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

Stem definitionDrug idCAS RN
chimeric origin 5385 1461640-62-9

Description:

MoleculeDescription

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

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
Neutropenia 379.03 33.31 195 4273 224709 90399270
Plasma cell myeloma refractory 193.06 33.31 35 4433 1021 90622958
Thrombocytopenia 154.90 33.31 107 4361 208618 90415361
COVID-19 152.88 33.31 98 4370 168745 90455234
Febrile infection 112.71 33.31 25 4443 2044 90621935
Thrombotic microangiopathy 110.79 33.31 38 4430 15705 90608274
Infusion related reaction 96.01 33.31 110 4358 416670 90207309
Cytokine release syndrome 89.54 33.31 38 4430 27935 90596044
COVID-19 pneumonia 87.02 33.31 33 4435 18144 90605835
Plasma cell myeloma 84.76 33.31 41 4427 40787 90583192
Lymphopenia 79.65 33.31 33 4435 22848 90601131
Anaemia 77.59 33.31 91 4377 352711 90271268
Hypogammaglobulinaemia 72.12 33.31 25 4443 10649 90613330
Neutrophil count decreased 68.24 33.31 43 4425 71489 90552490
Pneumonia 59.86 33.31 110 4358 637949 89986030
Tumour lysis syndrome 59.77 33.31 22 4446 11130 90612849
Disease progression 51.33 33.31 50 4418 156565 90467414
Spondylolysis 47.64 33.31 8 4460 147 90623832
Platelet count decreased 47.27 33.31 45 4423 136924 90487055
Pneumococcal sepsis 38.69 33.31 9 4459 909 90623070
Cardiac failure 37.81 33.31 36 4432 109460 90514519
Fracture pain 36.66 33.31 9 4459 1142 90622837
Craniocervical syndrome 36.06 33.31 6 4462 104 90623875
Pneumonia pneumococcal 33.33 33.31 10 4458 2692 90621287

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
Neutropenia 289.05 26.46 229 5601 199202 42416303
COVID-19 239.24 26.46 165 5665 115783 42499722
Infusion related reaction 180.65 26.46 109 5721 60697 42554808
Thrombocytopenia 124.41 26.46 141 5689 190138 42425367
IVth nerve paralysis 112.77 26.46 24 5806 567 42614938
IgA nephropathy 106.18 26.46 30 5800 2344 42613161
Pneumonia 87.20 26.46 183 5647 421966 42193539
Neutrophil count decreased 70.84 26.46 63 5767 63352 42552153
Plasma cell leukaemia 66.16 26.46 18 5812 1222 42614283
COVID-19 pneumonia 64.67 26.46 39 5791 21574 42593931
SARS-CoV-2 sepsis 58.14 26.46 12 5818 243 42615262
Infection 58.12 26.46 74 5756 111994 42503511
Squamous cell carcinoma of skin 54.38 26.46 29 5801 12697 42602808
Bronchitis 50.92 26.46 46 5784 47155 42568350
Respiratory tract infection 50.58 26.46 36 5794 26286 42589219
Anaemia 49.07 26.46 114 5716 280164 42335341
Respiratory tract infection viral 44.64 26.46 17 5813 3389 42612116
Febrile neutropenia 39.78 26.46 82 5748 185621 42429884
Basal cell carcinoma 38.92 26.46 29 5801 22704 42592801
Pyrexia 37.09 26.46 128 5702 393914 42221591
Lymphopenia 35.78 26.46 27 5803 21536 42593969
Bone pain 33.43 26.46 27 5803 23765 42591740
Thrombotic microangiopathy 32.57 26.46 22 5808 14760 42600745
Hypogammaglobulinaemia 31.84 26.46 20 5810 11871 42603634
Middle ear inflammation 31.64 26.46 7 5823 199 42615306
Infectious pleural effusion 31.56 26.46 13 5817 3182 42612323
Haemolytic uraemic syndrome 31.15 26.46 12 5818 2467 42613038
Factor VII deficiency 29.10 26.46 5 5825 35 42615470
Escherichia bacteraemia 28.57 26.46 14 5816 5135 42610370
Platelet count decreased 28.24 26.46 60 5770 138521 42476984
Pathological fracture 28.21 26.46 14 5816 5279 42610226
Pulmonary embolism 28.17 26.46 55 5775 119557 42495948
Polyneuropathy 27.97 26.46 22 5808 18639 42596866
Plasma cell myeloma 27.14 26.46 33 5797 47545 42567960
Stress echocardiogram abnormal 26.88 26.46 4 5826 9 42615496
Pulpitis dental 26.86 26.46 8 5822 752 42614753

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
Neutropenia 620.11 25.92 399 9752 374221 110204927
COVID-19 379.55 25.92 251 9900 244809 110334339
Thrombocytopenia 259.43 25.92 231 9920 348654 110230494
Infusion related reaction 188.54 25.92 202 9949 380960 110198188
Plasma cell myeloma refractory 181.00 25.92 41 10110 1960 110577188
COVID-19 pneumonia 154.32 25.92 73 10078 37070 110542078
Pneumonia 146.55 25.92 276 9875 876438 109702710
Neutrophil count decreased 135.74 25.92 102 10049 120839 110458309
Anaemia 129.13 25.92 201 9950 546885 110032263
IVth nerve paralysis 119.69 25.92 24 10127 635 110578513
Plasma cell myeloma 118.17 25.92 73 10078 62863 110516285
IgA nephropathy 109.38 25.92 30 10121 3143 110576005
Thrombotic microangiopathy 105.08 25.92 52 10099 29097 110550051
Lymphopenia 100.17 25.92 56 10095 40114 110539034
Hypogammaglobulinaemia 97.54 25.92 44 10107 20032 110559116
Platelet count decreased 76.80 25.92 100 10051 230343 110348805
Febrile infection 74.21 25.92 24 10127 4424 110574724
Febrile neutropenia 73.96 25.92 116 10035 316651 110262497
Respiratory tract infection 68.52 25.92 55 10096 71562 110507586
Pyrexia 67.71 25.92 208 9943 898057 109681091
Squamous cell carcinoma of skin 65.91 25.92 32 10119 17171 110561977
SARS-CoV-2 sepsis 62.45 25.92 12 10139 253 110578895
Respiratory tract infection viral 60.14 25.92 22 10129 5856 110573292
Bronchitis 58.39 25.92 72 10079 156960 110422188
Tumour lysis syndrome 53.44 25.92 34 10117 30767 110548381
Plasmacytoma 51.27 25.92 19 10132 5243 110573905
Pulmonary embolism 49.24 25.92 78 10073 214396 110364752
Disease progression 46.98 25.92 82 10069 243952 110335196
Infectious pleural effusion 45.24 25.92 17 10134 4874 110574274
Polyneuropathy 45.02 25.92 31 10120 31981 110547167
Osteolysis 39.75 25.92 16 10135 5507 110573641
Cytokine release syndrome 39.48 25.92 40 10111 70266 110508882
Spondylolysis 39.42 25.92 8 10143 225 110578923
Pathological fracture 39.05 25.92 20 10131 12012 110567136
Hypoproteinaemia 38.61 25.92 16 10135 5929 110573219
Pneumonia respiratory syncytial viral 38.51 25.92 13 10138 2736 110576412
Plasma cell leukaemia 37.84 25.92 12 10139 2076 110577072
Basal cell carcinoma 37.52 25.92 32 10119 45238 110533910
Febrile bone marrow aplasia 37.24 25.92 22 10129 17443 110561705
Hypocalcaemia 36.36 25.92 37 10114 65329 110513819
Middle ear inflammation 32.99 25.92 7 10144 246 110578902
Cytopenia 32.84 25.92 25 10126 30091 110549057
Craniocervical syndrome 32.34 25.92 6 10145 104 110579044
Cardiac failure 32.20 25.92 60 10091 187566 110391582
Infection 32.04 25.92 89 10062 362111 110217037
Fracture pain 31.14 25.92 9 10142 1139 110578009
Toxicity to various agents 30.59 25.92 4 10147 480551 110098597
Leukopenia 29.92 25.92 51 10100 148740 110430408
Pneumococcal sepsis 29.18 25.92 10 10141 2202 110576946
Stress echocardiogram abnormal 28.47 25.92 4 10147 9 110579139
Bronchopneumopathy 28.39 25.92 8 10143 925 110578223
Myelodysplastic syndrome 28.04 25.92 25 10126 37459 110541689
Drug interaction 27.78 25.92 6 10145 500177 110078971
Pneumonia pneumococcal 27.71 25.92 12 10139 4953 110574195
Escherichia bacteraemia 27.60 25.92 15 10136 10149 110568999
Influenza 26.46 25.92 52 10099 169049 110410099
Conjunctivitis viral 26.39 25.92 6 10145 291 110578857
Factor VII deficiency 26.13 25.92 5 10146 103 110579045
Bone pain 26.03 25.92 31 10120 65102 110514046

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

L01FC CD38 (Clusters of Differentiation 38) inhibitors 1 drug
daratumumab

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

DiseaseRelationSNOMED_IDDOID
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Lymphocyte differentiation antigen CD38 Tumour-associated antigen BINDING AGENT Kd 9.70 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
R30772KCU0 UNII
4039213 VANDF
4039214 VANDF
C4330502 UMLSCUI
CHEBI:755476 CHEBI
CHEMBL3545131 ChEMBL_ID
DB14811 DRUGBANK_ID
10068 INN_ID
C000599209 MESH_SUPPLEMENTAL_RECORD_UI
D11050 KEGG_DRUG
8719 IUPHAR_LIGAND_ID
860763005 SNOMEDCT_US
860769009 SNOMEDCT_US
331339 MMSL
38183 MMSL
38185 MMSL
d09517 MMSL
018293 NDDF
2282018 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 Escena HUMAN PRESCRIPTION DRUG LABEL 1 0024-0674 INJECTION, SOLUTION 140 mg SUBCUTANEOUS BLA 30 sections