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

Stem definitionDrug idCAS RN
humanized origin 5391 1491917-83-9

Description:

MoleculeDescription

Molfile

Synonyms:

  • sacituzumab
  • sacituzumab govitecan
  • sacituzumab govitecan-hziy
  • trodelvy
  • IMMU-132
  • TROP-2-SN-38
  • hRS7-SN-38-ADC
Sacituzumab govitecan-hziy is a Trop-2-directed antibody-drug conjugate. Sacituzumab is a humanized antibody that recognizes Trop-2. The small molecule, SN-38, is a topoisomerase I inhibitor, which is covalently attached to the antibody by a linker. Pharmacology data suggest that sacituzumab govitecan-hziy binds to Trop-2-expressing cancer cells and is internalized with the subsequent release of SN-38 via hydrolysis of the linker. SN-38 interacts with topoisomerase I and prevents re-ligation of topoisomerase I-induced single strand breaks. The resulting DNA damage leads to apoptosis and cell death. Sacituzumab govitecan-hziy decreased tumor growth in mouse xenograft models of triple-negative breast cancer
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
April 4, 2020 FDA IMMUNOMEDICS INC
Nov. 22, 2021 EMA GILEAD SCIENCES IRELAND UC

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
Disease progression 4243.78 32.35 1320 10791 155295 90461041
Neutropenia 967.99 32.35 508 11603 224396 90391940
Inappropriate schedule of product administration 629.89 32.35 334 11777 149599 90466737
Weight fluctuation 600.99 32.35 184 11927 19565 90596771
Death 561.78 32.35 472 11639 456079 90160257
Diarrhoea 385.22 32.35 543 11568 938647 89677689
Febrile neutropenia 244.97 32.35 188 11923 158161 90458175
Neutrophil count decreased 219.47 32.35 130 11981 71402 90544934
Neutropenic colitis 207.84 32.35 57 12054 4086 90612250
Metastases to central nervous system 166.90 32.35 69 12042 17473 90598863
Neutrophil count abnormal 131.97 32.35 40 12071 4088 90612248
Asthenia 122.50 32.35 239 11872 533512 90082824
Thrombocytopenia 115.90 32.35 141 11970 208584 90407752
Myelosuppression 113.24 32.35 77 12034 53514 90562822
Colitis 94.91 32.35 77 12034 69865 90546471
Heart rate increased 87.85 32.35 91 12020 112811 90503525
Metastases to liver 84.72 32.35 51 12060 28756 90587580
General physical condition abnormal 84.19 32.35 30 12081 5081 90611255
Pneumonitis 80.55 32.35 58 12053 44112 90572224
Febrile bone marrow aplasia 78.29 32.35 34 12077 9704 90606632
Weight decreased 74.93 32.35 160 11951 379750 90236586
Product preparation issue 67.63 32.35 21 12090 2325 90614011
Haematotoxicity 58.27 32.35 30 12081 12505 90603831
Anaemia 56.62 32.35 137 11974 352665 90263671
Cholinergic syndrome 56.30 32.35 14 12097 682 90615654
Haemoglobin abnormal 54.51 32.35 24 12087 7076 90609260
Metastases to meninges 54.33 32.35 20 12091 3715 90612621
Constipation 51.68 32.35 115 11996 280280 90336056
Mucosal inflammation 47.60 32.35 48 12063 57577 90558759
Product preparation error 46.09 32.35 24 12087 10237 90606099
Drug hypersensitivity 44.50 32.35 5 12106 463604 90152732
SARS-CoV-2 test positive 41.50 32.35 23 12088 11105 90605231
Drug intolerance 40.14 32.35 6 12105 447585 90168751
Cell death 39.48 32.35 15 12096 3040 90613296
COVID-19 38.98 32.35 76 12035 168767 90447569
Arthralgia 38.23 32.35 29 12082 778493 89837843
Alopecia 35.99 32.35 146 11965 494925 90121411
White blood cell count decreased 35.90 32.35 73 12038 167036 90449300
Neutropenic sepsis 35.79 32.35 25 12086 18105 90598231
Breast cancer metastatic 34.96 32.35 23 12088 15109 90601227
Septic shock 34.42 32.35 49 12062 84111 90532225
Metastases to bone 34.40 32.35 28 12083 25477 90590859
Condition aggravated 33.52 32.35 19 12092 595526 90020810

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
Febrile neutropenia 88.05 44.57 43 470 185660 42435162
Sepsis 59.54 44.57 34 479 199300 42421522
Neutropenic sepsis 50.79 44.57 15 498 15931 42604891
Neutropenic colitis 47.70 44.57 11 502 4459 42616363
Disease progression 46.79 44.57 26 487 143630 42477192
Colitis 45.31 44.57 18 495 46554 42574268

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
Disease progression 1862.88 29.40 714 8644 243320 110336621
Neutropenia 604.67 29.40 381 8977 374239 110205702
Weight fluctuation 563.70 29.40 162 9196 21983 110557958
Inappropriate schedule of product administration 331.79 29.40 209 9149 203428 110376513
Diarrhoea 327.70 29.40 438 8920 1139067 109440874
Death 288.30 29.40 323 9035 698546 109881395
Neutrophil count decreased 203.81 29.40 127 9231 120814 110459127
Febrile neutropenia 148.24 29.40 157 9201 316610 110263331
Neutropenic colitis 140.10 29.40 44 9314 8021 110571920
Metastases to central nervous system 118.03 29.40 51 9307 22766 110557175
Myelosuppression 114.96 29.40 81 9277 94259 110485682
Heart rate increased 92.66 29.40 85 9273 143749 110436192
Asthenia 84.31 29.40 182 9176 688817 109891124
Alopecia 81.18 29.40 125 9233 364628 110215313
Colitis 80.99 29.40 68 9290 102255 110477686
Metastases to liver 72.00 29.40 42 9316 35344 110544597
Weight decreased 65.76 29.40 131 9227 467926 110112015
Neutrophil count abnormal 60.91 29.40 21 9337 5111 110574830
Thrombocytopenia 50.57 29.40 99 9259 348786 110231155
Product preparation issue 47.58 29.40 15 9343 2764 110577177
Constipation 46.46 29.40 97 9261 357689 110222252
Weight increased 42.44 29.40 103 9255 419541 110160400
White blood cell count decreased 41.94 29.40 72 9286 229318 110350623
Fatigue 40.47 29.40 206 9152 1215752 109364189
Anaemia 39.93 29.40 119 9239 546967 110032974
Febrile bone marrow aplasia 38.91 29.40 22 9336 17443 110562498
Nausea 37.44 29.40 204 9154 1235486 109344455
Breast cancer metastatic 35.99 29.40 18 9340 11163 110568778
Energy increased 32.16 29.40 12 9346 3662 110576279
SARS-CoV-2 test positive 31.56 29.40 19 9339 16916 110563025
Metastases to bone 31.52 29.40 24 9334 31348 110548593
Haemoglobin abnormal 30.42 29.40 15 9343 9023 110570918
Flashback 29.66 29.40 7 9351 435 110579506

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FX17 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
Other monoclonal antibodies and antibody drug conjugates
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L01FX Other monoclonal antibodies and antibody drug conjugates 29 drugs
amivantamabbelantamab mafodotinblinatumomabbrentuximab vedotincatumaxomabdatopotamab deruxtecanelotuzumabelranatamabenfortumab vedotinepcoritamabgemtuzumab ozogamicinglofitamab show all 29 →

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

DiseaseRelationSNOMED_IDDOID
Triple negative breast neoplasms indication 706970001




🐶 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
DNA topoisomerase 1 Enzyme BINDING AGENT DRUG LABEL DRUG LABEL
Tumor-associated calcium signal transducer 2 Tumour-associated antigen ANTIBODY BINDING Kd 9.58 DRUG LABEL DRUG LABEL
IgG receptor FcRn large subunit p51 Membrane receptor ANTIBODY BINDING Kd 6.71 DRUG LABEL

External reference:

IDSource
D10985 KEGG_DRUG
M9BYU8XDQ6 UNII
1796566-95-4 SECONDARY_CAS_RN
4039353 VANDF
4039354 VANDF
C4086837 UMLSCUI
CHEBI:755547 CHEBI
CHEMBL3545262 ChEMBL_ID
91668186 PUBCHEM_CID
DB12893 DRUGBANK_ID
CHEMBL3707405 ChEMBL_ID
10097 INN_ID
C000608132 MESH_SUPPLEMENTAL_RECORD_UI
8253 IUPHAR_LIGAND_ID
871700000 SNOMEDCT_US
871701001 SNOMEDCT_US
871812009 SNOMEDCT_US
10418 INN_ID
333695 MMSL
38376 MMSL
38377 MMSL
d09554 MMSL
018344 NDDF
2360231 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TRODELVY HUMAN PRESCRIPTION DRUG LABEL 1 55135-132 POWDER, FOR SOLUTION 180 mg INTRAVENOUS BLA 35 sections