Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 4318 | 850140-72-6 |
None
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Hosey CM, Chan R, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
Sept. 25, 2013 | EMA | ||
July 12, 2013 | FDA | BOEHRINGER INGELHEIM |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Malignant neoplasm progression | 1640.57 | 26.81 | 554 | 7452 | 64372 | 46613684 |
Diarrhoea | 1166.95 | 26.81 | 863 | 7143 | 558739 | 46119317 |
Paronychia | 704.24 | 26.81 | 162 | 7844 | 4404 | 46673652 |
Stomatitis | 353.13 | 26.81 | 190 | 7816 | 68107 | 46609949 |
Metastases to central nervous system | 266.22 | 26.81 | 92 | 7914 | 11129 | 46666927 |
Rash | 251.75 | 26.81 | 306 | 7700 | 356206 | 46321850 |
Dermatitis acneiform | 203.70 | 26.81 | 59 | 7947 | 4011 | 46674045 |
Decreased appetite | 181.33 | 26.81 | 193 | 7813 | 193643 | 46484413 |
EGFR gene mutation | 145.75 | 26.81 | 25 | 7981 | 133 | 46677923 |
Skin toxicity | 131.15 | 26.81 | 41 | 7965 | 3613 | 46674443 |
Metastases to meninges | 123.95 | 26.81 | 34 | 7972 | 1893 | 46676163 |
Dehydration | 121.70 | 26.81 | 143 | 7863 | 159397 | 46518659 |
Acne | 93.15 | 26.81 | 52 | 7954 | 19867 | 46658189 |
Dry skin | 86.78 | 26.81 | 65 | 7941 | 40951 | 46637105 |
Non-small cell lung cancer | 67.67 | 26.81 | 24 | 7982 | 3120 | 46674936 |
Nail disorder | 67.47 | 26.81 | 31 | 7975 | 7865 | 46670191 |
Pleural effusion | 60.83 | 26.81 | 73 | 7933 | 82879 | 46595177 |
Skin fissures | 58.95 | 26.81 | 28 | 7978 | 7652 | 46670404 |
Mucosal inflammation | 57.42 | 26.81 | 50 | 7956 | 38926 | 46639130 |
Skin disorder | 55.53 | 26.81 | 39 | 7967 | 22224 | 46655832 |
Metastases to bone | 54.08 | 26.81 | 35 | 7971 | 17441 | 46660615 |
Vomiting | 53.11 | 26.81 | 184 | 7822 | 452610 | 46225446 |
Drug resistance | 49.40 | 26.81 | 33 | 7973 | 17335 | 46660721 |
Metastases to lung | 44.81 | 26.81 | 26 | 7980 | 10670 | 46667386 |
Cutaneous symptom | 43.81 | 26.81 | 9 | 7997 | 140 | 46677916 |
Interstitial lung disease | 42.04 | 26.81 | 49 | 7957 | 53900 | 46624156 |
Metastases to liver | 41.30 | 26.81 | 31 | 7975 | 19554 | 46658502 |
Arthralgia | 38.26 | 26.81 | 8 | 7998 | 364595 | 46313461 |
Gene mutation | 38.25 | 26.81 | 12 | 7994 | 1068 | 46676988 |
Onychoclasis | 37.19 | 26.81 | 18 | 7988 | 5126 | 46672930 |
Neoplasm progression | 34.86 | 26.81 | 32 | 7974 | 26651 | 46651405 |
Small cell lung cancer | 34.00 | 26.81 | 12 | 7994 | 1537 | 46676519 |
Acquired gene mutation | 31.12 | 26.81 | 9 | 7997 | 607 | 46677449 |
Oral pain | 30.97 | 26.81 | 29 | 7977 | 24768 | 46653288 |
Rash pustular | 29.44 | 26.81 | 17 | 7989 | 6912 | 46671144 |
Pneumonitis | 29.43 | 26.81 | 30 | 7976 | 28390 | 46649666 |
Epistaxis | 27.98 | 26.81 | 44 | 7962 | 64261 | 46613795 |
Prerenal failure | 27.29 | 26.81 | 10 | 7996 | 1427 | 46676629 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Malignant neoplasm progression | 1191.94 | 34.62 | 420 | 3619 | 71867 | 29876572 |
Diarrhoea | 555.37 | 34.62 | 409 | 3630 | 333694 | 29614745 |
Paronychia | 343.87 | 34.62 | 80 | 3959 | 2931 | 29945508 |
Rash | 247.11 | 34.62 | 204 | 3835 | 191685 | 29756754 |
Metastases to central nervous system | 243.14 | 34.62 | 73 | 3966 | 7211 | 29941228 |
Stomatitis | 214.28 | 34.62 | 103 | 3936 | 37176 | 29911263 |
EGFR gene mutation | 140.81 | 34.62 | 22 | 4017 | 78 | 29948361 |
Dermatitis acneiform | 103.47 | 34.62 | 36 | 4003 | 5653 | 29942786 |
Interstitial lung disease | 85.10 | 34.62 | 68 | 3971 | 60129 | 29888310 |
Decreased appetite | 76.08 | 34.62 | 97 | 3942 | 149813 | 29798626 |
Acne | 53.80 | 34.62 | 26 | 4013 | 9410 | 29939029 |
Skin toxicity | 53.11 | 34.62 | 19 | 4020 | 3230 | 29945209 |
Dehydration | 44.63 | 34.62 | 68 | 3971 | 123471 | 29824968 |
Metastases to bone | 44.40 | 34.62 | 23 | 4016 | 9635 | 29938804 |
Lymphangiosis carcinomatosa | 43.15 | 34.62 | 12 | 4027 | 897 | 29947542 |
Metastases to meninges | 39.86 | 34.62 | 12 | 4027 | 1187 | 29947252 |
Pleural effusion | 37.52 | 34.62 | 48 | 3991 | 74018 | 29874421 |
Nail disorder | 35.30 | 34.62 | 12 | 4027 | 1753 | 29946686 |
Source | Code | Description |
---|---|---|
ATC | L01EB03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors |
FDA MoA | N0000175076 | Protein Kinase Inhibitors |
FDA EPC | N0000175605 | Kinase Inhibitor |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D047428 | Protein Kinase Inhibitors |
CHEBI has role | CHEBI:35610 | cytostatic |
CHEBI has role | CHEBI:38637 | tyrosine kinase inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Non-small cell lung cancer, positive for epidermal growth factor receptor expression | indication | 426964009 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.1 | acidic |
pKa2 | 8.94 | Basic |
pKa3 | 4.09 | Basic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 20MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | Jan. 12, 2021 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE NON-RESISTANT EPIDERMAL GROWTH FACTOR RECEPTOR MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST |
EQ 30MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | Jan. 12, 2021 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE NON-RESISTANT EPIDERMAL GROWTH FACTOR RECEPTOR MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST |
EQ 40MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | Jan. 12, 2021 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE NON-RESISTANT EPIDERMAL GROWTH FACTOR RECEPTOR MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST |
EQ 20MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | April 15, 2023 | TREATMENT OF PATIENTS WITH METASTATIC, SQUAMOUS, NON-SMALL CELL LUNG CANCER PROGRESSING AFTER PLATINUM-BASED CHEMOTHERAPY |
EQ 30MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | April 15, 2023 | TREATMENT OF PATIENTS WITH METASTATIC, SQUAMOUS, NON-SMALL CELL LUNG CANCER PROGRESSING AFTER PLATINUM-BASED CHEMOTHERAPY |
EQ 40MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | April 15, 2023 | TREATMENT OF PATIENTS WITH METASTATIC, SQUAMOUS, NON-SMALL CELL LUNG CANCER PROGRESSING AFTER PLATINUM-BASED CHEMOTHERAPY |
EQ 20MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | Jan. 12, 2025 | FIRST-LINE TREATMENT OF METASTATIC NONSMALL CELL LUNG CANCER WHOSE TUMORS HAVE NON-RESISTANT EPIDERMAL GROWTH FACTOR MUTATIONS OTHER THAN EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST |
EQ 30MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | Jan. 12, 2025 | FIRST-LINE TREATMENT OF METASTATIC NONSMALL CELL LUNG CANCER WHOSE TUMORS HAVE NON-RESISTANT EPIDERMAL GROWTH FACTOR MUTATIONS OTHER THAN EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST |
EQ 40MG BASE | GILOTRIF | BOEHRINGER INGELHEIM | N201292 | July 12, 2013 | RX | TABLET | ORAL | Jan. 12, 2025 | FIRST-LINE TREATMENT OF METASTATIC NONSMALL CELL LUNG CANCER WHOSE TUMORS HAVE NON-RESISTANT EPIDERMAL GROWTH FACTOR MUTATIONS OTHER THAN EXON 19 DELETIONS OR EXON 21 (L858R) SUBSTITUTION MUTATIONS AS DETECTED BY AN FDA-APPROVED TEST |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Epidermal growth factor receptor | Kinase | INHIBITOR | Kd | 10 | CHEMBL | CHEMBL | |||
Receptor tyrosine-protein kinase erbB-2 | Kinase | INHIBITOR | Kd | 8.30 | CHEMBL | CHEMBL | |||
Receptor tyrosine-protein kinase erbB-4 | Kinase | INHIBITOR | Kd | 8.20 | CHEMBL | CHEMBL | |||
Mitogen-activated protein kinase 9 | Kinase | Kd | 5.68 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase Src | Kinase | Kd | 5.55 | CHEMBL | |||||
Dual specificity tyrosine-phosphorylation-regulated kinase 2 | Kinase | Kd | 5.74 | CHEMBL | |||||
Hepatocyte growth factor receptor | Kinase | Kd | 5.66 | CHEMBL | |||||
Casein kinase I isoform epsilon | Kinase | Kd | 5.89 | CHEMBL | |||||
Receptor-interacting serine/threonine-protein kinase 2 | Kinase | Kd | 5.57 | CHEMBL | |||||
Ribosomal protein S6 kinase alpha-6 | Kinase | Kd | 5.51 | CHEMBL | |||||
Cyclin-G-associated kinase | Kinase | Kd | 7.10 | CHEMBL | |||||
Serine/threonine-protein kinase SBK1 | Kinase | Kd | 5.32 | CHEMBL | |||||
Dual specificity mitogen-activated protein kinase kinase 5 | Kinase | Kd | 5.89 | CHEMBL | |||||
MAP kinase-interacting serine/threonine-protein kinase 1 | Kinase | Kd | 5.74 | CHEMBL | |||||
Tyrosine-protein kinase FRK | Kinase | Kd | 5.85 | CHEMBL | |||||
Serine/threonine-protein kinase 10 | Kinase | Kd | 5.37 | CHEMBL | |||||
Tyrosine-protein kinase HCK | Kinase | Kd | 5.66 | CHEMBL | |||||
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Kinase | Kd | 6.33 | CHEMBL | |||||
Citron Rho-interacting kinase | Kinase | Kd | 5.54 | CHEMBL | |||||
Homeodomain-interacting protein kinase 4 | Kinase | Kd | 6.44 | CHEMBL | |||||
Serine/threonine-protein kinase 17A | Kinase | Kd | 5.64 | CHEMBL | |||||
Ephrin type-A receptor 6 | Kinase | Kd | 6.47 | CHEMBL | |||||
STE20-like serine/threonine-protein kinase | Kinase | Kd | 5.43 | CHEMBL | |||||
MAP kinase-interacting serine/threonine-protein kinase 2 | Kinase | Kd | 5.80 | CHEMBL | |||||
Interleukin-1 receptor-associated kinase 1 | Kinase | Kd | 6.62 | CHEMBL | |||||
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform | Kinase | Kd | 5.89 | CHEMBL | |||||
Tyrosine-protein kinase Blk | Kinase | Kd | 6.66 | CHEMBL | |||||
Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Kinase | Kd | 5.55 | CHEMBL | |||||
Receptor tyrosine-protein kinase erbB-3 | Kinase | Kd | 5.35 | CHEMBL | |||||
Ephrin type-B receptor 6 | Kinase | Kd | 5.51 | CHEMBL | |||||
Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Kinase | Kd | 6.01 | CHEMBL | |||||
Tyrosine-protein kinase Lck | Kinase | Kd | 6.24 | CHEMBL | |||||
Tyrosine-protein kinase receptor UFO | Kinase | Kd | 5.28 | CHEMBL | |||||
Tyrosine-protein kinase TXK | Kinase | Kd | 5.51 | CHEMBL | |||||
Mitogen-activated protein kinase 10 | Kinase | Kd | 5.70 | CHEMBL | |||||
Mitogen-activated protein kinase 14 | Kinase | Kd | 5.89 | CHEMBL | |||||
Tyrosine-protein kinase ABL1 | Kinase | Kd | 6.64 | CHEMBL | |||||
Receptor-type tyrosine-protein kinase FLT3 | Kinase | Kd | 5.85 | CHEMBL |
ID | Source |
---|---|
41UD74L59M | UNII |
4032662 | VUID |
N0000188388 | NUI |
D09724 | KEGG_DRUG |
850140-73-7 | SECONDARY_CAS_RN |
4032662 | VANDF |
4032663 | VANDF |
C2987648 | UMLSCUI |
CHEBI:61390 | CHEBI |
0WM | PDB_CHEM_ID |
CHEMBL1173655 | ChEMBL_ID |
CHEMBL2105712 | ChEMBL_ID |
10184653 | PUBCHEM_CID |
CHEMBL2347958 | ChEMBL_ID |
DB08916 | DRUGBANK_ID |
D000077716 | MESH_DESCRIPTOR_UI |
9230 | INN_ID |
5667 | IUPHAR_LIGAND_ID |
1430268 | RXNORM |
204142 | MMSL |
29566 | MMSL |
d08113 | MMSL |
015117 | NDDF |
015118 | NDDF |
703579002 | SNOMEDCT_US |
703580004 | SNOMEDCT_US |
703582007 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Gilotrif | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0597-0137 | TABLET, FILM COATED | 30 mg | ORAL | NDA | 31 sections |
Gilotrif | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0597-0138 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 31 sections |
Gilotrif | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0597-0141 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 31 sections |