ocrelizumab Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
humanized origin 5223 637334-45-3

Description:

MoleculeDescription

Synonyms:

  • ocrelizumab
  • PR070769
  • ocrevus
The precise mechanism by which ocrelizumab exerts its therapeutic effects in multiple sclerosis is unknown, but is presumed to involve binding to CD20, a cell surface antigen present on pre-B and mature B lymphocytes. Following cell surface binding to B lymphocytes, ocrelizumab results in antibody-dependent cellular cytolysis and complement-mediated lysis.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
3.29 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 1, 2018 EMA Roche Registration GmbH
March 28, 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
COVID-19 863.41 19.23 314 18858 18261 46648629
Infusion related reaction 562.10 19.23 405 18767 100803 46566087
Multiple sclerosis relapse 552.50 19.23 292 18880 41833 46625057
Urinary tract infection 493.68 19.23 525 18647 219741 46447149
Throat irritation 450.06 19.23 225 18947 28676 46638214
Multiple sclerosis 368.29 19.23 187 18985 24604 46642286
Herpes zoster 263.36 19.23 220 18952 67652 46599238
Oral herpes 249.84 19.23 133 19039 19257 46647633
Nasopharyngitis 239.65 19.23 305 18867 153693 46513197
Ear pruritus 157.53 19.23 51 19121 2069 46664821
Intentional product use issue 146.97 19.23 142 19030 52638 46614252
B-lymphocyte count decreased 137.70 19.23 37 19135 773 46666117
Relapsing multiple sclerosis 123.30 19.23 23 19149 74 46666816
Fatigue 118.84 19.23 528 18644 608169 46058721
JC polyomavirus test positive 100.47 19.23 30 19142 927 46665963
Influenza 98.34 19.23 150 19022 89120 46577770
Oropharyngeal pain 96.75 19.23 135 19037 74033 46592857
Muscle spasticity 95.07 19.23 59 19113 11381 46655509
Herpes virus infection 88.64 19.23 42 19130 4740 46662150
Breast cancer 81.57 19.23 97 19075 45421 46621469
Hypoaesthesia 74.36 19.23 156 19016 118713 46548177
COVID-19 pneumonia 73.98 19.23 33 19139 3242 46663648
Pruritus 73.08 19.23 242 18930 242110 46424780
Drug ineffective 70.80 19.23 106 19066 677732 45989158
Genital herpes 70.64 19.23 26 19146 1553 46665337
Magnetic resonance imaging abnormal 69.69 19.23 30 19142 2706 46664184
Lymphopenia 66.38 19.23 53 19119 15240 46651650
Gait disturbance 63.84 19.23 166 19006 145097 46521793
Anaemia 55.49 19.23 18 19154 255761 46411129
Cystitis 55.20 19.23 77 19095 42164 46624726
Throat tightness 54.53 19.23 54 19118 20585 46646305
Acute kidney injury 54.05 19.23 15 19157 235840 46431050
Optic neuritis 51.00 19.23 33 19139 6838 46660052
Invasive ductal breast carcinoma 49.20 19.23 31 19141 6137 46660753
Muscular weakness 47.76 19.23 112 19060 91732 46575158
Pregnancy 47.23 19.23 57 19115 27080 46639810
SARS-CoV-2 test positive 45.42 19.23 20 19152 1905 46664985
Drug interaction 42.79 19.23 15 19157 203079 46463811
Upper respiratory tract infection 42.74 19.23 86 19086 63470 46603420
Cough 41.70 19.23 196 18976 230053 46436837
Coronavirus infection 41.21 19.23 21 19151 2773 46664117
Rhinorrhoea 38.84 19.23 70 19102 47595 46619295
Asthenia 38.16 19.23 238 18934 310837 46356053
Feeling hot 37.91 19.23 61 19111 37867 46629023
Cystitis noninfective 37.83 19.23 14 19158 849 46666041
Relapsing-remitting multiple sclerosis 37.81 19.23 12 19160 456 46666434
Joint swelling 37.22 19.23 11 19161 166062 46500828
Headache 36.53 19.23 327 18845 478025 46188865
Product dose omission issue 36.26 19.23 12 19160 168508 46498382
Diarrhoea 35.54 19.23 115 19057 559487 46107403
Drug hypersensitivity 35.33 19.23 29 19143 243796 46423094
Paraesthesia 35.04 19.23 117 19055 117320 46549570
Neuralgia 34.12 19.23 43 19129 21340 46645550
Haemoglobin decreased 33.95 19.23 6 19166 128943 46537947
Therapeutic response shortened 33.82 19.23 23 19149 5176 46661714
Thrombocytopenia 33.08 19.23 6 19166 126575 46540315
Papilloma viral infection 31.71 19.23 14 19158 1342 46665548
Hemiparesis 31.46 19.23 40 19132 20029 46646861
Weight increased 31.20 19.23 142 19030 164331 46502559
Urticaria 29.62 19.23 111 19061 117781 46549109
Flushing 29.53 19.23 75 19097 64539 46602351
Hyponatraemia 28.28 19.23 4 19168 101328 46565562
Platelet count decreased 27.80 19.23 4 19168 100020 46566870
Infection 27.34 19.23 118 19054 133474 46533416
Perinatal stroke 27.07 19.23 5 19167 15 46666875
Abdominal pain 26.86 19.23 33 19139 229998 46436892
Infection susceptibility increased 25.40 19.23 14 19158 2165 46664725
Muscle spasms 25.39 19.23 109 19063 123004 46543886
Immunodeficiency 25.24 19.23 29 19143 13077 46653813
Cardiac failure congestive 24.74 19.23 4 19168 91746 46575144
Balance disorder 24.55 19.23 70 19102 64451 46602439
Pharyngeal swelling 24.41 19.23 16 19156 3387 46663503
Limb discomfort 23.26 19.23 37 19135 22739 46644151
Ataxia 22.20 19.23 28 19144 13902 46652988
Urinary incontinence 22.10 19.23 41 19131 28489 46638401
Respiratory tract infection 21.88 19.23 42 19130 29930 46636960
Nasal herpes 21.43 19.23 7 19165 292 46666598
Lobular breast carcinoma in situ 21.35 19.23 5 19167 58 46666832
Pharyngeal disorder 20.90 19.23 11 19161 1552 46665338
Vulvovaginal mycotic infection 20.87 19.23 16 19156 4335 46662555
Overdose 20.67 19.23 8 19164 101971 46564919
Renal impairment 20.60 19.23 3 19169 74369 46592521
Vomiting 20.54 19.23 106 19066 452688 46214202
Disease progression 20.53 19.23 6 19166 91294 46575596
Neuropathy peripheral 20.38 19.23 6 19166 90887 46576003
No adverse event 20.29 19.23 44 19128 34187 46632703
Product use in unapproved indication 20.17 19.23 6 19166 90267 46576623
Illness 20.17 19.23 25 19147 12199 46654691
Pyelonephritis 20.06 19.23 28 19144 15329 46651561
Renal failure 19.79 19.23 11 19161 113583 46553307
Gastrointestinal infection 19.74 19.23 19 19153 6991 46659899
Anogenital warts 19.64 19.23 7 19165 381 46666509
Oedema peripheral 19.60 19.23 22 19150 159684 46507206
Hypokalaemia 19.40 19.23 6 19166 88018 46578872
Treatment failure 19.37 19.23 7 19165 93080 46573810

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
COVID-19 569.07 25.96 191 6001 17687 29928599
Multiple sclerosis relapse 421.69 25.96 135 6057 10727 29935559
Urinary tract infection 304.72 25.96 189 6003 73470 29872816
Multiple sclerosis 292.86 25.96 93 6099 7174 29939112
Infusion related reaction 159.43 25.96 101 6091 40463 29905823
Nasopharyngitis 123.45 25.96 100 6092 58749 29887537
Herpes zoster 118.67 25.96 75 6117 29868 29916418
Throat irritation 102.60 25.96 45 6147 8503 29937783
Influenza 87.24 25.96 72 6120 43326 29902960
Urosepsis 72.27 25.96 38 6154 10694 29935592
JC polyomavirus test positive 72.17 25.96 18 6174 568 29945718
Intentional product use issue 70.18 25.96 59 6133 36381 29909905
Pruritus 68.68 25.96 102 6090 118102 29828184
COVID-19 pneumonia 68.08 25.96 28 6164 4512 29941774
Muscular weakness 67.26 25.96 74 6118 63571 29882715
Magnetic resonance imaging abnormal 62.53 25.96 20 6172 1570 29944716
Ear pruritus 58.87 25.96 13 6179 238 29946048
Gait disturbance 54.49 25.96 72 6120 74705 29871581
SARS-CoV-2 test positive 46.20 25.96 16 6176 1606 29944680
Balance disorder 39.49 25.96 43 6149 36450 29909836
Fatigue 39.35 25.96 150 6042 320523 29625763
Oropharyngeal pain 38.81 25.96 38 6154 28458 29917828
Muscle spasticity 36.71 25.96 19 6173 5169 29941117
Oral herpes 36.45 25.96 18 6174 4437 29941849
Acute kidney injury 35.18 25.96 7 6185 273835 29672451
Cellulitis 33.96 25.96 45 6147 46739 29899547
Breast cancer 29.81 25.96 8 6184 338 29945948
Anaemia 29.62 25.96 4 6188 207988 29738298
Rectal polyp 29.36 25.96 9 6183 614 29945672
Lymphopenia 28.85 25.96 23 6169 13140 29933146
Urticaria 28.61 25.96 45 6147 54561 29891725
Cystitis 28.27 25.96 19 6173 8355 29937931
Relapsing-remitting multiple sclerosis 27.17 25.96 7 6185 252 29946034

Pharmacologic Action:

SourceCodeDescription
ATC L04AA36 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
FDA CS M0001357 Antibodies, Monoclonal
FDA CS M0556300 Antibodies, Monoclonal, Humanized
FDA MoA N0000175078 CD20-directed Antibody Interactions
FDA EPC N0000175657 CD20-directed Cytolytic Antibody
MeSH PA D007155 Immunologic Factors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Primary progressive multiple sclerosis indication 428700003 DOID:0050784

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
B-lymphocyte antigen CD20 Surface antigen ANTIBODY BINDING Kd 9.08 IUPHAR DRUG LABEL

External reference:

IDSource
4036552 VANDF
C1882138 UMLSCUI
CHEMBL2108041 ChEMBL_ID
D05218 KEGG_DRUG
DB11988 DRUGBANK_ID
C533411 MESH_SUPPLEMENTAL_RECORD_UI
7580 IUPHAR_LIGAND_ID
8636 INN_ID
A10SJL62JY UNII
1876366 RXNORM
254931 MMSL
32532 MMSL
d08538 MMSL
017151 NDDF
733464008 SNOMEDCT_US
763559000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
OCREVUS HUMAN PRESCRIPTION DRUG LABEL 1 50242-150 INJECTION 300 mg INTRAVENOUS BLA 29 sections