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| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5062 | 1421373-65-0 |
| Dose | Unit | Route |
|---|---|---|
| 80 | mg | O |
None
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.906 | High | 0.88 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 7.145 | High | 0.88 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 13.552 | 10^-6 cm/s | High | 0.88 |
| dh-clint | Dog hepatocyte intrinsic clearance | 14.622 | uL/min/10^6 cells | High | 0.88 |
| dppb | Dog plasma protein binding (% unbound) | 1.730 | % | High | 0.88 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 6.530 | % | High | 0.88 |
| herg | hERG pIC50 | 5.416 | pIC50 | High | 0.88 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.767 | uL/min/10^6 cells | High | 0.88 |
| hlm-clint | Human liver microsomal intrinsic clearance | 10.593 | uL/min/mg protein | High | 0.88 |
| hppb | Human plasma protein binding (% unbound) | 2.380 | % | High | 0.88 |
| kinase-safety-class | AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK4,CHEK1,CHEK2,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHA2,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FYN,GAK,GRK2,IGF1R,INSR,INSRR,IRAK1,IRAK3,IRAK4,ITK,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK3,MAPK7,MARK4,MELK,MKNK1,MKNK2,NTRK1,PDGFRB,PDK1,PDK2,PDK4,PLK1,PLK2,PLK3,PLK4,PRKCD,PTK6,RET,RIPK3,SIK2,SIK3,SRC,STK33,SYK,TEK,TNK1,TTK,ULK1,YES1 | 93 | |||
| kinase-selectivity-class | AAK1,ACVR2B,ALK,BLK,BMX,BTK,CAMK2D,EGFR,ERBB2,ERBB4,GAK,IGF1R,INSR,JAK3,LRRK2,MAP3K9,MAPK7,MINK1,MKNK2,PDK4,PLK2,STK33,TNK1 | 23 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 8.710 | High | 0.88 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 9.078 | High | 0.88 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 51.286 | High | 0.88 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.650 | High | 0.88 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 46.559 | High | 0.88 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.68 | |
| pppb | Pig plasma protein binding (% unbound) | 5.610 | % | High | 0.88 |
| rat-kpuu-brain | Rat brain Kpuu | 0.053 | % | High | 0.88 |
| rh-clint | Rat hepatocyte intrinsic clearance | 33.574 | uL/min/10^6 cells | High | 0.88 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 7.630 | % | High | 0.88 |
| rppb | Rat plasma protein binding (% unbound) | 1.970 | % | High | 0.88 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 679.204 | uM | High | 0.88 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 28, 2016 | PMDA | AstraZeneca K.K. | |
| Feb. 2, 2016 | EMA | AstraZeneca AB | |
| Nov. 13, 2015 | FDA | ASTRAZENECA PHARMS |
| 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 | 2994.57 | 24.12 | 1008 | 15922 | 105862 | 90505655 |
| Death | 2498.30 | 24.12 | 1345 | 15585 | 455206 | 90156311 |
| Drug resistance | 1268.92 | 24.12 | 390 | 16540 | 30059 | 90581458 |
| Acquired gene mutation | 1201.50 | 24.12 | 208 | 16722 | 1071 | 90610446 |
| Myelosuppression | 1030.60 | 24.12 | 384 | 16546 | 53207 | 90558310 |
| Metastases to central nervous system | 672.36 | 24.12 | 211 | 16719 | 17331 | 90594186 |
| Interstitial lung disease | 608.97 | 24.12 | 293 | 16637 | 76112 | 90535405 |
| Metastases to meninges | 417.46 | 24.12 | 104 | 16826 | 3631 | 90607886 |
| EGFR gene mutation | 397.66 | 24.12 | 67 | 16863 | 283 | 90611234 |
| Paronychia | 373.25 | 24.12 | 112 | 16818 | 7894 | 90603623 |
| Malignant transformation | 329.59 | 24.12 | 62 | 16868 | 540 | 90610977 |
| Disease progression | 256.22 | 24.12 | 221 | 16709 | 156394 | 90455123 |
| Pneumonitis | 248.24 | 24.12 | 134 | 16796 | 44036 | 90567481 |
| Hepatic function abnormal | 231.43 | 24.12 | 130 | 16800 | 46158 | 90565359 |
| Metastases to bone | 197.31 | 24.12 | 96 | 16834 | 25409 | 90586108 |
| Metastases to liver | 183.36 | 24.12 | 95 | 16835 | 28712 | 90582805 |
| Pleural effusion | 182.93 | 24.12 | 158 | 16772 | 111833 | 90499684 |
| Metastases to lung | 182.89 | 24.12 | 79 | 16851 | 15912 | 90595605 |
| Diarrhoea | 155.42 | 24.12 | 454 | 16476 | 938736 | 89672781 |
| Non-small cell lung cancer | 144.26 | 24.12 | 47 | 16883 | 4334 | 90607183 |
| Platelet count decreased | 136.03 | 24.12 | 147 | 16783 | 136822 | 90474695 |
| Dermatitis acneiform | 134.56 | 24.12 | 49 | 16881 | 6305 | 90605212 |
| Electrocardiogram QT prolonged | 130.10 | 24.12 | 108 | 16822 | 72348 | 90539169 |
| Cardiac failure | 120.23 | 24.12 | 124 | 16806 | 109372 | 90502145 |
| Skin toxicity | 102.89 | 24.12 | 41 | 16889 | 6738 | 90604779 |
| Blood creatine phosphokinase increased | 97.27 | 24.12 | 67 | 16863 | 33956 | 90577561 |
| Decreased appetite | 96.18 | 24.12 | 215 | 16715 | 376325 | 90235192 |
| Lymphangiosis carcinomatosa | 93.74 | 24.12 | 27 | 16903 | 1645 | 90609872 |
| Small cell lung cancer | 91.42 | 24.12 | 27 | 16903 | 1797 | 90609720 |
| Arthralgia | 90.31 | 24.12 | 18 | 16912 | 778504 | 89833013 |
| Gene mutation | 87.29 | 24.12 | 27 | 16903 | 2103 | 90609414 |
| Pain | 83.72 | 24.12 | 41 | 16889 | 996300 | 89615217 |
| Metastasis | 82.43 | 24.12 | 34 | 16896 | 6103 | 90605414 |
| Pulmonary embolism | 80.13 | 24.12 | 110 | 16820 | 130710 | 90480807 |
| Radiation pneumonitis | 78.03 | 24.12 | 24 | 16906 | 1834 | 90609683 |
| Ejection fraction decreased | 75.75 | 24.12 | 52 | 16878 | 26201 | 90585316 |
| Deep vein thrombosis | 75 | 24.12 | 89 | 16841 | 91531 | 90519986 |
| Carcinoembryonic antigen increased | 72.49 | 24.12 | 24 | 16906 | 2326 | 90609191 |
| Joint swelling | 71.74 | 24.12 | 6 | 16924 | 503294 | 90108223 |
| Cardiotoxicity | 67.99 | 24.12 | 36 | 16894 | 11353 | 90600164 |
| Cardiomyopathy | 67.88 | 24.12 | 44 | 16886 | 20162 | 90591355 |
| BRAF V600E mutation positive | 65.75 | 24.12 | 11 | 16919 | 44 | 90611473 |
| Neutrophil count decreased | 62.73 | 24.12 | 72 | 16858 | 71460 | 90540057 |
| Metastases to lymph nodes | 61.56 | 24.12 | 34 | 16896 | 11655 | 90599862 |
| Thrombocytopenia | 61.01 | 24.12 | 126 | 16804 | 208599 | 90402918 |
| Nasopharyngitis | 60.42 | 24.12 | 4 | 16926 | 407100 | 90204417 |
| Malignant pleural effusion | 55.92 | 24.12 | 21 | 16909 | 2943 | 90608574 |
| Abdominal discomfort | 53.28 | 24.12 | 12 | 16918 | 477316 | 90134201 |
| Weight increased | 51.99 | 24.12 | 8 | 16922 | 417919 | 90193598 |
| Swelling | 49.96 | 24.12 | 9 | 16921 | 419049 | 90192468 |
| Infusion related reaction | 49.58 | 24.12 | 9 | 16921 | 416771 | 90194746 |
| Sinusitis | 46.44 | 24.12 | 5 | 16925 | 343083 | 90268434 |
| Headache | 46.30 | 24.12 | 56 | 16874 | 862690 | 89748827 |
| Cardiac dysfunction | 45.18 | 24.12 | 19 | 16911 | 3578 | 90607939 |
| Metastases to pleura | 44.16 | 24.12 | 16 | 16914 | 2028 | 90609489 |
| Non-small cell lung cancer recurrent | 44.13 | 24.12 | 9 | 16921 | 123 | 90611394 |
| Torsade de pointes | 43.62 | 24.12 | 30 | 16900 | 15152 | 90596365 |
| Dry skin | 43.61 | 24.12 | 67 | 16863 | 88006 | 90523511 |
| Cardiac tamponade | 42.93 | 24.12 | 21 | 16909 | 5611 | 90605906 |
| Respiratory failure | 42.51 | 24.12 | 78 | 16852 | 118340 | 90493177 |
| Erythema multiforme | 41.95 | 24.12 | 27 | 16903 | 12219 | 90599298 |
| Hypersensitivity | 40.73 | 24.12 | 17 | 16913 | 454660 | 90156857 |
| Therapeutic product effect decreased | 40.37 | 24.12 | 3 | 16927 | 277568 | 90333949 |
| Cerebral infarction | 40.29 | 24.12 | 36 | 16894 | 26560 | 90584957 |
| Drug hypersensitivity | 38.92 | 24.12 | 19 | 16911 | 463590 | 90147927 |
| Musculoskeletal stiffness | 38.44 | 24.12 | 5 | 16925 | 296527 | 90314990 |
| Granulocyte count decreased | 37.80 | 24.12 | 15 | 16915 | 2437 | 90609080 |
| White blood cell count decreased | 37.68 | 24.12 | 91 | 16839 | 167018 | 90444499 |
| Hepatic cytolysis | 37.53 | 24.12 | 37 | 16893 | 30879 | 90580638 |
| Lung adenocarcinoma | 37.26 | 24.12 | 19 | 16911 | 5546 | 90605971 |
| Pancytopenia | 35.57 | 24.12 | 73 | 16857 | 120190 | 90491327 |
| Treatment failure | 35.20 | 24.12 | 7 | 16923 | 303921 | 90307596 |
| Discomfort | 34.68 | 24.12 | 5 | 16925 | 274330 | 90337187 |
| Neoplasm progression | 34.39 | 24.12 | 42 | 16888 | 44444 | 90567073 |
| Pericarditis | 33.97 | 24.12 | 5 | 16925 | 270146 | 90341371 |
| Pulmonary toxicity | 33.63 | 24.12 | 23 | 16907 | 11508 | 90600009 |
| Hepatotoxicity | 33.38 | 24.12 | 42 | 16888 | 45800 | 90565717 |
| Mobility decreased | 33.05 | 24.12 | 4 | 16926 | 250730 | 90360787 |
| Lower respiratory tract infection | 33.04 | 24.12 | 4 | 16926 | 250655 | 90360862 |
| Maternal exposure during pregnancy | 32.98 | 24.12 | 13 | 16917 | 360050 | 90251467 |
| Bone marrow failure | 32.66 | 24.12 | 35 | 16895 | 32186 | 90579331 |
| Lung disorder | 32.07 | 24.12 | 80 | 16850 | 149803 | 90461714 |
| Peripheral swelling | 31.64 | 24.12 | 19 | 16911 | 413087 | 90198430 |
| Rash | 31.56 | 24.12 | 255 | 16675 | 795845 | 89815672 |
| Pneumothorax | 31.15 | 24.12 | 27 | 16903 | 19140 | 90592377 |
| Contusion | 30.79 | 24.12 | 5 | 16925 | 251211 | 90360306 |
| Off label use | 30.60 | 24.12 | 327 | 16603 | 1101925 | 89509592 |
| Skin disorder | 30.58 | 24.12 | 36 | 16894 | 36670 | 90574847 |
| Impaired healing | 30.23 | 24.12 | 4 | 16926 | 234195 | 90377322 |
| Subacute cutaneous lupus erythematosus | 29.25 | 24.12 | 14 | 16916 | 3568 | 90607949 |
| Multiple-drug resistance | 28.77 | 24.12 | 18 | 16912 | 7758 | 90603759 |
| Anxiety | 28.67 | 24.12 | 11 | 16919 | 309761 | 90301756 |
| Wheezing | 28.59 | 24.12 | 5 | 16925 | 238075 | 90373442 |
| Hepatic enzyme increased | 28.46 | 24.12 | 16 | 16914 | 360720 | 90250797 |
| Cardiac failure acute | 28.35 | 24.12 | 21 | 16909 | 11908 | 90599609 |
| Non-small cell lung cancer metastatic | 27.84 | 24.12 | 9 | 16921 | 809 | 90610708 |
| Renal impairment | 27.71 | 24.12 | 61 | 16869 | 105360 | 90506157 |
| Acute pulmonary oedema | 27.69 | 24.12 | 19 | 16911 | 9561 | 90601956 |
| Insomnia | 27.47 | 24.12 | 14 | 16916 | 333460 | 90278057 |
| Hypertension | 27.46 | 24.12 | 27 | 16903 | 457505 | 90154012 |
| Haematotoxicity | 27.42 | 24.12 | 21 | 16909 | 12514 | 90599003 |
| Thrombophlebitis migrans | 27.28 | 24.12 | 7 | 16923 | 275 | 90611242 |
| Blister | 27.26 | 24.12 | 7 | 16923 | 254991 | 90356526 |
| Pain in extremity | 26.56 | 24.12 | 27 | 16903 | 450502 | 90161015 |
| Metastases to adrenals | 26.26 | 24.12 | 9 | 16921 | 969 | 90610548 |
| Eosinophilic pneumonia | 26.23 | 24.12 | 12 | 16918 | 2761 | 90608756 |
| Drug ineffective | 26.17 | 24.12 | 152 | 16778 | 1384146 | 89227371 |
| Osteoarthritis | 26.10 | 24.12 | 3 | 16927 | 195727 | 90415790 |
| Pericardial effusion | 25.64 | 24.12 | 33 | 16897 | 36800 | 90574717 |
| Migraine | 25.18 | 24.12 | 3 | 16927 | 190389 | 90421128 |
| Pulmonary alveolar haemorrhage | 25.04 | 24.12 | 15 | 16915 | 5983 | 90605534 |
| Onychoclasis | 24.57 | 24.12 | 16 | 16914 | 7383 | 90604134 |
| Ill-defined disorder | 24.24 | 24.12 | 3 | 16927 | 184888 | 90426629 |
| Immune thrombocytopenia | 24.17 | 24.12 | 20 | 16910 | 13306 | 90598211 |
| Stress cardiomyopathy | 24.13 | 24.12 | 20 | 16910 | 13335 | 90598182 |
| 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 | 1403.73 | 25.54 | 586 | 7696 | 107814 | 42505239 |
| Death | 844.95 | 25.54 | 703 | 7579 | 470482 | 42142571 |
| Drug resistance | 630.44 | 25.54 | 240 | 8042 | 34008 | 42579045 |
| Acquired gene mutation | 615.36 | 25.54 | 123 | 8159 | 1457 | 42611596 |
| Metastases to central nervous system | 427.48 | 25.54 | 133 | 8149 | 10222 | 42602831 |
| Myelosuppression | 313.29 | 25.54 | 154 | 8128 | 40307 | 42572746 |
| Interstitial lung disease | 273.81 | 25.54 | 177 | 8105 | 78285 | 42534768 |
| EGFR gene mutation | 272.46 | 25.54 | 46 | 8236 | 188 | 42612865 |
| Metastases to meninges | 269.68 | 25.54 | 65 | 8217 | 1896 | 42611157 |
| Pneumonitis | 142.46 | 25.54 | 93 | 8189 | 41625 | 42571428 |
| Hepatic function abnormal | 133.68 | 25.54 | 97 | 8185 | 51470 | 42561583 |
| Paronychia | 123.90 | 25.54 | 42 | 8240 | 4213 | 42608840 |
| Malignant transformation | 117.05 | 25.54 | 29 | 8253 | 949 | 42612104 |
| Metastases to liver | 113.90 | 25.54 | 58 | 8224 | 16268 | 42596785 |
| Metastases to lung | 111.22 | 25.54 | 51 | 8231 | 11373 | 42601680 |
| Metastases to bone | 107.37 | 25.54 | 54 | 8228 | 14755 | 42598298 |
| Disease progression | 86.39 | 25.54 | 122 | 8160 | 143534 | 42469519 |
| Pleural effusion | 68.17 | 25.54 | 89 | 8193 | 97077 | 42515976 |
| Dermatitis acneiform | 55.42 | 25.54 | 28 | 8254 | 7711 | 42605342 |
| Metastases to adrenals | 53.25 | 25.54 | 16 | 8266 | 1086 | 42611967 |
| Carcinoembryonic antigen increased | 47.58 | 25.54 | 14 | 8268 | 884 | 42612169 |
| Metastases to lymph nodes | 46.79 | 25.54 | 23 | 8259 | 5975 | 42607078 |
| BRAF V600E mutation positive | 46.74 | 25.54 | 8 | 8274 | 36 | 42613017 |
| Malignant pleural effusion | 44.24 | 25.54 | 16 | 8266 | 1939 | 42611114 |
| Lung disorder | 41.77 | 25.54 | 49 | 8233 | 47874 | 42565179 |
| Pulmonary embolism | 39.86 | 25.54 | 78 | 8204 | 119534 | 42493519 |
| Decreased appetite | 38.78 | 25.54 | 103 | 8179 | 193034 | 42420019 |
| Radiation pneumonitis | 34.64 | 25.54 | 15 | 8267 | 2918 | 42610135 |
| Rash | 34.47 | 25.54 | 125 | 8157 | 276829 | 42336224 |
| Pulmonary toxicity | 33.72 | 25.54 | 21 | 8261 | 8634 | 42604419 |
| Electrocardiogram QT prolonged | 33.70 | 25.54 | 44 | 8238 | 47901 | 42565152 |
| Metastasis | 33.62 | 25.54 | 17 | 8265 | 4688 | 42608365 |
| Lymphangiosis carcinomatosa | 33.21 | 25.54 | 11 | 8271 | 1026 | 42612027 |
| Genital tract inflammation | 32.45 | 25.54 | 6 | 8276 | 45 | 42613008 |
| Platelet count decreased | 29.93 | 25.54 | 76 | 8206 | 138505 | 42474548 |
| Drug-induced liver injury | 29.85 | 25.54 | 37 | 8245 | 38236 | 42574817 |
| Metastases to pleura | 29.79 | 25.54 | 9 | 8273 | 622 | 42612431 |
| Liver disorder | 28.82 | 25.54 | 37 | 8245 | 39607 | 42573446 |
| Gene mutation | 27.40 | 25.54 | 11 | 8271 | 1770 | 42611283 |
| 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 | 3075.96 | 22.72 | 1170 | 19619 | 173397 | 110395113 |
| Drug resistance | 1755.85 | 22.72 | 579 | 20210 | 55795 | 110512715 |
| Acquired gene mutation | 1662.44 | 22.72 | 308 | 20481 | 2446 | 110566064 |
| Death | 1495.13 | 22.72 | 1147 | 19642 | 697722 | 109870788 |
| Myelosuppression | 1240.20 | 22.72 | 514 | 20275 | 93826 | 110474684 |
| Interstitial lung disease | 826.04 | 22.72 | 438 | 20351 | 138896 | 110429614 |
| Metastases to central nervous system | 759.87 | 22.72 | 247 | 20542 | 22570 | 110545940 |
| EGFR gene mutation | 591.07 | 22.72 | 101 | 20688 | 469 | 110568041 |
| Paronychia | 430.65 | 22.72 | 135 | 20654 | 10946 | 110557564 |
| Malignant transformation | 422.16 | 22.72 | 89 | 20700 | 1436 | 110567074 |
| Metastases to meninges | 393.44 | 22.72 | 106 | 20683 | 5022 | 110563488 |
| Hepatic function abnormal | 374.23 | 22.72 | 224 | 20565 | 89071 | 110479439 |
| Metastases to lung | 283.14 | 22.72 | 120 | 20669 | 22943 | 110545567 |
| Metastases to liver | 272.43 | 22.72 | 133 | 20656 | 35253 | 110533257 |
| Pneumonitis | 269.75 | 22.72 | 172 | 20617 | 76359 | 110492151 |
| Metastases to bone | 266.03 | 22.72 | 126 | 20663 | 31246 | 110537264 |
| Pleural effusion | 227.03 | 22.72 | 219 | 20570 | 177490 | 110391020 |
| Dermatitis acneiform | 186.09 | 22.72 | 75 | 20714 | 12620 | 110555890 |
| Platelet count decreased | 176.70 | 22.72 | 217 | 20572 | 230226 | 110338284 |
| Electrocardiogram QT prolonged | 146.08 | 22.72 | 138 | 20651 | 108822 | 110459688 |
| Diarrhoea | 145.24 | 22.72 | 506 | 20283 | 1138999 | 109429511 |
| Disease progression | 132.14 | 22.72 | 194 | 20595 | 243840 | 110324670 |
| Lymphangiosis carcinomatosa | 125.31 | 22.72 | 37 | 20752 | 2445 | 110566065 |
| Decreased appetite | 123.00 | 22.72 | 274 | 20515 | 475572 | 110092938 |
| Cardiac failure | 117.59 | 22.72 | 160 | 20629 | 187466 | 110381044 |
| BRAF V600E mutation positive | 115.12 | 22.72 | 19 | 20770 | 68 | 110568442 |
| Malignant pleural effusion | 107.10 | 22.72 | 37 | 20752 | 4056 | 110564454 |
| Gene mutation | 105.48 | 22.72 | 35 | 20754 | 3394 | 110565116 |
| Carcinoembryonic antigen increased | 99.72 | 22.72 | 32 | 20757 | 2792 | 110565718 |
| Radiation pneumonitis | 99.63 | 22.72 | 36 | 20753 | 4500 | 110564010 |
| Metastases to lymph nodes | 99.43 | 22.72 | 51 | 20738 | 14981 | 110553529 |
| Small cell lung cancer | 95.09 | 22.72 | 32 | 20757 | 3240 | 110565270 |
| Pulmonary embolism | 86.37 | 22.72 | 149 | 20640 | 214325 | 110354185 |
| Blood creatine phosphokinase increased | 81.96 | 22.72 | 84 | 20705 | 72993 | 110495517 |
| Arthralgia | 77.70 | 22.72 | 25 | 20764 | 779607 | 109788903 |
| Ejection fraction decreased | 77.30 | 22.72 | 63 | 20726 | 40817 | 110527693 |
| Metastases to pleura | 75.41 | 22.72 | 24 | 20765 | 2039 | 110566471 |
| Skin toxicity | 75.11 | 22.72 | 39 | 20750 | 11744 | 110556766 |
| Metastasis | 72.49 | 22.72 | 34 | 20755 | 8233 | 110560277 |
| Pulmonary toxicity | 70.30 | 22.72 | 43 | 20746 | 17703 | 110550807 |
| Pain | 69.96 | 22.72 | 47 | 20742 | 954908 | 109613602 |
| Rash | 69.09 | 22.72 | 321 | 20468 | 820643 | 109747867 |
| Joint swelling | 67.26 | 22.72 | 4 | 20785 | 442841 | 110125669 |
| Lung disorder | 67.18 | 22.72 | 121 | 20668 | 179926 | 110388584 |
| Cardiotoxicity | 64.57 | 22.72 | 40 | 20749 | 16841 | 110551669 |
| Metastases to adrenals | 64.22 | 22.72 | 20 | 20769 | 1583 | 110566927 |
| Cardiomyopathy | 64.09 | 22.72 | 52 | 20737 | 33473 | 110535037 |
| Non-small cell lung cancer | 61.55 | 22.72 | 30 | 20759 | 7905 | 110560605 |
| Deep vein thrombosis | 61.35 | 22.72 | 101 | 20688 | 139786 | 110428724 |
| Cardiac dysfunction | 58.94 | 22.72 | 27 | 20762 | 6196 | 110562314 |
| Thrombocytopenia | 56.81 | 22.72 | 169 | 20620 | 348716 | 110219794 |
| Non-small cell lung cancer recurrent | 56.65 | 22.72 | 12 | 20777 | 198 | 110568312 |
| Nasopharyngitis | 55.77 | 22.72 | 5 | 20784 | 394356 | 110174154 |
| Pneumothorax | 55.67 | 22.72 | 49 | 20740 | 35236 | 110533274 |
| Cerebral infarction | 53.48 | 22.72 | 57 | 20732 | 51781 | 110516729 |
| Erythema multiforme | 49.62 | 22.72 | 37 | 20752 | 21060 | 110547450 |
| White blood cell count decreased | 49.20 | 22.72 | 123 | 20666 | 229267 | 110339243 |
| Drug-induced liver injury | 47.74 | 22.72 | 83 | 20706 | 119984 | 110448526 |
| Confusional state | 44.94 | 22.72 | 16 | 20773 | 468664 | 110099846 |
| Respiratory failure | 44.65 | 22.72 | 114 | 20675 | 215218 | 110353292 |
| Weight increased | 44.40 | 22.72 | 12 | 20777 | 419632 | 110148878 |
| Cardiac failure acute | 43.20 | 22.72 | 36 | 20753 | 24042 | 110544468 |
| Torsade de pointes | 43.08 | 22.72 | 35 | 20754 | 22565 | 110545945 |
| Dry skin | 42.25 | 22.72 | 74 | 20715 | 107579 | 110460931 |
| Neutrophil count decreased | 42.21 | 22.72 | 79 | 20710 | 120862 | 110447648 |
| Headache | 41.17 | 22.72 | 64 | 20725 | 882313 | 109686197 |
| Drug hypersensitivity | 41.04 | 22.72 | 17 | 20772 | 454073 | 110114437 |
| Granulocyte count decreased | 40.03 | 22.72 | 18 | 20771 | 3956 | 110564554 |
| Multiple-drug resistance | 39.88 | 22.72 | 27 | 20762 | 13208 | 110555302 |
| Arthropathy | 39.70 | 22.72 | 4 | 20785 | 287518 | 110280992 |
| Swelling | 39.14 | 22.72 | 9 | 20780 | 351032 | 110217478 |
| Liver disorder | 38.97 | 22.72 | 84 | 20705 | 142159 | 110426351 |
| Hypersensitivity | 38.36 | 22.72 | 14 | 20775 | 403984 | 110164526 |
| Lung adenocarcinoma | 37.51 | 22.72 | 23 | 20766 | 9508 | 110559002 |
| Abdominal discomfort | 36.81 | 22.72 | 14 | 20775 | 393844 | 110174666 |
| Hypertension | 36.07 | 22.72 | 26 | 20763 | 510058 | 110058452 |
| Pain in extremity | 35.54 | 22.72 | 24 | 20765 | 487094 | 110081416 |
| Metastases to kidney | 34.91 | 22.72 | 10 | 20779 | 593 | 110567917 |
| Erythema dyschromicum perstans | 34.89 | 22.72 | 7 | 20782 | 87 | 110568423 |
| Lower respiratory tract infection | 34.57 | 22.72 | 3 | 20786 | 243103 | 110325407 |
| Lung carcinoma cell type unspecified recurrent | 34.03 | 22.72 | 9 | 20780 | 396 | 110568114 |
| Pericardial effusion | 33.10 | 22.72 | 47 | 20742 | 57170 | 110511340 |
| Therapeutic product effect decreased | 32.21 | 22.72 | 4 | 20785 | 244312 | 110324198 |
| Left ventricular dysfunction | 31.91 | 22.72 | 30 | 20759 | 23463 | 110545047 |
| Hypotension | 31.76 | 22.72 | 31 | 20758 | 523818 | 110044692 |
| Maternal exposure during pregnancy | 31.66 | 22.72 | 5 | 20784 | 254878 | 110313632 |
| Musculoskeletal stiffness | 31.53 | 22.72 | 7 | 20782 | 279815 | 110288695 |
| Anxiety | 31.04 | 22.72 | 13 | 20776 | 345065 | 110223445 |
| TP53 gene mutation | 30.97 | 22.72 | 7 | 20782 | 158 | 110568352 |
| BRAF gene mutation | 30.92 | 22.72 | 6 | 20783 | 62 | 110568448 |
| Condition aggravated | 30.84 | 22.72 | 57 | 20732 | 734779 | 109833731 |
| Hepatotoxicity | 29.44 | 22.72 | 47 | 20742 | 63353 | 110505157 |
| Infusion related reaction | 28.86 | 22.72 | 18 | 20771 | 381144 | 110187366 |
| Insomnia | 28.75 | 22.72 | 16 | 20773 | 360574 | 110207936 |
| Renal impairment | 28.48 | 22.72 | 89 | 20700 | 188356 | 110380154 |
| Therapy partial responder | 28.48 | 22.72 | 35 | 20754 | 37026 | 110531484 |
| Bone marrow failure | 28.40 | 22.72 | 44 | 20745 | 57804 | 110510706 |
| Thrombophlebitis migrans | 28.27 | 22.72 | 9 | 20780 | 765 | 110567745 |
| HER2 gene amplification | 28.08 | 22.72 | 4 | 20785 | 3 | 110568507 |
| Subacute cutaneous lupus erythematosus | 27.51 | 22.72 | 15 | 20774 | 4979 | 110563531 |
| Hepatic enzyme increased | 27.43 | 22.72 | 13 | 20776 | 320879 | 110247631 |
| Gastrointestinal toxicity | 27.22 | 22.72 | 20 | 20769 | 11128 | 110557382 |
| Abdominal pain upper | 27.10 | 22.72 | 16 | 20773 | 349095 | 110219415 |
| Lung opacity | 26.43 | 22.72 | 20 | 20769 | 11632 | 110556878 |
| Genital tract inflammation | 26.03 | 22.72 | 6 | 20783 | 148 | 110568362 |
| Contusion | 25.97 | 22.72 | 6 | 20783 | 233355 | 110335155 |
| Pericarditis | 25.68 | 22.72 | 5 | 20784 | 219109 | 110349401 |
| Hypertransaminasaemia | 25.59 | 22.72 | 27 | 20762 | 24228 | 110544282 |
| Asthma | 24.91 | 22.72 | 8 | 20781 | 250283 | 110318227 |
| Hyperhidrosis | 24.85 | 22.72 | 3 | 20786 | 187295 | 110381215 |
| Cardiac tamponade | 24.75 | 22.72 | 19 | 20770 | 11288 | 110557222 |
| Retroperitoneal fibrosis | 24.35 | 22.72 | 8 | 20781 | 752 | 110567758 |
| Wheezing | 23.95 | 22.72 | 9 | 20780 | 255221 | 110313289 |
| Neoplasm progression | 23.54 | 22.72 | 43 | 20746 | 64552 | 110503958 |
| Non-small cell lung cancer stage IV | 23.19 | 22.72 | 6 | 20783 | 242 | 110568268 |
| Blister | 23.11 | 22.72 | 7 | 20782 | 227369 | 110341141 |
| Adenosquamous cell carcinoma | 22.99 | 22.72 | 4 | 20785 | 21 | 110568489 |
| Discomfort | 22.95 | 22.72 | 6 | 20783 | 214701 | 110353809 |
| Mobility decreased | 22.91 | 22.72 | 8 | 20781 | 237414 | 110331096 |
| Mouth ulceration | 22.78 | 22.72 | 36 | 20753 | 48102 | 110520408 |
None
| Source | Code | Description |
|---|---|---|
| ATC | L01EB04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Epidermal growth factor receptor (EGFR) tyrosine 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 MoA | N0000175082 | Kinase Inhibitors |
| FDA EPC | N0000175605 | Kinase Inhibitor |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
| FDA MoA | N0000191266 | Cytochrome P450 1A2 Inducers |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:74440 | epidermal growth factor receptor antagonist |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Non-small cell lung cancer, positive for epidermal growth factor receptor expression | indication | 426964009 |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.64 | acidic |
| pKa2 | 7.93 | Basic |
| pKa3 | 5.6 | Basic |
| pKa4 | 1.32 | Basic |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NSCLC WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NSCLC WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 9732058 | July 25, 2032 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NSCLC WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NSCLC WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 8946235 | Aug. 8, 2032 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NSCLC WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NSCLC WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 10183020 | Jan. 2, 2035 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 12465608 | Nov. 26, 2042 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | 12465608 | Nov. 26, 2042 | TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | Feb. 16, 2027 | IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY FOR THE FIRST-LINE TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | Feb. 16, 2027 | IN COMBINATION WITH PEMETREXED AND PLATINUM-BASED CHEMOTHERAPY FOR THE FIRST-LINE TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | Sept. 25, 2027 | TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING CONCURRENT OR SEQUENTIAL PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | Sept. 25, 2027 | TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED, UNRESECTABLE (STAGE III) NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE DISEASE HAS NOT PROGRESSED DURING OR FOLLOWING CONCURRENT OR SEQUENTIAL PLATINUM-BASED CHEMORADIATION THERAPY AND WHOSE TUMORS HAVE EGFR EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 40MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | Dec. 18, 2027 | FOR ADJUVANT THERAPY AFTER TUMOR RESECTION IN ADULT PATIENTS WITH NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST |
| EQ 80MG BASE | TAGRISSO | ASTRAZENECA | N208065 | Nov. 13, 2015 | RX | TABLET | ORAL | Dec. 18, 2027 | FOR ADJUVANT THERAPY AFTER TUMOR RESECTION IN ADULT PATIENTS WITH NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R 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 | IC50 | 7.82 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.79 | CHEMBL | |||||
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Enzyme | Kd | 5.44 | CHEMBL | |||||
| Receptor tyrosine-protein kinase erbB-2 | Kinase | IC50 | 8.32 | CHEMBL | |||||
| Insulin receptor | Kinase | IC50 | 6.04 | CHEMBL | |||||
| ALK tyrosine kinase receptor | Kinase | IC50 | 6.75 | CHEMBL | |||||
| Activated CDC42 kinase 1 | Kinase | IC50 | 7.15 | CHEMBL | |||||
| Tyrosine-protein kinase BTK | Kinase | Kd | 6.28 | CHEMBL | |||||
| Tyrosine-protein kinase JAK3 | Kinase | IC50 | 7.45 | CHEMBL | |||||
| Receptor tyrosine-protein kinase erbB-3 | Kinase | IC50 | 8.68 | CHEMBL | |||||
| Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Kinase | Kd | 5.53 | CHEMBL | |||||
| Lysine-specific histone demethylase 1A | Enzyme | IC50 | 5.40 | CHEMBL | |||||
| Dipeptidyl peptidase 1 | Enzyme | IC50 | 4.48 | CHEMBL | |||||
| Cysteine--tRNA ligase, cytoplasmic | Enzyme | Kd | 7.92 | CHEMBL | |||||
| Tyrosine-protein kinase Tec | Kinase | Kd | 6.49 | CHEMBL | |||||
| Epidermal growth factor receptor | Kinase | IC50 | 7.09 | CHEMBL |
| ID | Source |
|---|---|
| 3C06JJ0Z2O | UNII |
| 1421373-66-1 | SECONDARY_CAS_RN |
| 4035124 | VANDF |
| C4058811 | UMLSCUI |
| CHEBI:90943 | CHEBI |
| YY3 | PDB_CHEM_ID |
| CHEMBL3353410 | ChEMBL_ID |
| 71496458 | PUBCHEM_CID |
| DB09330 | DRUGBANK_ID |
| CHEMBL3545063 | ChEMBL_ID |
| 10043 | INN_ID |
| C000596361 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7719 | IUPHAR_LIGAND_ID |
| 1721559 | RXNORM |
| 237132 | MMSL |
| 31292 | MMSL |
| d08397 | MMSL |
| 016583 | NDDF |
| 016584 | NDDF |
| 716032009 | SNOMEDCT_US |
| 734660003 | SNOMEDCT_US |
| 781312009 | SNOMEDCT_US |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| TAGRISSO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-1248 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 28 sections |
| TAGRISSO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-1251 | TABLET, FILM COATED | 80 mg | ORAL | NDA | 28 sections |
| TAGRISSO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-1349 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 28 sections |
| TAGRISSO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-1350 | TABLET, FILM COATED | 80 mg | ORAL | NDA | 28 sections |