sacituzumab govitecan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

Approvals:

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

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 1948.21 33.44 649 5924 122109 63360340
Inappropriate schedule of product administration 602.95 33.44 266 6307 103699 63378750
Weight fluctuation 542.15 33.44 138 6435 9681 63472768
Neutropenia 373.48 33.44 229 6344 174776 63307673
Death 243.19 33.44 242 6331 374139 63108310
Diarrhoea 175.21 33.44 284 6289 715082 62767367
Neutropenic colitis 143.91 33.44 38 6535 3057 63479392
Neutrophil count decreased 143.59 33.44 83 6490 56323 63426126
Febrile neutropenia 129.09 33.44 103 6470 118346 63364103
Heart rate increased 86.01 33.44 74 6499 94164 63388285
General physical condition abnormal 84.50 33.44 27 6546 4247 63478202
Weight decreased 79.71 33.44 119 6454 276679 63205770
Neutrophil count abnormal 77.19 33.44 23 6550 2869 63479580
Colitis 65.50 33.44 48 6525 48480 63433969
Asthenia 63.30 33.44 129 6444 383475 63098974
Off label use 61.21 33.44 180 6393 674282 62808167
Metastases to central nervous system 58.17 33.44 28 6545 13077 63469372
COVID-19 48.29 33.44 59 6514 113044 63369405
Weight increased 44.45 33.44 89 6484 260703 63221746
Febrile bone marrow aplasia 42.98 33.44 19 6554 7306 63475143
SARS-CoV-2 test positive 38.15 33.44 18 6555 8038 63474411
Product preparation issue 37.32 33.44 11 6562 1321 63481128
Intentional dose omission 35.07 33.44 17 6556 8058 63474391

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 94.84 45.08 37 257 136812 34819825
Sepsis 49.42 45.08 25 269 166536 34790101

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 878.52 34.35 345 4255 184017 79555771
Weight fluctuation 519.84 34.35 123 4477 11552 79728236
Inappropriate schedule of product administration 350.94 34.35 165 4435 133463 79606325
Neutropenia 161.88 34.35 133 4467 287577 79452211
Death 133.50 34.35 163 4437 566351 79173437
Diarrhoea 123.20 34.35 197 4403 880292 78859496
Neutrophil count decreased 102.29 34.35 65 4535 93894 79645894
Heart rate increased 98.94 34.35 70 4530 120654 79619134
Neutropenic colitis 92.39 34.35 27 4573 5680 79734108
Febrile neutropenia 88.27 34.35 86 4514 230913 79508875
Weight decreased 73.38 34.35 96 4504 355102 79384686
Weight increased 66.83 34.35 81 4519 277305 79462483
Neutrophil count abnormal 49.74 34.35 15 4585 3511 79736277
Alopecia 46.83 34.35 62 4538 231293 79508495
Metastases to central nervous system 42.04 34.35 20 4580 16355 79723433
Colitis 39.12 34.35 33 4567 73274 79666514

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

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
C4086837 UMLSCUI
CHEMBL3545262 ChEMBL_ID
91668186 PUBCHEM_CID
DB12893 DRUGBANK_ID
CHEMBL3707405 ChEMBL_ID
8253 IUPHAR_LIGAND_ID
018344 NDDF
871700000 SNOMEDCT_US
871701001 SNOMEDCT_US
871812009 SNOMEDCT_US
4039353 VANDF
4039354 VANDF
10418 INN_ID
2360231 RXNORM
333695 MMSL
38376 MMSL
38377 MMSL
d09554 MMSL
C000608132 MESH_SUPPLEMENTAL_RECORD_UI
10097 INN_ID

Pharmaceutical products:

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