 29832 2371 32481302
Primary hypothyroidism 28.24 14.14 7 29846 43 32483630
Silent thyroiditis 28.24 14.14 7 29846 43 32483630
Optic neuritis 28.07 14.14 24 29829 3378 32480295
Agitation 27.70 14.14 9 29844 57227 32426446
Autoimmune uveitis 27.62 14.14 5 29848 3 32483670
Haemoglobin decreased 27.56 14.14 42 29811 119629 32364044
Decreased appetite 27.39 14.14 246 29607 160567 32323106
Hospitalisation 26.91 14.14 6 29847 48965 32434708
Enteritis 26.46 14.14 33 29820 7228 32476445
Stevens-Johnson syndrome 26.21 14.14 55 29798 18654 32465019
Paraneoplastic neurological syndrome 25.95 14.14 6 29847 26 32483647
Electrocardiogram QT prolonged 25.93 14.14 3 29850 39638 32444035
Bradycardia 25.76 14.14 17 29836 71545 32412128
Aggression 25.72 14.14 3 29850 39386 32444287
Insomnia 25.31 14.14 33 29820 100315 32383358
International normalised ratio increased 25.02 14.14 7 29846 49028 32434645
Pericardial effusion 24.85 14.14 61 29792 22941 32460732
Dermatitis 24.70 14.14 35 29818 8669 32475004
Transaminases increased 23.54 14.14 63 29790 24965 32458708
Lichen planus 23.48 14.14 13 29840 900 32482773
Latent autoimmune diabetes in adults 23.40 14.14 6 29847 43 32483630
Autoimmune disorder 23.26 14.14 16 29837 1631 32482042
Keratoacanthoma 23.19 14.14 11 29842 550 32483123
Blood thyroid stimulating hormone increased 23.12 14.14 21 29832 3201 32480472
Mixed liver injury 22.93 14.14 19 29834 2561 32481112
Autoimmune neuropathy 22.83 14.14 6 29847 48 32483625
Drug ineffective 22.72 14.14 234 29619 383243 32100430
Respiratory failure 22.54 14.14 172 29681 107010 32376663
Somnolence 22.42 14.14 38 29815 103759 32379914
Cardiac failure congestive 22.34 14.14 27 29826 84825 32398848
Hypertransaminasaemia 22.05 14.14 23 29830 4151 32479522
Hypotension 21.93 14.14 113 29740 215997 32267676
Cancer pain 21.90 14.14 19 29834 2727 32480946
Pain in extremity 21.79 14.14 48 29805 118853 32364820
Hypersensitivity 21.78 14.14 13 29840 57745 32425928
Adrenal disorder 21.42 14.14 11 29842 654 32483019
Blood pressure increased 21.16 14.14 25 29828 79329 32404344
Hallucination 21.06 14.14 11 29842 52608 32431065
Unevaluable event 20.86 14.14 3 29850 33583 32450090
Intentional product misuse 20.66 14.14 4 29849 36047 32447626
Injection site pain 20.42 14.14 3 29850 33055 32450618
Cardiac arrest 20.38 14.14 36 29817 96740 32386933
Blood thyroid stimulating hormone abnormal 20.37 14.14 8 29845 251 32483422
Paraneoplastic syndrome 20.35 14.14 10 29843 541 32483132
Guillain-Barre syndrome 20.14 14.14 25 29828 5449 32478224
Pulmonary sarcoidosis 20.11 14.14 10 29843 555 32483118
Loss of consciousness 20.04 14.14 28 29825 82679 32400994
Dermatomyositis 20.02 14.14 13 29840 1204 32482469
Cutaneous sarcoidosis 19.98 14.14 7 29846 158 32483515
Cholangitis 19.96 14.14 31 29822 8327 32475346
Rheumatoid nodule 19.74 14.14 16 29837 2091 32481582
Rash maculo-papular 19.17 14.14 63 29790 27959 32455714
Muscle spasms 18.97 14.14 22 29831 70396 32413277
Lymph node abscess 18.44 14.14 4 29849 12 32483661
Malignant pleural effusion 18.33 14.14 13 29840 1392 32482281
Limbic encephalitis 18.08 14.14 8 29845 340 32483333
Chest discomfort 17.98 14.14 12 29841 50218 32433455
Autoimmune cholangitis 17.98 14.14 3 29850 0 32483673
Non-small cell lung cancer stage III 17.98 14.14 3 29850 0 32483673
Overgrowth fungal 17.98 14.14 3 29850 0 32483673
Immune-mediated encephalopathy 17.97 14.14 4 29849 14 32483659
Transitional cell carcinoma recurrent 17.97 14.14 4 29849 14 32483659
Non-small cell lung cancer 17.83 14.14 20 29833 3917 32479756
Lymphangiosis carcinomatosa 17.77 14.14 11 29842 938 32482735
Autoimmune haemolytic anaemia 17.76 14.14 21 29832 4353 32479320
Syncope 17.67 14.14 35 29818 90089 32393584
Bacterial diarrhoea 17.52 14.14 5 29848 56 32483617
Pyrexia 17.42 14.14 400 29453 319568 32164105
Adrenalitis 17.36 14.14 4 29849 17 32483656
Tremor 17.32 14.14 30 29823 81247 32402426
Thyroid hormones increased 17.28 14.14 5 29848 59 32483614
Anti-thyroid antibody positive 17.20 14.14 5 29848 60 32483613
Metastases to skin 17.15 14.14 8 29845 385 32483288
Pancreatic failure 16.99 14.14 10 29843 778 32482895
Angina pectoris 16.96 14.14 4 29849 31422 32452251
Coma 16.91 14.14 9 29844 42603 32441070
Tumour ulceration 16.91 14.14 5 29848 64 32483609
Cardiac tamponade 16.81 14.14 22 29831 5053 32478620
Blood thyroid stimulating hormone decreased 16.65 14.14 14 29839 1926 32481747
Seizure 16.61 14.14 45 29808 103809 32379864
Blood bilirubin increased 16.50 14.14 75 29778 38709 32444964
Joint swelling 16.42 14.14 14 29839 51721 32431952
Dyspepsia 16.34 14.14 5 29848 33050 32450623
Myocardial infarction 16.20 14.14 60 29793 125616 32358057
Blood corticotrophin decreased 16.19 14.14 6 29847 160 32483513
Abdominal distension 16.13 14.14 14 29839 51281 32432392
Nasopharyngitis 16.05 14.14 21 29832 63766 32419907
Hepatitis E virus test positive 15.81 14.14 4 29849 27 32483646
Treatment noncompliance 15.63 14.14 3 29850 27199 32456474
Autoimmune myositis 15.60 14.14 5 29848 85 32483588
Hepatic enzyme increased 15.30 14.14 71 29782 36966 32446707
Radiation necrosis 15.28 14.14 5 29848 91 32483582
Large intestine perforation 15.18 14.14 27 29826 8103 32475570
Coronary artery disease 15.11 14.14 14 29839 49692 32433981
Cachexia 15.11 14.14 25 29828 7084 32476589
Meningitis aseptic 14.97 14.14 15 29838 2582 32481091
Condition aggravated 14.88 14.14 83 29770 155578 32328095
Stoma site dermatitis 14.69 14.14 3 29850 6 32483667
Immunisation reaction 14.69 14.14 3 29850 6 32483667
Tumour rupture 14.50 14.14 6 29847 216 32483457
Haematoma 14.40 14.14 3 29850 25681 32457992
Tumour pain 14.30 14.14 10 29843 1047 32482626
Tumour haemorrhage 14.25 14.14 15 29838 2736 32480937
Dysphagia 14.25 14.14 101 29752 61375 32422298

Pharmacologic Action:

SourceCodeDescription
ATC L01FF02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
PD-1/PDL-1 (Programmed cell death protein 1/death ligand 1) inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000074322 Antineoplastic Agents, Immunological
MeSH PA D000082082 Immune Checkpoint Inhibitors
FDA MoA N0000191259 Programmed Death Receptor-1-directed Antibody Interactions
FDA EPC N0000191260 Programmed Death Receptor-1 Blocking Antibody

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Unresectable urothelial carcinoma indication 27090000 DOID:2671
Non-small cell lung cancer indication 254637007 DOID:3908
Malignant tumor of head and/or neck indication 255056009
Squamous cell carcinoma of esophagus indication 276804009 DOID:3748
Metastatic malignant melanoma indication 443493003
Metastatic renal cell carcinoma indication 702392008
Triple negative breast neoplasms indication 706970001
Microsatellite instability-high colorectal cancer indication 737058005
Classical Hodgkin lymphoma indication 762690000

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Programmed cell death protein 1 Membrane receptor ANTIBODY BINDING Kd 10 IUPHAR DRUG LABEL

External reference:

IDSource
D10574 KEGG_DRUG
4033703 VUID
N0000191088 NUI
4033703 VANDF
CHEMBL3137343 ChEMBL_ID
C582435 MESH_SUPPLEMENTAL_RECORD_UI
7499 IUPHAR_LIGAND_ID
9798 INN_ID
DB09037 DRUGBANK_ID
DPT0O3T46P UNII
1547545 RXNORM
228586 MMSL
30533 MMSL
d08287 MMSL
015666 NDDF
716125002 SNOMEDCT_US
763541003 SNOMEDCT_US
C3658706 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KEYTRUDA HUMAN PRESCRIPTION DRUG LABEL 1 0006-3026 INJECTION, SOLUTION 25 mg INTRAVENOUS BLA 29 sections
KEYTRUDA HUMAN PRESCRIPTION DRUG LABEL 1 0006-3026 INJECTION, SOLUTION 25 mg INTRAVENOUS BLA 29 sections
KEYTRUDA HUMAN PRESCRIPTION DRUG LABEL 1 0006-3029 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 29 sections
KEYTRUDA HUMAN PRESCRIPTION DRUG LABEL 1 0006-3029 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 50 mg INTRAVENOUS BLA 29 sections