Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 4715 | 849217-68-1 |
Dose | Unit | Route |
---|---|---|
60 | mg | O |
None
Date | Agency | Company | Orphan |
---|---|---|---|
March 21, 2014 | EMA | TMC Pharma Services Ltd | |
March 25, 2020 | PMDA | Takeda Pharmaceutical Company Limited | |
Nov. 29, 2012 | FDA | EXELIXIS |
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 |
---|---|---|---|---|---|---|
Palmar-plantar erythrodysaesthesia syndrome | 899.15 | 25.15 | 265 | 9018 | 22750 | 63456989 |
Malignant neoplasm progression | 688.52 | 25.15 | 302 | 8981 | 81819 | 63397920 |
Diarrhoea | 335.93 | 25.15 | 462 | 8821 | 714904 | 62764835 |
Hepatic function abnormal | 214.94 | 25.15 | 106 | 9177 | 37036 | 63442703 |
Decreased appetite | 205.27 | 25.15 | 216 | 9067 | 250836 | 63228903 |
Hypothyroidism | 170.44 | 25.15 | 95 | 9188 | 42537 | 63437202 |
Taste disorder | 160.09 | 25.15 | 64 | 9219 | 13598 | 63466141 |
Hypertension | 139.52 | 25.15 | 187 | 9096 | 279116 | 63200623 |
Stomatitis | 134.31 | 25.15 | 131 | 9152 | 138594 | 63341145 |
Hair colour changes | 121.71 | 25.15 | 36 | 9247 | 3091 | 63476648 |
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 |
---|---|---|---|---|---|---|
Palmar-plantar erythrodysaesthesia syndrome | 2324.70 | 20.55 | 723 | 22192 | 16072 | 34917944 |
Malignant neoplasm progression | 1210.67 | 20.55 | 738 | 22177 | 87308 | 34846708 |
Diarrhoea | 772.46 | 20.55 | 1097 | 21818 | 388815 | 34545201 |
Hypothyroidism | 592.24 | 20.55 | 284 | 22631 | 20618 | 34913398 |
Hepatic function abnormal | 589.94 | 20.55 | 365 | 22550 | 43998 | 34890018 |
Decreased appetite | 494.72 | 20.55 | 575 | 22340 | 165817 | 34768199 |
Hypertension | 421.00 | 20.55 | 481 | 22434 | 135962 | 34798054 |
Stomatitis | 397.62 | 20.55 | 281 | 22634 | 42233 | 34891783 |
Taste disorder | 381.88 | 20.55 | 152 | 22763 | 7003 | 34927013 |
Proteinuria | 341.51 | 20.55 | 189 | 22726 | 18453 | 34915563 |
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 |
---|---|---|---|---|---|---|
Palmar-plantar erythrodysaesthesia syndrome | 2856.79 | 21.03 | 853 | 26439 | 32281 | 79684815 |
Malignant neoplasm progression | 1027.60 | 21.03 | 616 | 26676 | 135374 | 79581722 |
Diarrhoea | 898.08 | 21.03 | 1285 | 26007 | 879204 | 78837892 |
Hepatic function abnormal | 809.59 | 21.03 | 426 | 26866 | 72681 | 79644415 |
Hypothyroidism | 736.92 | 21.03 | 359 | 26933 | 52033 | 79665063 |
Decreased appetite | 610.43 | 21.03 | 664 | 26628 | 341754 | 79375342 |
Hypertension | 501.14 | 21.03 | 590 | 26702 | 330402 | 79386694 |
Taste disorder | 484.90 | 21.03 | 188 | 27104 | 15635 | 79701461 |
Proteinuria | 401.25 | 21.03 | 204 | 27088 | 32298 | 79684798 |
Stomatitis | 350.51 | 21.03 | 334 | 26958 | 146423 | 79570673 |
None
Source | Code | Description |
---|---|---|
ATC | L01EX07 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors |
CHEBI has role | CHEBI:35610 | antineoplastic agents |
CHEBI has role | CHEBI:38637 | tyrosine kinase inhibitors |
CHEBI has role | CHEBI:50266 | Prodrugs |
FDA EPC | N0000175605 | Kinase Inhibitor |
FDA MoA | N0000175076 | Protein Kinase Inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Liver cell carcinoma | indication | 109841003 | DOID:684 |
Medullary thyroid carcinoma | indication | 255032005 | DOID:3973 |
Renal cell carcinoma | indication | 702391001 | DOID:4450 |
Metastatic renal cell carcinoma | indication | 702392008 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.15 | acidic |
pKa2 | 11.76 | acidic |
pKa3 | 4.95 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 8497284 | Sept. 24, 2024 | TREATMENT OF ADVANCED RENAL CELL CARCINOMA |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 8497284 | Sept. 24, 2024 | TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 8497284 | Sept. 24, 2024 | TREATMENT OF RENAL CELL CARCINOMA |
EQ 20MG BASE | COMETRIQ | EXELIXIS | N203756 | Nov. 29, 2012 | RX | CAPSULE | ORAL | 11098015 | Jan. 15, 2030 | METHOD OF TREATING MEDULLARY THYROID CANCER |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 11098015 | Jan. 15, 2030 | TREATMENT OF ADVANCED RENAL CELL CARCINOMA |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 11098015 | Jan. 15, 2030 | TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 11098015 | Jan. 15, 2030 | TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 11098015 | Jan. 15, 2030 | TREATMENT OF RENAL CELL CARCINOMA |
EQ 20MG BASE | COMETRIQ | EXELIXIS | N203756 | Nov. 29, 2012 | RX | CAPSULE | ORAL | 8877776 | Oct. 8, 2030 | METHOD OF TREATING MEDULLARY THYROID CANCER |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | 8877776 | Oct. 8, 2030 | TREATMENT OF DIFFERENTIATED THYROID CANCER THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Jan. 22, 2024 | FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Sept. 17, 2024 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Jan. 14, 2026 | INDICATED FOR TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB |
EQ 20MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Sept. 17, 2028 | THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE |
EQ 40MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Jan. 22, 2024 | FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB |
EQ 40MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Sept. 17, 2024 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE |
EQ 40MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Jan. 14, 2026 | INDICATED FOR TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC) WHO HAVE BEEN PREVIOUSLY TREATED WITH SORAFENIB |
EQ 40MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Sept. 17, 2028 | THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE |
EQ 60MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Jan. 22, 2024 | FOR THE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA, AS A FIRST-LINE TREATMENT IN COMBINATION WITH NIVOLUMAB |
EQ 60MG BASE | CABOMETYX | EXELIXIS INC | N208692 | April 25, 2016 | RX | TABLET | ORAL | Sept. 17, 2024 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH LOCALLY ADVANCED OR METASTATIC DIFFERENTIATED THYROID CANCER (DTC) THAT HAS PROGRESSED FOLLOWING PRIOR VEGFR-TARGETED THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY OR INELIGIBLE |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Mast/stem cell growth factor receptor Kit | Kinase | INHIBITOR | IC50 | 8.34 | WOMBAT-PK | DRUG LABEL | |||
Receptor-type tyrosine-protein kinase FLT3 | Kinase | INHIBITOR | IC50 | 7.95 | WOMBAT-PK | DRUG LABEL | |||
Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | INHIBITOR | IC50 | 8.28 | WOMBAT-PK | DRUG LABEL | |||
Vascular endothelial growth factor receptor 2 | Kinase | INHIBITOR | IC50 | 10.46 | WOMBAT-PK | DRUG LABEL | |||
Angiopoietin-1 receptor | Kinase | INHIBITOR | IC50 | 7.85 | WOMBAT-PK | DRUG LABEL | |||
Hepatocyte growth factor receptor | Kinase | INHIBITOR | IC50 | 8.89 | WOMBAT-PK | DRUG LABEL | |||
Ephrin type-A receptor 2 | Kinase | Kd | 6.13 | CHEMBL | |||||
Vascular endothelial growth factor receptor 1 | Kinase | IC50 | 7.92 | CHEMBL | |||||
Vascular endothelial growth factor receptor 3 | Kinase | IC50 | 8.22 | CHEMBL | |||||
Tyrosine-protein kinase HCK | Kinase | Kd | 5.96 | CHEMBL |
ID | Source |
---|---|
014768 | NDDF |
014782 | NDDF |
1140909-48-3 | SECONDARY_CAS_RN |
1363267 | RXNORM |
194795 | MMSL |
1C39JW444G | UNII |
240294 | MMSL |
25102847 | PUBCHEM_CID |
28993 | MMSL |
31609 | MMSL |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-023 | TABLET | 60 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-023 | TABLET | 60 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-023 | TABLET | 60 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-024 | TABLET | 20 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-024 | TABLET | 20 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-024 | TABLET | 20 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-025 | TABLET | 40 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-025 | TABLET | 40 mg | ORAL | NDA | 27 sections |
CABOMETYX | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-025 | TABLET | 40 mg | ORAL | NDA | 27 sections |
COMETRIQ | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42388-013 | CAPSULE | 20 mg | ORAL | NDA | 27 sections |