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

Stem definitionDrug idCAS RN
humanized origin 4957 380610-27-5

Description:

MoleculeDescription

Synonyms:

  • pertuzumab
  • perjeta
  • rhuMAb 2C4
a humanized HER-2 monoclonal antibody; prevents ERBB2 receptor protein from binding (dimerizing) to other receptors in the HER family
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 4, 2013 EMA
June 8, 2012 FDA GENENTECH

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
Diarrhoea 2902.33 50.19 1064 4831 82500 2269690
Ejection fraction decreased 979.41 50.19 220 5675 2581 2349609
Febrile neutropenia 942.28 50.19 281 5614 10601 2341589
Fatigue 796.70 50.19 440 5455 84433 2267757
Dyspnoea 685.29 50.19 389 5506 78344 2273846
Nausea 680.19 50.19 439 5456 111750 2240440
Neutropenia 638.01 50.19 249 5646 21299 2330891
Neuropathy peripheral 608.53 50.19 204 5691 11228 2340962
Rash 598.39 50.19 324 5571 59234 2292956
Pyrexia 569.48 50.19 303 5592 53405 2298785
Disease progression 560.74 50.19 213 5682 16882 2335308
Polyneuropathy 468.69 50.19 111 5784 1652 2350538
Mucosal inflammation 455.47 50.19 136 5759 5088 2347102
Vomiting 452.78 50.19 289 5606 71313 2280877
Decreased appetite 416.08 50.19 201 5694 28690 2323500
Interstitial lung disease 401.62 50.19 136 5759 7676 2344514
Chills 401.08 50.19 163 5732 15389 2336801
Alopecia 397.00 50.19 179 5716 21822 2330368
Stomatitis 391.41 50.19 141 5754 9569 2342621
Cardiotoxicity 339.08 50.19 80 5815 1167 2351023
Metastases to central nervous system 338.64 50.19 89 5806 2059 2350131
Pleural effusion 334.24 50.19 132 5763 11536 2340654
Dehydration 320.19 50.19 155 5740 22140 2330050
Infusion related reaction 316.61 50.19 121 5774 9675 2342515
Pneumonia 300.57 50.19 195 5700 49101 2303089
Pneumonitis 299.87 50.19 93 5802 3946 2348244
Epistaxis 288.28 50.19 113 5782 9666 2342524
Hypokalaemia 278.89 50.19 113 5782 10541 2341649
Peripheral sensory neuropathy 274.36 50.19 65 5830 965 2351225
Cardiac failure 268.38 50.19 114 5781 11980 2340210
Constipation 267.78 50.19 136 5759 21493 2330697
Palmar-plantar erythrodysaesthesia syndrome 263.20 50.19 85 5810 4116 2348074
Neutropenic sepsis 257.52 50.19 66 5829 1376 2350814
Anaemia 255.41 50.19 155 5740 34637 2317553
General physical health deterioration 241.79 50.19 111 5784 14028 2338162
Urinary tract infection 239.44 50.19 141 5754 29801 2322389
Dysgeusia 225.68 50.19 91 5804 8368 2343822
Cellulitis 225.05 50.19 93 5802 9108 2343082
Cough 223.77 50.19 140 5755 32977 2319213
Left ventricular dysfunction 217.71 50.19 56 5839 1184 2351006
Bone pain 200.11 50.19 85 5810 8911 2343279
Asthenia 197.30 50.19 148 5747 46778 2305412
Lower respiratory tract infection 189.50 50.19 71 5824 5353 2346837
Weight decreased 179.16 50.19 115 5780 28256 2323934
Death 176.99 50.19 176 5719 81292 2270898
Hypoaesthesia 176.78 50.19 101 5794 20114 2332076
Metastases to bone 175.70 50.19 54 5841 2215 2349975
Metastases to liver 173.96 50.19 57 5838 2884 2349306
Myalgia 173.61 50.19 105 5790 23228 2328962
Chest discomfort 163.72 50.19 86 5809 14509 2337681
Metastases to lung 159.01 50.19 47 5848 1684 2350506
Erythema 158.83 50.19 102 5793 25057 2327133
Pruritus 158.67 50.19 126 5769 43214 2308976
Back pain 158.25 50.19 111 5784 31548 2320642
Colitis 155.96 50.19 61 5834 5165 2347025
Hypersensitivity 154.76 50.19 98 5797 23495 2328695
Sepsis 152.61 50.19 89 5806 18399 2333791
Headache 150.10 50.19 160 5735 80019 2272171
Hypotension 148.92 50.19 108 5787 32328 2319862
Paraesthesia 147.98 50.19 93 5802 21995 2330195
Tachycardia 146.11 50.19 83 5812 16326 2335864
Nasopharyngitis 145.60 50.19 92 5803 21964 2330226
Abdominal pain 138.88 50.19 106 5789 34268 2317922
Rhinorrhoea 137.88 50.19 62 5833 7438 2344752
Erysipelas 135.64 50.19 37 5858 986 2351204
Skin toxicity 135.34 50.19 35 5860 755 2351435
Dyspepsia 133.61 50.19 66 5829 9778 2342412
Cardiomyopathy 132.78 50.19 46 5849 2761 2349429
Dry skin 131.93 50.19 58 5837 6594 2345596
Oxygen saturation decreased 130.88 50.19 60 5835 7526 2344664
Malaise 129.56 50.19 125 5770 55460 2296730
Lacrimation increased 124.73 50.19 44 5851 2786 2349404
Onycholysis 124.61 50.19 27 5868 260 2351930
Arthralgia 120.72 50.19 119 5776 54166 2298024
Malignant neoplasm progression 117.85 50.19 65 5830 12063 2340127
Acute kidney injury 116.34 50.19 88 5807 28034 2324156
Pain 114.76 50.19 123 5772 61734 2290456
Dysuria 114.04 50.19 45 5850 3896 2348294
Dizziness 112.97 50.19 119 5776 58546 2293644
Breast cancer 112.27 50.19 58 5837 9437 2342753
Metastasis 106.69 50.19 30 5865 896 2351294
Leukopenia 105.57 50.19 57 5838 10139 2342051
Breast cancer metastatic 104.74 50.19 36 5859 2108 2350082
Abdominal pain upper 104.53 50.19 75 5820 22025 2330165
Hot flush 102.83 50.19 50 5845 7149 2345041
Off label use 100.57 50.19 125 5770 73473 2278717
Lymphoedema 100.40 50.19 30 5865 1115 2351075
Oedema peripheral 99.66 50.19 75 5820 23688 2328502
Platelet count decreased 99.38 50.19 64 5831 15749 2336441
Pulmonary embolism 98.66 50.19 67 5828 18016 2334174
Flushing 97.47 50.19 57 5838 11814 2340376
Anaphylactic reaction 96.98 50.19 53 5842 9652 2342538
Pericardial effusion 96.13 50.19 40 5855 3969 2348221
Radiation skin injury 94.64 50.19 20 5875 169 2352021
Lethargy 93.72 50.19 50 5845 8680 2343510
Pancytopenia 91.42 50.19 54 5841 11398 2340792
Nail dystrophy 91.23 50.19 17 5878 68 2352122
Neoplasm progression 90.26 50.19 40 5855 4628 2347562
Nail toxicity 87.77 50.19 16 5879 55 2352135
Nail disorder 87.75 50.19 27 5868 1109 2351081
Red cell distribution width increased 85.50 50.19 23 5872 580 2351610
Pain in extremity 84.82 50.19 88 5807 42452 2309738
Onychomadesis 84.81 50.19 22 5873 480 2351710
Hypertension 80.06 50.19 70 5825 27291 2324899
Dyspnoea exertional 79.49 50.19 39 5856 5681 2346509
Drug ineffective 78.95 50.19 132 5763 101492 2250698
Gastritis 78.24 50.19 36 5859 4545 2347645
Peripheral swelling 76.99 50.19 57 5838 17540 2334650
Vascular device infection 76.59 50.19 19 5876 344 2351846
Haematotoxicity 74.58 50.19 24 5871 1143 2351047
Cardiac dysfunction 74.02 50.19 16 5879 152 2352038
Pulmonary mass 73.77 50.19 27 5868 1899 2350291
Lung infiltration 73.09 50.19 28 5867 2236 2349954
Thrombocytopenia 72.75 50.19 57 5838 19074 2333116
Blood magnesium decreased 71.82 50.19 24 5871 1288 2350902
Hypomagnesaemia 69.71 50.19 28 5867 2536 2349654
Palpitations 69.07 50.19 52 5843 16404 2335786
Tumour pain 68.88 50.19 15 5880 148 2352042
Ill-defined disorder 68.71 50.19 30 5865 3348 2348842
Breast pain 66.87 50.19 23 5872 1348 2350842
Neutrophil count decreased 65.96 50.19 36 5859 6531 2345659
Mastitis 65.91 50.19 18 5877 481 2351709
Nail discolouration 64.94 50.19 18 5877 509 2351681
Onychoclasis 64.93 50.19 20 5875 824 2351366
Chest pain 64.82 50.19 63 5832 28074 2324116
Cystitis noninfective 63.59 50.19 14 5881 146 2352044
Dry mouth 63.45 50.19 38 5857 8215 2343975
Device related infection 63.23 50.19 28 5867 3231 2348959
Osteosclerosis 62.48 50.19 16 5879 331 2351859
Bone marrow failure 62.22 50.19 33 5862 5653 2346537
Respiratory tract infection 60.58 50.19 29 5866 4000 2348190
Haemoglobin decreased 60.34 50.19 50 5845 18101 2334089
Skin disorder 60.33 50.19 28 5867 3603 2348587
Clostridium difficile infection 59.86 50.19 26 5869 2864 2349326
Ascites 59.76 50.19 32 5863 5588 2346602
Influenza like illness 59.25 50.19 42 5853 12072 2340118
Enterocolitis infectious 58.84 50.19 14 5881 211 2351979
Hypocalcaemia 58.54 50.19 28 5867 3855 2348335
Osteolysis 58.32 50.19 16 5879 435 2351755
Insomnia 58.01 50.19 57 5838 25730 2326460
Dermatitis acneiform 57.32 50.19 18 5877 791 2351399
Painful respiration 57.23 50.19 15 5880 341 2351849
Dysphagia 57.16 50.19 42 5853 12763 2339427
Vertigo 56.50 50.19 37 5858 9347 2342843
Infection 56.49 50.19 48 5847 17981 2334209
Mean platelet volume decreased 56.10 50.19 12 5883 108 2352082
Lymphocyte count decreased 56.08 50.19 26 5869 3337 2348853
Oral pain 55.83 50.19 26 5869 3371 2348819
Productive cough 55.74 50.19 30 5865 5291 2346899
Gastroenteritis 55.24 50.19 25 5870 3035 2349155
Mastectomy 54.83 50.19 14 5881 286 2351904
Tremor 54.72 50.19 50 5845 20611 2331579
HER-2 positive breast cancer 54.51 50.19 11 5884 72 2352118
Intentional product use issue 54.38 50.19 26 5869 3576 2348614
Tongue coated 53.85 50.19 13 5882 209 2351981
Skin exfoliation 53.37 50.19 30 5865 5760 2346430
Mitral valve incompetence 53.00 50.19 23 5872 2527 2349663
Respiratory failure 52.91 50.19 41 5854 13487 2338703
Vascular fragility 51.36 50.19 9 5886 23 2352167
Blood pressure increased 50.72 50.19 44 5851 16942 2335248
Hyperhidrosis 50.24 50.19 42 5853 15380 2336810

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
Carbohydrate antigen 15-3 increased 84.76 49.16 9 181 6 1746585
Intentional product use issue 82.94 49.16 17 173 2702 1743889
Tidal volume decreased 66.97 49.16 7 183 3 1746588
Pulmonary hypoplasia 57.29 49.16 8 182 119 1746472
Off label use 55.54 49.16 22 168 38549 1708042
Hepatic lesion 53.36 49.16 9 181 483 1746108

Pharmacologic Action:

SourceCodeDescription
ATC L01XC13 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Monoclonal antibodies
FDA EPC N0000175661 HER2/neu Receptor Antagonist
FDA MoA N0000020008 HER2/Neu/cerbB2 Antagonists
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000074322 Antineoplastic Agents, Immunological

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
HER2-positive carcinoma of breast indication 427685000

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
Receptor tyrosine-protein kinase erbB-2 Kinase ANTIBODY BINDING UNKNOWN DRUG LABEL

External reference:

IDSource
D05446 KEGG_DRUG
4031566 VUID
N0000185031 NUI
C1328025 UMLSCUI
704227006 SNOMEDCT_US
1298944 RXNORM
28589 MMSL
d07874 MMSL
014427 NDDF
4031566 VANDF
704226002 SNOMEDCT_US
K16AIQ8CTM UNII
8380 INN_ID
DB06366 DRUGBANK_ID
CHEMBL2007641 ChEMBL_ID
5046 IUPHAR_LIGAND_ID
C485206 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PERJETA HUMAN PRESCRIPTION DRUG LABEL 1 50242-145 INJECTION, SOLUTION, CONCENTRATE 30 mg INTRAVENOUS BLA 18 sections