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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 1548 231277-92-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lapatinib tosilate hydrate
  • lapatinib tosilate
  • lapatinib
  • GW 572016X
  • tyverb
  • lapatinib ditosylate
  • GW572016F
  • lapatinib ditosilate
  • lapatinib ditosilate hydrate
  • lapatinib ditosylate hydrate
A quinazoline derivative that inhibits EPIDERMAL GROWTH FACTOR RECEPTOR and HER2 (RECEPTOR, ERBB-2) tyrosine kinases. It is used for the treatment of advanced or metastatic breast cancer, where tumors overexpress HER2.
  • Molecular weight: 581.06
  • Formula: C29H26ClFN4O4S
  • CLOGP: 5.82
  • LIPINSKI: 2
  • HAC: 8
  • HDO: 2
  • TPSA: 106.35
  • ALOGS: -4.42
  • ROTB: 11
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.25 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 30.73 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 24 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.298 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 41.495 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.405 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 8.810 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.280 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 0.390 % High 1
herg hERG pIC50 4.961 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 23.605 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 59.429 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.260 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT3,ALK,AURKA,AURKB,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,ERBB4,FLT3,GRK2,INSR,IRAK1,IRAK3,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK10,MAPK7,MARK4,MET,MTOR,NTRK1,NTRK2,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,SRC,STK33,SYK,TEK,TTK,ULK1,YES1 67
kinase-selectivity-class ACVR2A,ACVR2B,ALK,AURKA,AXL,BLK,BRAF,CAMK2B,CAMK2D,CDK9,DDR1,EGFR,EPHB4,ERBB2,ERBB4,FLT3,JAK1,MAP2K6,MAP3K10,MAP3K21,MAP4K3,MAPK7,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKCD,PRKDC,RIPK3,SIK2,SIK3,STK33,TTK 33
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 38.019 High 1
mh-clint Mouse hepatocyte intrinsic clearance 35.318 High 1
mppb Mouse plasma protein binding (% unbound) 0.190 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 31.989 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 0.280 % High 1
rh-clint Rat hepatocyte intrinsic clearance 64.269 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 0.520 % High 1
rppb Rat plasma protein binding (% unbound) 0.190 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 0.869 uM High 1

Approvals:

DateAgencyCompanyOrphan
June 10, 2008 EMA
March 13, 2007 FDA NOVARTIS PHARMS CORP

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
Palmar-plantar erythrodysaesthesia syndrome 2086.25 22.51 619 25331 27404 90575093
Diarrhoea 1620.20 22.51 1634 24316 937556 89664941
Disease progression 1062.37 22.51 621 25329 155994 90446503
Metastases to central nervous system 909.09 22.51 294 25656 17248 90585249
Malignant neoplasm progression 496.69 22.51 334 25616 106536 90495961
Paronychia 405.64 22.51 132 25818 7874 90594623
Neutropenia 380.69 22.51 391 25559 224513 90377984
Metastases to lung 326.73 22.51 135 25815 15856 90586641
Metastases to liver 323.12 22.51 160 25790 28647 90573850
Dehydration 293.12 22.51 318 25632 194129 90408368
Metastases to lymph nodes 274.24 22.51 109 25841 11580 90590917
Metastases to bone 269.34 22.51 136 25814 25369 90577128
Breast cancer metastatic 237.44 22.51 106 25844 15026 90587471
Ejection fraction decreased 234.18 22.51 125 25825 26128 90576369
Blood bilirubin increased 223.80 22.51 145 25805 43325 90559172
Vomiting 200.35 22.51 585 25365 787708 89814789
Skin toxicity 197.46 22.51 74 25876 6705 90595792
Death 196.69 22.51 415 25535 456136 90146361
Skin fissures 182.54 22.51 98 25852 20711 90581786
Jaundice 158.88 22.51 105 25845 32412 90570085
Metastases to skin 157.63 22.51 47 25903 2093 90600404
Mucosal inflammation 153.03 22.51 129 25821 57496 90545001
Hypokalaemia 124.64 22.51 170 25780 130946 90471551
Nausea 123.49 22.51 634 25316 1109682 89492815
Gastrointestinal toxicity 122.44 22.51 58 25892 9409 90593088
Hepatic function abnormal 121.61 22.51 103 25847 46185 90556312
Febrile neutropenia 115.25 22.51 181 25769 158168 90444329
Hepatotoxicity 108.27 22.51 96 25854 45746 90556751
Hyperbilirubinaemia 103.98 22.51 59 25891 13877 90588620
Alanine aminotransferase increased 102.85 22.51 147 25803 118191 90484306
Pleural effusion 101.60 22.51 142 25808 111849 90490648
Lymphangiosis carcinomatosa 98.78 22.51 31 25919 1641 90600856
Vascular device infection 98.44 22.51 54 25896 11898 90590599
Streptococcal sepsis 96.70 22.51 37 25913 3547 90598950
Haematotoxicity 96.04 22.51 54 25896 12481 90590016
Cardiotoxicity 95.31 22.51 52 25898 11337 90591160
Dry skin 92.58 22.51 120 25830 87953 90514544
Weight increased 87.62 22.51 9 25941 417918 90184579
Brain oedema 87.00 22.51 57 25893 17328 90585169
Joint swelling 84.91 22.51 20 25930 503280 90099217
Condition aggravated 83.69 22.51 33 25917 595512 90006985
Rash 80.87 22.51 444 25506 795656 89806841
Nail bed inflammation 80.40 22.51 27 25923 1774 90600723
Pseudomonal sepsis 80.06 22.51 34 25916 4268 90598229
Nasal mucosal disorder 79.59 22.51 27 25923 1830 90600667
Drug hypersensitivity 77.06 22.51 19 25931 463590 90138907
Asthenia 75.91 22.51 328 25622 533423 90069074
Pyrexia 75.70 22.51 381 25569 660104 89942393
Glossodynia 72.71 22.51 5 25945 321774 90280723
Arthralgia 69.99 22.51 72 25878 778450 89824047
Maternal exposure during pregnancy 69.94 22.51 10 25940 360053 90242444
Metastasis 68.51 22.51 34 25916 6103 90596394
Therapeutic product effect decreased 66.76 22.51 3 25947 277568 90324929
Neuropathy peripheral 63.97 22.51 129 25821 136841 90465656
Aspartate aminotransferase increased 60.55 22.51 107 25843 102830 90499667
Wound 59.80 22.51 8 25942 302972 90299525
Breast cancer 59.23 22.51 75 25875 53686 90548811
Dermatitis acneiform 58.74 22.51 31 25919 6323 90596174
Decreased appetite 58.60 22.51 238 25712 376302 90226195
Thrombocytopenia 58.51 22.51 161 25789 208564 90393933
Off label use 58.40 22.51 145 25805 1102107 89500390
Infusion related reaction 55.43 22.51 25 25925 416755 90185742
Sinusitis 55.18 22.51 15 25935 343073 90259424
Cellulitis 55.08 22.51 96 25854 91241 90511256
Neoplasm progression 52.10 22.51 64 25886 44422 90558075
Stomatitis 52.10 22.51 185 25765 274513 90327984
Musculoskeletal stiffness 51.53 22.51 11 25939 296521 90305976
Mobility decreased 50.99 22.51 6 25944 250728 90351769
Discomfort 50.15 22.51 9 25941 274326 90328171
Ascites 50.07 22.51 65 25885 47675 90554822
Leukopenia 49.59 22.51 97 25853 100613 90501884
Asthma 48.73 22.51 6 25944 242154 90360343
Hypertension 47.40 22.51 37 25913 457495 90145002
Second primary malignancy 47.04 22.51 32 25918 10346 90592151
Varicose vein 46.67 22.51 28 25922 7299 90595198
Type 2 diabetes mellitus 46.36 22.51 3 25947 203241 90399256
Superior vena cava syndrome 45.02 22.51 14 25936 719 90601778
Neurotoxicity 44.89 22.51 42 25908 21425 90581072
Recurrent cancer 44.32 22.51 19 25931 2440 90600057
Lower respiratory tract infection 44.16 22.51 9 25941 250650 90351847
Folliculitis 43.84 22.51 4 25946 204349 90398148
Anaemia 43.46 22.51 208 25742 352594 90249903
Botryomycosis 43.29 22.51 8 25942 38 90602459
Swelling 43.26 22.51 34 25916 419024 90183473
Metastatic neoplasm 43.12 22.51 23 25927 4792 90597705
Wheezing 43.10 22.51 8 25942 238072 90364425
Pericarditis 43.07 22.51 12 25938 270139 90332358
Biliary dilatation 42.54 22.51 19 25931 2692 90599805
Drug ineffective 42.28 22.51 229 25721 1384069 89218428
Gamma-glutamyltransferase increased 41.88 22.51 53 25897 37899 90564598
Breast neoplasm 41.51 22.51 16 25934 1564 90600933
Fall 40.51 22.51 47 25903 481763 90120734
Metastases to spine 39.61 22.51 20 25930 3723 90598774
Neoplasm 39.28 22.51 27 25923 8876 90593621
Pain 39.21 22.51 150 25800 996191 89606306
Onychalgia 38.78 22.51 14 25936 1140 90601357
Contusion 38.51 22.51 12 25938 251204 90351293
Transaminases 38.20 22.51 8 25942 79 90602418
Skin exfoliation 37.88 22.51 69 25881 67844 90534653
Breast cancer recurrent 37.58 22.51 22 25928 5481 90597016
Brain neoplasm 37.38 22.51 21 25929 4843 90597654
Eczema 36.43 22.51 59 25891 52811 90549686
Skin mass 36.29 22.51 24 25926 7406 90595091
Onycholysis 36.18 22.51 16 25934 2214 90600283
Abdominal discomfort 35.54 22.51 51 25899 477277 90125220
Exposure during pregnancy 35.46 22.51 12 25938 238398 90364099
Hepatic failure 35.43 22.51 50 25900 39678 90562819
Candida infection 35.13 22.51 46 25904 34011 90568486
Product dose omission issue 35.01 22.51 20 25930 291667 90310830
Central nervous system lesion 34.93 22.51 28 25922 11618 90590879
Impaired healing 34.47 22.51 12 25938 234187 90368310
Performance status decreased 34.31 22.51 19 25931 4261 90598236
Leukonychia 33.82 22.51 7 25943 65 90602432
Erythema 33.33 22.51 142 25808 229104 90373393
Intracranial pressure increased 33.27 22.51 22 25928 6789 90595708
Left ventricular dysfunction 33.20 22.51 30 25920 14639 90587858
Anal erythema 32.92 22.51 9 25941 292 90602205
Peripheral swelling 32.91 22.51 42 25908 413064 90189433
Nasopharyngitis 32.84 22.51 41 25909 407063 90195434
Epistaxis 32.60 22.51 74 25876 85051 90517446
Hormone receptor positive breast cancer 32.08 22.51 11 25939 770 90601727
Erysipelas 32.02 22.51 24 25926 9028 90593469
Psoriasis 31.40 22.51 3 25947 147751 90454746
Product use issue 31.30 22.51 29 25921 329890 90272607
Limbal stem cell deficiency 31.15 22.51 6 25944 37 90602460
Nail infection 30.95 22.51 15 25935 2557 90599940
Plantar erythema 30.93 22.51 8 25942 209 90602288
Pericardial effusion 30.86 22.51 45 25905 36788 90565709
Neoplasm malignant 30.75 22.51 43 25907 33837 90568660
Completed suicide 30.68 22.51 3 25947 145055 90457442
Subclavian vein thrombosis 30.57 22.51 14 25936 2102 90600395
Radiation necrosis 29.69 22.51 10 25940 663 90601834
Drug intolerance 29.37 22.51 52 25898 447539 90154958
Tumour marker increased 28.95 22.51 19 25931 5788 90596709
Gastrointestinal bacterial infection 28.60 22.51 11 25939 1069 90601428
Hypersensitivity 27.91 22.51 55 25895 454622 90147875
Alopecia 27.79 22.51 63 25887 495008 90107489
Neoplasm recurrence 27.60 22.51 15 25935 3244 90599253
Injury 27.55 22.51 11 25939 197338 90405159
Osteonecrosis of jaw 27.44 22.51 44 25906 39059 90563438
Pulmonary embolism 27.29 22.51 91 25859 130729 90471768
Brain cancer metastatic 27.20 22.51 7 25943 179 90602318
Injection site pain 27.15 22.51 8 25942 173691 90428806
Urticaria 26.81 22.51 30 25920 312704 90289793
Polyneuropathy 26.24 22.51 30 25920 19311 90583186
Treatment failure 26.22 22.51 29 25921 303899 90298598
Sleep disorder 26.11 22.51 12 25938 198018 90404479
Radiation pneumonitis 25.93 22.51 12 25938 1846 90600651
Arthritis 25.62 22.51 8 25942 167307 90435190
Feeling abnormal 25.60 22.51 8 25942 167227 90435270
Pneumonitis 24.78 22.51 45 25905 44125 90558372
Lung infiltration 24.72 22.51 26 25924 15256 90587241
Dyschezia 23.74 22.51 13 25937 2852 90599645
Ingrowing nail 23.73 22.51 13 25937 2854 90599643
Jaundice cholestatic 23.64 22.51 21 25929 10022 90592475
Depression 23.47 22.51 31 25919 300570 90301927
Osteoradionecrosis 23.45 22.51 6 25944 150 90602347
Restlessness 23.44 22.51 39 25911 35681 90566816
Rash pustular 23.39 22.51 19 25931 8030 90594467
Malignant pleural effusion 23.33 22.51 13 25937 2951 90599546
Drug interaction 23.17 22.51 27 25923 276426 90326071
Metastases to meninges 23.08 22.51 14 25936 3721 90598776

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
Duodenal ulcer perforation 49.11 32.41 11 1117 1765 42618442
Diarrhoea 45.59 32.41 58 1070 460791 42159416
Dehydration 36.43 32.41 30 1098 141737 42478470
Metastases to lung 36.27 32.41 13 1115 11411 42608796

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
Palmar-plantar erythrodysaesthesia syndrome 1326.16 21.85 422 18147 40603 110530127
Diarrhoea 1088.90 21.85 1128 17441 1138377 109432353
Disease progression 695.70 21.85 459 18110 243575 110327155
Metastases to central nervous system 659.98 21.85 216 18353 22601 110548129
Malignant neoplasm progression 378.39 21.85 278 18291 174289 110396441
Metastases to lung 296.27 21.85 120 18449 22943 110547787
Paronychia 268.96 21.85 92 18477 10989 110559741
Metastases to lymph nodes 259.70 21.85 97 18472 14935 110555795
Metastases to liver 249.97 21.85 121 18448 35265 110535465
Breast cancer metastatic 237.34 21.85 84 18485 11097 110559633
Metastases to bone 214.74 21.85 105 18464 31267 110539463
Dehydration 191.45 21.85 235 18334 279276 110291454
Metastases to skin 169.57 21.85 45 18524 2254 110568476
Vomiting 164.38 21.85 425 18144 910250 109660480
Ejection fraction decreased 164.33 21.85 96 18473 40784 110529946
Skin fissures 147.11 21.85 75 18494 24383 110546347
Neutropenia 143.78 21.85 239 18330 374381 110196349
Gastrointestinal toxicity 126.14 21.85 53 18516 11095 110559635
Blood bilirubin increased 116.82 21.85 99 18470 75873 110494857
Skin toxicity 107.10 21.85 48 18521 11735 110558995
Streptococcal sepsis 103.43 21.85 37 18532 5035 110565695
Nausea 102.80 21.85 444 18125 1235246 109335484
Vascular device infection 100.35 21.85 51 18518 16461 110554269
Death 97.96 21.85 298 18271 698571 109872159
Mucosal inflammation 96.88 21.85 99 18470 96042 110474688
Hepatotoxicity 96.19 21.85 82 18487 63318 110507412
Nail bed inflammation 95.80 21.85 28 18541 2002 110568728
Nasal mucosal disorder 93.41 21.85 27 18542 1856 110568874
Jaundice 92.71 21.85 78 18491 59158 110511572
Hypokalaemia 83.06 21.85 126 18443 182322 110388408
Lymphangiosis carcinomatosa 81.90 21.85 26 18543 2456 110568274
Haematotoxicity 80.73 21.85 48 18521 21034 110549696
Hyperbilirubinaemia 80.48 21.85 55 18514 30616 110540114
Pseudomonal sepsis 73.23 21.85 34 18535 9012 110561718
Asthenia 70.93 21.85 265 18304 688734 109881996
Cardiotoxicity 68.75 21.85 40 18529 16841 110553889
Varicose vein 65.40 21.85 29 18540 6911 110563819
Pleural effusion 62.22 21.85 109 18460 177600 110393130
Condition aggravated 62.02 21.85 23 18546 734813 109835917
Brain oedema 61.54 21.85 47 18522 31051 110539679
Metastasis 54.54 21.85 27 18542 8240 110562490
Rash 49.16 21.85 269 18300 820695 109750035
Weight increased 47.41 21.85 7 18562 419637 110151093
Dry skin 47.06 21.85 73 18496 107580 110463150
Metastases to spine 42.99 21.85 20 18549 5323 110565407
Botryomycosis 42.46 21.85 8 18561 79 110570651
Dermatitis acneiform 41.18 21.85 26 18543 12669 110558061
Hormone receptor positive breast cancer 41.15 21.85 11 18558 566 110570164
Onycholysis 40.92 21.85 16 18553 2783 110567947
Drug hypersensitivity 40.36 21.85 13 18556 454077 110116653
Hepatic function abnormal 39.65 21.85 61 18508 89234 110481496
Second primary malignancy 39.52 21.85 29 18540 18039 110552691
Joint swelling 38.79 21.85 13 18556 442832 110127898
Recurrent cancer 37.80 21.85 16 18553 3407 110567323
Subclavian vein thrombosis 37.25 21.85 15 18554 2817 110567913
Candida infection 37.08 21.85 43 18526 47966 110522764
Neuropathy peripheral 36.59 21.85 88 18481 179189 110391541
Transaminases 36.47 21.85 7 18562 77 110570653
Breast cancer recurrent 36.01 21.85 16 18553 3830 110566900
Eczema 35.83 21.85 52 18517 72241 110498489
Infusion related reaction 35.52 21.85 10 18559 381152 110189578
Leukonychia 34.84 21.85 7 18562 99 110570631
Tumour marker increased 34.79 21.85 17 18552 5043 110565687
Skin mass 34.10 21.85 21 18548 9795 110560935
Onychalgia 33.79 21.85 11 18558 1126 110569604
Biliary dilatation 33.68 21.85 15 18554 3610 110567120
Arthralgia 32.96 21.85 50 18519 779582 109791148
Drug interaction 32.62 21.85 22 18547 500161 110070569
Fall 32.58 21.85 32 18537 603450 109967280
Osteonecrosis of jaw 32.16 21.85 40 18529 47977 110522753
Alanine aminotransferase increased 32.07 21.85 85 18484 183688 110387042
Stomatitis 32.01 21.85 109 18460 270133 110300597
Limbal stem cell deficiency 30.85 21.85 6 18563 71 110570659
Breast cancer 30.57 21.85 35 18534 38507 110532223
Decreased appetite 30.48 21.85 159 18410 475687 110095043
Invasive ductal breast carcinoma 30.42 21.85 17 18552 6629 110564101
Central nervous system lesion 29.66 21.85 23 18546 15530 110555200
Metastatic neoplasm 29.58 21.85 16 18553 5857 110564873
Metastases to the mediastinum 29.06 21.85 9 18560 784 110569946
Erysipelas 28.51 21.85 21 18548 13137 110557593
Neoplasm progression 28.49 21.85 44 18525 64551 110506179
Intracranial pressure increased 27.88 21.85 19 18550 10516 110560214
Gastrointestinal bacterial infection 27.62 21.85 10 18559 1408 110569322
Hypertension 27.57 21.85 27 18542 510057 110060673
Abdominal pain 27.26 21.85 163 18406 512826 110057904
Restlessness 27.20 21.85 40 18529 56219 110514511
Wheezing 27.15 21.85 5 18564 255225 110315505
Pyrexia 26.92 21.85 249 18320 898016 109672714
Mobility decreased 26.70 21.85 4 18565 237418 110333312
Neurotoxicity 26.42 21.85 34 18535 42173 110528557
Performance status decreased 26.41 21.85 16 18553 7250 110563480
Off label use 26.02 21.85 147 18422 1500038 109070692
Cellulitis 25.86 21.85 62 18507 125954 110444776
HER2 positive breast cancer 25.72 21.85 7 18562 386 110570344
Discomfort 25.62 21.85 3 18566 214704 110356026
Left ventricular dysfunction 25.12 21.85 25 18544 23468 110547262
Musculoskeletal stiffness 24.86 21.85 8 18561 279814 110290916
Febrile neutropenia 24.68 21.85 112 18457 316655 110254075
Glossodynia 24.38 21.85 4 18565 222000 110348730
Lower respiratory tract infection 23.35 21.85 6 18563 243100 110327630
Brain neoplasm 23.15 21.85 14 18555 6323 110564407
Neoplasm recurrence 22.91 21.85 13 18556 5219 110565511
Product dose omission issue 22.56 21.85 13 18556 321769 110248961
Plantar erythema 22.54 21.85 6 18563 304 110570426
Pericardial effusion 22.52 21.85 37 18532 57180 110513550
Cholangitis 22.49 21.85 20 18549 16315 110554415
Metastases to chest wall 21.97 21.85 7 18562 669 110570061
Fatigue 21.86 21.85 305 18264 1215653 109355077

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EH01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor

Related Drugs by ATC class:

L01EH Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors 4 drugs
neratinibsevabertinibtucatinibzongertinib

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

DiseaseRelationSNOMED_IDDOID
HER2-positive carcinoma of breast indication 427685000
Torsades de pointes contraindication 31722008
Hypokalemia contraindication 43339004
Hepatic failure contraindication 59927004
Interstitial pneumonia contraindication 64667001
Left heart failure contraindication 85232009
Prolonged QT interval contraindication 111975006
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
Drug-induced hepatitis contraindication 235876009
Pregnancy, function contraindication 289908002
Severe diarrhea contraindication 409587002
Breastfeeding (mother) contraindication 413712001
Congenital long QT syndrome contraindication 442917000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.62 Basic
pKa2 4.99 Basic

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 INHIBITOR Kd 8.15 CHEMBL CHEMBL
Epidermal growth factor receptor Kinase INHIBITOR Kd 9.04 CHEMBL CHEMBL
Platelet-derived growth factor receptor beta Kinase IC50 5.07 CHEMBL
Tyrosine-protein kinase ABL1 Kinase IC50 4.64 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 5.46 CHEMBL
Solute carrier organic anion transporter family member 1B1 Transporter WOMBAT-PK
Cyclin-dependent kinase 2 Kinase IC50 4.96 CHEMBL
Insulin receptor Kinase AGONIST IC50 4.77 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 7.27 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.59 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 5.44 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 5.48 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 7 Kinase Kd 5.36 CHEMBL
Receptor tyrosine-protein kinase erbB-3 Kinase Kd 5.26 CHEMBL
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta Kinase Kd 6.17 CHEMBL
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma Kinase Kd 5.12 CHEMBL
Phosphatidylinositol 4-kinase beta Kinase Kd 6.03 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 5.96 CHEMBL
Multidrug resistance protein 1 Transporter WOMBAT-PK
ATP-binding cassette sub-family G member 2 Transporter EC50 5.50 CHEMBL
Tubulin alpha-1A chain Structural Kd 7.27 CHEMBL
Replicase polyprotein 1ab Enzyme Ki 4.64 CHEMBL

External reference:

IDSource
4026029 VUID
N0000179782 NUI
D04024 KEGG_DRUG
388082-78-8 SECONDARY_CAS_RN
4026029 VANDF
C1506770 UMLSCUI
FMM PDB_CHEM_ID
CHEMBL554 ChEMBL_ID
CHEMBL1201179 ChEMBL_ID
D000077341 MESH_DESCRIPTOR_UI
DB01259 DRUGBANK_ID
5692 IUPHAR_LIGAND_ID
8378 INN_ID
0VUA21238F UNII
208908 PUBCHEM_CID
480167 RXNORM
339254 MMSL
d06672 MMSL
012020 NDDF
012022 NDDF
425466009 SNOMEDCT_US
425820005 SNOMEDCT_US
426238006 SNOMEDCT_US
CHEBI:192581 CHEBI
0VUA21238F INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TYKERB HUMAN PRESCRIPTION DRUG LABEL 1 0078-0671 TABLET 250 mg ORAL NDA 34 sections
Lapatinib HUMAN PRESCRIPTION DRUG LABEL 1 0480-3237 TABLET, FILM COATED 250 mg ORAL ANDA 34 sections
Lapatinib HUMAN PRESCRIPTION DRUG LABEL 1 42291-035 TABLET, FILM COATED 250 mg ORAL ANDA 34 sections
Lapatinib Human Prescription Drug Label 1 68180-801 TABLET 250 mg ORAL ANDA 28 sections