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

Stem definition	Drug id	CAS RN
humanized origin	5391	1491917-83-9

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company	Orphan
Nov. 22, 2021	EMA	GILEAD SCIENCES IRELAND UC
April 4, 2020	FDA	IMMUNOMEDICS INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
DNA topoisomerase 1	Enzyme	P11387	TOP1_HUMAN	BINDING AGENT			DRUG LABEL	DRUG LABEL
Tumor-associated calcium signal transducer 2	Tumour-associated antigen	P09758	TACD2_HUMAN	ANTIBODY BINDING	Kd	9.58	DRUG LABEL	DRUG LABEL
IgG receptor FcRn large subunit p51	Membrane receptor	P55899	FCGRN_HUMAN	ANTIBODY BINDING	Kd	6.71	DRUG LABEL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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