trastuzumab deruxtecan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
humanized origin 5367 1826843-81-5

Description:

MoleculeDescription

Synonyms:

  • trastuzumab deruxtecan
  • enhertu
  • DS-8201a
  • fam-trastuzumab deruxtecan-nxki
Fam-trastuzumab deruxtecan-nxki is a HER2-directed antibody-drug conjugate. The antibody is a humanized anti-HER2 IgG1. The small molecule, DXd, is a topoisomerase I inhibitor attached to the antibody by a cleavable linker. Following binding to HER2 on tumor cells, fam-trastuzumab deruxtecan-nxki undergoes internalization and intracellular linker cleavage by lysosomal enzymes. Upon release, the membrane-permeable DXd causes DNA damage and apoptotic cell death.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
18 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
March 25, 2020 PMDA Daiichi Sankyo Company, Limited
Jan. 18, 2021 EMA DAIICHI SANKYO EUROPE GmbH
Dec. 20, 2019 FDA DAIICHI SANKYO

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
Interstitial lung disease 2548.06 29.47 841 17632 75564 90534410
Myelosuppression 1815.95 29.47 598 17875 52993 90556981
Disease progression 1418.70 29.47 672 17801 155943 90454031
Pneumonitis 924.93 29.47 345 18128 43825 90566149
Death 748.80 29.47 667 17806 455884 90154090
Metastases to central nervous system 605.43 29.47 199 18274 17343 90592631
Nausea 386.19 29.47 753 17720 1109563 89500411
No adverse event 356.77 29.47 203 18270 67779 90542195
Malignant neoplasm progression 325.62 29.47 226 18247 106644 90503330
Metastases to liver 239.27 29.47 117 18356 28690 90581284
Ejection fraction decreased 219.15 29.47 107 18366 26146 90583828
Neutrophil count decreased 217.06 29.47 151 18322 71381 90538593
Off label use 195.32 29.47 577 17896 1101675 89508299
Intentional product use issue 187.85 29.47 226 18247 216666 90393308
Metastases to meninges 181.24 29.47 55 18418 3680 90606294
Neutropenia 179.67 29.47 225 18248 224679 90385295
Pulmonary toxicity 176.87 29.47 72 18401 11459 90598515
Pneumocystis jirovecii pneumonia 159.39 29.47 81 18392 21535 90588439
Ascites 157.12 29.47 106 18367 47634 90562340
Metastases to bone 152.31 29.47 83 18390 25422 90584552
Metastases to lung 135.90 29.47 66 18407 15925 90594049
Metastases to skin 132.23 29.47 38 18435 2102 90607872
Metastases to lymph nodes 123.26 29.47 56 18417 11633 90598341
Pleural effusion 121.03 29.47 131 18342 111860 90498114
Vomiting 114.37 29.47 386 18087 787907 89822067
Arthralgia 102.05 29.47 18 18455 778504 89831470
Platelet count decreased 101.28 29.47 132 18341 136837 90473137
Therapy change 101.00 29.47 44 18429 8278 90601696
Diarrhoea 90.41 29.47 404 18069 938786 89671188
Joint swelling 85.88 29.47 4 18469 503296 90106678
Underdose 85.85 29.47 78 18395 53939 90556035
Vascular device infection 82.92 29.47 43 18430 11909 90598065
Nail bed inflammation 80.91 29.47 25 18448 1776 90608198
Nasal mucosal disorder 80.15 29.47 25 18448 1832 90608142
Streptococcal sepsis 74.84 29.47 28 18445 3556 90606418
Lung opacity 73.19 29.47 32 18441 6070 90603904
Pain 70.49 29.47 60 18413 996281 89613693
Thrombocytopenia 69.56 29.47 140 18333 208585 90401389
Drug hypersensitivity 66.95 29.47 8 18465 463601 90146373
Pseudomonal sepsis 66.43 29.47 27 18446 4275 90605699
Radiation necrosis 65.08 29.47 17 18456 656 90609318
Asthenia 64.01 29.47 246 18227 533505 90076469
Arthropathy 62.15 29.47 3 18470 366239 90243735
Fatigue 62.02 29.47 424 18049 1153599 89456375
COVID-19 62.00 29.47 118 18355 168725 90441249
Hepatic cytolysis 62.00 29.47 51 18422 30865 90579109
Cell death 60.65 29.47 23 18450 3032 90606942
Hepatic failure 60.45 29.47 56 18417 39672 90570302
Abdominal discomfort 60.38 29.47 12 18461 477316 90132658
Peripheral swelling 59.96 29.47 7 18466 413099 90196875
Gastrointestinal toxicity 59.82 29.47 32 18441 9435 90600539
Skin fissures 58.58 29.47 42 18431 20767 90589207
Pancytopenia 58.34 29.47 95 18378 120168 90489806
Sinusitis 57.61 29.47 3 18470 343085 90266889
White blood cell count decreased 56.74 29.47 113 18360 166996 90442978
Swelling 56.32 29.47 9 18464 419049 90190925
Hepatic function abnormal 55.02 29.47 57 18416 46231 90563743
Pseudocirrhosis 54.93 29.47 16 18457 928 90609046
Lymphangiosis carcinomatosa 53.75 29.47 18 18455 1654 90608320
Paronychia 53.24 29.47 28 18445 7978 90601996
Decreased appetite 53.07 29.47 183 18290 376357 90233617
Ventricular dysfunction 52.80 29.47 22 18451 3709 90606265
Varicose vein 52.67 29.47 27 18446 7300 90602674
Hypersensitivity 52.39 29.47 14 18459 454663 90155311
Anaemia 51.94 29.47 174 18299 352628 90257346
Radiation pneumonitis 51.89 29.47 18 18455 1840 90608134
Urticaria 51.68 29.47 3 18470 312731 90297243
Toxicity to various agents 51.60 29.47 152 18321 287694 90322280
Rash 50.29 29.47 53 18420 796047 89813927
Cardiac dysfunction 50.20 29.47 21 18452 3576 90606398
Hypertension 49.22 29.47 16 18457 457516 90152458
Brain oedema 48.73 29.47 35 18438 17350 90592624
Nasopharyngitis 47.91 29.47 12 18461 407092 90202882
Febrile neutropenia 47.77 29.47 102 18371 158247 90451727
Pruritus 46.98 29.47 26 18447 541499 90068475
Haematotoxicity 46.47 29.47 30 18443 12505 90597469
Hemianopia 46.17 29.47 17 18456 2065 90607909
Therapeutic product effect decreased 42.06 29.47 4 18469 277567 90332407
Blood bilirubin increased 42.00 29.47 48 18425 43422 90566552
Pulmonary embolism 41.47 29.47 86 18387 130734 90479240
Pneumocystis jirovecii infection 39.97 29.47 15 18458 1921 90608053
Contusion 39.76 29.47 3 18470 251213 90358761
Depression 39.17 29.47 7 18466 300594 90309380
Anxiety 38.70 29.47 8 18465 309764 90300210
Drug ineffective 38.51 29.47 149 18324 1384149 89225825
Headache 38.08 29.47 74 18399 862672 89747302
Blister 37.78 29.47 4 18469 254994 90354980
Pneumothorax 37.14 29.47 31 18442 19136 90590838
Drug interaction 36.98 29.47 6 18467 276447 90333527
Discomfort 36.59 29.47 6 18467 274329 90335645
Sepsis 36.13 29.47 99 18374 179715 90430259
Product use in unapproved indication 35.71 29.47 12 18461 336224 90273750
Treatment failure 35.66 29.47 9 18464 303919 90306055
Hypoaesthesia 35.56 29.47 10 18463 314200 90295774
Infusion related reaction 34.72 29.47 21 18452 416759 90193215
Pain in extremity 34.43 29.47 25 18448 450504 90159470
Hepatotoxicity 33.55 29.47 44 18429 45798 90564176
Asthma 32.97 29.47 5 18468 242155 90367819
Confusional state 32.81 29.47 19 18454 386186 90223788
Pneumonia bacterial 31.90 29.47 24 18449 12766 90597208
Respiratory failure 30.89 29.47 72 18401 118346 90491628
Mobility decreased 30.24 29.47 7 18466 250727 90359247
Portal hypertension 30.01 29.47 16 18457 4685 90605289
Excessive eye blinking 29.68 29.47 11 18462 1361 90608613

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
Disease progression 494.35 53.74 212 2223 143444 42475456
Interstitial lung disease 248.84 53.74 110 2325 78352 42540548
Underdose 149.50 53.74 50 2385 16616 42602284
Off label use 140.01 53.74 175 2260 638160 41980740
Death 118.76 53.74 139 2296 471046 42147854
Myelosuppression 115.86 53.74 53 2382 40408 42578492
Pneumonitis 108.10 53.74 51 2384 41667 42577233
Decreased appetite 100.72 53.74 85 2350 193052 42425848
Metastases to central nervous system 100.52 53.74 33 2402 10322 42608578
Neutrophil count decreased 96.04 53.74 54 2381 63361 42555539
No adverse event 58.35 53.74 33 2402 38988 42579912
Metastases to liver 54.99 53.74 24 2411 16302 42602598

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
Myelosuppression 1822.75 28.58 616 13737 93724 110481222
Disease progression 1476.85 28.58 688 13665 243346 110331600
Interstitial lung disease 1273.96 28.58 526 13827 138808 110436138
Pneumonitis 552.20 28.58 245 14108 76286 110498660
Metastases to central nervous system 506.27 28.58 166 14187 22651 110552295
Death 356.29 28.58 444 13909 698425 109876521
Neutrophil count decreased 298.04 28.58 189 14164 120752 110454194
Nausea 247.10 28.58 512 13841 1235178 109339768
Underdose 240.01 28.58 131 14222 63423 110511523
Metastases to liver 219.18 28.58 102 14251 35284 110539662
Malignant neoplasm progression 145.48 28.58 144 14209 174423 110400523
Platelet count decreased 138.83 28.58 160 14193 230283 110344663
Ejection fraction decreased 131.79 28.58 76 14277 40804 110534142
Metastases to meninges 128.67 28.58 41 14312 5087 110569859
Metastases to lymph nodes 127.36 28.58 54 14299 14978 110559968
Decreased appetite 123.41 28.58 221 14132 475625 110099321
Metastases to lung 119.99 28.58 59 14294 23004 110551942
Pulmonary toxicity 115.60 28.58 53 14300 17693 110557253
Metastases to bone 113.76 28.58 63 14290 31309 110543637
Metastases to skin 108.65 28.58 30 14323 2269 110572677
Ascites 105.28 28.58 91 14262 92717 110482229
Pneumocystis jirovecii pneumonia 100.65 28.58 65 14288 42670 110532276
Intentional product use issue 99.93 28.58 141 14212 247765 110327181
Nasal mucosal disorder 95.61 28.58 26 14327 1857 110573089
Off label use 95.50 28.58 415 13938 1499770 109075176
Nail bed inflammation 93.68 28.58 26 14327 2004 110572942
White blood cell count decreased 93.23 28.58 131 14222 229259 110345687
Pleural effusion 89.92 28.58 113 14240 177596 110397350
Vascular device infection 85.17 28.58 42 14311 16470 110558476
Vomiting 83.25 28.58 283 14070 910392 109664554
No adverse event 82.92 28.58 72 14281 73767 110501179
Neutropenia 82.05 28.58 162 14191 374458 110200488
Streptococcal sepsis 81.46 28.58 29 14324 5043 110569903
Pancytopenia 78.25 28.58 115 14238 209498 110365448
Varicose vein 72.61 28.58 29 14324 6911 110568035
Skin fissures 69.70 28.58 42 14311 24416 110550530
Anaemia 66.54 28.58 188 14165 546898 110028048
Febrile neutropenia 64.56 28.58 133 14220 316634 110258312
Pseudomonal sepsis 62.01 28.58 28 14325 9018 110565928
Arthralgia 61.78 28.58 13 14340 779619 109795327
Paronychia 56.59 28.58 28 14325 11053 110563893
Diarrhoea 55.96 28.58 293 14060 1139212 109435734
Thrombocytopenia 54.77 28.58 132 14221 348753 110226193
Therapy change 53.26 28.58 26 14327 9971 110564975
Pain 48.91 28.58 32 14321 954923 109620023
Ventricular dysfunction 47.55 28.58 22 14331 7489 110567457
Lung opacity 46.66 28.58 25 14328 11627 110563319
KL-6 increased 44.98 28.58 10 14343 307 110574639
Hemianopia 44.55 28.58 16 14337 2852 110572094
Pseudocirrhosis 43.41 28.58 12 14341 911 110574035
Pneumonia bacterial 43.10 28.58 32 14321 26229 110548717
Lymphangiosis carcinomatosa 42.94 28.58 15 14338 2467 110572479
Brain oedema 42.52 28.58 34 14319 31064 110543882
COVID-19 42.00 28.58 96 14257 244964 110329982
Rash 41.35 28.58 28 14325 820936 109754010
Drug interaction 40.28 28.58 8 14345 500175 110074771
Radiation necrosis 39.69 28.58 11 14342 843 110574103
Hepatic function abnormal 39.22 28.58 53 14300 89242 110485704
Radiation pneumonitis 37.44 28.58 16 14337 4520 110570426
Hypertension 37.41 28.58 10 14343 510074 110064872
Eastern Cooperative Oncology Group performance status worsened 36.69 28.58 14 14339 2955 110571991
Peripheral swelling 35.77 28.58 5 14348 404029 110170917
Hepatic failure 35.18 28.58 44 14309 68695 110506251
Product use in unapproved indication 34.29 28.58 8 14345 447369 110127577
Anxiety 33.74 28.58 3 14350 345075 110229871
Blood bilirubin increased 33.22 28.58 45 14308 75927 110499019
Pneumothorax 32.89 28.58 31 14322 35254 110539692
Pain in extremity 31.37 28.58 12 14341 487106 110087840
Breast cancer metastatic 31.33 28.58 19 14334 11162 110563784
Confusional state 31.10 28.58 11 14342 468669 110106277
Urticaria 30.56 28.58 3 14350 318854 110256092
Abdominal discomfort 30.27 28.58 7 14346 393851 110181095
Asthenia 30.17 28.58 172 14181 688827 109886119

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FD04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L01FD HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors 5 drugs
margetuximabpertuzumabtrastuzumabtrastuzumab emtansinezanidatamab-hrii

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

DiseaseRelationSNOMED_IDDOID
Advanced HER2 positive gastric or gastroesophageal junction (GEJ) adenocarcinoma indication 187734007
Metastatic human epidermal growth factor 2 positive carcinoma of breast indication 459391000124109
HER2 positive non-small cell lung cancer indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
Receptor tyrosine-protein kinase erbB-2 Kinase BINDING AGENT Kd 8.13 SCIENTIFIC LITERATURE DRUG LABEL
DNA topoisomerase 1 Enzyme INHIBITOR IC50 7.51 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
4039045 VANDF
CHEBI:757286 CHEBI
CHEMBL4297844 ChEMBL_ID
D11529 KEGG_DRUG
C000614160 MESH_SUPPLEMENTAL_RECORD_UI
DB14962 DRUGBANK_ID
838469001 SNOMEDCT_US
838478007 SNOMEDCT_US
C4726900 UMLSCUI
10516 INN_ID
328684 MMSL
37925 MMSL
018237 NDDF
5384HK7574 UNII
2267574 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Enhertu HUMAN PRESCRIPTION DRUG LABEL 1 65597-406 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 100 mg INTRAVENOUS BLA 33 sections