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

Stem definitionDrug idCAS RN
humanized origin 5268 1610943-06-0

Description:

MoleculeDescription

Molfile

Synonyms:

  • emicizumab
  • emicizumab-kxwh
  • hemlibra
  • ACE910
  • emicizumab (genetical recombination)
Emicizumab-kxwh is a humanized monoclonal modified immunoglobulin G4 (IgG4) antibody with a bispecific antibody structure binding factor IXa and factor X. Emicizumab-kxwh has an approximate molecular weight of 145.6 kDa and is produced in genetically engineered mammalian (Chinese hamster ovary) cells. Emicizumab-kxwh has no structural relationship or sequence homology to FVIII and, as such, does not induce or enhance the development of direct inhibitors to FVIII. Emicizumab-kxwh bridges activated factor IX and factor X to restore the function of missing activated factor VIII that is needed for effective hemostasis.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
15 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Feb. 23, 2018 EMA Roche Registration Limited
March 23, 2018 PMDA Chugai Pharmaceutical Co., Ltd.
Nov. 16, 2017 FDA GENENTECH 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
Off label use 257.88 131.19 102 203 1102150 89525992
No adverse event 240.69 131.19 53 252 67929 90560213

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
Haemorrhage 2072.15 37.61 613 5163 59950 42555609
Haemarthrosis 1590.70 37.61 298 5478 3700 42611859
No adverse event 920.35 37.61 299 5477 38722 42576837
Muscle haemorrhage 399.36 37.61 96 5680 4029 42611530
Traumatic haemorrhage 356.80 37.61 71 5705 1206 42614353
Fall 150.24 37.61 171 5605 234349 42381210
Activated partial thromboplastin time prolonged 148.74 37.61 62 5714 15841 42599718
Injury 143.95 37.61 67 5709 22249 42593310
Spontaneous haemorrhage 143.73 37.61 29 5747 528 42615031
Drug specific antibody present 141.33 37.61 42 5734 3964 42611595
Anti factor VIII antibody positive 131.12 37.61 21 5755 90 42615469
Haematoma 126.58 37.61 66 5710 27957 42587602
Off label use 123.32 37.61 267 5509 638068 41977491
Factor VIII inhibition 121.24 37.61 23 5753 299 42615260
Head injury 118.03 37.61 57 5719 20525 42595034
Contusion 89.66 37.61 61 5715 41924 42573635
Haemophilic arthropathy 82.07 37.61 16 5760 242 42615317
Anti factor VIII antibody increased 82.05 37.61 12 5764 23 42615536
Injection site reaction 76.63 37.61 39 5737 15682 42599877
Post procedural haemorrhage 76.06 37.61 33 5743 9279 42606280
Arthralgia 75.28 37.61 114 5662 205124 42410435
Haematoma muscle 73.47 37.61 22 5754 2128 42613431
Joint injury 70.34 37.61 36 5740 14640 42600919
Inhibiting antibodies 63.54 37.61 9 5767 12 42615547
Limb injury 62.56 37.61 33 5743 14272 42601287
Haemorrhage intracranial 62.26 37.61 35 5741 17157 42598402
Haemorrhage subcutaneous 60.82 37.61 20 5756 2626 42612933
Mouth haemorrhage 57.11 37.61 24 5752 6237 42609322
Epistaxis 53.45 37.61 55 5721 66771 42548788
Ligament sprain 51.07 37.61 20 5756 4338 42611221
Haematuria 48.82 37.61 49 5727 57750 42557809
Haemophilic pseudotumour 47.44 37.61 6 5770 0 42615559
Gingival bleeding 41.19 37.61 21 5755 8464 42607095
Intermenstrual bleeding 39.54 37.61 5 5771 0 42615559
Joint swelling 38.90 37.61 47 5729 67975 42547584
Joint microhaemorrhage 38.85 37.61 7 5769 67 42615492

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
Haemorrhage 1824 35.41 493 4445 106199 110478162
Haemarthrosis 1396.32 35.41 247 4691 7082 110577279
No adverse event 780.78 35.41 236 4702 73603 110510758
Muscle haemorrhage 433.90 35.41 92 4846 6777 110577584
Traumatic haemorrhage 329.33 35.41 59 4879 1785 110582576
Off label use 207.14 35.41 290 4648 1499895 109084466
Activated partial thromboplastin time prolonged 199.49 35.41 63 4875 22305 110562056
Head injury 155.70 35.41 62 4876 42955 110541406
Anti factor VIII antibody positive 146.47 35.41 20 4918 89 110584272
Haematoma 134.18 35.41 61 4877 58415 110525946
Drug specific antibody present 119.59 35.41 34 4904 8400 110575961
Spontaneous haemorrhage 116.38 35.41 23 4915 1185 110583176
Fall 109.06 35.41 134 4804 603348 109981013
Factor VIII inhibition 108.93 35.41 18 4920 332 110584029
Inhibiting antibodies 73.53 35.41 9 4929 12 110584349
Haemophilic arthropathy 73.48 35.41 12 4926 205 110584156
Haematuria 68.73 35.41 44 4894 82961 110501400
Anti factor VIII antibody increased 67.30 35.41 9 4929 33 110584328
Limb injury 67.04 35.41 33 4905 37603 110546758
Haemorrhage subcutaneous 63.77 35.41 19 4919 5520 110578841
Joint injury 62.23 35.41 32 4906 39962 110544399
Injury 61.72 35.41 56 4882 177209 110407152
Haematoma muscle 60.28 35.41 17 4921 4073 110580288
Haemorrhage intracranial 59.46 35.41 28 4910 28941 110555420
Post procedural haemorrhage 58.31 35.41 23 4915 15489 110568872
Epistaxis 55.07 35.41 46 4892 130326 110454035
Mouth haemorrhage 50.70 35.41 20 4918 13468 110570893
Gingival bleeding 46.41 35.41 21 4917 19818 110564543
Haemophilic pseudotumour 45.09 35.41 5 4933 0 110584361
Gastrointestinal haemorrhage 43.83 35.41 45 4893 165473 110418888
Intra-abdominal haemorrhage 39.23 35.41 13 4925 5329 110579032
Cerebral haemorrhage 38.45 35.41 28 4910 64940 110519421
Contusion 37.43 35.41 49 4889 233312 110351049

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B02BX06 BLOOD AND BLOOD FORMING ORGANS
ANTIHEMORRHAGICS
VITAMIN K AND OTHER HEMOSTATICS
Other systemic hemostatics

Related Drugs by ATC class:

B02BX Other systemic hemostatics 10 drugs
avatrombopagcarbazochromeconcizumabeltrombopagetamsylatefitusiranfostamatiniblusutrombopagmarstacimab-hncqromiplostim

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

DiseaseRelationSNOMED_IDDOID
Hereditary factor VIII deficiency disease indication 28293008 DOID:12134




🐶 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
Coagulation factor X Enzyme ANTIBODY BINDING Kd 5.73 IUPHAR
Coagulation factor IX Enzyme ANTIBODY BINDING Kd 5.80 IUPHAR

External reference:

IDSource
7NL2E3F6K3 UNII
4037121 VANDF
4037122 VANDF
C4278463 UMLSCUI
CHEBI:755960 CHEBI
CHEMBL3833393 ChEMBL_ID
DB13923 DRUGBANK_ID
D10821 KEGG_DRUG
10115 INN_ID
C000608208 MESH_SUPPLEMENTAL_RECORD_UI
9744 IUPHAR_LIGAND_ID
763611007 SNOMEDCT_US
763612000 SNOMEDCT_US
265731 MMSL
33262 MMSL
33390 MMSL
d08677 MMSL
017412 NDDF
1989794 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Hemlibra HUMAN PRESCRIPTION DRUG LABEL 1 50242-920 INJECTION, SOLUTION 30 mg SUBCUTANEOUS BLA 29 sections
Hemlibra HUMAN PRESCRIPTION DRUG LABEL 1 50242-921 INJECTION, SOLUTION 60 mg SUBCUTANEOUS BLA 29 sections
Hemlibra HUMAN PRESCRIPTION DRUG LABEL 1 50242-922 INJECTION, SOLUTION 105 mg SUBCUTANEOUS BLA 29 sections
Hemlibra HUMAN PRESCRIPTION DRUG LABEL 1 50242-923 INJECTION, SOLUTION 150 mg SUBCUTANEOUS BLA 29 sections
Hemlibra HUMAN PRESCRIPTION DRUG LABEL 1 50242-927 INJECTION, SOLUTION 12 mg SUBCUTANEOUS BLA 29 sections
Hemlibra HUMAN PRESCRIPTION DRUG LABEL 1 50242-930 INJECTION, SOLUTION 300 mg SUBCUTANEOUS BLA 29 sections