nilotinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 1932 | 641571-10-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Nilotinib is an inhibitor of the BCR-ABL kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. In vitro, nilotinib inhibited BCR-ABL mediated proliferation of murine leukemic cell lines and human cell lines derived from patients with Ph+ CML. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from BCR-ABL kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine BCR-ABL xenograft model.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.60 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 4 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 21.58 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 30 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 29, 2007 | FDA | NOVARTIS |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Cytogenetic analysis abnormal | 617.53 | 16.17 | 124 | 21631 | 796 | 63466471 |
| Peripheral arterial occlusive disease | 355.71 | 16.17 | 107 | 21648 | 4094 | 63463173 |
| Electrocardiogram QT prolonged | 346.19 | 16.17 | 229 | 21526 | 59301 | 63407966 |
| Blast crisis in myelogenous leukaemia | 245.46 | 16.17 | 53 | 21702 | 504 | 63466763 |
| Drug resistance | 218.00 | 16.17 | 121 | 21634 | 22812 | 63444455 |
| Second primary malignancy | 217.20 | 16.17 | 87 | 21668 | 7866 | 63459401 |
| Chronic myeloid leukaemia transformation | 212.37 | 16.17 | 37 | 21718 | 91 | 63467176 |
| Lipase increased | 189.12 | 16.17 | 84 | 21671 | 9816 | 63457451 |
| Philadelphia chromosome positive | 180.98 | 16.17 | 39 | 21716 | 367 | 63466900 |
| Pleural effusion | 167.17 | 16.17 | 182 | 21573 | 93028 | 63374239 |
| Rash | 138.89 | 16.17 | 464 | 21291 | 560407 | 62906860 |
| Bone pain | 127.51 | 16.17 | 123 | 21632 | 54518 | 63412749 |
| Blood bilirubin increased | 127.39 | 16.17 | 104 | 21651 | 37036 | 63430231 |
| Myocardial infarction | 122.88 | 16.17 | 161 | 21594 | 99732 | 63367535 |
| Intermittent claudication | 118.44 | 16.17 | 38 | 21717 | 1801 | 63465466 |
| Malignant neoplasm progression | 116.29 | 16.17 | 142 | 21613 | 81979 | 63385288 |
| Peripheral artery stenosis | 114.37 | 16.17 | 29 | 21726 | 579 | 63466688 |
| Off label use | 106.88 | 16.17 | 49 | 21706 | 674413 | 62792854 |
| Chronic myeloid leukaemia recurrent | 95.58 | 16.17 | 21 | 21734 | 218 | 63467049 |
| Death | 95.26 | 16.17 | 313 | 21442 | 374068 | 63093199 |
| Thrombocytopenia | 95.15 | 16.17 | 179 | 21576 | 150978 | 63316289 |
| Acute myocardial infarction | 91.79 | 16.17 | 81 | 21674 | 32043 | 63435224 |
| Arteriosclerosis | 89.88 | 16.17 | 51 | 21704 | 10015 | 63457252 |
| Platelet count decreased | 85.16 | 16.17 | 147 | 21608 | 115975 | 63351292 |
| Pancreatitis | 84.76 | 16.17 | 94 | 21661 | 48961 | 63418306 |
| Myalgia | 81.82 | 16.17 | 165 | 21590 | 146364 | 63320903 |
| White blood cell count increased | 77.00 | 16.17 | 89 | 21666 | 48472 | 63418795 |
| Acute lymphocytic leukaemia recurrent | 69.58 | 16.17 | 27 | 21728 | 2242 | 63465025 |
| Angina pectoris | 68.80 | 16.17 | 67 | 21688 | 30011 | 63437256 |
| Peripheral vascular disorder | 66.10 | 16.17 | 35 | 21720 | 6000 | 63461267 |
| Platelet count increased | 65.82 | 16.17 | 52 | 21703 | 17659 | 63449608 |
| Condition aggravated | 63.90 | 16.17 | 29 | 21726 | 402188 | 63065079 |
| Pancytopenia | 63.70 | 16.17 | 117 | 21638 | 96816 | 63370451 |
| Joint swelling | 63.40 | 16.17 | 17 | 21738 | 327649 | 63139618 |
| Haematotoxicity | 61.60 | 16.17 | 39 | 21716 | 9337 | 63457930 |
| Pruritus | 60.12 | 16.17 | 264 | 21491 | 361189 | 63106078 |
| Blast cell crisis | 59.73 | 16.17 | 12 | 21743 | 77 | 63467190 |
| Cerebrovascular accident | 57.14 | 16.17 | 119 | 21636 | 107905 | 63359362 |
| Arthropathy | 56.49 | 16.17 | 7 | 21748 | 234785 | 63232482 |
| Systemic lupus erythematosus | 56.15 | 16.17 | 4 | 21751 | 208914 | 63258353 |
| Normal newborn | 55.56 | 16.17 | 35 | 21720 | 8306 | 63458961 |
| Gene mutation identification test positive | 54.15 | 16.17 | 12 | 21743 | 130 | 63467137 |
| Carotid artery stenosis | 53.86 | 16.17 | 29 | 21726 | 5141 | 63462126 |
| Myocardial ischaemia | 52.67 | 16.17 | 40 | 21715 | 12819 | 63454448 |
| Hyperbilirubinaemia | 52.64 | 16.17 | 38 | 21717 | 11276 | 63455991 |
| Pericardial effusion | 52.60 | 16.17 | 58 | 21697 | 30000 | 63437267 |
| Rheumatoid arthritis | 51.33 | 16.17 | 12 | 21743 | 253807 | 63213460 |
| Splenomegaly | 50.83 | 16.17 | 37 | 21718 | 11120 | 63456147 |
| Therapeutic response delayed | 48.06 | 16.17 | 15 | 21740 | 649 | 63466618 |
| Glossodynia | 46.45 | 16.17 | 4 | 21751 | 178872 | 63288395 |
| Exposure via father | 46.39 | 16.17 | 12 | 21743 | 260 | 63467007 |
| Labelled drug-food interaction medication error | 45.85 | 16.17 | 11 | 21744 | 173 | 63467094 |
| Blood glucose increased | 45.14 | 16.17 | 93 | 21662 | 83663 | 63383604 |
| Exposure via partner | 44.34 | 16.17 | 10 | 21745 | 118 | 63467149 |
| Coronary artery disease | 44.19 | 16.17 | 55 | 21700 | 32322 | 63434945 |
| Anaemia | 44.01 | 16.17 | 208 | 21547 | 293222 | 63174045 |
| Thrombocytosis | 42.78 | 16.17 | 26 | 21729 | 5792 | 63461475 |
| Polymerase chain reaction positive | 42.56 | 16.17 | 10 | 21745 | 143 | 63467124 |
| Diabetes mellitus | 41.32 | 16.17 | 71 | 21684 | 55739 | 63411528 |
| Drug hypersensitivity | 41.21 | 16.17 | 28 | 21727 | 310659 | 63156608 |
| Bone marrow failure | 40.36 | 16.17 | 50 | 21705 | 29240 | 63438027 |
| Dry skin | 40.33 | 16.17 | 71 | 21684 | 56816 | 63410451 |
| Drug ineffective | 39.25 | 16.17 | 205 | 21550 | 1044560 | 62422707 |
| Chronic myeloid leukaemia | 38.97 | 16.17 | 18 | 21737 | 2300 | 63464967 |
| Arterial disorder | 38.64 | 16.17 | 15 | 21740 | 1246 | 63466021 |
| Xanthelasma | 38.28 | 16.17 | 8 | 21747 | 64 | 63467203 |
| Amylase increased | 38.24 | 16.17 | 25 | 21730 | 6320 | 63460947 |
| Palpitations | 37.71 | 16.17 | 104 | 21651 | 112666 | 63354601 |
| Cytopenia | 36.66 | 16.17 | 31 | 21724 | 11570 | 63455697 |
| Arterial occlusive disease | 34.75 | 16.17 | 23 | 21732 | 5935 | 63461332 |
| Leukaemia recurrent | 34.33 | 16.17 | 14 | 21741 | 1324 | 63465943 |
| Product use issue | 33.28 | 16.17 | 17 | 21738 | 220503 | 63246764 |
| Musculoskeletal stiffness | 33.08 | 16.17 | 11 | 21744 | 184607 | 63282660 |
| Skin disorder | 32.33 | 16.17 | 45 | 21710 | 29462 | 63437805 |
| Concomitant disease aggravated | 32.24 | 16.17 | 26 | 21729 | 9086 | 63458181 |
| Acute coronary syndrome | 31.88 | 16.17 | 27 | 21728 | 10099 | 63457168 |
| Basophil count increased | 31.53 | 16.17 | 12 | 21743 | 945 | 63466322 |
| Peripheral artery occlusion | 31.33 | 16.17 | 13 | 21742 | 1285 | 63465982 |
| Concomitant disease progression | 31.05 | 16.17 | 15 | 21740 | 2119 | 63465148 |
| Intentional product use issue | 30.28 | 16.17 | 4 | 21751 | 127888 | 63339379 |
| Food interaction | 29.39 | 16.17 | 11 | 21744 | 827 | 63466440 |
| Sinusitis | 29.27 | 16.17 | 21 | 21734 | 226632 | 63240635 |
| Peripheral ischaemia | 28.86 | 16.17 | 19 | 21736 | 4859 | 63462408 |
| Wound | 28.77 | 16.17 | 10 | 21745 | 163253 | 63304014 |
| Discomfort | 28.24 | 16.17 | 11 | 21744 | 167363 | 63299904 |
| Gamma-glutamyltransferase increased | 27.46 | 16.17 | 45 | 21710 | 33986 | 63433281 |
| Lower respiratory tract infection | 27.24 | 16.17 | 6 | 21749 | 132301 | 63334966 |
| Abdominal pain upper | 27.11 | 16.17 | 141 | 21614 | 206303 | 63260964 |
| Hypersensitivity | 26.49 | 16.17 | 37 | 21718 | 292648 | 63174619 |
| Abdominal pain | 26.10 | 16.17 | 181 | 21574 | 293275 | 63173992 |
| Pain in extremity | 25.22 | 16.17 | 197 | 21558 | 331289 | 63135978 |
| Hypotension | 25.13 | 16.17 | 34 | 21721 | 272570 | 63194697 |
| Muscle spasms | 25.07 | 16.17 | 113 | 21642 | 156037 | 63311230 |
| Cardiac failure | 24.79 | 16.17 | 77 | 21678 | 89065 | 63378202 |
| Impaired healing | 24.78 | 16.17 | 3 | 21752 | 102539 | 63364728 |
| Pregnancy of partner | 24.77 | 16.17 | 5 | 21750 | 33 | 63467234 |
| Blast cell count increased | 23.82 | 16.17 | 8 | 21747 | 438 | 63466829 |
| Swelling | 23.75 | 16.17 | 36 | 21719 | 275342 | 63191925 |
| Transaminases increased | 23.33 | 16.17 | 40 | 21715 | 31327 | 63435940 |
| Acute kidney injury | 23.14 | 16.17 | 34 | 21721 | 263381 | 63203886 |
| Alanine aminotransferase increased | 22.97 | 16.17 | 83 | 21672 | 103687 | 63363580 |
| Fluid retention | 22.94 | 16.17 | 58 | 21697 | 59628 | 63407639 |
| Haemolytic transfusion reaction | 22.91 | 16.17 | 4 | 21751 | 10 | 63467257 |
| Gangrene | 22.79 | 16.17 | 18 | 21737 | 6105 | 63461162 |
| Chest pain | 22.72 | 16.17 | 139 | 21616 | 215820 | 63251447 |
| Keratosis pilaris | 22.66 | 16.17 | 5 | 21750 | 53 | 63467214 |
| Atrial fibrillation | 22.28 | 16.17 | 89 | 21666 | 116547 | 63350720 |
| Mobility decreased | 22.08 | 16.17 | 7 | 21748 | 121152 | 63346115 |
| Stomatitis | 21.98 | 16.17 | 10 | 21745 | 138715 | 63328552 |
| Hyperglycaemia | 21.97 | 16.17 | 46 | 21709 | 41821 | 63425446 |
| Leukocytosis | 21.88 | 16.17 | 35 | 21720 | 25900 | 63441367 |
| Therapeutic response decreased | 21.81 | 16.17 | 58 | 21697 | 61467 | 63405800 |
| Collateral circulation | 21.49 | 16.17 | 4 | 21751 | 16 | 63467251 |
| Confusional state | 21.26 | 16.17 | 30 | 21725 | 236350 | 63230917 |
| Hepatic function abnormal | 20.89 | 16.17 | 42 | 21713 | 37100 | 63430167 |
| Neoplasm malignant | 20.81 | 16.17 | 37 | 21718 | 29824 | 63437443 |
| Exposure during pregnancy | 20.62 | 16.17 | 14 | 21741 | 155533 | 63311734 |
| Blood lactate dehydrogenase increased | 20.61 | 16.17 | 32 | 21723 | 23084 | 63444183 |
| Coronary artery insufficiency | 20.31 | 16.17 | 5 | 21750 | 88 | 63467179 |
| Haemoglobin decreased | 20.23 | 16.17 | 101 | 21654 | 145384 | 63321883 |
| Pericarditis | 20.06 | 16.17 | 10 | 21745 | 131569 | 63335698 |
| Dyslipidaemia | 19.83 | 16.17 | 18 | 21737 | 7375 | 63459892 |
| Toxicity to various agents | 19.74 | 16.17 | 34 | 21721 | 247216 | 63220051 |
| Hypercholesterolaemia | 19.68 | 16.17 | 30 | 21725 | 21304 | 63445963 |
| Pancreatic enzymes increased | 19.64 | 16.17 | 8 | 21747 | 754 | 63466513 |
| Jaundice | 18.80 | 16.17 | 35 | 21720 | 29216 | 63438051 |
| Cerebrovascular stenosis | 18.72 | 16.17 | 4 | 21751 | 36 | 63467231 |
| Overdose | 18.69 | 16.17 | 8 | 21747 | 115070 | 63352197 |
| Skin sensitisation | 18.45 | 16.17 | 8 | 21747 | 881 | 63466386 |
| Hepatic infection | 18.38 | 16.17 | 7 | 21748 | 552 | 63466715 |
| Ill-defined disorder | 18.33 | 16.17 | 3 | 21752 | 81752 | 63385515 |
| Oxygen saturation decreased | 18.26 | 16.17 | 4 | 21751 | 88581 | 63378686 |
| Angiopathy | 18.12 | 16.17 | 14 | 21741 | 4599 | 63462668 |
| Fibromyalgia | 17.92 | 16.17 | 3 | 21752 | 80417 | 63386850 |
| Coronary artery stenosis | 17.77 | 16.17 | 14 | 21741 | 4730 | 63462537 |
| Calculus bladder | 17.60 | 16.17 | 7 | 21748 | 620 | 63466647 |
| Cerebral infarction | 17.16 | 16.17 | 30 | 21725 | 23863 | 63443404 |
| Therapeutic product effect incomplete | 16.92 | 16.17 | 11 | 21744 | 125045 | 63342222 |
| Extremity necrosis | 16.67 | 16.17 | 9 | 21746 | 1604 | 63465663 |
| Vertebral artery stenosis | 16.61 | 16.17 | 4 | 21751 | 64 | 63467203 |
| Gene mutation | 16.40 | 16.17 | 9 | 21746 | 1656 | 63465611 |
| Oncologic complication | 16.40 | 16.17 | 5 | 21750 | 200 | 63467067 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Cytogenetic analysis abnormal | 452.94 | 14.99 | 104 | 23296 | 635 | 34932896 |
| Blast crisis in myelogenous leukaemia | 397.06 | 14.99 | 90 | 23310 | 514 | 34933017 |
| Second primary malignancy | 384.80 | 14.99 | 158 | 23242 | 7728 | 34925803 |
| Electrocardiogram QT prolonged | 380.88 | 14.99 | 272 | 23128 | 40680 | 34892851 |
| Peripheral arterial occlusive disease | 375.24 | 14.99 | 143 | 23257 | 5731 | 34927800 |
| Drug resistance | 228.94 | 14.99 | 167 | 23233 | 25760 | 34907771 |
| Angina pectoris | 224.00 | 14.99 | 178 | 23222 | 31185 | 34902346 |
| Pleural effusion | 222.06 | 14.99 | 273 | 23127 | 81273 | 34852258 |
| Intermittent claudication | 218.29 | 14.99 | 75 | 23325 | 2219 | 34931312 |
| Myocardial infarction | 176.01 | 14.99 | 301 | 23099 | 120784 | 34812747 |
| Rash | 163.55 | 14.99 | 418 | 22982 | 222334 | 34711197 |
| Lipase increased | 158.41 | 14.99 | 91 | 23309 | 9325 | 34924206 |
| Death | 158.40 | 14.99 | 603 | 22797 | 397446 | 34536085 |
| Off label use | 156.48 | 14.99 | 44 | 23356 | 419480 | 34514051 |
| Drug intolerance | 153.31 | 14.99 | 194 | 23206 | 59376 | 34874155 |
| Chronic myeloid leukaemia transformation | 138.81 | 14.99 | 30 | 23370 | 132 | 34933399 |
| Coronary artery stenosis | 128.15 | 14.99 | 80 | 23320 | 9536 | 34923995 |
| Chronic myeloid leukaemia recurrent | 121.20 | 14.99 | 28 | 23372 | 176 | 34933355 |
| Philadelphia chromosome positive | 118.49 | 14.99 | 31 | 23369 | 345 | 34933186 |
| Pancreatitis | 103.72 | 14.99 | 129 | 23271 | 38762 | 34894769 |
| Blood bilirubin increased | 100.48 | 14.99 | 126 | 23274 | 38170 | 34895361 |
| Peripheral artery stenosis | 96.74 | 14.99 | 32 | 23368 | 840 | 34932691 |
| Malignant neoplasm progression | 92.89 | 14.99 | 191 | 23209 | 87855 | 34845676 |
| Acute myocardial infarction | 92.00 | 14.99 | 144 | 23256 | 53575 | 34879956 |
| White blood cell count increased | 88.79 | 14.99 | 123 | 23277 | 41028 | 34892503 |
| Myocardial ischaemia | 85.87 | 14.99 | 80 | 23320 | 17328 | 34916203 |
| Peripheral vascular disorder | 85.57 | 14.99 | 49 | 23351 | 4987 | 34928544 |
| Coronary artery disease | 84.82 | 14.99 | 131 | 23269 | 48174 | 34885357 |
| Acute kidney injury | 84.33 | 14.99 | 50 | 23350 | 304938 | 34628593 |
| Arterial disorder | 81.62 | 14.99 | 31 | 23369 | 1228 | 34932303 |
| Platelet count decreased | 79.70 | 14.99 | 217 | 23183 | 119500 | 34814031 |
| Hypotension | 66.05 | 14.99 | 33 | 23367 | 221616 | 34711915 |
| Carotid artery stenosis | 64.96 | 14.99 | 41 | 23359 | 4978 | 34928553 |
| Abdominal pain upper | 62.69 | 14.99 | 144 | 23256 | 71346 | 34862185 |
| Toxicity to various agents | 60.95 | 14.99 | 29 | 23371 | 200333 | 34733198 |
| Concomitant disease aggravated | 60.19 | 14.99 | 41 | 23359 | 5660 | 34927871 |
| Acute coronary syndrome | 58.76 | 14.99 | 58 | 23342 | 13487 | 34920044 |
| Chest pain | 57.48 | 14.99 | 201 | 23199 | 126561 | 34806970 |
| Peripheral artery occlusion | 56.33 | 14.99 | 26 | 23374 | 1686 | 34931845 |
| Thrombocytopenia | 56.17 | 14.99 | 230 | 23170 | 156017 | 34777514 |
| Polymerase chain reaction positive | 56.09 | 14.99 | 14 | 23386 | 127 | 34933404 |
| Concomitant disease progression | 55.21 | 14.99 | 29 | 23371 | 2489 | 34931042 |
| Blast cell crisis | 55.18 | 14.99 | 13 | 23387 | 90 | 34933441 |
| Gene mutation identification test positive | 54.51 | 14.99 | 14 | 23386 | 144 | 34933387 |
| Splenomegaly | 53.44 | 14.99 | 58 | 23342 | 15059 | 34918472 |
| Arterial stenosis | 52.25 | 14.99 | 22 | 23378 | 1144 | 34932387 |
| Arteriosclerosis | 51.45 | 14.99 | 51 | 23349 | 11917 | 34921614 |
| Bone pain | 49.41 | 14.99 | 65 | 23335 | 20621 | 34912910 |
| Loss of therapeutic response | 46.70 | 14.99 | 17 | 23383 | 597 | 34932934 |
| Exposure via father | 46.67 | 14.99 | 12 | 23388 | 124 | 34933407 |
| Labelled drug-food interaction medication error | 42.13 | 14.99 | 9 | 23391 | 37 | 34933494 |
| Pruritus | 40.40 | 14.99 | 195 | 23205 | 141786 | 34791745 |
| Peripheral ischaemia | 39.95 | 14.99 | 32 | 23368 | 5655 | 34927876 |
| Gene mutation | 39.02 | 14.99 | 19 | 23381 | 1389 | 34932142 |
| Angina unstable | 38.23 | 14.99 | 43 | 23357 | 11610 | 34921921 |
| Cerebral infarction | 38.10 | 14.99 | 67 | 23333 | 27388 | 34906143 |
| Overdose | 36.77 | 14.99 | 8 | 23392 | 91051 | 34842480 |
| Confusional state | 36.51 | 14.99 | 26 | 23374 | 144134 | 34789397 |
| Therapeutic response decreased | 36.19 | 14.99 | 68 | 23332 | 29245 | 34904286 |
| Cerebral artery stenosis | 35.34 | 14.99 | 12 | 23388 | 342 | 34933189 |
| Acoustic neuroma | 34.99 | 14.99 | 10 | 23390 | 158 | 34933373 |
| Amylase increased | 34.49 | 14.99 | 30 | 23370 | 5938 | 34927593 |
| Condition aggravated | 34.47 | 14.99 | 47 | 23353 | 192149 | 34741382 |
| Infarction | 34.41 | 14.99 | 22 | 23378 | 2731 | 34930800 |
| Chronic myeloid leukaemia | 33.45 | 14.99 | 20 | 23380 | 2204 | 34931327 |
| Fall | 33.09 | 14.99 | 53 | 23347 | 202832 | 34730699 |
| Cerebrovascular accident | 32.94 | 14.99 | 128 | 23272 | 84683 | 34848848 |
| Myalgia | 32.72 | 14.99 | 127 | 23273 | 83983 | 34849548 |
| Hyperglycaemia | 31.83 | 14.99 | 77 | 23323 | 39403 | 34894128 |
| Paternal exposure during pregnancy | 30.87 | 14.99 | 7 | 23393 | 40 | 34933491 |
| Blood glucose increased | 30.36 | 14.99 | 106 | 23294 | 66612 | 34866919 |
| Pericardial effusion | 30.18 | 14.99 | 57 | 23343 | 24605 | 34908926 |
| Leukocytosis | 29.92 | 14.99 | 56 | 23344 | 24009 | 34909522 |
| Hypercholesterolaemia | 29.89 | 14.99 | 33 | 23367 | 8729 | 34924802 |
| Arterial thrombosis | 29.16 | 14.99 | 16 | 23384 | 1499 | 34932032 |
| Drug interaction | 29.04 | 14.99 | 68 | 23332 | 225878 | 34707653 |
| Coronary artery occlusion | 28.61 | 14.99 | 36 | 23364 | 10926 | 34922605 |
| Oedematous pancreatitis | 27.82 | 14.99 | 11 | 23389 | 486 | 34933045 |
| Cardiovascular disorder | 27.81 | 14.99 | 34 | 23366 | 10022 | 34923509 |
| Drug hypersensitivity | 27.10 | 14.99 | 10 | 23390 | 80519 | 34853012 |
| Tremor | 26.57 | 14.99 | 11 | 23389 | 82576 | 34850955 |
| Myopathy toxic | 26.07 | 14.99 | 11 | 23389 | 575 | 34932956 |
| Karyotype analysis abnormal | 24.71 | 14.99 | 6 | 23394 | 48 | 34933483 |
| Diabetes mellitus | 24.45 | 14.99 | 78 | 23322 | 46795 | 34886736 |
| Ischaemia | 24.43 | 14.99 | 22 | 23378 | 4558 | 34928973 |
| Gangrene | 24.41 | 14.99 | 22 | 23378 | 4564 | 34928967 |
| Hallucination | 24.17 | 14.99 | 3 | 23397 | 51495 | 34882036 |
| Dehydration | 24.08 | 14.99 | 31 | 23369 | 129938 | 34803593 |
| Fatigue | 23.91 | 14.99 | 364 | 23036 | 370289 | 34563242 |
| Clonal evolution | 23.70 | 14.99 | 7 | 23393 | 125 | 34933406 |
| Hyponatraemia | 23.56 | 14.99 | 13 | 23387 | 82678 | 34850853 |
| Pain in extremity | 23.49 | 14.99 | 155 | 23245 | 126358 | 34807173 |
| Muscle spasms | 22.74 | 14.99 | 105 | 23295 | 74896 | 34858635 |
| Gamma-glutamyltransferase increased | 22.48 | 14.99 | 56 | 23344 | 29175 | 34904356 |
| Central nervous system leukaemia | 22.05 | 14.99 | 8 | 23392 | 278 | 34933253 |
| Agitation | 21.30 | 14.99 | 6 | 23394 | 57393 | 34876138 |
| Blast cells present | 20.91 | 14.99 | 9 | 23391 | 494 | 34933037 |
| Chloroma | 20.52 | 14.99 | 9 | 23391 | 517 | 34933014 |
| Product blister packaging issue | 20.32 | 14.99 | 6 | 23394 | 107 | 34933424 |
| Necrosis | 20.29 | 14.99 | 22 | 23378 | 5701 | 34927830 |
| Arteritis | 19.99 | 14.99 | 8 | 23392 | 365 | 34933166 |
| Basophil count increased | 19.98 | 14.99 | 9 | 23391 | 551 | 34932980 |
| Atrial fibrillation | 19.79 | 14.99 | 145 | 23255 | 122248 | 34811283 |
| Myeloproliferative neoplasm | 19.71 | 14.99 | 9 | 23391 | 569 | 34932962 |
| Intentional overdose | 19.42 | 14.99 | 3 | 23397 | 43671 | 34889860 |
| Febrile neutropenia | 19.36 | 14.99 | 39 | 23361 | 136810 | 34796721 |
| Gelatinous transformation of the bone marrow | 19.23 | 14.99 | 4 | 23396 | 14 | 34933517 |
| Hepatic infection | 18.81 | 14.99 | 9 | 23391 | 633 | 34932898 |
| Abdominal pain | 18.56 | 14.99 | 179 | 23221 | 163439 | 34770092 |
| Chest discomfort | 18.54 | 14.99 | 79 | 23321 | 54451 | 34879080 |
| Intentional product misuse | 18.42 | 14.99 | 4 | 23396 | 45607 | 34887924 |
| Bone marrow failure | 18.39 | 14.99 | 52 | 23348 | 29201 | 34904330 |
| Haemoglobin decreased | 18.35 | 14.99 | 141 | 23259 | 120631 | 34812900 |
| Headache | 18.30 | 14.99 | 210 | 23190 | 200425 | 34733106 |
| Acne | 18.00 | 14.99 | 29 | 23371 | 11037 | 34922494 |
| Leukaemia recurrent | 17.97 | 14.99 | 12 | 23388 | 1603 | 34931928 |
| Arterial occlusive disease | 17.76 | 14.99 | 18 | 23382 | 4316 | 34929215 |
| Intentional product use issue | 17.63 | 14.99 | 9 | 23391 | 59807 | 34873724 |
| Cytopenia | 17.58 | 14.99 | 31 | 23369 | 12692 | 34920839 |
| Rectosigmoid cancer | 17.54 | 14.99 | 6 | 23394 | 175 | 34933356 |
| Delirium | 17.48 | 14.99 | 4 | 23396 | 43987 | 34889544 |
| Acquired gene mutation | 17.36 | 14.99 | 11 | 23389 | 1344 | 34932187 |
| Vascular stenosis | 17.19 | 14.99 | 6 | 23394 | 186 | 34933345 |
| Oncologic complication | 17.07 | 14.99 | 7 | 23393 | 340 | 34933191 |
| Pulmonary hypertension | 17.06 | 14.99 | 41 | 23359 | 20883 | 34912648 |
| B-cell small lymphocytic lymphoma | 16.75 | 14.99 | 6 | 23394 | 201 | 34933330 |
| Angiopathy | 16.50 | 14.99 | 17 | 23383 | 4156 | 34929375 |
| Rheumatoid arthritis | 16.18 | 14.99 | 3 | 23397 | 38235 | 34895296 |
| Oxygen saturation decreased | 16.00 | 14.99 | 8 | 23392 | 53810 | 34879721 |
| Pancreatic toxicity | 15.50 | 14.99 | 4 | 23396 | 42 | 34933489 |
| Somnolence | 15.43 | 14.99 | 32 | 23368 | 111084 | 34822447 |
| Metabolic acidosis | 15.42 | 14.99 | 5 | 23395 | 43675 | 34889856 |
| Gait apraxia | 15.32 | 14.99 | 3 | 23397 | 7 | 34933524 |
| Neoplasm malignant | 15.16 | 14.99 | 38 | 23362 | 19867 | 34913664 |
| Pulmonary embolism | 15.02 | 14.99 | 23 | 23377 | 89723 | 34843808 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Cytogenetic analysis abnormal | 827.14 | 14.81 | 168 | 30122 | 1022 | 79713076 |
| Peripheral arterial occlusive disease | 456.97 | 14.81 | 156 | 30134 | 8102 | 79705996 |
| Electrocardiogram QT prolonged | 450.30 | 14.81 | 329 | 29961 | 90057 | 79624041 |
| Blast crisis in myelogenous leukaemia | 431.66 | 14.81 | 93 | 30197 | 780 | 79713318 |
| Second primary malignancy | 424.16 | 14.81 | 171 | 30119 | 14179 | 79699919 |
| Drug resistance | 349.44 | 14.81 | 211 | 30079 | 42002 | 79672096 |
| Pleural effusion | 323.87 | 14.81 | 334 | 29956 | 144928 | 79569170 |
| Chronic myeloid leukaemia transformation | 267.15 | 14.81 | 51 | 30239 | 212 | 79713886 |
| Lipase increased | 255.87 | 14.81 | 125 | 30165 | 16341 | 79697757 |
| Philadelphia chromosome positive | 223.40 | 14.81 | 52 | 30238 | 638 | 79713460 |
| Myocardial infarction | 203.29 | 14.81 | 297 | 29993 | 183832 | 79530266 |
| Rash | 200.05 | 14.81 | 575 | 29715 | 577783 | 79136315 |
| Angina pectoris | 197.62 | 14.81 | 161 | 30129 | 51571 | 79662527 |
| Intermittent claudication | 197.58 | 14.81 | 67 | 30223 | 3404 | 79710694 |
| Blood bilirubin increased | 184.16 | 14.81 | 172 | 30118 | 66060 | 79648038 |
| Death | 176.59 | 14.81 | 543 | 29747 | 565971 | 79148127 |
| Platelet count decreased | 175.57 | 14.81 | 286 | 30004 | 194378 | 79519720 |
| Off label use | 154.91 | 14.81 | 76 | 30214 | 907139 | 78806959 |
| Acute myocardial infarction | 139.67 | 14.81 | 159 | 30131 | 76877 | 79637221 |
| Malignant neoplasm progression | 139.43 | 14.81 | 212 | 30078 | 135778 | 79578320 |
| Peripheral artery stenosis | 135.97 | 14.81 | 40 | 30250 | 1271 | 79712827 |
| Chronic myeloid leukaemia recurrent | 125.78 | 14.81 | 28 | 30262 | 277 | 79713821 |
| White blood cell count increased | 118.60 | 14.81 | 144 | 30146 | 74489 | 79639609 |
| Pancreatitis | 111.72 | 14.81 | 134 | 30156 | 68441 | 79645657 |
| Bone pain | 104.33 | 14.81 | 117 | 30173 | 55625 | 79658473 |
| Myocardial ischaemia | 100.74 | 14.81 | 81 | 30209 | 25438 | 79688660 |
| Thrombocytopenia | 100.37 | 14.81 | 273 | 30017 | 264986 | 79449112 |
| Gene mutation identification test positive | 96.96 | 14.81 | 22 | 30268 | 239 | 79713859 |
| Coronary artery stenosis | 94.54 | 14.81 | 59 | 30231 | 12425 | 79701673 |
| Arterial disorder | 88.63 | 14.81 | 32 | 30258 | 1958 | 79712140 |
| Acute coronary syndrome | 87.53 | 14.81 | 69 | 30221 | 21064 | 79693034 |
| Carotid artery stenosis | 86.16 | 14.81 | 49 | 30241 | 8709 | 79705389 |
| Arteriosclerosis | 78.71 | 14.81 | 61 | 30229 | 18166 | 79695932 |
| Splenomegaly | 75.87 | 14.81 | 63 | 30227 | 20691 | 79693407 |
| Coronary artery disease | 75.58 | 14.81 | 108 | 30182 | 65366 | 79648732 |
| Peripheral vascular disorder | 73.86 | 14.81 | 43 | 30247 | 7987 | 79706111 |
| Hypotension | 71.74 | 14.81 | 39 | 30251 | 440278 | 79273820 |
| Polymerase chain reaction positive | 71.27 | 14.81 | 18 | 30272 | 317 | 79713781 |
| Condition aggravated | 71.19 | 14.81 | 52 | 30238 | 501072 | 79213026 |
| Acute kidney injury | 69.84 | 14.81 | 57 | 30233 | 519347 | 79194751 |
| Myalgia | 68.09 | 14.81 | 189 | 30101 | 185452 | 79528646 |
| Blood glucose increased | 68.09 | 14.81 | 141 | 30149 | 114834 | 79599264 |
| Acute lymphocytic leukaemia recurrent | 67.83 | 14.81 | 34 | 30256 | 4690 | 79709408 |
| Toxicity to various agents | 67.71 | 14.81 | 38 | 30252 | 421502 | 79292596 |
| Pericardial effusion | 61.99 | 14.81 | 82 | 30208 | 46155 | 79667943 |
| Cerebral infarction | 61.23 | 14.81 | 81 | 30209 | 45595 | 79668503 |
| Rheumatoid arthritis | 60.46 | 14.81 | 5 | 30285 | 208465 | 79505633 |
| Hyperbilirubinaemia | 59.28 | 14.81 | 59 | 30231 | 24459 | 79689639 |
| Pruritus | 59.12 | 14.81 | 301 | 29989 | 394347 | 79319751 |
| Amylase increased | 58.42 | 14.81 | 42 | 30248 | 11167 | 79702931 |
| Concomitant disease aggravated | 56.70 | 14.81 | 44 | 30246 | 13123 | 79700975 |
| Hyperglycaemia | 56.17 | 14.81 | 98 | 30192 | 70237 | 79643861 |
| Joint swelling | 55.74 | 14.81 | 20 | 30270 | 288626 | 79425472 |
| Peripheral artery occlusion | 53.95 | 14.81 | 24 | 30266 | 2533 | 79711565 |
| Haemoglobin decreased | 53.79 | 14.81 | 196 | 30094 | 221923 | 79492175 |
| Blast cell crisis | 51.95 | 14.81 | 12 | 30278 | 142 | 79713956 |
| Pancytopenia | 51.42 | 14.81 | 159 | 30131 | 165586 | 79548512 |
| Bone marrow failure | 51.35 | 14.81 | 79 | 30211 | 51028 | 79663070 |
| Gamma-glutamyltransferase increased | 50.07 | 14.81 | 81 | 30209 | 54599 | 79659499 |
| Concomitant disease progression | 49.88 | 14.81 | 25 | 30265 | 3448 | 79710650 |
| Arterial stenosis | 49.01 | 14.81 | 19 | 30271 | 1417 | 79712681 |
| Chronic myeloid leukaemia | 48.61 | 14.81 | 25 | 30265 | 3639 | 79710459 |
| Drug hypersensitivity | 46.46 | 14.81 | 28 | 30262 | 298888 | 79415210 |
| Chest pain | 46.27 | 14.81 | 221 | 30069 | 282083 | 79432015 |
| Abdominal pain upper | 44.81 | 14.81 | 186 | 30104 | 223633 | 79490465 |
| Confusional state | 43.81 | 14.81 | 34 | 30256 | 317963 | 79396135 |
| Platelet count increased | 43.57 | 14.81 | 48 | 30242 | 22358 | 79691740 |
| Cerebrovascular accident | 42.74 | 14.81 | 143 | 30147 | 155149 | 79558949 |
| Peripheral ischaemia | 41.59 | 14.81 | 32 | 30258 | 9425 | 79704673 |
| Drug intolerance | 41.29 | 14.81 | 204 | 30086 | 263915 | 79450183 |
| Acquired gene mutation | 40.93 | 14.81 | 19 | 30271 | 2214 | 79711884 |
| Overdose | 40.57 | 14.81 | 10 | 30280 | 184196 | 79529902 |
| Gene mutation | 40.54 | 14.81 | 20 | 30270 | 2666 | 79711432 |
| Therapeutic response decreased | 39.57 | 14.81 | 82 | 30208 | 66771 | 79647327 |
| Therapeutic response delayed | 38.59 | 14.81 | 15 | 30275 | 1127 | 79712971 |
| Arthropathy | 38.27 | 14.81 | 10 | 30280 | 177101 | 79536997 |
| Arterial occlusive disease | 38.04 | 14.81 | 29 | 30261 | 8427 | 79705671 |
| Cerebral artery stenosis | 36.70 | 14.81 | 13 | 30277 | 752 | 79713346 |
| Acne | 34.57 | 14.81 | 47 | 30243 | 27143 | 79686955 |
| Leukaemia recurrent | 34.14 | 14.81 | 18 | 30272 | 2756 | 79711342 |
| Haematotoxicity | 33.25 | 14.81 | 35 | 30255 | 15484 | 79698614 |
| Fall | 32.64 | 14.81 | 87 | 30203 | 487542 | 79226556 |
| Atrial fibrillation | 32.45 | 14.81 | 155 | 30135 | 197731 | 79516367 |
| Gangrene | 32.32 | 14.81 | 27 | 30263 | 8937 | 79705161 |
| Anaemia | 32.09 | 14.81 | 283 | 30007 | 444732 | 79269366 |
| Leukocytosis | 31.42 | 14.81 | 58 | 30232 | 43397 | 79670701 |
| Cardiac failure | 31.22 | 14.81 | 129 | 30161 | 154713 | 79559385 |
| Diabetes mellitus | 30.89 | 14.81 | 82 | 30208 | 78308 | 79635790 |
| Abdominal pain | 30.32 | 14.81 | 252 | 30038 | 389317 | 79324781 |
| White blood cell count decreased | 29.80 | 14.81 | 146 | 30144 | 188142 | 79525956 |
| Angina unstable | 29.73 | 14.81 | 34 | 30256 | 16493 | 79697605 |
| Drug ineffective | 29.46 | 14.81 | 266 | 30024 | 1080647 | 78633451 |
| Sinusitis | 29.41 | 14.81 | 19 | 30271 | 195482 | 79518616 |
| Karyotype analysis abnormal | 29.18 | 14.81 | 6 | 30284 | 39 | 79714059 |
| Angiopathy | 29.05 | 14.81 | 23 | 30267 | 7059 | 79707039 |
| Dry skin | 28.71 | 14.81 | 73 | 30217 | 67922 | 79646176 |
| Cytopenia | 28.63 | 14.81 | 37 | 30253 | 20346 | 79693752 |
| Infarction | 28.16 | 14.81 | 19 | 30271 | 4563 | 79709535 |
| Clonal evolution | 28.16 | 14.81 | 8 | 30282 | 224 | 79713874 |
| Muscle spasms | 28.02 | 14.81 | 136 | 30154 | 174594 | 79539504 |
| Hypercholesterolaemia | 27.97 | 14.81 | 39 | 30251 | 23056 | 79691042 |
| Blood lactate dehydrogenase increased | 27.97 | 14.81 | 52 | 30238 | 39118 | 79674980 |
| Keratosis pilaris | 27.36 | 14.81 | 6 | 30284 | 55 | 79714043 |
| Thrombocytosis | 27.32 | 14.81 | 24 | 30266 | 8502 | 79705596 |
| Intentional product use issue | 26.95 | 14.81 | 12 | 30278 | 152100 | 79561998 |
| Pancreatic toxicity | 26.89 | 14.81 | 6 | 30284 | 60 | 79714038 |
| Oxygen saturation decreased | 26.54 | 14.81 | 8 | 30282 | 129039 | 79585059 |
| Pain in extremity | 26.35 | 14.81 | 232 | 30058 | 364306 | 79349792 |
| Mobility decreased | 26.19 | 14.81 | 7 | 30283 | 122168 | 79591930 |
| Palpitations | 25.92 | 14.81 | 106 | 30184 | 126504 | 79587594 |
| Xanthelasma | 25.83 | 14.81 | 7 | 30283 | 164 | 79713934 |
| Hyponatraemia | 25.79 | 14.81 | 18 | 30272 | 177830 | 79536268 |
| Labelled drug-food interaction medication error | 25.79 | 14.81 | 7 | 30283 | 165 | 79713933 |
| Alanine aminotransferase increased | 25.68 | 14.81 | 126 | 30164 | 162444 | 79551654 |
| Exposure during pregnancy | 25.39 | 14.81 | 4 | 30286 | 101128 | 79612970 |
| Hepatic function abnormal | 25.36 | 14.81 | 73 | 30217 | 73034 | 79641064 |
| Hypersensitivity | 25.05 | 14.81 | 38 | 30252 | 262201 | 79451897 |
| Coronary artery occlusion | 25.04 | 14.81 | 30 | 30260 | 15285 | 79698813 |
| Musculoskeletal stiffness | 25.00 | 14.81 | 18 | 30272 | 174990 | 79539108 |
| Glossodynia | 23.97 | 14.81 | 5 | 30285 | 103332 | 79610766 |
| Arterial thrombosis | 23.75 | 14.81 | 14 | 30276 | 2660 | 79711438 |
| Central nervous system leukaemia | 23.37 | 14.81 | 8 | 30282 | 418 | 79713680 |
| Intentional product misuse | 23.36 | 14.81 | 4 | 30286 | 95161 | 79618937 |
| Transformation to acute myeloid leukaemia | 23.12 | 14.81 | 10 | 30280 | 987 | 79713111 |
| Blast cell count increased | 22.78 | 14.81 | 11 | 30279 | 1399 | 79712699 |
| Hepatic infection | 22.71 | 14.81 | 10 | 30280 | 1030 | 79713068 |
| Product use issue | 22.45 | 14.81 | 28 | 30262 | 209794 | 79504304 |
| Basophil count increased | 22.12 | 14.81 | 11 | 30279 | 1492 | 79712606 |
| Chronic myeloid leukaemia (in remission) | 21.96 | 14.81 | 4 | 30286 | 12 | 79714086 |
| Haemolytic transfusion reaction | 21.72 | 14.81 | 4 | 30286 | 13 | 79714085 |
| Acoustic neuroma | 21.69 | 14.81 | 7 | 30283 | 304 | 79713794 |
| Lower respiratory tract infection | 21.66 | 14.81 | 11 | 30279 | 129209 | 79584889 |
| Oedematous pancreatitis | 21.60 | 14.81 | 10 | 30280 | 1158 | 79712940 |
| Wheezing | 20.99 | 14.81 | 9 | 30281 | 116655 | 79597443 |
| Loss of therapeutic response | 20.93 | 14.81 | 9 | 30281 | 875 | 79713223 |
| Paternal exposure during pregnancy | 20.93 | 14.81 | 5 | 30285 | 69 | 79714029 |
| Drug interaction | 20.88 | 14.81 | 84 | 30206 | 415099 | 79298999 |
| Splenitis | 20.63 | 14.81 | 3 | 30287 | 0 | 79714098 |
| Vascular stenosis | 20.62 | 14.81 | 8 | 30282 | 598 | 79713500 |
| Skin disorder | 20.51 | 14.81 | 42 | 30248 | 33901 | 79680197 |
| Asthma | 20.49 | 14.81 | 13 | 30277 | 135082 | 79579016 |
| Therapy non-responder | 20.27 | 14.81 | 79 | 30211 | 92226 | 79621872 |
| Blood creatine phosphokinase increased | 20.10 | 14.81 | 63 | 30227 | 66027 | 79648071 |
| Ischaemic stroke | 20.02 | 14.81 | 41 | 30249 | 33090 | 79681008 |
| Myeloproliferative neoplasm | 19.96 | 14.81 | 9 | 30281 | 980 | 79713118 |
| Urinary tract infection | 19.87 | 14.81 | 47 | 30243 | 274465 | 79439633 |
| Exposure via father | 19.80 | 14.81 | 5 | 30285 | 88 | 79714010 |
| Cardiovascular disorder | 19.72 | 14.81 | 29 | 30261 | 17996 | 79696102 |
| Necrosis | 19.61 | 14.81 | 21 | 30269 | 9472 | 79704626 |
| Dyslipidaemia | 19.37 | 14.81 | 23 | 30267 | 11610 | 79702488 |
| Liver disorder | 19.30 | 14.81 | 66 | 30224 | 72351 | 79641747 |
| Suicide attempt | 19.26 | 14.81 | 4 | 30286 | 82928 | 79631170 |
| Agitation | 19.07 | 14.81 | 7 | 30283 | 99708 | 79614390 |
| Myopathy toxic | 19.06 | 14.81 | 9 | 30281 | 1089 | 79713009 |
| Chromosome analysis abnormal | 18.90 | 14.81 | 6 | 30284 | 247 | 79713851 |
| Chloroma | 18.76 | 14.81 | 8 | 30282 | 762 | 79713336 |
| Stomatitis | 18.58 | 14.81 | 17 | 30273 | 146740 | 79567358 |
| Tremor | 17.88 | 14.81 | 23 | 30267 | 170060 | 79544038 |
| Delirium | 17.85 | 14.81 | 5 | 30285 | 84622 | 79629476 |
| Hepatotoxicity | 17.54 | 14.81 | 51 | 30239 | 51301 | 79662797 |
| Pancreatic enzymes increased | 17.21 | 14.81 | 9 | 30281 | 1356 | 79712742 |
| Metabolic acidosis | 17.18 | 14.81 | 5 | 30285 | 82524 | 79631574 |
| Suicidal ideation | 17.08 | 14.81 | 4 | 30286 | 76336 | 79637762 |
| Normal newborn | 17.06 | 14.81 | 17 | 30273 | 7055 | 79707043 |
| Skin sensitisation | 16.80 | 14.81 | 8 | 30282 | 987 | 79713111 |
| Discomfort | 16.57 | 14.81 | 14 | 30276 | 125603 | 79588495 |
| Pyrexia | 16.53 | 14.81 | 355 | 29935 | 678354 | 79035744 |
| Neoplasm progression | 16.39 | 14.81 | 50 | 30240 | 51632 | 79662466 |
| Dyslalia | 16.23 | 14.81 | 8 | 30282 | 1064 | 79713034 |
| Aspartate aminotransferase increased | 16.19 | 14.81 | 99 | 30191 | 138542 | 79575556 |
| Coronary artery insufficiency | 16.19 | 14.81 | 5 | 30285 | 188 | 79713910 |
| Vertebral artery stenosis | 16.16 | 14.81 | 5 | 30285 | 189 | 79713909 |
| Recurrent cancer | 16.15 | 14.81 | 11 | 30279 | 2682 | 79711416 |
| Therapeutic product effect incomplete | 16.11 | 14.81 | 18 | 30272 | 141627 | 79572471 |
| Vaginal odour | 15.86 | 14.81 | 6 | 30284 | 419 | 79713679 |
| Peripheral artery thrombosis | 15.79 | 14.81 | 12 | 30278 | 3471 | 79710627 |
| Ill-defined disorder | 15.67 | 14.81 | 3 | 30287 | 65872 | 79648226 |
| Jaundice | 15.44 | 14.81 | 50 | 30240 | 53299 | 79660799 |
| Supraventricular extrasystoles | 15.40 | 14.81 | 16 | 30274 | 6971 | 79707127 |
| Cardiac tamponade | 14.88 | 14.81 | 18 | 30272 | 9258 | 79704840 |
| Coma | 14.83 | 14.81 | 10 | 30280 | 100639 | 79613459 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01EA03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS BCR-ABL tyrosine kinase inhibitors |
| FDA MoA | N0000020009 | Bcr-Abl Tyrosine Kinase Inhibitors |
| FDA EPC | N0000175605 | Kinase Inhibitor |
| FDA MoA | N0000182137 | Cytochrome P450 2D6 Inhibitors |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000187062 | Cytochrome P450 2C8 Inhibitors |
| FDA MoA | N0000187063 | Cytochrome P450 2C8 Inducers |
| FDA MoA | N0000187064 | Cytochrome P450 2B6 Inducers |
| FDA MoA | N0000191272 | UGT1A1 Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:38637 | tyrosine kinase inhibitors |
| CHEBI has role | CHEBI:149553 | anticoronaviral drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic phase chronic myeloid leukemia | indication | 413847001 | |
| Philadelphia Chromosome Positive Chronic Myelocytic Leukemia | indication | ||
| Chronic Myelocytic Leukemia Accelerated Phase | indication | ||
| Hypophosphatemia | contraindication | 4996001 | |
| Hypocalcemia | contraindication | 5291005 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Hyperkalemia | contraindication | 14140009 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Torsades de pointes | contraindication | 31722008 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hypokalemia | contraindication | 43339004 | |
| Gastrectomy | contraindication | 53442002 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Pancreatitis | contraindication | 75694006 | DOID:4989 |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Hyponatremia | contraindication | 89627008 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Hypomagnesemia | contraindication | 190855004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Elevated Serum Lipase | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.89 | acidic |
| pKa2 | 6.03 | Basic |
| pKa3 | 3.97 | Basic |
| pKa4 | 2.2 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | 7169791 | July 4, 2023 | A METHOD FOR THE TREATMENT OF LEUKEMIAS |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | 8389537 | July 18, 2026 | TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML) |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | 8415363 | July 18, 2026 | TREATMENT OF NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH + CML) |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | 8415363 | July 18, 2026 | TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML) |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | 9061029 | April 7, 2032 | TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML) |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | 9061029 | April 7, 2032 | TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML) BY ADMINISTERING NILOTINIB DISPERSED IN A FRUIT PREPARATION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | March 22, 2025 | TREATMENT OF PEDIATRIC PATIENTS GREATER THAN OR EQUAL TO 1 YEAR OF AGE WITH CHRONIC PHASE PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA WITH RESISTANCE OR INTOLERANCE TO PRIOR TYROSINE-KINASE INHIBITOR THERAPY |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | March 22, 2025 | TREATMENT OF PEDIATRIC PATIENTS GREATER THAN OR EQUAL TO 1 YEAR OF AGE WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML) IN CHRONIC PHASE |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | Sept. 22, 2025 | PEDIATRIC EXCLUSIVITY |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | Sept. 23, 2028 | TREATMENT OF PEDIATRIC PATIENTS GREATER THAN OR EQUAL TO 1 YEAR OF AGE WITH ACCELERATED PHASE PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) WITH RESISTANCE ORINTOLERANCE TO PRIOR TYROSINE-KINASE INHIBITOR (TKI) THERAPY |
| EQ 50MG BASE | TASIGNA | NOVARTIS | N022068 | March 22, 2018 | RX | CAPSULE | ORAL | March 23, 2029 | PEDIATRIC EXCLUSIVITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase ABL1 | Kinase | INHIBITOR | Kd | 8.44 | CHEMBL | CHEMBL | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 6.35 | CHEMBL | |||||
| Carbonic anhydrase 2 | Enzyme | Ki | 8.39 | CHEMBL | |||||
| ATP-binding cassette sub-family G member 2 | Transporter | IC50 | 5.60 | CHEMBL | |||||
| Carbonic anhydrase 1 | Enzyme | Ki | 7.53 | CHEMBL | |||||
| Carbonic anhydrase 4 | Enzyme | Ki | 6.35 | CHEMBL | |||||
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Enzyme | IC50 | 6.42 | CHEMBL | |||||
| Carbonic anhydrase 9 | Enzyme | Ki | 7.38 | CHEMBL | |||||
| Carbonic anhydrase 12 | Enzyme | Ki | 6.52 | CHEMBL | |||||
| Platelet-derived growth factor receptor beta | Kinase | Kd | 7.80 | CHEMBL | |||||
| Mast/stem cell growth factor receptor Kit | Kinase | Kd | 7.77 | CHEMBL | |||||
| Carbonic anhydrase 5A, mitochondrial | Enzyme | Ki | 5.26 | CHEMBL | |||||
| Carbonic anhydrase 5B, mitochondrial | Enzyme | Ki | 4.83 | CHEMBL | |||||
| Carbonic anhydrase 7 | Enzyme | Ki | 7 | CHEMBL | |||||
| Proto-oncogene tyrosine-protein kinase Src | Kinase | Kd | 5.72 | CHEMBL | |||||
| Tyrosine-protein kinase Lck | Kinase | Kd | 7.33 | CHEMBL | |||||
| Tyrosine-protein kinase Yes | Kinase | Kd | 5.96 | CHEMBL | |||||
| Tyrosine-protein kinase Fyn | Kinase | Kd | 5.80 | CHEMBL | |||||
| Ephrin type-A receptor 2 | Kinase | Kd | 6.64 | CHEMBL | |||||
| RAF proto-oncogene serine/threonine-protein kinase | Kinase | Kd | 5.41 | CHEMBL | |||||
| Serine/threonine-protein kinase B-raf | Kinase | Kd | 6.24 | CHEMBL | |||||
| Receptor-type tyrosine-protein kinase FLT3 | Kinase | Kd | 4.40 | CHEMBL | |||||
| Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | Kd | 6.06 | CHEMBL | |||||
| Macrophage colony-stimulating factor 1 receptor | Kinase | Kd | 7.35 | CHEMBL | |||||
| Platelet-derived growth factor receptor alpha | Kinase | Kd | 7.13 | CHEMBL | |||||
| Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Kinase | Kd | 6.48 | CHEMBL | |||||
| Insulin receptor | Kinase | Ki | 5.39 | PDSP | |||||
| Mitogen-activated protein kinase 8 | Kinase | Kd | 6.35 | CHEMBL | |||||
| Tyrosine-protein kinase HCK | Kinase | Kd | 6.41 | CHEMBL | |||||
| Carbonic anhydrase 3 | Enzyme | Ki | 6.35 | CHEMBL | |||||
| Carbonic anhydrase 6 | Enzyme | Ki | 6.34 | CHEMBL | |||||
| Mitogen-activated protein kinase 10 | Kinase | Kd | 5.70 | CHEMBL | |||||
| Tyrosine-protein kinase JAK2 | Kinase | Ki | 5.07 | PDSP | |||||
| Angiopoietin-1 receptor | Kinase | Kd | 6 | CHEMBL | |||||
| Ephrin type-A receptor 8 | Kinase | Kd | 7.43 | CHEMBL | |||||
| Tyrosine-protein kinase Lyn | Kinase | Kd | 7 | CHEMBL | |||||
| Cytoplasmic tyrosine-protein kinase BMX | Kinase | Ki | 5.32 | PDSP | |||||
| Carbonic anhydrase 14 | Enzyme | Ki | 6.65 | CHEMBL | |||||
| Fibroblast growth factor receptor 1 | Kinase | Ki | 5.10 | PDSP | |||||
| Serine/threonine-protein kinase 10 | Kinase | Kd | 5.17 | CHEMBL | |||||
| Abelson tyrosine-protein kinase 2 | Kinase | Kd | 7.59 | CHEMBL | |||||
| Mitogen-activated protein kinase 11 | Kinase | Kd | 7.44 | CHEMBL | |||||
| Ephrin type-A receptor 5 | Kinase | Kd | 5.72 | CHEMBL | |||||
| Ephrin type-A receptor 4 | Kinase | Kd | 6.48 | CHEMBL | |||||
| Fibroblast growth factor receptor 2 | Kinase | Ki | 5.14 | PDSP | |||||
| Ephrin type-A receptor 6 | Kinase | Kd | 6.19 | CHEMBL | |||||
| Tyrosine-protein kinase Fgr | Kinase | Kd | 6.49 | CHEMBL | |||||
| Ephrin type-A receptor 3 | Kinase | Kd | 6.96 | CHEMBL | |||||
| Mitogen-activated protein kinase 14 | Kinase | Kd | 6.34 | CHEMBL | |||||
| Tyrosine-protein kinase FRK | Kinase | Kd | 7.07 | CHEMBL | |||||
| Dual specificity protein kinase CLK1 | Kinase | Kd | 5.68 | CHEMBL | |||||
| Ephrin type-B receptor 1 | Kinase | Kd | 5.89 | CHEMBL | |||||
| Dual specificity protein kinase CLK4 | Kinase | Kd | 5.15 | CHEMBL | |||||
| Mitogen-activated protein kinase 9 | Kinase | Kd | 5.24 | CHEMBL | |||||
| Epithelial discoidin domain-containing receptor 1 | Kinase | Kd | 8.96 | CHEMBL | |||||
| Ephrin type-B receptor 4 | Kinase | Kd | 6.14 | CHEMBL | |||||
| BDNF/NT-3 growth factors receptor | Kinase | Kd | 6.31 | CHEMBL | |||||
| Ephrin type-B receptor 2 | Kinase | Kd | 6.19 | CHEMBL | |||||
| Mitogen-activated protein kinase kinase kinase MLT | Kinase | Kd | 7.96 | CHEMBL | |||||
| Tyrosine-protein kinase receptor Tie-1 | Kinase | Kd | 6 | CHEMBL | |||||
| NT-3 growth factor receptor | Kinase | Kd | 6.22 | CHEMBL | |||||
| Serine/threonine-protein kinase TNNI3K | Kinase | Kd | 6.44 | CHEMBL | |||||
| Discoidin domain-containing receptor 2 | Kinase | Kd | 8.22 | CHEMBL | |||||
| Mitogen-activated protein kinase kinase kinase kinase 1 | Kinase | Kd | 6.05 | CHEMBL | |||||
| Tyrosine-protein kinase Blk | Kinase | Kd | 6.30 | CHEMBL | |||||
| Serine/threonine-protein kinase MRCK beta | Kinase | Kd | 6.04 | CHEMBL | |||||
| Ephrin type-A receptor 1 | Kinase | Kd | 6.23 | CHEMBL | |||||
| Ephrin type-B receptor 3 | Kinase | Kd | 6 | CHEMBL | |||||
| Ephrin type-B receptor 6 | Kinase | Kd | 6.30 | CHEMBL | |||||
| Serine/threonine-protein kinase TAO1 | Kinase | Kd | 5.33 | CHEMBL | |||||
| Serine/threonine-protein kinase TAO3 | Kinase | Kd | 5.77 | CHEMBL | |||||
| Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Kinase | Kd | 5.06 | CHEMBL | |||||
| Dual specificity mitogen-activated protein kinase kinase 5 | Kinase | Kd | 6.72 | CHEMBL | |||||
| Bcr/Abl fusion protein | Kinase | IC50 | 9.48 | CHEMBL | |||||
| Ferrochelatase, mitochondrial | Enzyme | Kd | 5.38 | CHEMBL | |||||
| Receptor-interacting serine/threonine-protein kinase 3 | Kinase | Kd | 5.89 | CHEMBL | |||||
| Integrin-linked protein kinase | Kinase | Kd | 7.70 | CHEMBL | |||||
| Tyrosine-protein kinase CSK | Kinase | Kd | 5.62 | CHEMBL | |||||
| Carbonic anhydrase 13 | Enzyme | Ki | 5.33 | CHEMBL | |||||
| Carbonic anhydrase 15 | Enzyme | Ki | 7.10 | CHEMBL | |||||
| Calcium-dependent protein kinase 1 | Kinase | Kd | 6.10 | CHEMBL | |||||
| Macrophage colony-stimulating factor 1 receptor | Unclassified | IC50 | 6.27 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4026964 | VUID |
| N0000176124 | NUI |
| D06413 | KEGG_DRUG |
| 923288-90-8 | SECONDARY_CAS_RN |
| 4026964 | VANDF |
| C1721377 | UMLSCUI |
| CHEBI:52172 | CHEBI |
| NIL | PDB_CHEM_ID |
| CHEMBL255863 | ChEMBL_ID |
| CHEMBL1201740 | ChEMBL_ID |
| DB04868 | DRUGBANK_ID |
| C498826 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5697 | IUPHAR_LIGAND_ID |
| 8654 | INN_ID |
| F41401512X | UNII |
| 644241 | PUBCHEM_CID |
| 662281 | RXNORM |
| 127956 | MMSL |
| 24733 | MMSL |
| d07057 | MMSL |
| 012401 | NDDF |
| 427941004 | SNOMEDCT_US |
| 428468009 | SNOMEDCT_US |
| 438943005 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Tasigna | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0526 | CAPSULE | 200 mg | ORAL | NDA | 33 sections |
| Tasigna | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0526 | CAPSULE | 200 mg | ORAL | NDA | 33 sections |
| Tasigna | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0592 | CAPSULE | 150 mg | ORAL | NDA | 33 sections |
| Tasigna | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0592 | CAPSULE | 150 mg | ORAL | NDA | 33 sections |
| Tasigna | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0951 | CAPSULE | 50 mg | ORAL | NDA | 33 sections |
| Tasigna | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0951 | CAPSULE | 50 mg | ORAL | NDA | 33 sections |