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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 1282 184475-35-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ZD1839
  • gefitinib
  • iressa
  • ZD 1839
Gefitinib reversibly inhibits the kinase activity of wild-type and certain activating mutations of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor, thereby inhibiting further downstream signalling and blocking EGFR-dependent proliferation.
  • Molecular weight: 446.91
  • Formula: C22H24ClFN4O3
  • CLOGP: 5.25
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 1
  • TPSA: 68.74
  • ALOGS: -4.22
  • ROTB: 8
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.25 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) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 8 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 60 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 23 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 12 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.09 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 34 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.854 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.553 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 19.055 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 7.112 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 4.620 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 14.780 % High 1
herg hERG pIC50 5.342 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 4.519 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 59.156 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 4.190 % High 1
kinase-safety-class ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CAMK2G,CDK5,CDK9,CHEK1,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3B,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK11,MAPK12,MAPK14,MAPK7,MAPKAPK2,MARK4,MELK,MET,MKNK1,MKNK2,MTOR,NTRK1,NTRK2,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,PTK6,RET,RIPK3,SIK2,SIK3,SRC,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,YES1 98
kinase-selectivity-class ALK,AURKA,AXL,BLK,BRAF,CAMK2D,CHEK1,CSF1R,DDR1,EGFR,EPHA2,EPHB4,ERBB2,ERBB4,FLT3,JAK1,KDR,KIT,LCK,LYN,MAP3K10,MAP3K21,MAPK7,MARK4,MET,MKNK1,MTOR,PDK4,SIK2,SIK3,STK33,SYK,TTK,YES1 34
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 10.093 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 12.882 High 1
mh-clint Mouse hepatocyte intrinsic clearance 12.560 High 1
mppb Mouse plasma protein binding (% unbound) 3.950 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 19.815 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 7.980 % High 1
rat-kpuu-brain Rat brain Kpuu 0.029 % High 1
rh-clint Rat hepatocyte intrinsic clearance 10 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 24.190 % High 1
rppb Rat plasma protein binding (% unbound) 4.090 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 4.742 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 5, 2003 FDA

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
Malignant neoplasm progression 1523.87 25.37 495 6981 106375 90514596
Drug resistance 934.65 25.37 256 7220 30193 90590778
Acquired gene mutation 627.58 25.37 106 7370 1173 90619798
EGFR gene mutation 406.28 25.37 61 7415 289 90620682
Metastases to central nervous system 364.30 25.37 109 7367 17433 90603538
Interstitial lung disease 276.89 25.37 132 7344 76273 90544698
Hepatic function abnormal 250.83 25.37 106 7370 46182 90574789
Disease progression 217.28 25.37 144 7332 156471 90464500
Malignant transformation 214.47 25.37 38 7438 564 90620407
Paronychia 167.17 25.37 50 7426 7956 90613015
Metastases to meninges 159.95 25.37 41 7435 3694 90617277
Diarrhoea 157.41 25.37 278 7198 938912 89682059
Liver disorder 127.07 25.37 94 7382 121175 90499796
Metastases to lung 108.26 25.37 43 7433 15948 90605023
Metastases to bone 101.24 25.37 47 7429 25458 90595513
Dermatitis acneiform 96.07 25.37 31 7445 6323 90614648
Pleural effusion 81.25 25.37 70 7406 111921 90509050
Metastases to liver 75.40 25.37 40 7436 28767 90592204
Gene mutation 74.90 25.37 20 7456 2110 90618861
Small cell lung cancer 73.11 25.37 19 7457 1805 90619166
Lung disorder 65.70 25.37 71 7405 149812 90471159
Skin toxicity 52.12 25.37 20 7456 6759 90614212
Metastasis 43.26 25.37 17 7459 6120 90614851
Hepatotoxicity 42.33 25.37 33 7443 45809 90575162
Skin disorder 41.88 25.37 30 7446 36676 90584295
Rash 39.22 25.37 149 7327 795951 89825020
Death 37.57 25.37 102 7374 456449 90164522
Leukoencephalopathy 32.61 25.37 13 7463 4860 90616111
Sarcomatoid carcinoma 32.58 25.37 5 7471 28 90620943
Pneumothorax 32.36 25.37 20 7456 19147 90601824
Arthralgia 32.28 25.37 12 7464 778510 89842461
Pneumonitis 30.76 25.37 27 7449 44143 90576828
Therapy partial responder 29.80 25.37 20 7456 22023 90598948
Carcinoembryonic antigen increased 29.63 25.37 10 7466 2340 90618631
Lung carcinoma cell type unspecified recurrent 29.28 25.37 6 7470 198 90620773
Dehydration 28.92 25.37 55 7421 194392 90426579
Lymphangiosis carcinomatosa 28.75 25.37 9 7467 1663 90619308
Growth of eyelashes 28.46 25.37 6 7470 228 90620743
Malignant pleural effusion 27.36 25.37 10 7466 2954 90618017
Dry skin 27.35 25.37 35 7441 88038 90532933
PRIDE syndrome 27.18 25.37 4 7472 16 90620955
Metastases to lymph nodes 27.15 25.37 15 7461 11674 90609297
Alanine aminotransferase increased 26.24 25.37 40 7436 118298 90502673

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
Malignant neoplasm progression 637.69 25.06 298 5152 108102 42507783
Drug resistance 389.97 25.06 151 5299 34097 42581788
Acquired gene mutation 345.87 25.06 71 5379 1509 42614376
Interstitial lung disease 284.07 25.06 156 5294 78306 42537579
EGFR gene mutation 248.10 25.06 40 5410 194 42615691
Metastases to central nervous system 140.43 25.06 52 5398 10303 42605582
Lung disorder 139.97 25.06 83 5367 47840 42568045
Disease progression 117.03 25.06 116 5334 143540 42472345
Rash 93.08 25.06 143 5307 276811 42339074
Malignant transformation 91.91 25.06 22 5428 956 42614929
Metastases to bone 87.11 25.06 41 5409 14768 42601117
Metastases to lung 80.93 25.06 36 5414 11388 42604497
Metastases to meninges 76.73 25.06 22 5428 1939 42613946
Hepatic function abnormal 72.77 25.06 57 5393 51510 42564375
Metastases to liver 65.86 25.06 35 5415 16291 42599594
Diarrhoea 55.68 25.06 156 5294 460693 42155192
Mitochondrial aspartate aminotransferase increased 50.91 25.06 7 5443 7 42615878
Dermatitis acneiform 50.39 25.06 23 5427 7716 42608169
Metastases to pleura 48.12 25.06 12 5438 619 42615266
Paronychia 42.08 25.06 17 5433 4238 42611647
Liver disorder 41.71 25.06 37 5413 39607 42576278
Lymphangiosis carcinomatosa 37.75 25.06 11 5439 1026 42614859
Dehydration 30.10 25.06 60 5390 141707 42474178
Pleural effusion 28.07 25.06 47 5403 97119 42518766
Metastases to lymph nodes 27.44 25.06 14 5436 5984 42609901
Malignant pleural effusion 27.15 25.06 10 5440 1945 42613940
Vomiting 25.42 25.06 88 5362 289635 42326250

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
Malignant neoplasm progression 1713.84 24.11 652 10938 173915 110403794
Drug resistance 1218.47 24.11 381 11209 55993 110521716
Acquired gene mutation 922.27 24.11 171 11419 2583 110575126
EGFR gene mutation 605.76 24.11 95 11495 475 110577234
Interstitial lung disease 500.10 24.11 258 11332 139076 110438633
Metastases to central nervous system 424.84 24.11 138 11452 22679 110555030
Hepatic function abnormal 313.15 24.11 163 11427 89132 110488577
Malignant transformation 266.55 24.11 55 11535 1470 110576239
Disease progression 203.77 24.11 183 11407 243851 110333858
Metastases to meninges 200.22 24.11 55 11535 5073 110572636
Metastases to bone 182.09 24.11 81 11509 31291 110546418
Paronychia 178.00 24.11 60 11530 11021 110566688
Diarrhoea 171.74 24.11 371 11219 1139134 109438575
Metastases to lung 161.52 24.11 68 11522 22995 110554714
Liver disorder 156.24 24.11 125 11465 142118 110435591
Lung disorder 148.13 24.11 134 11456 179913 110397796
Dermatitis acneiform 136.40 24.11 51 11539 12644 110565065
Rash 119.41 24.11 264 11326 820700 109757009
Metastases to liver 113.67 24.11 61 11529 35325 110542384
Pleural effusion 99.04 24.11 107 11483 177602 110400107
Gene mutation 85.71 24.11 26 11564 3403 110574306
Small cell lung cancer 78.33 24.11 24 11566 3248 110574461
Metastasis 66.76 24.11 27 11563 8240 110569469
Skin toxicity 63.80 24.11 29 11561 11754 110565955
Lymphangiosis carcinomatosa 62.81 24.11 19 11571 2463 110575246
Metastases to lymph nodes 60.01 24.11 30 11560 15002 110562707
Metastases to pleura 57.43 24.11 17 11573 2046 110575663
Malignant pleural effusion 53.47 24.11 19 11571 4074 110573635
Mitochondrial aspartate aminotransferase increased 52.30 24.11 7 11583 7 110577702
Hepatotoxicity 49.72 24.11 46 11544 63354 110514355
Skin disorder 45.52 24.11 37 11553 42876 110534833
Arthralgia 41.47 24.11 15 11575 779617 109798092
Dehydration 40.47 24.11 90 11500 279421 110298288
Metastases to adrenals 39.40 24.11 12 11578 1591 110576118
Cystitis haemorrhagic 39.06 24.11 21 11569 12188 110565521
Leukoencephalopathy 38.63 24.11 19 11571 9176 110568533
Respiratory failure 36.56 24.11 74 11516 215258 110362451
Pneumothorax 36.53 24.11 30 11560 35255 110542454
Carcinoembryonic antigen increased 36.48 24.11 13 11577 2811 110574898
Sarcomatoid carcinoma 36.39 24.11 6 11584 43 110577666
Alanine aminotransferase increased 35.89 24.11 67 11523 183706 110394003
Decreased appetite 35.45 24.11 120 11470 475726 110101983
Drug hypersensitivity 33.77 24.11 4 11586 454086 110123623
PRIDE syndrome 31.86 24.11 5 11585 25 110577684
Therapy partial responder 31.22 24.11 28 11562 37033 110540676
Pneumonitis 30.74 24.11 39 11551 76492 110501217
Lung infiltration 29.91 24.11 23 11567 24605 110553104
Peripheral swelling 28.97 24.11 4 11586 404030 110173679
Lung carcinoma cell type unspecified recurrent 28.78 24.11 7 11583 398 110577311
Pneumatosis intestinalis 28.21 24.11 15 11575 8514 110569195
Cerebral infarction 26.72 24.11 30 11560 51808 110525901
Weight increased 26.09 24.11 6 11584 419638 110158071
Pulmonary embolism 25.52 24.11 64 11526 214410 110363299
Aspartate aminotransferase increased 24.83 24.11 53 11537 159883 110417826
Dry skin 24.53 24.11 42 11548 107611 110470098
Pain 24.49 24.11 39 11551 954916 109622793

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EB01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Epidermal growth factor receptor (EGFR) 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:74440 epidermal growth factor receptor antagonist

Related Drugs by ATC class:

L01EB Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors 8 drugs
afatinibdacomitiniberlotinibicotiniblazertinibmobocertinibolmutinibosimertinib

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

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Non-small cell lung cancer, positive for epidermal growth factor receptor expression indication 426964009
Fibrosis of lung contraindication 51615001 DOID:3770
Acute nephropathy contraindication 58574008
Interstitial pneumonia contraindication 64667001
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Breastfeeding (mother) contraindication 413712001
Non-small cell lung cancer, negative for epidermal growth factor receptor expression contraindication 427038005




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.65 Basic
pKa2 5.8 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
Epidermal growth factor receptor Kinase INHIBITOR Ki 9.40 CHEMBL CHEMBL
Ephrin type-A receptor 8 Kinase Kd 5.74 CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform Kinase Kd 5.43 CHEMBL
Serine/threonine-protein kinase 17B Kinase Kd 5.42 CHEMBL
Hepatocyte growth factor receptor Kinase Kd 5.46 CHEMBL
Multidrug resistance protein 1 Transporter IC50 4.70 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 5.96 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 6.64 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 5.74 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 6.20 CHEMBL
Serine/threonine-protein kinase B-raf Kinase IC50 5.70 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 6 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 5.77 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 5.72 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase Kd 5.96 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase Kd 5.57 CHEMBL
Death-associated protein kinase 3 Kinase Kd 5.24 CHEMBL
Tyrosine-protein kinase HCK Kinase Kd 5.36 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 6.39 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.64 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 5.72 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 6.33 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 5.80 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 5.82 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 5.70 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 6.23 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.16 CHEMBL
Casein kinase I isoform epsilon Kinase Kd 6.37 CHEMBL
Tyrosine-protein kinase Fgr Kinase Kd 5.59 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 5.24 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.26 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 5.70 CHEMBL
Beta-secretase 1 Enzyme IC50 4.70 CHEMBL
Cyclin-G-associated kinase Kinase Kd 8.15 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 6.28 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 5.89 CHEMBL
Activated CDC42 kinase 1 Kinase IC50 5.64 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 6.04 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 6.44 CHEMBL
Mitogen-activated protein kinase 9 Kinase Kd 5.85 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 5.60 CHEMBL
Protein-tyrosine kinase 6 Kinase IC50 6.01 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 5.74 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 6.21 CHEMBL
Serine/threonine-protein kinase D1 Kinase Kd 5.46 CHEMBL
Serine/threonine-protein kinase DCLK3 Kinase Kd 5.54 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 5.34 CHEMBL
Casein kinase I isoform delta Kinase Kd 5.49 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 5.22 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase Kd 6.54 CHEMBL
Serine/threonine-protein kinase NLK Kinase Kd 5.38 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 5.82 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 5.68 CHEMBL
Myotonin-protein kinase Kinase Kd 5.16 CHEMBL
Leukocyte tyrosine kinase receptor Kinase Kd 5.26 CHEMBL
Serine/threonine-protein kinase pim-3 Kinase Kd 5.24 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 5.92 CHEMBL
Citron Rho-interacting kinase Kinase Kd 5.89 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 5.40 CHEMBL
Mitogen-activated protein kinase 6 Kinase Kd 5.80 CHEMBL
Mitogen-activated protein kinase 4 Kinase Kd 5.51 CHEMBL
Ribosomal protein S6 kinase alpha-4 Kinase Kd 5.92 CHEMBL
Misshapen-like kinase 1 Kinase Kd 5.74 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase Kd 6.27 CHEMBL
Serine/threonine-protein kinase Chk2 Kinase Kd 6.10 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.49 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.51 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 7.16 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 5.48 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 5.68 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 6.62 CHEMBL
Receptor tyrosine-protein kinase erbB-3 Kinase Kd 6.10 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 6.25 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 5.12 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 6.22 CHEMBL
Nucleotide-binding oligomerization domain-containing protein 2 Cytosolic other IC50 5.97 CHEMBL
Ferrochelatase, mitochondrial Enzyme Kd 5.17 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.57 CHEMBL
Acyl-CoA dehydrogenase family member 10 Enzyme Kd 4.47 CHEMBL
Transcription factor p65 Transcription factor IC50 7.26 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 6 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 5.42 SCIENTIFIC LITERATURE
Serine/threonine-protein kinase ULK3 Kinase Kd 5.85 CHEMBL
Tubulin alpha-1A chain Structural Kd 6.39 CHEMBL
Cruzipain Enzyme IC50 4.06 CHEMBL
Quinolone resistance protein NorA Transporter IC50 5.01 CHEMBL
Epidermal growth factor receptor Kinase IC50 7.84 CHEMBL

External reference:

IDSource
4021392 VUID
N0000148810 NUI
D01977 KEGG_DRUG
4021392 VANDF
C1122962 UMLSCUI
CHEBI:49668 CHEBI
IRE PDB_CHEM_ID
CHEMBL939 ChEMBL_ID
D000077156 MESH_DESCRIPTOR_UI
DB00317 DRUGBANK_ID
4941 IUPHAR_LIGAND_ID
8204 INN_ID
S65743JHBS UNII
123631 PUBCHEM_CID
281883 RXNORM
17257 MMSL
256478 MMSL
46712 MMSL
d04868 MMSL
009981 NDDF
398685009 SNOMEDCT_US
407100002 SNOMEDCT_US
S65743JHBS INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
IRESSA HUMAN PRESCRIPTION DRUG LABEL 1 0310-0482 TABLET, COATED 250 mg ORAL NDA 26 sections
Gefitinib HUMAN PRESCRIPTION DRUG LABEL 1 0480-4053 TABLET, FILM COATED 250 mg ORAL ANDA 26 sections
Gefitinib HUMAN PRESCRIPTION DRUG LABEL 1 50742-366 TABLET, COATED 250 mg ORAL ANDA 26 sections
Gefitinib HUMAN PRESCRIPTION DRUG LABEL 1 67184-0531 TABLET, COATED 250 mg ORAL ANDA 26 sections
Gefitinib Human Prescription Drug Label 1 69339-168 TABLET, FILM COATED 250 mg ORAL ANDA 25 sections
Gefitinib Human Prescription Drug Label 1 69339-168 TABLET, FILM COATED 250 mg ORAL ANDA 25 sections