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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5389 937263-43-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tucatinib
  • tukysa
  • ARRY-380
  • ONT-380
Tucatinib is a tyrosine kinase inhibitor of HER2. In vitro, tucatinib inhibits phosphorylation of HER2 and HER3, resulting in inhibition of downstream MAPK and AKT signaling and cell proliferation, and showed anti-tumor activity in HER2 expressing tumor cells. In vivo, tucatinib inhibited the growth of HER2 expressing tumors. The combination of tucatinib and trastuzumab showed increased anti-tumor activity in vitro and in vivo compared to either drug alone
  • Molecular weight: 480.53
  • Formula: C26H24N8O2
  • CLOGP: 5.19
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 2
  • TPSA: 110.85
  • ALOGS: -5.08
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.60 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.806 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 21.878 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 16.406 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 11.194 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 6.040 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 17.880 % High 1
herg hERG pIC50 5.057 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 10.116 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 67.608 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 4.030 % High 1
kinase-safety-class ACVR2A,ACVR2B,ALK,AURKA,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK9,CSF1R,DDR1,EGFR,EPHA2,EPHB4,ERBB2,ERBB4,FLT3,GRK2,ITK,JAK1,KDR,KIT,LYN,MAP3K10,MAP3K21,MAP4K1,MAP4K3,MAPK10,MAPK7,MARK4,MET,MTOR,NTRK1,NTRK2,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,SRC,STK33,TEK,TTK,ULK1 50
kinase-selectivity-class ACVR2B,AURKA,BLK,BMX,BRAF,CAMK2D,CSF1R,DDR1,EGFR,ERBB2,ERBB4,FLT3,KDR,KIT,LYN,MAP2K6,MAP3K21,MAPK7,PDK4,RIPK3,SIK2,SIK3,STK33 23
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 31.696 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 44.875 High 1
mh-clint Mouse hepatocyte intrinsic clearance 25.942 High 1
mppb Mouse plasma protein binding (% unbound) 2.520 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 44.361 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) 8.050 % High 1
rat-kpuu-brain Rat brain Kpuu 0.009 % High 1
rh-clint Rat hepatocyte intrinsic clearance 14.655 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 26.410 % High 1
rppb Rat plasma protein binding (% unbound) 2.540 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 3.793 uM High 1

Approvals:

DateAgencyCompanyOrphan
Feb. 11, 2021 EMA SEAGEN B.V
April 17, 2020 FDA SEATTLE GENETICS

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 880.71 27.28 843 11754 938347 89677503
Metastases to central nervous system 567.93 27.28 173 12424 17369 90598481
Palmar-plantar erythrodysaesthesia syndrome 565.60 27.28 193 12404 27830 90588020
Malignant neoplasm progression 475.70 27.28 251 12346 106619 90509231
Neoplasm progression 309.94 27.28 142 12455 44344 90571506
Disease progression 212.46 27.28 175 12422 156440 90459410
Hyperbilirubinaemia 190.45 27.28 72 12525 13864 90601986
Nausea 177.55 27.28 439 12158 1109877 89505973
Death 142.63 27.28 239 12358 456312 90159538
Fatigue 141.55 27.28 414 12183 1153609 89462241
Hepatic cytolysis 138.26 27.28 73 12524 30843 90585007
Hospice care 132.08 27.28 50 12547 9654 90606196
Unevaluable event 125.42 27.28 84 12513 54764 90561086
Product dose omission issue 120.72 27.28 174 12423 291513 90324337
Skin fissures 118.92 27.28 58 12539 20751 90595099
Metastases to meninges 112.95 27.28 35 12562 3700 90612150
Blood bilirubin increased 110.15 27.28 71 12526 43399 90572451
Brain oedema 97.97 27.28 48 12549 17337 90598513
Streptococcal sepsis 93.47 27.28 30 12567 3554 90612296
Ejection fraction decreased 92.56 27.28 53 12544 26200 90589650
Nail bed inflammation 90.37 27.28 25 12572 1776 90614074
Paronychia 90.32 27.28 36 12561 7970 90607880
Nasal mucosal disorder 89.61 27.28 25 12572 1832 90614018
Vascular device infection 88.97 27.28 40 12557 11912 90603938
Metastases to lymph nodes 86.63 27.28 39 12558 11650 90604200
Pseudomonal sepsis 84.19 27.28 29 12568 4273 90611577
Metastases to lung 83.72 27.28 42 12555 15949 90599901
Hemianopia 73.59 27.28 22 12575 2060 90613790
Hospitalisation 62.74 27.28 83 12514 128017 90487833
Dehydration 62.06 27.28 103 12494 194344 90421506
Metastases to bone 60.53 27.28 40 12557 25465 90590385
Psychological trauma 59.77 27.28 17 12580 1336 90614514
Vomiting 57.64 27.28 239 12358 788054 89827796
Hepatotoxicity 57.40 27.28 49 12548 45793 90570057
Candida infection 56.67 27.28 43 12554 34014 90581836
Blood lactate dehydrogenase abnormal 56.56 27.28 13 12584 433 90615417
Varicose vein 56.06 27.28 25 12572 7302 90608548
Gamma-glutamyltransferase abnormal 53.92 27.28 13 12584 534 90615316
Neurological decompensation 51.13 27.28 19 12578 3482 90612368
Carcinoembryonic antigen increased 50.52 27.28 17 12580 2333 90613517
Epilepsy 49.37 27.28 59 12538 82147 90533703
Breast cancer metastatic 49.22 27.28 29 12568 15103 90600747
Botryomycosis 49.06 27.28 8 12589 38 90615812
Skin discolouration 48.73 27.28 44 12553 44271 90571579
Dihydropyrimidine dehydrogenase deficiency 47.34 27.28 9 12588 115 90615735
Radiotherapy 47.01 27.28 13 12584 922 90614928
Neuropathy peripheral 46.99 27.28 75 12522 136895 90478955
Haemolysis 46.46 27.28 23 12574 8487 90607363
Asthenia 46.36 27.28 171 12426 533580 90082270
Condition aggravated 45.91 27.28 13 12584 595532 90020318
Drug hypersensitivity 44.33 27.28 6 12591 463603 90152247
Infusion related reaction 43.36 27.28 4 12593 416776 90199074
Pneumonitis 43.04 27.28 41 12556 44129 90571721
Dry skin 43.00 27.28 57 12540 88016 90527834
Coagulation factor decreased 42.92 27.28 9 12588 194 90615656
Cell death 42.50 27.28 16 12581 3039 90612811
Decreased appetite 40.86 27.28 130 12467 376410 90239440
Glossopharyngeal nerve paralysis 40.62 27.28 7 12590 49 90615801
Brain natriuretic peptide decreased 39.58 27.28 7 12590 58 90615792
Thrombocytopenia 38.80 27.28 88 12509 208637 90407213
Illness 38.41 27.28 52 12545 81917 90533933
Brain operation 37.03 27.28 10 12587 649 90615201
Restlessness 36.41 27.28 34 12563 35686 90580164
Gram stain positive 36.23 27.28 7 12590 98 90615752
Drug ineffective 36.01 27.28 88 12509 1384210 89231640
Herpangina 35.62 27.28 6 12591 36 90615814
Brain neoplasm 35.31 27.28 16 12581 4848 90611002
Blood potassium decreased 35.00 27.28 38 12559 47689 90568161
Hyperproteinaemia 33.20 27.28 7 12590 155 90615695
Coagulation test abnormal 33.19 27.28 10 12587 961 90614889
Metastases to liver 32.45 27.28 29 12568 28778 90587072
Brain cancer metastatic 32.24 27.28 7 12590 179 90615671
Hypokalaemia 32.21 27.28 62 12535 131054 90484796
Joint swelling 31.98 27.28 15 12582 503285 90112565
Maternal exposure during pregnancy 31.40 27.28 6 12591 360057 90255793
Treatment failure 31.37 27.28 3 12594 303925 90311925
Constipation 30.56 27.28 97 12500 280298 90335552
Papillary thyroid cancer 30.28 27.28 12 12585 2615 90613235
Aspartate aminotransferase increased 29.47 27.28 52 12545 102885 90512965
Nasopharyngitis 29.34 27.28 10 12587 407094 90208756
Metastases to adrenals 28.87 27.28 9 12588 969 90614881
Liver function test increased 28.45 27.28 46 12551 84809 90531041
Radiation necrosis 27.69 27.28 8 12589 665 90615185
Sinusitis 27.32 27.28 7 12590 343081 90272769

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
Nose deformity 95.79 66.77 13 477 253 42620592
Ear malformation 92.15 66.77 13 477 339 42620506
Hypertelorism 84.82 66.77 13 477 606 42620239
Polydactyly 75.85 66.77 13 477 1221 42619624

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
Metastases to central nervous system 418.59 28.86 124 7594 22693 110558888
Palmar-plantar erythrodysaesthesia syndrome 317.09 28.86 116 7602 40909 110540672
Diarrhoea 309.54 28.86 386 7332 1139119 109442462
Neoplasm progression 211.93 28.86 99 7619 64496 110517085
Malignant neoplasm progression 188.48 28.86 129 7589 174438 110407143
Hyperbilirubinaemia 180.06 28.86 71 7647 30600 110550981
Hepatic cytolysis 146.10 28.86 73 7645 54980 110526601
Skin fissures 124.12 28.86 51 7667 24407 110557174
Nasal mucosal disorder 111.65 28.86 26 7692 1857 110579724
Nail bed inflammation 109.71 28.86 26 7692 2004 110579577
Streptococcal sepsis 108.06 28.86 31 7687 5041 110576540
Metastases to lymph nodes 103.15 28.86 39 7679 14993 110566588
Vascular device infection 103.13 28.86 40 7678 16472 110565109
Ejection fraction decreased 96.18 28.86 50 7668 40830 110540751
Metastases to meninges 94.48 28.86 28 7690 5100 110576481
Paronychia 91.71 28.86 33 7685 11048 110570533
Pseudomonal sepsis 86.52 28.86 30 7688 9016 110572565
Metastases to lung 80.68 28.86 37 7681 23026 110558555
Off label use 80.02 28.86 257 7461 1499928 109081653
Varicose vein 78.09 28.86 26 7692 6914 110574667
Hemianopia 76.95 28.86 21 7697 2847 110578734
Brain oedema 75.92 28.86 39 7679 31059 110550522
Disease progression 70.60 28.86 86 7632 243948 110337633
Epilepsy 69.75 28.86 57 7661 100152 110481429
Nausea 67.81 28.86 214 7504 1235476 109346105
Psychological trauma 67.81 28.86 17 7701 1656 110579925
Metastases to bone 67.06 28.86 36 7682 31336 110550245
Neurological decompensation 62.64 28.86 22 7696 6861 110574720
Death 62.36 28.86 145 7573 698724 109882857
Blood lactate dehydrogenase abnormal 60.55 28.86 13 7705 640 110580941
Gamma-glutamyltransferase abnormal 56.02 28.86 13 7705 914 110580667
Carcinoembryonic antigen increased 54.56 28.86 16 7702 2808 110578773
Blood bilirubin increased 54.51 28.86 44 7674 75928 110505653
Candida infection 52.90 28.86 36 7682 47973 110533608
Hepatotoxicity 52.57 28.86 40 7678 63360 110518221
Botryomycosis 49.48 28.86 8 7710 79 110581502
Dihydropyrimidine dehydrogenase deficiency 48.55 28.86 9 7709 207 110581374
Fatigue 47.10 28.86 188 7530 1215770 109365811
Restlessness 45.56 28.86 35 7683 56224 110525357
Coagulation factor decreased 44.40 28.86 9 7709 334 110581247
Asthenia 43.86 28.86 126 7592 688873 109892708
Glossopharyngeal nerve paralysis 43.59 28.86 7 7711 66 110581515
Cell death 43.28 28.86 16 7702 5775 110575806
Hypokalaemia 42.81 28.86 58 7660 182390 110399191
Brain natriuretic peptide decreased 42.77 28.86 7 7711 75 110581506
Metastases to liver 42.50 28.86 28 7690 35358 110546223
Vomiting 41.99 28.86 149 7569 910526 109671055
Pneumonitis 38.09 28.86 36 7682 76495 110505086
Herpangina 38.03 28.86 6 7712 50 110581531
Papillary thyroid cancer 37.23 28.86 12 7706 2882 110578699
Breast cancer metastatic 36.18 28.86 17 7701 11164 110570417
Eczema 35.97 28.86 34 7684 72259 110509322
Coagulation test abnormal 35.15 28.86 10 7708 1576 110580005
Hyperproteinaemia 33.26 28.86 7 7711 313 110581268
Aphthous ulcer 31.05 28.86 19 7699 21117 110560464
Metastases to adrenals 30.61 28.86 9 7709 1594 110579987
Cholestasis 29.56 28.86 29 7689 64489 110517092
Thrombocytopenia 29.48 28.86 71 7647 348814 110232767
Drug ineffective 29.40 28.86 38 7680 1520502 109061079

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EH03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA MoA N0000020001 Tyrosine Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

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

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

DiseaseRelationSNOMED_IDDOID
Metastatic human epidermal growth factor 2 positive carcinoma of breast indication 459391000124109




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.87 Basic
pKa2 5.0 Basic
pKa3 3.09 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 9693989 May 9, 2027 TREATMENT OF BREAST CANCER INCLUDING HER2 (ERBB2)-POSITIVE OR -OVEREXPRESSING BREAST CANCER
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 9693989 May 9, 2027 TREATMENT OF BREAST CANCER INCLUDING HER2 (ERBB2)-POSITIVE OR -OVEREXPRESSING BREAST CANCER
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 9457093 Oct. 12, 2032 TREATMENT OF BREAST CANCER INCLUDING HER2 (ERBB2)-POSITIVE OR -OVEREXPRESSING BREAST CANCER
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 9457093 Oct. 12, 2032 TREATMENT OF BREAST CANCER INCLUDING HER2 (ERBB2)-POSITIVE OR -OVEREXPRESSING BREAST CANCER
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 11504370 March 25, 2033 TREATMENT OF BREAST CANCER INCLUDING HER2 (ERBB2)-POSITIVE OR -OVEREXPRESSING BREAST CANCER
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 11504370 March 25, 2033 TREATMENT OF BREAST CANCER INCLUDING HER2 (ERBB2)-POSITIVE OR -OVEREXPRESSING BREAST CANCER
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 11207324 April 27, 2038 COMBINATION TREATMENT WITH TUCATINIB AND TRASTUZUMAB OF ADULTS WITH RAS WILD-TYPE HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING PREVIOUS TREATMENT AS CLAIMED
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 11666572 April 27, 2038 COMBINATION TREATMENT WITH TUCATINIB AND TRASTUZUMAB OF ADULTS WITH RAS WILD-TYPE HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING PREVIOUS TREATMENT AS CLAIMED
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 12048698 April 27, 2038 COMBINATION TREATMENT WITH TUCATINIB AND TRASTUZUMAB OF ADULTS WITH RAS WILD-TYPE HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING PREVIOUS TREATMENT AS CLAIMED
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 11207324 April 27, 2038 COMBINATION TREATMENT WITH TUCATINIB AND TRASTUZUMAB OF ADULTS WITH RAS WILD-TYPE HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING PREVIOUS TREATMENT AS CLAIMED
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 11666572 April 27, 2038 COMBINATION TREATMENT WITH TUCATINIB AND TRASTUZUMAB OF ADULTS WITH RAS WILD-TYPE HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING PREVIOUS TREATMENT AS CLAIMED
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL 12048698 April 27, 2038 COMBINATION TREATMENT WITH TUCATINIB AND TRASTUZUMAB OF ADULTS WITH RAS WILD-TYPE HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING PREVIOUS TREATMENT AS CLAIMED

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL Jan. 19, 2026 TUCATINIB IN COMBINATION WITH TRASTUZUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH RAS WILD-TYPE, HER2-POSITIVE, UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL Jan. 19, 2026 TUCATINIB IN COMBINATION WITH TRASTUZUMAB FOR THE TREATMENT OF ADULT PATIENTS WITH RAS WILD-TYPE, HER2-POSITIVE, UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL April 17, 2027 INDICATED FOR USE IN COMBINATION WITH TRASTUZUMAB AND CAPECITABINE FOR TREATMENT OF ADULT PATIENTS WITH METASTATIC HER2-POSITIVE BREAST CANCER AND BRAIN METASTASES, WHO HAVE RECEIVED ONE OR MORE PRIOR ANTI-HER2-BASED REGIMENS IN THE METASTATIC SETTING
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL April 17, 2027 INDICATED FOR USE IN COMBINATION WITH TRASTUZUMAB AND CAPECITABINE FOR TREATMENT OF ADULT PATIENTS WITH METASTATIC HER2-POSITIVE BREAST CANCER AND BRAIN METASTASES, WHO HAVE RECEIVED ONE OR MORE PRIOR ANTI-HER2-BASED REGIMENS IN THE METASTATIC SETTING
150MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL Jan. 19, 2030 TREATMENT OF ADULT PATIENTS WITH RAS WILD-TYPE, HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY
50MG TUKYSA SEAGEN N213411 April 17, 2020 RX TABLET ORAL Jan. 19, 2030 TREATMENT OF ADULT PATIENTS WITH RAS WILD-TYPE, HER2-POSITIVE UNRESECTABLE OR METASTATIC COLORECTAL CANCER THAT HAS PROGRESSED FOLLOWING TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
ERBB2/ERBB3 Kinase INHIBITOR IC50 8.16 SCIENTIFIC LITERATURE DRUG LABEL
Epidermal growth factor receptor Kinase INHIBITOR IC50 6.35 IUPHAR
Ferrochelatase, mitochondrial Enzyme Kd 5.41 CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 5.61 CHEMBL
Myosin-14 Enzyme Kd 6.73 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase INHIBITOR IC50 6.50 SCIENTIFIC LITERATURE
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.97 CHEMBL

External reference:

IDSource
234248D0HH UNII
4039346 VANDF
C4519167 UMLSCUI
CHEBI:756373 CHEBI
A1A PDB_CHEM_ID
CHEMBL3989868 ChEMBL_ID
51039094 PUBCHEM_CID
DB11652 DRUGBANK_ID
9997 INN_ID
C000705452 MESH_SUPPLEMENTAL_RECORD_UI
D11141 KEGG_DRUG
9922 IUPHAR_LIGAND_ID
871698009 SNOMEDCT_US
871715004 SNOMEDCT_US
333110 MMSL
38332 MMSL
d09542 MMSL
018332 NDDF
2361285 RXNORM
234248D0HH INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TUKYSA HUMAN PRESCRIPTION DRUG LABEL 1 51144-001 TABLET 50 mg ORAL NDA 31 sections
TUKYSA HUMAN PRESCRIPTION DRUG LABEL 1 51144-002 TABLET 150 mg ORAL NDA 31 sections