pemetrexed ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antineoplastics; thymidylate synthetase inhibitors 2073 137281-23-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • LY231514
  • pemetrexed diacid monohydrate
  • pemetrexed sodium
  • pemetrexed sodium hydrate
  • pemetrexed
  • pemetrexed disodium
  • alimta
  • pemetrexed disodium heptahydrate
Pemetrexed is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication. In vitro studies show that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase (GARFT), which are folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is taken into cells by membrane carriers such as the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT.
  • Molecular weight: 427.42
  • Formula: C20H21N5O6
  • CLOGP: -0.12
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 6
  • TPSA: 186.97
  • ALOGS: -3.97
  • ROTB: 9

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 100 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 80 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.38 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.15 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.30 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.19 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.85 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 20, 2004 EMA ELI LILLY NEDERLAND B.V.
Feb. 4, 2004 FDA LILLY
Jan. 4, 2007 PMDA Eli Lilly Japan K.K.

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 1138.68 18.70 545 19839 81576 63387062
Disease progression 414.89 18.70 331 20053 122427 63346211
Pancytopenia 309.49 18.70 253 20131 96680 63371958
Anaemia 266.18 18.70 394 19990 293036 63175602
Drug resistance 217.02 18.70 118 20266 22815 63445823
Neutropenia 212.72 18.70 271 20113 174734 63293904
Thrombocytopenia 185.07 18.70 235 20149 150922 63317716
Tubulointerstitial nephritis 178.90 18.70 99 20285 19804 63448834
Neoplasm progression 173.71 18.70 121 20263 36307 63432331
Therapy partial responder 169.43 18.70 78 20306 10580 63458058
Pneumonitis 140.51 18.70 105 20279 35117 63433521
Acquired gene mutation 139.62 18.70 37 20347 946 63467692
Metastases to central nervous system 133.95 18.70 71 20313 13034 63455604
Non-small cell lung cancer 128.42 18.70 47 20337 3548 63465090
Febrile neutropenia 127.56 18.70 173 20211 118276 63350362
Bone marrow failure 125.11 18.70 91 20293 29199 63439439
Acute kidney injury 104.04 18.70 248 20136 263167 63205471
Myelosuppression 97.51 18.70 72 20312 23631 63445007
Renal tubular necrosis 90.35 18.70 53 20331 11825 63456813
Arthralgia 87.31 18.70 37 20347 569673 62898965
Haematotoxicity 82.48 18.70 46 20338 9330 63459308
Pulmonary embolism 82.28 18.70 140 20244 116544 63352094
Metastases to adrenals 81.67 18.70 23 20361 742 63467896
Mucosal inflammation 80.74 18.70 87 20297 46841 63421797
Nephropathy toxic 79.30 18.70 45 20339 9434 63459204
Joint swelling 76.82 18.70 8 20376 327658 63140980
EGFR gene mutation 76.43 18.70 18 20366 279 63468359
Pain 75.75 18.70 76 20308 740552 62728086
Death 75.07 18.70 277 20107 374104 63094534
Pleural effusion 74.01 18.70 118 20266 93092 63375546
Immune-mediated hepatitis 72.42 18.70 24 20360 1347 63467291
Blood creatinine increased 72.22 18.70 113 20271 87731 63380907
Myocarditis 70.55 18.70 43 20341 10282 63458356
Dehydration 65.94 18.70 161 20223 173193 63295445
Abdominal discomfort 65.43 18.70 12 20372 320873 63147765
Nephritis 65.08 18.70 26 20358 2490 63466148
Subacute cutaneous lupus erythematosus 63.84 18.70 26 20358 2617 63466021
Colitis 61.70 18.70 77 20307 48451 63420187
Haemoptysis 61.65 18.70 60 20324 28666 63439972
Metastases to meninges 60.82 18.70 25 20359 2577 63466061
Neutrophil count decreased 60.05 18.70 82 20302 56324 63412314
Interstitial lung disease 59.96 18.70 86 20298 61822 63406816
Posterior reversible encephalopathy syndrome 58.86 18.70 47 20337 17298 63451340
Hepatocellular injury 58.40 18.70 57 20327 27324 63441314
Maternal exposure during pregnancy 58.29 18.70 3 20381 220059 63248579
Immune-mediated lung disease 58.12 18.70 17 20367 629 63468009
Fall 57.62 18.70 27 20357 392307 63076331
Contraindicated product administered 57.54 18.70 3 20381 217645 63250993
Pericardial effusion 57.53 18.70 59 20325 29999 63438639
General physical health deterioration 56.37 18.70 167 20217 201235 63267403
Skin toxicity 55.23 18.70 28 20356 4686 63463952
Osteonecrosis of jaw 55.01 18.70 62 20322 35061 63433577
Sinusitis 54.49 18.70 5 20379 226648 63241990
Renal failure 54.34 18.70 118 20266 117534 63351104
Lung adenocarcinoma 52.97 18.70 27 20357 4570 63464068
Drug hypersensitivity 52.84 18.70 17 20367 310670 63157968
Immune-mediated hepatic disorder 52.79 18.70 15 20369 500 63468138
Hepatitis 51.97 18.70 64 20320 39724 63428914
Product dose omission issue 51.72 18.70 7 20377 234306 63234332
Leukopenia 48.31 18.70 88 20296 77202 63391436
Malignant pleural effusion 47.53 18.70 21 20363 2585 63466053
Renal tubular disorder 46.95 18.70 21 20363 2661 63465977
Nasopharyngitis 46.74 18.70 12 20372 254245 63214393
Hepatotoxicity 45.85 18.70 58 20326 36983 63431655
Peripheral ischaemia 45.84 18.70 25 20359 4853 63463785
Glossodynia 45.65 18.70 3 20381 178873 63289765
Hypothyroidism 45.41 18.70 62 20322 42570 63426068
Melanoderma 45.32 18.70 11 20373 195 63468443
Metastases to bone 45.28 18.70 44 20340 20975 63447663
Rheumatoid arthritis 44.75 18.70 13 20371 253806 63214832
Lymphangiosis carcinomatosa 44.69 18.70 17 20367 1428 63467210
Lung cancer metastatic 44.52 18.70 20 20364 2560 63466078
Hepatic function abnormal 44.15 18.70 57 20327 37085 63431553
Immune-mediated pancreatitis 44.03 18.70 10 20374 131 63468507
Radiation pneumonitis 43.19 18.70 17 20367 1566 63467072
Proteinuria 42.98 18.70 41 20343 19104 63449534
Nausea 42.40 18.70 439 19945 854032 62614606
Metastases to lung 42.09 18.70 34 20350 12716 63455922
Therapeutic product effect decreased 42.09 18.70 6 20378 193181 63275457
Malignant transformation 42.09 18.70 12 20372 405 63468233
Swelling 41.89 18.70 18 20366 275360 63193278
Immune-mediated enterocolitis 41.71 18.70 18 20366 2093 63466545
Gamma-glutamyltransferase increased 41.66 18.70 53 20331 33978 63434660
Platelet count decreased 41.12 18.70 105 20279 116017 63352621
Hyperamylasaemia 40.42 18.70 12 20372 468 63468170
Tumour associated fever 39.79 18.70 11 20373 331 63468307
Arthropathy 39.63 18.70 13 20371 234779 63233859
Peripheral swelling 39.47 18.70 18 20366 265924 63202714
Metastases to liver 39.20 18.70 43 20341 23596 63445042
White blood cell count decreased 38.55 18.70 115 20269 138989 63329649
Systemic lupus erythematosus 38.12 18.70 10 20374 208908 63259730
Vomiting 37.54 18.70 307 20077 559310 62909328
Jaw operation 37.47 18.70 13 20371 839 63467799
Oesophagitis 37.27 18.70 34 20350 14974 63453664
Non-small cell lung cancer metastatic 37.07 18.70 12 20372 625 63468013
Hypokalaemia 36.89 18.70 94 20290 103710 63364928
Rash maculo-papular 36.43 18.70 48 20336 31848 63436790
Metastasis 36.42 18.70 22 20362 5175 63463463
Immune-mediated dermatitis 36.10 18.70 9 20375 179 63468459
Nephrogenic diabetes insipidus 35.97 18.70 13 20371 946 63467692
Wound 35.72 18.70 5 20379 163258 63305380
Toxic skin eruption 35.59 18.70 31 20353 12854 63455784
Gene mutation 35.56 18.70 15 20369 1650 63466988
Weight increased 35.19 18.70 20 20364 260772 63207866
Hepatitis toxic 34.30 18.70 18 20366 3235 63465403
Performance status decreased 32.22 18.70 18 20366 3660 63464978
Immune-mediated myocarditis 31.93 18.70 9 20375 291 63468347
Secondary hypertension 31.73 18.70 8 20376 167 63468471
Insomnia 31.27 18.70 15 20369 215237 63253401
Sepsis 31.15 18.70 114 20270 153009 63315629
BRAF V600E mutation positive 30.89 18.70 6 20378 34 63468604
Anaphylactic shock 30.83 18.70 38 20346 23595 63445043
Asthma 30.15 18.70 3 20381 127558 63341080
Infusion related reaction 30.13 18.70 21 20363 245500 63223138
Paronychia 30.10 18.70 20 20364 5545 63463093
Decreased appetite 29.77 18.70 159 20225 250893 63217745
Tracheal fistula 29.56 18.70 6 20378 44 63468594
Hypertransaminasaemia 29.27 18.70 21 20363 6588 63462050
Exposure during pregnancy 29.23 18.70 7 20377 155540 63313098
Respiratory failure 28.96 18.70 85 20299 101773 63366865
Cardiotoxicity 28.91 18.70 23 20361 8415 63460223
Discomfort 28.71 18.70 9 20375 167365 63301273
Autoimmune dermatitis 28.64 18.70 7 20377 128 63468510
Blister 28.34 18.70 4 20380 129810 63338828
Mixed deafness 28.30 18.70 5 20379 15 63468623
Transaminases increased 28.07 18.70 42 20342 31325 63437313
Lung neoplasm malignant 27.95 18.70 33 20351 19600 63449038
Hypomagnesaemia 27.92 18.70 40 20344 28697 63439941
Immune-mediated nephritis 27.90 18.70 7 20377 143 63468495
Hypophysitis 27.78 18.70 13 20371 1828 63466810
Drug intolerance 27.77 18.70 35 20349 308626 63160012
Adenocarcinoma 27.39 18.70 15 20369 2935 63465703
Neonatal respiratory depression 27.30 18.70 6 20378 67 63468571
Asthenia 27.04 18.70 213 20171 383391 63085247
Renal arteriosclerosis 26.98 18.70 6 20378 71 63468567
Hypocalcaemia 26.32 18.70 41 20343 31672 63436966
Contusion 25.85 18.70 8 20376 150036 63318602
Sarcomatoid carcinoma 25.80 18.70 5 20379 28 63468610
Muscle spasms 25.72 18.70 9 20375 156141 63312497
Non-small cell lung cancer recurrent 25.66 18.70 6 20378 90 63468548
Autoimmune myocarditis 25.24 18.70 6 20378 97 63468541
Pain in extremity 24.56 18.70 43 20341 331443 63137195
Cholestasis 24.35 18.70 38 20346 29396 63439242
Multiple-drug resistance 24.22 18.70 17 20367 5153 63463485
Vascular purpura 24.05 18.70 11 20373 1467 63467171
Feeling abnormal 23.68 18.70 9 20375 148383 63320255
Non-small cell lung cancer stage IV 23.63 18.70 6 20378 129 63468509
Headache 23.56 18.70 114 20270 633127 62835511
Febrile infection 23.51 18.70 11 20373 1546 63467092
Renal impairment 23.48 18.70 72 20312 88283 63380355
Systemic infection 23.42 18.70 16 20368 4644 63463994
Thrombophlebitis migrans 23.33 18.70 6 20378 136 63468502
Febrile bone marrow aplasia 23.06 18.70 19 20365 7306 63461332
Migraine 22.99 18.70 3 20381 103343 63365295
Immune-mediated hypothyroidism 22.92 18.70 7 20377 301 63468337
Dizziness 22.73 18.70 67 20317 429858 63038780
Autoimmune colitis 22.70 18.70 8 20376 541 63468097
Depression 22.56 18.70 18 20366 196474 63272164
Dermatitis bullous 22.56 18.70 20 20364 8488 63460150
Drug ineffective 22.55 18.70 221 20163 1044544 62424094
Dose calculation error 22.40 18.70 6 20378 160 63468478
Carcinoembryonic antigen increased 22.19 18.70 11 20373 1754 63466884
Metastatic neoplasm 22.18 18.70 15 20369 4280 63464358
Hepatic cytolysis 22.10 18.70 26 20358 15381 63453257
Leukoencephalopathy 21.82 18.70 15 20369 4398 63464240
Unmasking of previously unidentified disease 21.53 18.70 9 20375 967 63467671
Toxic epidermal necrolysis 21.37 18.70 33 20351 25301 63443337
Bicytopenia 21.24 18.70 12 20372 2493 63466145
Focal segmental glomerulosclerosis 21.02 18.70 10 20374 1458 63467180
Cholangitis 20.88 18.70 16 20368 5545 63463093
Burkholderia pseudomallei infection 20.70 18.70 4 20380 22 63468616
Meningitis herpes 20.67 18.70 6 20378 216 63468422
Alopecia 20.56 18.70 49 20335 337487 63131151
Ischaemic stroke 20.46 18.70 27 20357 17930 63450708
Gastrointestinal toxicity 20.13 18.70 18 20366 7723 63460915
Epistaxis 20.01 18.70 60 20324 72665 63395973
Skin hyperpigmentation 19.99 18.70 16 20368 5905 63462733
Diverticular perforation 19.81 18.70 13 20371 3529 63465109
Embolism 19.80 18.70 18 20366 7888 63460750
Diarrhoea 19.53 18.70 330 20054 715036 62753602
Pericarditis 19.36 18.70 9 20375 131570 63337068
Bronchitis 19.24 18.70 8 20376 124927 63343711
Nephropathy 19.03 18.70 16 20368 6325 63462313
Immune-mediated cholangitis 18.78 18.70 4 20380 38 63468600

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 1002.57 16.70 744 30998 87302 34837887
Pancytopenia 508.11 16.70 523 31219 94634 34830555
Interstitial lung disease 307.41 16.70 336 31406 64946 34860243
Neutropenia 293.06 16.70 516 31226 156262 34768927
Anaemia 286.79 16.70 644 31098 232691 34692498
Thrombocytopenia 278.84 16.70 504 31238 155743 34769446
Disease progression 225.71 16.70 374 31368 107703 34817486
Myelosuppression 166.83 16.70 139 31603 19126 34906063
Pneumonitis 163.83 16.70 177 31565 33701 34891488
Bone marrow failure 161.40 16.70 164 31578 29089 34896100
Febrile neutropenia 153.47 16.70 365 31377 136484 34788705
General physical health deterioration 149.12 16.70 347 31395 127922 34797267
Febrile bone marrow aplasia 144.26 16.70 91 31651 8118 34917071
Mucosal inflammation 135.28 16.70 171 31571 38451 34886738
Immune-mediated hepatic disorder 126.71 16.70 44 31698 979 34924210
Neoplasm progression 121.95 16.70 127 31615 23173 34902016
Immune-mediated lung disease 118.14 16.70 47 31695 1544 34923645
Tubulointerstitial nephritis 100.11 16.70 109 31633 20915 34904274
Decreased appetite 98.29 16.70 353 31389 166039 34759150
Therapy partial responder 97.25 16.70 76 31666 9540 34915649
Pleural effusion 96.15 16.70 222 31520 81324 34843865
Leukopenia 93.46 16.70 188 31554 62668 34862521
Neutrophil count decreased 84.65 16.70 160 31582 50944 34874245
Haematotoxicity 81.22 16.70 64 31678 8130 34917059
Metastases to central nervous system 81.14 16.70 64 31678 8141 34917048
Immune-mediated enterocolitis 75.58 16.70 41 31701 2758 34922431
Colitis 75.06 16.70 128 31614 37622 34887567
Completed suicide 72.84 16.70 4 31738 98164 34827025
Product dose omission issue 72.65 16.70 11 31731 119700 34805489
Skin toxicity 71.69 16.70 48 31694 4736 34920453
Non-small cell lung cancer 70.02 16.70 44 31698 3896 34921293
Platelet count decreased 68.91 16.70 252 31490 119465 34805724
Enteritis 66.85 16.70 57 31685 8085 34917104
Neutropenic sepsis 66.62 16.70 72 31670 13695 34911494
Lichenoid keratosis 60.21 16.70 34 31708 2474 34922715
Aplasia 59.24 16.70 42 31700 4546 34920643
Drug interaction 59.11 16.70 71 31671 225875 34699314
EGFR gene mutation 57.78 16.70 16 31726 161 34925028
Fall 57.16 16.70 60 31682 202825 34722364
Pseudocellulitis 54.05 16.70 12 31730 42 34925147
Adrenocorticotropic hormone deficiency 53.46 16.70 23 31719 924 34924265
Immune-mediated adverse reaction 53.27 16.70 20 31722 560 34924629
Diarrhoea 52.42 16.70 562 31180 389350 34535839
Tumour pseudoprogression 52.41 16.70 19 31723 481 34924708
Hypopituitarism 52.26 16.70 30 31712 2252 34922937
Septic shock 51.67 16.70 163 31579 71671 34853518
Immune-mediated renal disorder 50.54 16.70 14 31728 141 34925048
Hepatic cytolysis 50.42 16.70 64 31678 14432 34910757
Headache 49.38 16.70 66 31676 200569 34724620
Pulmonary toxicity 48.37 16.70 42 31700 6105 34919084
Nephropathy toxic 47.67 16.70 58 31684 12530 34912659
Overdose 47.60 16.70 12 31730 91047 34834142
Vomiting 46.77 16.70 384 31358 247237 34677952
Dehydration 45.79 16.70 236 31506 129733 34795456
Extremity necrosis 45.36 16.70 26 31716 1946 34923243
Respiratory failure 45.32 16.70 207 31535 108365 34816824
Nausea 42.43 16.70 483 31259 339425 34585764
Pain in extremity 42.09 16.70 32 31710 126481 34798708
Bradycardia 41.27 16.70 9 31733 75409 34849780
Muscle spasms 40.94 16.70 9 31733 74992 34850197
White blood cell count decreased 40.59 16.70 183 31559 95262 34829927
Pulmonary embolism 40.38 16.70 175 31567 89571 34835618
Haemoptysis 39.77 16.70 94 31648 34912 34890277
Pneumothorax 39.61 16.70 66 31676 19026 34906163
Hiccups 39.06 16.70 47 31695 10035 34915154
Drug resistance 39.03 16.70 78 31664 25849 34899340
Lung adenocarcinoma 38.96 16.70 33 31709 4638 34920551
Large intestine perforation 38.58 16.70 43 31699 8460 34916729
Radiation pneumonitis 38.39 16.70 26 31716 2614 34922575
Superior vena cava syndrome 37.85 16.70 16 31726 615 34924574
Rash 37.59 16.70 337 31405 222415 34702774
Lung disorder 37.09 16.70 91 31651 34605 34890584
Acquired gene mutation 37.00 16.70 20 31722 1335 34923854
Blood pressure increased 36.73 16.70 17 31725 88085 34837104
Hypersensitivity pneumonitis 36.61 16.70 21 31721 1574 34923615
Tremor 35.91 16.70 15 31727 82572 34842617
Acute kidney injury 35.62 16.70 428 31314 304560 34620629
Hepatocellular injury 34.85 16.70 68 31674 22143 34903046
Drug ineffective 34.19 16.70 259 31483 456492 34468697
Erysipelas 33.84 16.70 31 31711 4832 34920357
Eastern Cooperative Oncology Group performance status worsened 33.59 16.70 17 31725 991 34924198
Nasopharyngitis 33.29 16.70 11 31731 69957 34855232
Pneumonia 33.27 16.70 487 31255 362140 34563049
Toxicity to various agents 31.64 16.70 86 31656 200276 34724913
Immune-mediated myocarditis 31.34 16.70 15 31727 774 34924415
Pyrexia 31.23 16.70 449 31293 332564 34592625
Small intestinal perforation 30.66 16.70 21 31721 2150 34923039
Nephritis 30.63 16.70 22 31720 2429 34922760
Peritonitis 30.56 16.70 54 31688 16311 34908878
Metastases to meninges 30.35 16.70 18 31724 1436 34923753
Secondary adrenocortical insufficiency 30.17 16.70 18 31724 1452 34923737
Paraneoplastic syndrome 29.80 16.70 13 31729 540 34924649
Immune-mediated hypothyroidism 29.64 16.70 11 31731 298 34924891
Flagellate dermatitis 29.30 16.70 8 31734 76 34925113
Hypothyroidism 29.23 16.70 61 31681 20841 34904348
Musculoskeletal stiffness 28.97 16.70 4 31738 46676 34878513
Metastases to bone 28.41 16.70 44 31698 11926 34913263
Feeling abnormal 28.28 16.70 11 31731 63224 34861965
Disseminated intravascular coagulation 27.44 16.70 61 31681 21755 34903434
Peripheral swelling 27.23 16.70 18 31724 76523 34848666
Rhabdomyolysis 27.12 16.70 14 31728 68149 34857040
Depression 26.98 16.70 29 31713 97069 34828120
Weight increased 26.73 16.70 27 31715 93006 34832183
Anxiety 26.20 16.70 31 31711 99397 34825792
Performance status decreased 26.15 16.70 25 31717 4112 34921077
Lung cancer metastatic 25.97 16.70 21 31721 2766 34922423
Prostate cancer 25.57 16.70 3 31739 39646 34885543
Cardiac failure congestive 25.28 16.70 23 31719 83247 34841942
Injection site pain 25.03 16.70 3 31739 39002 34886187
Epistaxis 24.97 16.70 112 31630 58139 34867050
Renal failure 24.85 16.70 203 31539 130354 34794835
Immune-mediated dermatitis 24.84 16.70 10 31732 339 34924850
Insomnia 24.70 16.70 35 31707 103872 34821317
Hallucination 24.66 16.70 8 31734 51490 34873699
Adrenal insufficiency 24.50 16.70 45 31697 14002 34911187
Hypercreatininaemia 24.50 16.70 11 31731 490 34924699
Malignant pleural effusion 24.44 16.70 16 31726 1520 34923669
Sepsis 24.08 16.70 244 31498 166317 34758872
Agitation 24.04 16.70 11 31731 57388 34867801
Cardiac disorder 23.89 16.70 5 31737 43121 34882068
Pancreatic toxicity 23.85 16.70 6 31736 40 34925149
Neutropenic colitis 23.77 16.70 21 31721 3123 34922066
Dacryostenosis acquired 23.64 16.70 9 31733 262 34924927
Pericardial effusion 23.56 16.70 62 31680 24600 34900589
Arthralgia 23.23 16.70 78 31664 169963 34755226
Pericarditis malignant 23.23 16.70 6 31736 45 34925144
Purpura 23.22 16.70 37 31705 10274 34914915
Metastases to liver 22.87 16.70 43 31699 13620 34911569
Epidermolysis 22.81 16.70 9 31733 289 34924900
Autoimmune haemolytic anaemia 22.60 16.70 24 31718 4472 34920717
Hyperthyroidism 22.55 16.70 37 31705 10529 34914660
Electrocardiogram QT prolonged 22.17 16.70 5 31737 40947 34884242
Haemophagocytic lymphohistiocytosis 21.93 16.70 41 31701 12932 34912257
Gastrointestinal perforation 21.91 16.70 22 31720 3841 34921348
Asthma 21.56 16.70 6 31736 42650 34882539
Abdominal discomfort 21.37 16.70 14 31728 59821 34865368
Myalgia 21.34 16.70 27 31715 84083 34841106
Oral papule 21.25 16.70 4 31738 4 34925185
Opsoclonus myoclonus 21.10 16.70 6 31736 67 34925122
Dizziness 20.81 16.70 115 31627 218406 34706783
Lymphangiosis carcinomatosa 20.67 16.70 12 31730 920 34924269
Acute generalised exanthematous pustulosis 20.59 16.70 28 31714 6748 34918441
Myocarditis 20.39 16.70 41 31701 13641 34911548
Memory impairment 20.27 16.70 7 31735 43311 34881878
Immune-mediated adrenal insuficiency 20.14 16.70 7 31735 156 34925033
Hyperpyrexia 19.84 16.70 18 31724 2770 34922419
Dyspnoea 19.75 16.70 464 31278 376318 34548871
Superior mesenteric artery syndrome 19.73 16.70 6 31736 86 34925103
Renal impairment 19.64 16.70 150 31592 94363 34830826
Toxic epidermal necrolysis 19.25 16.70 53 31689 21593 34903596
Hypoglycaemia 19.23 16.70 13 31729 54627 34870562
Occipital neuralgia 19.19 16.70 5 31737 39 34925150
Immune-mediated neuropathy 18.97 16.70 5 31737 41 34925148
Vision blurred 18.95 16.70 9 31733 45954 34879235
Non-small cell lung cancer metastatic 18.89 16.70 10 31732 640 34924549
Thrombophlebitis migrans 18.85 16.70 7 31735 190 34924999
Tracheo-oesophageal fistula 18.79 16.70 9 31733 465 34924724
Intentional product use issue 18.78 16.70 16 31726 59800 34865389
Hypertransaminasaemia 18.31 16.70 24 31718 5582 34919607
Wrong technique in product usage process 18.30 16.70 5 31737 35981 34889208
Bicytopenia 18.17 16.70 16 31726 2368 34922821
Rash maculo-papular 18.13 16.70 62 31680 28389 34896800
Immune thrombocytopenia 18.13 16.70 31 31711 9121 34916068
Hepatitis 17.86 16.70 55 31687 23849 34901340
Dysphagia 17.74 16.70 107 31635 62274 34862915
Mobility decreased 17.74 16.70 3 31739 30125 34895064
Laryngeal leukoplakia 17.65 16.70 5 31737 55 34925134
Hyperhidrosis 17.49 16.70 26 31716 75666 34849523
Immune-mediated pancreatitis 17.38 16.70 6 31736 131 34925058
Lymphangitis 17.30 16.70 9 31733 556 34924633
Somnolence 17.28 16.70 48 31694 111068 34814121
Aphthous ulcer 17.28 16.70 22 31720 4973 34920216
Coma 17.27 16.70 10 31732 45668 34879521
Immune-mediated hepatitis 17.15 16.70 15 31727 2200 34922989
Rheumatoid nodule 17.11 16.70 17 31725 2930 34922259
Tumour necrosis 17.11 16.70 12 31730 1276 34923913
Diaphragmatic rupture 17.04 16.70 4 31738 19 34925170
Vasculitis 17.01 16.70 34 31708 11262 34913927
Heart rate decreased 16.94 16.70 4 31738 31741 34893448
Granulocyte count increased 16.91 16.70 8 31734 402 34924787
Asthenia 16.71 16.70 314 31428 244937 34680252
Human chorionic gonadotropin increased 16.71 16.70 4 31738 21 34925168

FDA Adverse Event Reporting System (Geriatric)

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 1803.73 15.54 1043 42251 134947 79566147
Pancytopenia 756.91 15.54 664 42630 165081 79536013
Disease progression 584.72 15.54 604 42690 183758 79517336
Anaemia 476.67 15.54 859 42435 444156 79256938
Neutropenia 441.59 15.54 654 42640 287056 79414038
Thrombocytopenia 427.33 15.54 617 42677 264642 79436452
Interstitial lung disease 340.47 15.54 360 42934 112240 79588854
Pneumonitis 277.41 15.54 244 43050 60616 79640478
Myelosuppression 269.26 15.54 202 43092 40094 79661000
Tubulointerstitial nephritis 267.42 15.54 197 43097 38038 79663056
Therapy partial responder 266.17 15.54 147 43147 17250 79683844
Bone marrow failure 265.77 15.54 221 43073 50886 79650208
Febrile neutropenia 246.45 15.54 446 42848 230553 79470541
Drug resistance 239.36 15.54 192 43102 42021 79659073
Neoplasm progression 227.13 15.54 203 43091 51479 79649615
Metastases to central nervous system 198.74 15.54 119 43175 16256 79684838
Immune-mediated hepatic disorder 191.01 15.54 59 43235 1535 79699559
Immune-mediated lung disease 181.67 15.54 62 43232 2228 79698866
Non-small cell lung cancer 181.26 15.54 82 43212 6278 79694816
Acquired gene mutation 159.89 15.54 56 43238 2177 79698917
Haematotoxicity 155.91 15.54 100 43194 15419 79685675
Febrile bone marrow aplasia 151.24 15.54 92 43202 12928 79688166
General physical health deterioration 151.01 15.54 407 42887 274831 79426263
Mucosal inflammation 148.68 15.54 194 43100 75386 79625708
Acute kidney injury 147.83 15.54 615 42679 518789 79182305
Skin toxicity 140.35 15.54 75 43219 8239 79692855
EGFR gene mutation 137.96 15.54 35 43259 429 79700665
Colitis 136.23 15.54 183 43111 73124 79627970
Leukopenia 127.90 15.54 228 43066 116285 79584809
Pleural effusion 127.03 15.54 258 43036 145004 79556090
Neutrophil count decreased 123.16 15.54 199 43095 93760 79607334
Completed suicide 119.24 15.54 3 43291 245764 79455330
Immune-mediated enterocolitis 115.04 15.54 55 43239 4775 79696319
Fall 114.68 15.54 61 43233 487568 79213526
Decreased appetite 111.33 15.54 423 42871 341995 79359099
Arthralgia 107.10 15.54 92 43202 571711 79129383
Pain 103.23 15.54 139 43155 703663 78997431
Nephropathy toxic 101.34 15.54 86 43208 20333 79680761
Platelet count decreased 94.00 15.54 275 43019 194389 79506705
Joint swelling 93.72 15.54 21 43273 288625 79412469
Product dose omission issue 93.57 15.54 12 43282 247525 79453569
Hepatocellular injury 90.22 15.54 120 43174 47473 79653621
Tumour pseudoprogression 89.31 15.54 27 43267 652 79700442
Lichenoid keratosis 84.04 15.54 42 43252 4015 79697079
Lung cancer metastatic 81.69 15.54 40 43254 3659 79697435
Headache 81.55 15.54 144 43150 653628 79047466
Lung adenocarcinoma 79.79 15.54 51 43243 7813 79693281
Metastases to meninges 79.70 15.54 39 43255 3562 79697532
Nasopharyngitis 79.39 15.54 20 43274 253861 79447233
Musculoskeletal stiffness 78.44 15.54 4 43290 175004 79526090
Abdominal discomfort 77.92 15.54 20 43274 250707 79450387
Myocarditis 77.41 15.54 76 43218 21657 79679437
Renal tubular necrosis 77.22 15.54 81 43213 24958 79676136
Pulmonary embolism 76.71 15.54 236 43058 171418 79529676
Radiation pneumonitis 76.45 15.54 39 43255 3894 79697200
Haemoptysis 75.25 15.54 120 43174 55879 79645215
Hypothyroidism 74.19 15.54 115 43179 52277 79648817
Hepatic cytolysis 73.51 15.54 82 43212 27069 79674025
Aplasia 72.68 15.54 48 43246 7772 79693322
Contraindicated product administered 72.56 15.54 3 43291 157535 79543559
Blood creatinine increased 70.98 15.54 215 43079 154842 79546252
Immune-mediated hepatitis 70.33 15.54 36 43258 3620 79697474
Pain in extremity 70.19 15.54 57 43237 364481 79336613
Hypopituitarism 69.85 15.54 35 43259 3364 79697730
Peripheral swelling 68.99 15.54 30 43264 269587 79431507
Subacute cutaneous lupus erythematosus 68.31 15.54 35 43259 3526 79697568
Osteonecrosis of jaw 67.04 15.54 99 43195 43127 79657967
Immune-mediated adverse reaction 66.23 15.54 23 43271 871 79700223
Pericardial effusion 66.18 15.54 102 43192 46135 79654959
Nephritis 65.51 15.54 36 43258 4178 79696916
Enteritis 65.45 15.54 58 43236 14525 79686569
Immune-mediated renal disorder 64.56 15.54 16 43278 177 79700917
Metastases to liver 64.10 15.54 78 43216 28236 79672858
Sinusitis 63.88 15.54 14 43280 195487 79505607
Septic shock 63.62 15.54 178 43116 122623 79578471
Diarrhoea 63.53 15.54 743 42551 879746 78821348
Adrenocorticotropic hormone deficiency 63.36 15.54 25 43269 1360 79699734
Pseudocellulitis 61.83 15.54 13 43281 63 79701031
Therapeutic product effect decreased 61.77 15.54 8 43286 163855 79537239
Maternal exposure during pregnancy 61.57 15.54 3 43291 136535 79564559
Pulmonary toxicity 61.24 15.54 53 43241 12861 79688233
Metastases to adrenals 60.82 15.54 24 43270 1306 79699788
Weight increased 60.42 15.54 38 43256 277348 79423746
Hepatic function abnormal 59.33 15.54 126 43168 72981 79628113
Respiratory failure 59.08 15.54 224 43070 180687 79520407
Hepatitis 58.48 15.54 107 43187 55620 79645474
Renal failure 57.71 15.54 239 43055 200729 79500365
Drug hypersensitivity 57.20 15.54 47 43247 298869 79402225
Immune-mediated myocarditis 56.94 15.54 22 43272 1131 79699963
Rash maculo-papular 55.50 15.54 105 43189 55973 79645121
Arthropathy 55.26 15.54 14 43280 177097 79523997
Injection site pain 55.07 15.54 4 43290 129834 79571260
Immune-mediated dermatitis 54.84 15.54 18 43276 572 79700522
White blood cell count decreased 54.12 15.54 224 43070 188064 79513030
Neutropenic sepsis 54.01 15.54 70 43224 26994 79674100
Immune-mediated pancreatitis 53.06 15.54 15 43279 284 79700810
Immune-mediated hypothyroidism 52.78 15.54 18 43276 645 79700449
Lymphangiosis carcinomatosa 52.74 15.54 25 43269 2129 79698965
Melanoderma 52.63 15.54 16 43278 394 79700700
Swelling 52.50 15.54 26 43268 216685 79484409
Muscle spasms 52.27 15.54 15 43279 174715 79526379
Extremity necrosis 51.90 15.54 28 43266 3133 79697961
Pyrexia 50.75 15.54 577 42717 678132 79022962
Rheumatoid arthritis 50.52 15.54 25 43269 208445 79492649
Drug intolerance 49.94 15.54 42 43252 264077 79437017
Depression 49.59 15.54 28 43266 216762 79484332
Overdose 49.53 15.54 19 43275 184187 79516907
Wound 48.08 15.54 4 43290 116175 79584919
Asthma 47.67 15.54 8 43286 135087 79566007
Gene mutation 47.51 15.54 25 43269 2661 79698433
Pneumothorax 47.02 15.54 67 43227 28256 79672838
Hypertransaminasaemia 46.81 15.54 44 43250 11880 79689214
Hepatotoxicity 45.77 15.54 92 43202 51260 79649834
Hyperthyroidism 45.19 15.54 58 43236 22151 79678943
Malignant pleural effusion 44.77 15.54 26 43268 3354 79697740
Dizziness 44.72 15.54 142 43152 526299 79174795
Hypophysitis 44.72 15.54 28 43266 4138 79696956
Blood pressure increased 44.59 15.54 30 43264 211330 79489764
Dehydration 44.51 15.54 258 43036 247929 79453165
Glossodynia 44.35 15.54 3 43291 103334 79597760
Contusion 44.08 15.54 13 43281 148763 79552331
Vomiting 43.59 15.54 552 42742 665276 79035818
Hiccups 43.24 15.54 39 43255 9992 79691102
Renal impairment 43.22 15.54 185 43109 157598 79543496
Thrombophlebitis migrans 43.02 15.54 14 43280 433 79700661
Toxic epidermal necrolysis 42.30 15.54 82 43212 44499 79656595
Sepsis 41.95 15.54 270 43024 269158 79431936
Toxic skin eruption 41.91 15.54 56 43238 22237 79678857
Feeling abnormal 41.84 15.54 17 43277 159182 79541912
Bicytopenia 41.80 15.54 28 43266 4642 79696452
Insomnia 41.61 15.54 43 43251 245127 79455967
Tracheal fistula 41.24 15.54 11 43283 166 79700928
Infusion related reaction 40.66 15.54 39 43255 230198 79470896
Peritonitis 40.32 15.54 62 43232 27974 79673120
Intentional product misuse 40.16 15.54 3 43291 95162 79605932
Bradycardia 39.88 15.54 12 43282 135545 79565549
Performance status decreased 39.38 15.54 30 43264 6083 79695011
Malignant transformation 38.86 15.54 17 43277 1201 79699893
Tremor 38.84 15.54 22 43272 170061 79531033
Skin hyperpigmentation 38.80 15.54 32 43262 7271 79693823
Proteinuria 38.74 15.54 66 43228 32436 79668658
Non-small cell lung cancer metastatic 37.99 15.54 16 43278 1030 79700064
Exposure during pregnancy 37.95 15.54 5 43289 101127 79599967
Nausea 37.93 15.54 729 42565 956467 78744627
Metastases to pleura 37.93 15.54 18 43276 1536 79699558
Tumour associated fever 36.90 15.54 15 43279 882 79700212
Secondary adrenocortical insufficiency 36.81 15.54 22 43272 2992 79698102
Transaminases increased 36.14 15.54 84 43210 51659 79649435
Pericarditis malignant 35.55 15.54 8 43286 56 79701038
Oesophagitis 35.33 15.54 54 43240 24235 79676859
Small intestinal perforation 34.99 15.54 22 43272 3275 79697819
Metastases to lung 34.72 15.54 46 43248 18117 79682977
Autoimmune colitis 34.20 15.54 17 43277 1606 79699488
Adrenal insufficiency 34.15 15.54 58 43236 28429 79672665
Suicide attempt 33.92 15.54 3 43291 82929 79618165
Mobility decreased 33.85 15.54 12 43282 122163 79578931
Osteoarthritis 33.53 15.54 4 43290 87305 79613789
Hypersensitivity 33.28 15.54 57 43237 262182 79438912
Gamma-glutamyltransferase increased 33.09 15.54 84 43210 54596 79646498
Large intestine perforation 32.76 15.54 40 43254 14527 79686567
Haemophagocytic lymphohistiocytosis 32.40 15.54 49 43245 21788 79679306
Metastases to bone 32.33 15.54 52 43242 24375 79676719
Erysipelas 31.50 15.54 34 43260 10816 79690278
Jaw operation 31.18 15.54 13 43281 816 79700278
Blister 31 15.54 13 43281 119463 79581631
Toxicity to various agents 30.88 15.54 121 43173 421419 79279675
Asthenia 30.82 15.54 418 42876 511271 79189823
Influenza 30.70 15.54 16 43278 129590 79571504
Anxiety 30.64 15.54 55 43239 248457 79452637
Suicidal ideation 30.59 15.54 3 43291 76337 79624757
Drug interaction 30.52 15.54 119 43175 415064 79286030
Systemic lupus erythematosus 30.14 15.54 14 43280 121135 79579959
Hypersensitivity pneumonitis 30.10 15.54 21 43273 3718 79697376
Pancreatic toxicity 29.96 15.54 7 43287 59 79701035
Epistaxis 29.94 15.54 130 43164 111385 79589709
Nephrogenic diabetes insipidus 29.82 15.54 17 43277 2117 79698977
Hypoaesthesia 29.81 15.54 32 43262 179320 79521774
Disseminated intravascular coagulation 29.33 15.54 62 43232 35780 79665314
Carcinoembryonic antigen increased 29.28 15.54 17 43277 2192 79698902
Memory impairment 29.24 15.54 12 43282 111722 79589372
Purpura 29.24 15.54 44 43250 19483 79681611
Discomfort 29.03 15.54 16 43278 125601 79575493
Cholangitis 28.60 15.54 35 43259 12741 79688353
Pneumonia 28.55 15.54 510 42784 659736 79041358
Paraneoplastic syndrome 28.22 15.54 13 43281 1037 79700057
Nasal congestion 28.21 15.54 4 43290 76548 79624546
Gastrointestinal toxicity 28.21 15.54 28 43266 8081 79693013
Metastasis 28.19 15.54 26 43268 6854 79694240
Peripheral ischaemia 28.10 15.54 30 43264 9427 79691667
Hepatic enzyme increased 27.75 15.54 35 43259 182575 79518519
Treatment failure 27.69 15.54 31 43263 170455 79530639
Somnolence 27.61 15.54 55 43239 238926 79462168
Renal tubular disorder 27.53 15.54 25 43269 6461 79694633
Cholestasis 27.42 15.54 76 43218 52033 79649061
Sarcomatoid carcinoma 26.79 15.54 6 43288 41 79701053
Gastrointestinal perforation 26.73 15.54 24 43270 6113 79694981
Hospitalisation 26.54 15.54 9 43285 94227 79606867
Multiple-drug resistance 26.27 15.54 28 43266 8780 79692314
Neutropenic colitis 26.21 15.54 23 43271 5684 79695410
Mixed deafness 26.20 15.54 5 43289 13 79701081
Immune-mediated cholangitis 26.08 15.54 8 43286 203 79700891
Superior vena cava syndrome 26.07 15.54 13 43281 1236 79699858
BRAF V600E mutation positive 25.96 15.54 6 43288 48 79701046
Rash 25.79 15.54 449 42845 577909 79123185
Non-small cell lung cancer recurrent 25.36 15.54 7 43287 121 79700973
Loss of personal independence in daily activities 25.30 15.54 12 43282 102568 79598526
Immune-mediated nephritis 25.03 15.54 10 43284 562 79700532
Eastern Cooperative Oncology Group performance status worsened 25.03 15.54 15 43279 2050 79699044
Lung neoplasm malignant 25.01 15.54 50 43244 27742 79673352
Cardiotoxicity 24.95 15.54 32 43262 12207 79688887
Oesophagobronchial fistula 24.56 15.54 8 43286 248 79700846
Metastatic neoplasm 24.53 15.54 21 43273 5021 79696073
Posterior reversible encephalopathy syndrome 24.51 15.54 48 43246 26233 79674861
Autoimmune myocarditis 24.33 15.54 9 43285 410 79700684
Hepatitis toxic 24.15 15.54 21 43273 5126 79695968
Hyperamylasaemia 24.13 15.54 12 43282 1135 79699959
Hyperhidrosis 24.11 15.54 28 43266 151464 79549630
Flagellate dermatitis 24.06 15.54 8 43286 265 79700829
Lung adenocarcinoma recurrent 23.82 15.54 5 43289 24 79701070
Autoimmune dermatitis 23.60 15.54 7 43287 158 79700936
Oral papule 23.31 15.54 4 43290 4 79701090
Malaise 23.28 15.54 163 43131 489706 79211388
Intentional product use issue 23.27 15.54 29 43265 152083 79549011
Lung disorder 23.24 15.54 96 43198 80461 79620633
Heart rate decreased 23.02 15.54 5 43289 70311 79630783
Cardiac failure congestive 23.01 15.54 26 43268 142376 79558718
Sleep disorder 22.75 15.54 9 43285 85668 79615426
Adenocarcinoma 22.70 15.54 18 43276 3868 79697226
Acute coronary syndrome 22.70 15.54 41 43253 21092 79680002
Urinary tract infection 22.60 15.54 75 43219 274437 79426657
Enterocolitis 22.15 15.54 33 43261 14479 79686615
Autoimmune haemolytic anaemia 22.15 15.54 25 43269 8355 79692739
Bronchitis 22.05 15.54 23 43271 130621 79570473
Hypoglycaemia 21.98 15.54 14 43280 101580 79599514
Dacryostenosis acquired 21.92 15.54 9 43285 543 79700551
Immune-mediated adrenal insuficiency 21.71 15.54 7 43287 210 79700884
Gastrooesophageal reflux disease 21.70 15.54 15 43279 104231 79596863
Secondary hypertension 21.43 15.54 8 43286 374 79700720
Alopecia 21.33 15.54 60 43234 231295 79469799
Myasthenic syndrome 21.31 15.54 10 43284 832 79700262
Fulminant type 1 diabetes mellitus 21.23 15.54 12 43282 1471 79699623
Hyperpyrexia 21.13 15.54 21 43273 6071 79695023
Tracheo-oesophageal fistula 21.11 15.54 9 43285 597 79700497
Radiation neuropathy 21.07 15.54 4 43290 10 79701084
Cardiac disorder 20.88 15.54 5 43289 65752 79635342
Cerebral infarction 20.55 15.54 63 43231 45613 79655481
Death 20.50 15.54 426 42868 566088 79135006
Coma 20.27 15.54 15 43279 100634 79600460
Laryngeal leukoplakia 20.12 15.54 5 43289 56 79701038
Oropharyngeal pain 19.91 15.54 18 43276 109335 79591759
Constipation 19.87 15.54 238 43056 282812 79418282
Diverticular perforation 19.86 15.54 20 43274 5873 79695221
Immune thrombocytopenia 19.71 15.54 35 43259 17770 79683324
Adrenal disorder 19.50 15.54 13 43281 2138 79698956
Back pain 19.38 15.54 92 43202 304088 79397006
Immune-mediated hyperthyroidism 19.25 15.54 6 43288 161 79700933
Pulmonary artery thrombosis 19.22 15.54 11 43283 1381 79699713
Hypercreatininaemia 19.19 15.54 10 43284 1043 79700051
Lymphangitis 19.10 15.54 11 43283 1397 79699697
Impaired healing 19.07 15.54 12 43282 87643 79613451
Drug ineffective 18.95 15.54 445 42849 1080468 78620626
Incorrect dose administered 18.84 15.54 9 43285 76621 79624473
Renal arteriosclerosis 18.80 15.54 7 43287 325 79700769
Ureteric dilatation 18.77 15.54 6 43288 175 79700919
Pericardial effusion malignant 18.67 15.54 6 43288 178 79700916
Agitation 18.65 15.54 16 43278 99699 79601395
Hypokalaemia 18.62 15.54 138 43156 143902 79557192
Vision blurred 18.61 15.54 18 43276 105880 79595214
Abdominal pain upper 18.52 15.54 61 43233 223758 79477336
Superior mesenteric artery syndrome 18.42 15.54 6 43288 186 79700908
Capillary leak syndrome 18.39 15.54 16 43278 3909 79697185
Hallucination 18.30 15.54 12 43282 85733 79615361
Small cell lung cancer 18.25 15.54 14 43280 2866 79698228
Urticaria 17.84 15.54 47 43247 185154 79515940
Intestinal perforation 17.70 15.54 33 43261 17393 79683701
Product use issue 17.49 15.54 57 43237 209765 79491329
Embolism 17.47 15.54 29 43265 13953 79687141
Arthritis 17.46 15.54 22 43272 114858 79586236
Dyspepsia 17.39 15.54 20 43274 108667 79592427
Opsoclonus myoclonus 17.31 15.54 6 43288 226 79700868
Meningitis herpes 17.28 15.54 6 43288 227 79700867
Psoriasis 17.22 15.54 14 43280 89573 79611521
Myalgia 17.21 15.54 48 43246 185593 79515501
Dose calculation error 17.13 15.54 6 43288 233 79700861
Oral fungal infection 17.02 15.54 15 43279 3728 79697366
Lip oedema 16.96 15.54 19 43275 6297 79694797
Muscle injury 16.85 15.54 3 43291 48558 79652536
Acute generalised exanthematous pustulosis 16.69 15.54 32 43262 17222 79683872
Leukoencephalopathy 16.59 15.54 21 43273 7908 79693186
Heart rate increased 16.47 15.54 25 43269 120699 79580395
Hypocalcaemia 16.42 15.54 62 43232 49862 79651232
Allergic colitis 16.42 15.54 4 43290 41 79701053
Autoimmune nephritis 16.34 15.54 8 43286 731 79700363
Wrong technique in product usage process 16.23 15.54 10 43284 73865 79627229
Liver disorder 16.17 15.54 80 43214 72337 79628757
Amnesia 16.13 15.54 7 43287 63050 79638044
Scleroderma-like reaction 15.97 15.54 5 43289 136 79700958
Fluid retention 15.97 15.54 9 43285 69800 79631294
Tumour necrosis 15.95 15.54 11 43283 1911 79699183
Injection site reaction 15.84 15.54 5 43289 54780 79646314
Burning sensation 15.83 15.54 6 43288 58626 79642468
Kidney fibrosis 15.74 15.54 14 43280 3521 79697573
Cataract 15.73 15.54 7 43287 62113 79638981
Hypotension 15.70 15.54 158 43136 440159 79260935
Palpitations 15.61 15.54 28 43266 126582 79574512

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01BA04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
ANTIMETABOLITES
Folic acid analogues
FDA MoA N0000000111 Folic Acid Metabolism Inhibitors
FDA EPC N0000175584 Folate Analog Metabolic Inhibitor
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005493 Folic Acid Antagonists
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
CHEBI has role CHEBI:35221 antimetabolite
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50683 dihydrofolic acid reductase inhibitors
CHEBI has role CHEBI:63720 dTMP synthase inhibitors
CHEBI has role CHEBI:63721 glycinamide ribonucleotide formyltransferase inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Malignant mesothelioma of pleura indication 254645002 DOID:7474
Kidney disease contraindication 90708001 DOID:557
Impaired renal function disorder contraindication 197663003
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Breastfeeding (mother) contraindication 413712001
Concomitant yellow fever vaccine contraindication 871717007




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.34 acidic
pKa2 5.15 acidic
pKa3 9.45 acidic
pKa4 13.09 acidic
pKa5 3.95 Basic

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
Thymidylate synthase Enzyme INHIBITOR IC50 6.47 WOMBAT-PK CHEMBL
Dihydrofolate reductase Enzyme INHIBITOR IC50 5.18 WOMBAT-PK CHEMBL
Trifunctional purine biosynthetic protein adenosine-3 Enzyme INHIBITOR Ki 6.42 CHEMBL DRUG LABEL
Serine hydroxymethyltransferase, cytosolic Enzyme Kd 4.77 CHEMBL
Folate receptor beta Membrane receptor IC50 7.22 CHEMBL
Proton-coupled folate transporter Transporter Ki 7.03 CHEMBL
Folate transporter 1 Transporter IC50 6.86 CHEMBL
Folate receptor alpha Membrane receptor IC50 7.38 CHEMBL
Folylpolyglutamate synthase, mitochondrial Enzyme WOMBAT-PK
Bifunctional dihydrofolate reductase-thymidylate synthase Enzyme IC50 6.37 CHEMBL
Dihydrofolate reductase Enzyme Ki 6.25 CHEMBL
Dihydrofolate reductase Enzyme IC50 5.64 CHEMBL
Thymidylate synthase Enzyme IC50 4.82 CHEMBL
Dihydrofolate reductase Enzyme IC50 5.64 CHEMBL
Thymidylate synthase Enzyme Ki 6.47 CHEMBL
Thymidylate synthase Enzyme IC50 4.70 CHEMBL
Thymidylate synthase Enzyme Ki 6.26 CHEMBL
Dihydrofolate reductase Enzyme IC50 5.64 CHEMBL
Thymidylate synthase Enzyme IC50 5.96 CHEMBL
Thymidylate synthase (EC 2.1.1.45) (TS) (TSase) Enzyme IC50 4.12 CHEMBL
Trifunctional purine biosynthetic protein adenosine-3 Enzyme INHIBITOR Ki 5.03 IUPHAR

External reference:

IDSource
4021417 VUID
N0000148831 NUI
D03828 KEGG_DRUG
150399-23-8 SECONDARY_CAS_RN
4021417 VANDF
C0210657 UMLSCUI
CHEBI:63724 CHEBI
4DW PDB_CHEM_ID
CHEMBL225072 ChEMBL_ID
CHEMBL2360464 ChEMBL_ID
D000068437 MESH_DESCRIPTOR_UI
DB00642 DRUGBANK_ID
135410875 PUBCHEM_CID
6837 IUPHAR_LIGAND_ID
7675 INN_ID
357166-29-1 SECONDARY_CAS_RN
04Q9AIZ7NO UNII
1666923 RXNORM
17856 MMSL
238966 MMSL
32871 MMSL
48646 MMSL
d05047 MMSL
008494 NDDF
008495 NDDF
409159000 SNOMEDCT_US
411089001 SNOMEDCT_US
735172002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Alimta HUMAN PRESCRIPTION DRUG LABEL 1 0002-7623 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS NDA 33 sections
Alimta HUMAN PRESCRIPTION DRUG LABEL 1 0002-7623 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS NDA 33 sections
Alimta HUMAN PRESCRIPTION DRUG LABEL 1 0002-7623 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS NDA 33 sections
Alimta HUMAN PRESCRIPTION DRUG LABEL 1 0002-7640 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS NDA 33 sections
Alimta HUMAN PRESCRIPTION DRUG LABEL 1 0002-7640 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS NDA 33 sections
Alimta HUMAN PRESCRIPTION DRUG LABEL 1 0002-7640 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS NDA 33 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0338-0720 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 27 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0338-0720 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 27 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0338-0722 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENTRICULAR ANDA 27 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0338-0722 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENTRICULAR ANDA 27 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0409-0004 INJECTION, SOLUTION, CONCENTRATE 1 g INTRAVENOUS NDA 30 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0409-0020 INJECTION, SOLUTION, CONCENTRATE 100 mg INTRAVENOUS NDA 30 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0409-0021 INJECTION, SOLUTION, CONCENTRATE 500 mg INTRAVENOUS NDA 30 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0409-1045 INJECTION, SOLUTION, CONCENTRATE 100 mg INTRAVENOUS NDA 32 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0409-2188 INJECTION, SOLUTION, CONCENTRATE 500 mg INTRAVENOUS NDA 32 sections
PEMETREXED HUMAN PRESCRIPTION DRUG LABEL 1 0409-3532 INJECTION, SOLUTION, CONCENTRATE 1 g INTRAVENOUS NDA 32 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 0781-3518 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 27 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 0781-3518 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 27 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 0781-3519 INJECTION, SOLUTION 500 mg INTRAVENOUS NDA 27 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 0781-3519 INJECTION, SOLUTION 500 mg INTRAVENOUS NDA 27 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 0781-3520 INJECTION, SOLUTION 1000 mg INTRAVENOUS NDA 27 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 0781-3520 INJECTION, SOLUTION 1000 mg INTRAVENOUS NDA 27 sections
Pemetrexed disodium HUMAN PRESCRIPTION DRUG LABEL 1 43598-370 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 g INTRAVENOUS ANDA 28 sections
Pemetrexed disodium HUMAN PRESCRIPTION DRUG LABEL 1 43598-370 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 g INTRAVENOUS ANDA 28 sections
Pemetrexed disodium HUMAN PRESCRIPTION DRUG LABEL 1 43598-386 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 28 sections
Pemetrexed disodium HUMAN PRESCRIPTION DRUG LABEL 1 43598-386 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 28 sections
Pemetrexed disodium HUMAN PRESCRIPTION DRUG LABEL 1 43598-387 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 28 sections
Pemetrexed disodium HUMAN PRESCRIPTION DRUG LABEL 1 43598-387 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAVENOUS ANDA 28 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 60505-6065 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 27 sections
Pemetrexed HUMAN PRESCRIPTION DRUG LABEL 1 60505-6065 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS ANDA 27 sections