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

Stem definition	Drug id	CAS RN
chimeric origin	5385	1461640-62-9

Description:

Molecule	Description
Synonyms: isatuximab isatuximab-irfc sarclisa SAR650984 hu38SB19 isatuximab (genetical recombination)	Isatuximab-irfc is an IgG1-derived monoclonal antibody that binds to CD38 expressed on the surface of hematopoietic and tumor cells, including multiple myeloma cells. Isatuximab-irfc induces apoptosis of tumor cells and activation of immune effector mechanisms including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), and complement dependent cytotoxicity (CDC). Isatuximab-irfc inhibits the ADP-ribosyl cyclase activity of CD38. Isatuximab-irfc can activate natural killer (NK) cells in the absence of CD38-positive target tumor cells and suppresses CD38-positive T-regulatory cells. The combination of isatuximab-irfc and pomalidomide enhanced ADCC activity and direct tumor cell killing compared to that of isatuximab-irfc alone in vitro, and enhanced antitumor activity compared to the activity of isatuximab-irfc or pomalidomide alone in a human multiple myeloma xenograft model Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

isatuximab
isatuximab-irfc
sarclisa
SAR650984
hu38SB19
isatuximab (genetical recombination)

Isatuximab-irfc is an IgG1-derived monoclonal antibody that binds to CD38 expressed on the surface of hematopoietic and tumor cells, including multiple myeloma cells. Isatuximab-irfc induces apoptosis of tumor cells and activation of immune effector mechanisms including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), and complement dependent cytotoxicity (CDC). Isatuximab-irfc inhibits the ADP-ribosyl cyclase activity of CD38. Isatuximab-irfc can activate natural killer (NK) cells in the absence of CD38-positive target tumor cells and suppresses CD38-positive T-regulatory cells. The combination of isatuximab-irfc and pomalidomide enhanced ADCC activity and direct tumor cell killing compared to that of isatuximab-irfc alone in vitro, and enhanced antitumor activity compared to the activity of isatuximab-irfc or pomalidomide alone in a human multiple myeloma xenograft model

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
May 30, 2020	EMA	Sanofi-Aventis groupe
March 2, 2020	FDA	SANOFI AVENTIS US
June 29, 2020	PMDA	Sanofi K.K.

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
Neutropenia	182.28	36.64	90	1621	174915	63312396
Infusion related reaction	98.17	36.64	68	1643	245453	63241858
COVID-19	96.41	36.64	51	1660	113052	63374259
Febrile infection	91.24	36.64	18	1693	1539	63485772
Lymphopenia	77.74	36.64	26	1685	18301	63469010
Pneumonia	66.75	36.64	71	1640	456696	63030615
COVID-19 pneumonia	59.61	36.64	20	1691	14189	63473122
Tumour lysis syndrome	51.36	36.64	16	1695	8974	63478337
Pneumococcal sepsis	46.55	36.64	9	1702	691	63486620
Pneumonia pneumococcal	46.48	36.64	11	1700	2204	63485107
Plasma cell myeloma refractory	45.77	36.64	8	1703	351	63486960

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
COVID-19	193.14	30.09	99	2414	77451	34876967
Neutropenia	153.86	30.09	110	2403	156668	34797750
Infusion related reaction	123.88	30.09	65	2448	52992	34901426
COVID-19 pneumonia	61.10	30.09	28	2485	16939	34937479
Pneumonia	48.41	30.09	90	2423	362537	34591881
Febrile neutropenia	44.78	30.09	52	2461	136797	34817621
Infection	42.92	30.09	42	2471	90873	34863545
Thrombocytopenia	40.81	30.09	53	2460	156194	34798224
Haemolytic uraemic syndrome	39.68	30.09	12	2501	2274	34952144
SARS-CoV-2 sepsis	39.24	30.09	7	2506	125	34954293
Pyrexia	31.69	30.09	72	2441	332941	34621477
Squamous cell carcinoma of skin	30.13	30.09	15	2498	10866	34943552

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
Neutropenia	288.16	31.74	181	3976	287529	79452702
COVID-19	264.39	31.74	139	4018	157535	79582696
Infusion related reaction	176.74	31.74	123	4034	230114	79510117
COVID-19 pneumonia	120.00	31.74	48	4109	28801	79711430
Pneumonia	103.88	31.74	148	4009	660098	79080133
Lymphopenia	87.48	31.74	39	4118	30518	79709713
Febrile neutropenia	78.42	31.74	77	4080	230922	79509309
Thrombocytopenia	67.81	31.74	76	4081	265183	79475048
Pyrexia	65.32	31.74	122	4035	678587	79061644
Plasma cell myeloma refractory	46.59	31.74	10	4147	662	79739569
Febrile infection	43.24	31.74	13	4144	3333	79736898
Tumour lysis syndrome	42.43	31.74	22	4135	23917	79716314
Febrile bone marrow aplasia	41.72	31.74	18	4139	13002	79727229
SARS-CoV-2 sepsis	41.28	31.74	7	4150	129	79740102
Pulmonary embolism	40.08	31.74	47	4110	171607	79568624
Polyneuropathy	36.61	31.74	20	4137	24131	79716100
Bronchopneumopathy	34.17	31.74	8	4149	785	79739446

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01FC02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES CD38 (Clusters of Differentiation 38) inhibitors
FDA CS	M0001357	Antibodies, Monoclonal
FDA MoA	N0000192335	CD38-directed Antibody Interactions
FDA EPC	N0000192336	CD38-directed Cytolytic Antibody

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

Disease	Relation	SNOMED_ID	DOID
Multiple myeloma	indication	109989006	DOID:9538

🐶 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])	Mechanism action	Bioact source	MoA source
Lymphocyte differentiation antigen CD38	Tumour-associated antigen	P28907	CD38_HUMAN	BINDING AGENT	Kd	9.70		SCIENTIFIC LITERATURE	DRUG LABEL

External reference:

ID	Source
R30772KCU0	UNII
C4330502	UMLSCUI
CHEMBL3545131	ChEMBL_ID
DB14811	DRUGBANK_ID
10068	INN_ID
D11050	KEGG_DRUG
8719	IUPHAR_LIGAND_ID
018293	NDDF
860763005	SNOMEDCT_US
860769009	SNOMEDCT_US
4039213	VANDF
4039214	VANDF
2282018	RXNORM
331339	MMSL
38183	MMSL
38185	MMSL
d09517	MMSL
C000599209	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Sarclisa	HUMAN PRESCRIPTION DRUG LABEL	1	0024-0654	INJECTION, SOLUTION, CONCENTRATE	100 mg	INTRAVENOUS	BLA	30 sections
Sarclisa	HUMAN PRESCRIPTION DRUG LABEL	1	0024-0654	INJECTION, SOLUTION, CONCENTRATE	100 mg	INTRAVENOUS	BLA	30 sections
Sarclisa	HUMAN PRESCRIPTION DRUG LABEL	1	0024-0654	INJECTION, SOLUTION, CONCENTRATE	100 mg	INTRAVENOUS	BLA	30 sections
Sarclisa	HUMAN PRESCRIPTION DRUG LABEL	1	0024-0656	INJECTION, SOLUTION, CONCENTRATE	500 mg	INTRAVENOUS	BLA	30 sections
Sarclisa	HUMAN PRESCRIPTION DRUG LABEL	1	0024-0656	INJECTION, SOLUTION, CONCENTRATE	500 mg	INTRAVENOUS	BLA	30 sections
Sarclisa	HUMAN PRESCRIPTION DRUG LABEL	1	0024-0656	INJECTION, SOLUTION, CONCENTRATE	500 mg	INTRAVENOUS	BLA	30 sections