Stem definition | Drug id | CAS RN |
---|---|---|
antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives | 2351 | 84449-90-1 |
Dose | Unit | Route |
---|---|---|
60 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 0.01 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 0.10 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 21.12 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 2 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 7.50 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 10.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.05 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 12.10 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 5, 1998 | EMA | ELI LILLY NEDERLAND B.V. | |
Dec. 9, 1997 | FDA | LILLY |
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 |
---|---|---|---|---|---|---|
Endometrial cancer | 256.13 | 12.17 | 77 | 20265 | 3148 | 63465532 |
Breast cancer | 236.54 | 12.17 | 163 | 20179 | 48220 | 63420460 |
Deep vein thrombosis | 171.10 | 12.17 | 170 | 20172 | 83630 | 63385050 |
Retinal vein thrombosis | 143.67 | 12.17 | 33 | 20309 | 457 | 63468223 |
Bone density decreased | 137.84 | 12.17 | 75 | 20267 | 14537 | 63454143 |
Pulmonary embolism | 136.08 | 12.17 | 177 | 20165 | 116507 | 63352173 |
Fracture | 114.99 | 12.17 | 74 | 20268 | 19510 | 63449170 |
Femur fracture | 110.70 | 12.17 | 98 | 20244 | 41658 | 63427022 |
Spinal compression fracture | 104.25 | 12.17 | 62 | 20280 | 14221 | 63454459 |
Retinal vein occlusion | 84.02 | 12.17 | 30 | 20312 | 2113 | 63466567 |
Hip fracture | 81.77 | 12.17 | 71 | 20271 | 29403 | 63439277 |
Transient ischaemic attack | 72.22 | 12.17 | 74 | 20268 | 37679 | 63431001 |
Body height decreased | 71.60 | 12.17 | 43 | 20299 | 10035 | 63458645 |
Cerebral infarction | 71.26 | 12.17 | 60 | 20282 | 23833 | 63444847 |
Fall | 70.53 | 12.17 | 280 | 20062 | 392054 | 63076626 |
Thoracic vertebral fracture | 68.04 | 12.17 | 32 | 20310 | 4560 | 63464120 |
Compression fracture | 66.13 | 12.17 | 35 | 20307 | 6413 | 63462267 |
Pelvic fracture | 65.22 | 12.17 | 45 | 20297 | 13303 | 63455377 |
Drug ineffective | 63.58 | 12.17 | 152 | 20190 | 1044613 | 62424067 |
Breast cancer in situ | 62.50 | 12.17 | 22 | 20320 | 1486 | 63467194 |
Breast cancer female | 62.26 | 12.17 | 44 | 20298 | 13515 | 63455165 |
Lumbar vertebral fracture | 58.07 | 12.17 | 31 | 20311 | 5779 | 63462901 |
Cerebrovascular accident | 57.86 | 12.17 | 115 | 20227 | 107909 | 63360771 |
Oestrogen receptor assay positive | 57.45 | 12.17 | 16 | 20326 | 496 | 63468184 |
Spinal fracture | 56.80 | 12.17 | 47 | 20295 | 18224 | 63450456 |
Visual acuity reduced | 53.43 | 12.17 | 49 | 20293 | 21777 | 63446903 |
Osteonecrosis of jaw | 53.42 | 12.17 | 61 | 20281 | 35062 | 63433618 |
Off label use | 53.16 | 12.17 | 84 | 20258 | 674378 | 62794302 |
Infusion related reaction | 50.27 | 12.17 | 9 | 20333 | 245512 | 63223168 |
Product use issue | 49.96 | 12.17 | 6 | 20336 | 220514 | 63248166 |
Toxicity to various agents | 48.64 | 12.17 | 10 | 20332 | 247240 | 63221440 |
Low turnover osteopathy | 46.59 | 12.17 | 24 | 20318 | 4161 | 63464519 |
Systemic lupus erythematosus | 44.22 | 12.17 | 7 | 20335 | 208911 | 63259769 |
Ovarian cancer | 43.75 | 12.17 | 26 | 20316 | 5950 | 63462730 |
Osteonecrosis | 43.17 | 12.17 | 46 | 20296 | 24484 | 63444196 |
Synovitis | 42.55 | 12.17 | 5 | 20337 | 186913 | 63281767 |
Endometrial cancer stage I | 42.51 | 12.17 | 11 | 20331 | 256 | 63468424 |
Wrist fracture | 42.33 | 12.17 | 35 | 20307 | 13552 | 63455128 |
Postmenopausal haemorrhage | 41.50 | 12.17 | 18 | 20324 | 2124 | 63466556 |
Hot flush | 41.00 | 12.17 | 65 | 20277 | 51094 | 63417586 |
Muscle spasms | 40.55 | 12.17 | 126 | 20216 | 156024 | 63312656 |
Glossodynia | 40.18 | 12.17 | 5 | 20337 | 178871 | 63289809 |
Treatment failure | 39.24 | 12.17 | 8 | 20334 | 199035 | 63269645 |
Product complaint | 37.84 | 12.17 | 32 | 20310 | 12777 | 63455903 |
Myocardial infarction | 37.23 | 12.17 | 92 | 20250 | 99801 | 63368879 |
Drug intolerance | 36.97 | 12.17 | 27 | 20315 | 308634 | 63160046 |
Retinal vascular thrombosis | 36.17 | 12.17 | 9 | 20333 | 178 | 63468502 |
Uterine cancer | 35.72 | 12.17 | 21 | 20321 | 4712 | 63463968 |
Blindness unilateral | 35.19 | 12.17 | 23 | 20319 | 6218 | 63462462 |
Rheumatoid arthritis | 33.36 | 12.17 | 20 | 20322 | 253799 | 63214881 |
Uterine polyp | 32.59 | 12.17 | 15 | 20327 | 2035 | 63466645 |
Cataract | 32.05 | 12.17 | 62 | 20280 | 56991 | 63411689 |
Alopecia | 30.52 | 12.17 | 38 | 20304 | 337498 | 63131182 |
Therapeutic product effect decreased | 30.27 | 12.17 | 12 | 20330 | 193175 | 63275505 |
Oedema peripheral | 29.80 | 12.17 | 130 | 20212 | 189381 | 63279299 |
Endometrial cancer stage II | 28.83 | 12.17 | 5 | 20337 | 13 | 63468667 |
Pericarditis | 28.77 | 12.17 | 4 | 20338 | 131575 | 63337105 |
Multiple fractures | 28.53 | 12.17 | 23 | 20319 | 8595 | 63460085 |
Hyperlipidaemia | 28.09 | 12.17 | 33 | 20309 | 19538 | 63449142 |
Stress fracture | 27.96 | 12.17 | 22 | 20320 | 7941 | 63460739 |
Intentional product use issue | 27.70 | 12.17 | 4 | 20338 | 127888 | 63340792 |
Rib fracture | 27.41 | 12.17 | 35 | 20307 | 22562 | 63446118 |
Retinal haemorrhage | 27.26 | 12.17 | 18 | 20324 | 4951 | 63463729 |
Therapeutic product effect incomplete | 26.88 | 12.17 | 4 | 20338 | 125052 | 63343628 |
Intestinal pseudo-obstruction | 25.62 | 12.17 | 10 | 20332 | 902 | 63467778 |
Lumbar spinal stenosis | 25.32 | 12.17 | 17 | 20325 | 4805 | 63463875 |
Lower respiratory tract infection | 24.69 | 12.17 | 6 | 20336 | 132301 | 63336379 |
Back pain | 24.16 | 12.17 | 156 | 20186 | 263989 | 63204691 |
Injection site haemorrhage | 23.91 | 12.17 | 34 | 20308 | 24280 | 63444400 |
Embolism | 23.87 | 12.17 | 20 | 20322 | 7886 | 63460794 |
Joint swelling | 22.81 | 12.17 | 44 | 20298 | 327622 | 63141058 |
Wound | 22.68 | 12.17 | 12 | 20330 | 163251 | 63305429 |
Femoral neck fracture | 22.56 | 12.17 | 20 | 20322 | 8503 | 63460177 |
Hepatic enzyme increased | 22.56 | 12.17 | 19 | 20323 | 202309 | 63266371 |
Ischaemic stroke | 22.07 | 12.17 | 28 | 20314 | 17929 | 63450751 |
Breast cancer recurrent | 22.07 | 12.17 | 15 | 20327 | 4326 | 63464354 |
Swelling | 21.88 | 12.17 | 34 | 20308 | 275344 | 63193336 |
Thrombosis | 21.39 | 12.17 | 57 | 20285 | 64698 | 63403982 |
Embolism venous | 21.22 | 12.17 | 13 | 20329 | 3141 | 63465539 |
General physical health deterioration | 21.15 | 12.17 | 20 | 20322 | 201382 | 63267298 |
Oestrogen receptor assay negative | 21.14 | 12.17 | 3 | 20339 | 0 | 63468680 |
Pain | 21.09 | 12.17 | 145 | 20197 | 740483 | 62728197 |
Product use in unapproved indication | 20.99 | 12.17 | 16 | 20326 | 179064 | 63289616 |
Peripheral swelling | 20.97 | 12.17 | 33 | 20309 | 265909 | 63202771 |
Dementia Alzheimer's type | 20.84 | 12.17 | 9 | 20333 | 1051 | 63467629 |
Intramedullary rod insertion | 20.30 | 12.17 | 11 | 20331 | 2112 | 63466568 |
Diverticulum | 20.24 | 12.17 | 22 | 20320 | 11969 | 63456711 |
Bone pain | 20.00 | 12.17 | 50 | 20292 | 54591 | 63414089 |
Osteopenia | 19.94 | 12.17 | 28 | 20314 | 19757 | 63448923 |
Fibrocystic breast disease | 19.82 | 12.17 | 9 | 20333 | 1183 | 63467497 |
Feeling abnormal | 19.77 | 12.17 | 97 | 20245 | 148295 | 63320385 |
Spinal osteoarthritis | 19.52 | 12.17 | 25 | 20317 | 16161 | 63452519 |
Psoriatic arthropathy | 19.50 | 12.17 | 3 | 20339 | 91517 | 63377163 |
Uterine leiomyoma | 19.36 | 12.17 | 19 | 20323 | 9179 | 63459501 |
Endometrial hyperplasia | 19.05 | 12.17 | 8 | 20334 | 872 | 63467808 |
Infection | 18.48 | 12.17 | 28 | 20314 | 229145 | 63239535 |
Fractured sacrum | 18.05 | 12.17 | 10 | 20332 | 2006 | 63466674 |
Humerus fracture | 18.00 | 12.17 | 18 | 20324 | 8898 | 63459782 |
Helicobacter infection | 17.72 | 12.17 | 4 | 20338 | 92781 | 63375899 |
Blood calcium increased | 17.28 | 12.17 | 18 | 20324 | 9332 | 63459348 |
Colitis ischaemic | 16.96 | 12.17 | 19 | 20323 | 10689 | 63457991 |
Fracture nonunion | 16.84 | 12.17 | 10 | 20332 | 2285 | 63466395 |
Coronary artery disease | 16.75 | 12.17 | 34 | 20308 | 32343 | 63436337 |
Colon cancer | 16.46 | 12.17 | 18 | 20324 | 9860 | 63458820 |
Musculoskeletal stiffness | 16.44 | 12.17 | 21 | 20321 | 184597 | 63284083 |
Intervertebral disc protrusion | 16.13 | 12.17 | 28 | 20314 | 23681 | 63444999 |
Foot fracture | 15.96 | 12.17 | 28 | 20314 | 23886 | 63444794 |
Kyphosis | 15.90 | 12.17 | 10 | 20332 | 2530 | 63466150 |
Insulinoma | 15.89 | 12.17 | 4 | 20338 | 83 | 63468597 |
Thrombotic stroke | 15.56 | 12.17 | 6 | 20336 | 524 | 63468156 |
Breast swelling | 15.47 | 12.17 | 8 | 20334 | 1398 | 63467282 |
Pleurisy | 15.31 | 12.17 | 16 | 20326 | 8324 | 63460356 |
Vision blurred | 15.15 | 12.17 | 64 | 20278 | 91860 | 63376820 |
Jaw disorder | 15.06 | 12.17 | 13 | 20329 | 5336 | 63463344 |
Radius fracture | 14.87 | 12.17 | 11 | 20331 | 3624 | 63465056 |
Endometrial hypertrophy | 14.59 | 12.17 | 5 | 20337 | 312 | 63468368 |
Gastrooesophageal reflux disease | 14.55 | 12.17 | 65 | 20277 | 95574 | 63373106 |
Pathological fracture | 14.55 | 12.17 | 16 | 20326 | 8818 | 63459862 |
Haemorrhage subcutaneous | 14.44 | 12.17 | 10 | 20332 | 2973 | 63465707 |
Lung neoplasm malignant | 14.44 | 12.17 | 24 | 20318 | 19609 | 63449071 |
Erythema multiforme | 14.35 | 12.17 | 17 | 20325 | 10152 | 63458528 |
Gastrointestinal tract adenoma | 14.27 | 12.17 | 5 | 20337 | 333 | 63468347 |
Bone disorder | 14.27 | 12.17 | 25 | 20317 | 21301 | 63447379 |
Osteomyelitis | 14.27 | 12.17 | 28 | 20314 | 25992 | 63442688 |
Drug abuse | 14.10 | 12.17 | 3 | 20339 | 72515 | 63396165 |
Subacute hepatic failure | 14.07 | 12.17 | 4 | 20338 | 134 | 63468546 |
Glaucoma | 13.75 | 12.17 | 23 | 20319 | 18882 | 63449798 |
Atrophic vulvovaginitis | 13.75 | 12.17 | 8 | 20334 | 1760 | 63466920 |
Altered state of consciousness | 13.65 | 12.17 | 27 | 20315 | 25203 | 63443477 |
Sarcoma uterus | 13.53 | 12.17 | 3 | 20339 | 35 | 63468645 |
Tibia fracture | 13.52 | 12.17 | 12 | 20330 | 5108 | 63463572 |
Abdominal discomfort | 13.46 | 12.17 | 55 | 20287 | 320830 | 63147850 |
Breast calcifications | 13.28 | 12.17 | 7 | 20335 | 1271 | 63467409 |
Exostosis of jaw | 13.23 | 12.17 | 7 | 20335 | 1282 | 63467398 |
Visual field defect | 12.79 | 12.17 | 13 | 20329 | 6548 | 63462132 |
Ligament sprain | 12.73 | 12.17 | 18 | 20324 | 12782 | 63455898 |
Intentional overdose | 12.64 | 12.17 | 4 | 20338 | 74148 | 63394532 |
Atrial fibrillation | 12.62 | 12.17 | 72 | 20270 | 116564 | 63352116 |
Intervertebral disc degeneration | 12.61 | 12.17 | 20 | 20322 | 15712 | 63452968 |
Vascular headache | 12.54 | 12.17 | 3 | 20339 | 50 | 63468630 |
Osteoporotic fracture | 12.40 | 12.17 | 10 | 20332 | 3736 | 63464944 |
Acute myocardial infarction | 12.40 | 12.17 | 30 | 20312 | 32094 | 63436586 |
Hypersensitivity | 12.38 | 12.17 | 50 | 20292 | 292635 | 63176045 |
Aortic aneurysm | 12.18 | 12.17 | 10 | 20332 | 3834 | 63464846 |
None
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 |
---|---|---|---|---|---|---|
Endometrial cancer | 160.54 | 13.04 | 43 | 14509 | 2051 | 79727785 |
Bone density decreased | 125.25 | 13.04 | 57 | 14495 | 13290 | 79716546 |
Breast cancer | 111.28 | 13.04 | 72 | 14480 | 33709 | 79696127 |
Retinal vein thrombosis | 107.60 | 13.04 | 25 | 14527 | 660 | 79729176 |
Deep vein thrombosis | 105.61 | 13.04 | 120 | 14432 | 120799 | 79609037 |
Spinal compression fracture | 97.90 | 13.04 | 52 | 14500 | 16906 | 79712930 |
Femur fracture | 82.11 | 13.04 | 63 | 14489 | 38589 | 79691247 |
Thoracic vertebral fracture | 81.25 | 13.04 | 32 | 14520 | 5221 | 79724615 |
Pulmonary embolism | 76.85 | 13.04 | 123 | 14429 | 171531 | 79558305 |
Oestrogen receptor assay positive | 73.39 | 13.04 | 16 | 14536 | 314 | 79729522 |
Body height decreased | 72.26 | 13.04 | 34 | 14518 | 8546 | 79721290 |
Fracture | 68.20 | 13.04 | 45 | 14507 | 21756 | 79708080 |
Breast cancer female | 62.94 | 13.04 | 34 | 14518 | 11427 | 79718409 |
Hip fracture | 60.69 | 13.04 | 48 | 14504 | 30713 | 79699123 |
Lumbar vertebral fracture | 56.60 | 13.04 | 27 | 14525 | 6995 | 79722841 |
Transient ischaemic attack | 54.13 | 13.04 | 57 | 14495 | 52638 | 79677198 |
Retinal vein occlusion | 54.06 | 13.04 | 21 | 14531 | 3302 | 79726534 |
Pelvic fracture | 52.89 | 13.04 | 31 | 14521 | 12173 | 79717663 |
Endometrial cancer stage I | 51.89 | 13.04 | 11 | 14541 | 188 | 79729648 |
Spinal fracture | 51.04 | 13.04 | 35 | 14517 | 18019 | 79711817 |
Compression fracture | 49.52 | 13.04 | 24 | 14528 | 6436 | 79723400 |
Fall | 48.95 | 13.04 | 197 | 14355 | 487432 | 79242404 |
Toxicity to various agents | 48.77 | 13.04 | 9 | 14543 | 421531 | 79308305 |
Wrist fracture | 48.31 | 13.04 | 29 | 14523 | 11892 | 79717944 |
Off label use | 46.07 | 13.04 | 59 | 14493 | 907156 | 78822680 |
Breast cancer in situ | 43.36 | 13.04 | 13 | 14539 | 933 | 79728903 |
Product complaint | 42.83 | 13.04 | 28 | 14524 | 13321 | 79716515 |
Visual acuity reduced | 41.72 | 13.04 | 38 | 14514 | 29431 | 79700405 |
Cerebrovascular accident | 41.32 | 13.04 | 89 | 14463 | 155203 | 79574633 |
Postmenopausal haemorrhage | 40.90 | 13.04 | 14 | 14538 | 1538 | 79728298 |
Hot flush | 37.29 | 13.04 | 48 | 14504 | 54829 | 79675007 |
Multiple fractures | 36.40 | 13.04 | 21 | 14531 | 8005 | 79721831 |
Muscle spasms | 35.39 | 13.04 | 90 | 14462 | 174640 | 79555196 |
Osteonecrosis of jaw | 34.50 | 13.04 | 41 | 14511 | 43185 | 79686651 |
Ovarian cancer | 34.39 | 13.04 | 16 | 14536 | 3918 | 79725918 |
Endometrial cancer stage II | 33.67 | 13.04 | 5 | 14547 | 7 | 79729829 |
Uterine polyp | 33.01 | 13.04 | 12 | 14540 | 1572 | 79728264 |
Injection site haemorrhage | 31.97 | 13.04 | 32 | 14520 | 27838 | 79701998 |
Osteonecrosis | 30.80 | 13.04 | 33 | 14519 | 31062 | 79698774 |
Uterine cancer | 29.16 | 13.04 | 14 | 14538 | 3677 | 79726159 |
Drug ineffective | 28.30 | 13.04 | 102 | 14450 | 1080811 | 78649025 |
Bone pain | 26.36 | 13.04 | 41 | 14511 | 55701 | 79674135 |
Oedema peripheral | 26.09 | 13.04 | 103 | 14449 | 252185 | 79477651 |
Feeling abnormal | 25.26 | 13.04 | 75 | 14477 | 159124 | 79570712 |
Cerebral infarction | 25.03 | 13.04 | 36 | 14516 | 45640 | 79684196 |
Completed suicide | 23.10 | 13.04 | 8 | 14544 | 245759 | 79484077 |
Infusion related reaction | 22.51 | 13.04 | 7 | 14545 | 230230 | 79499606 |
Hyperlipidaemia | 21.23 | 13.04 | 25 | 14527 | 26068 | 79703768 |
Product use issue | 21.20 | 13.04 | 6 | 14546 | 209816 | 79520020 |
Blindness unilateral | 21.17 | 13.04 | 15 | 14537 | 8131 | 79721705 |
Death | 21.07 | 13.04 | 45 | 14507 | 566469 | 79163367 |
Cataract | 20.55 | 13.04 | 39 | 14513 | 62081 | 79667755 |
Myocardial infarction | 20.52 | 13.04 | 77 | 14475 | 184052 | 79545784 |
Low turnover osteopathy | 20.28 | 13.04 | 9 | 14543 | 1977 | 79727859 |
Blood calcium increased | 20.02 | 13.04 | 16 | 14536 | 10384 | 79719452 |
Back pain | 19.49 | 13.04 | 108 | 14444 | 304072 | 79425764 |
Ischaemic stroke | 19.47 | 13.04 | 27 | 14525 | 33104 | 79696732 |
Diverticulum | 18.75 | 13.04 | 18 | 14534 | 14878 | 79714958 |
Fractured sacrum | 18.57 | 13.04 | 8 | 14544 | 1635 | 79728201 |
Intentional product use issue | 18.10 | 13.04 | 3 | 14549 | 152109 | 79577727 |
Intestinal pseudo-obstruction | 17.93 | 13.04 | 9 | 14543 | 2600 | 79727236 |
Intervertebral disc degeneration | 17.87 | 13.04 | 18 | 14534 | 15767 | 79714069 |
Endometrial hyperplasia | 17.79 | 13.04 | 6 | 14546 | 630 | 79729206 |
Injection site erythema | 17.64 | 13.04 | 42 | 14510 | 78155 | 79651681 |
General physical health deterioration | 17.14 | 13.04 | 15 | 14537 | 275223 | 79454613 |
Atrophic vulvovaginitis | 17.14 | 13.04 | 7 | 14545 | 1254 | 79728582 |
Uterine leiomyoma | 17.06 | 13.04 | 12 | 14540 | 6431 | 79723405 |
Stress fracture | 16.99 | 13.04 | 12 | 14540 | 6468 | 79723368 |
Treatment failure | 16.99 | 13.04 | 5 | 14547 | 170481 | 79559355 |
Drug intolerance | 16.93 | 13.04 | 14 | 14538 | 264105 | 79465731 |
Retinal haemorrhage | 16.58 | 13.04 | 13 | 14539 | 8204 | 79721632 |
Insulinoma | 16.47 | 13.04 | 4 | 14548 | 128 | 79729708 |
Femoral neck fracture | 16.38 | 13.04 | 14 | 14538 | 9970 | 79719866 |
Foot fracture | 16.15 | 13.04 | 20 | 14532 | 21961 | 79707875 |
Synovitis | 15.81 | 13.04 | 4 | 14548 | 150730 | 79579106 |
Acute kidney injury | 15.61 | 13.04 | 46 | 14506 | 519358 | 79210478 |
Osteomyelitis | 15.29 | 13.04 | 24 | 14528 | 32841 | 79696995 |
Rib fracture | 15.27 | 13.04 | 22 | 14530 | 27925 | 79701911 |
Product use in unapproved indication | 15.16 | 13.04 | 14 | 14538 | 250345 | 79479491 |
Endometrial hypertrophy | 15.16 | 13.04 | 4 | 14548 | 180 | 79729656 |
Dementia Alzheimer's type | 15.03 | 13.04 | 6 | 14546 | 1013 | 79728823 |
Jaw disorder | 14.85 | 13.04 | 10 | 14542 | 4996 | 79724840 |
Erythema multiforme | 14.51 | 13.04 | 17 | 14535 | 17634 | 79712202 |
Therapeutic product effect incomplete | 14.40 | 13.04 | 4 | 14548 | 141641 | 79588195 |
Tibia fracture | 14.23 | 13.04 | 10 | 14542 | 5351 | 79724485 |
Vascular headache | 14.17 | 13.04 | 3 | 14549 | 51 | 79729785 |
Breast cancer recurrent | 14.06 | 13.04 | 8 | 14544 | 2969 | 79726867 |
Osteoporotic fracture | 13.86 | 13.04 | 9 | 14543 | 4231 | 79725605 |
Benign vulval neoplasm | 13.75 | 13.04 | 3 | 14549 | 59 | 79729777 |
Fibrocystic breast disease | 13.68 | 13.04 | 5 | 14547 | 665 | 79729171 |
Bone disorder | 13.42 | 13.04 | 17 | 14535 | 19096 | 79710740 |
Breast swelling | 13.28 | 13.04 | 6 | 14546 | 1374 | 79728462 |
Thrombotic stroke | 13.12 | 13.04 | 5 | 14547 | 746 | 79729090 |
None
Source | Code | Description |
---|---|---|
ATC | G03XC01 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM Selective estrogen receptor modulators |
FDA MoA | N0000000168 | Selective Estrogen Receptor Modulators |
CHEBI has role | CHEBI:50646 | antiosteoporotic |
CHEBI has role | CHEBI:50837 | oestrogen antagonist |
FDA EPC | N0000175826 | Estrogen Agonist/Antagonist |
MeSH PA | D050071 | Bone Density Conservation Agents |
MeSH PA | D004965 | Estrogen Antagonists |
MeSH PA | D020847 | Estrogen Receptor Modulators |
MeSH PA | D006727 | Hormone Antagonists |
MeSH PA | D020845 | Selective Estrogen Receptor Modulators |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Postmenopausal osteoporosis | indication | 102447009 | |
Prevention of Breast Carcinoma | indication | ||
Prevention of Glucocorticoid-Induced Osteoporosis | off-label use | ||
Lupus anticoagulant disorder | contraindication | 19267009 | |
Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
Thrombosis of retinal vein | contraindication | 46085004 | |
Chronic heart failure | contraindication | 48447003 | |
Atrial fibrillation | contraindication | 49436004 | DOID:0060224 |
Thrombophlebitis | contraindication | 64156001 | DOID:3875 |
Deep venous thrombosis | contraindication | 128053003 | |
Impaired renal function disorder | contraindication | 197663003 | |
Cerebrovascular accident | contraindication | 230690007 | |
Pulmonary thromboembolism | contraindication | 233935004 | |
Thrombophilia | contraindication | 234467004 | DOID:2452 |
Disease of liver | contraindication | 235856003 | DOID:409 |
Transient ischemic attack | contraindication | 266257000 | DOID:224 |
Pregnancy, function | contraindication | 289908002 | |
Hypertriglyceridemia | contraindication | 302870006 | |
Cardiovascular event risk | contraindication | 395112001 | |
Breastfeeding (mother) | contraindication | 413712001 | |
Disorder of coronary artery | contraindication | 414024009 | |
Smokes tobacco daily | contraindication | 449868002 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.13 | acidic |
pKa2 | 8.6 | acidic |
pKa3 | 9.15 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Estrogen receptor beta | Nuclear hormone receptor | MODULATOR | EC50 | 8 | WOMBAT-PK | CHEMBL | |||
Estrogen receptor | Nuclear hormone receptor | ANTAGONIST | IC50 | 9.40 | WOMBAT-PK | IUPHAR | |||
D(2) dopamine receptor | GPCR | Ki | 6.41 | DRUG MATRIX | |||||
Adenosine receptor A2a | GPCR | Ki | 5.93 | DRUG MATRIX | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 6.21 | DRUG MATRIX | |||||
Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.42 | CHEMBL | |||||
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Enzyme | Ki | 9 | WOMBAT-PK | |||||
Sodium-dependent serotonin transporter | Transporter | Ki | 5.72 | DRUG MATRIX | |||||
Sodium-dependent noradrenaline transporter | Transporter | Ki | 6.55 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.38 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 2B | GPCR | Ki | 7.16 | CHEMBL | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.21 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.30 | WOMBAT-PK | |||||
Alpha-2B adrenergic receptor | GPCR | Ki | 5.77 | DRUG MATRIX | |||||
D(3) dopamine receptor | GPCR | Ki | 6.28 | DRUG MATRIX | |||||
Aldehyde oxidase | Enzyme | IC50 | 8.54 | WOMBAT-PK | |||||
5-hydroxytryptamine receptor 1D | GPCR | Ki | 6.52 | WOMBAT-PK | |||||
Alpha-2C adrenergic receptor | GPCR | Ki | 6.97 | DRUG MATRIX | |||||
Sodium-dependent dopamine transporter | Transporter | Ki | 5.83 | DRUG MATRIX | |||||
Nuclear receptor subfamily 1 group I member 2 | Nuclear hormone receptor | EC50 | 4.93 | CHEMBL | |||||
Alpha-1D adrenergic receptor | GPCR | Ki | 6.32 | DRUG MATRIX | |||||
Kappa-type opioid receptor | GPCR | Ki | 6.19 | DRUG MATRIX | |||||
Delta-type opioid receptor | GPCR | Ki | 5.63 | DRUG MATRIX | |||||
Acetylcholinesterase | Enzyme | IC50 | 6.40 | DRUG MATRIX | |||||
Cytochrome P450 2C9 | Enzyme | IC50 | 5.70 | DRUG MATRIX | |||||
G-protein coupled estrogen receptor 1 | GPCR | EC50 | 6.50 | WOMBAT-PK | |||||
Interleukin-6 | Cytokine | IC50 | 8.05 | WOMBAT-PK | |||||
Tyrosine-protein kinase Fyn | Kinase | IC50 | 5.44 | DRUG MATRIX | |||||
Bile acid receptor | Nuclear hormone receptor | IC50 | 4.94 | CHEMBL | |||||
Substance-K receptor | GPCR | Ki | 5.88 | DRUG MATRIX | |||||
Phospholipase D1 | Enzyme | IC50 | 5.40 | CHEMBL | |||||
Phospholipase D2 | Enzyme | IC50 | 5.47 | CHEMBL | |||||
Lysine-specific histone demethylase 1A | Enzyme | IC50 | 5.68 | CHEMBL | |||||
Complement C5 | Secreted | Kd | 6.15 | CHEMBL | |||||
Mu-type opioid receptor | GPCR | Ki | 6.32 | DRUG MATRIX | |||||
HLA class I histocompatibility antigen, A-3 alpha chain | Unclassified | Kd | 4.66 | CHEMBL | |||||
D(1A) dopamine receptor | GPCR | Ki | 5.71 | DRUG MATRIX | |||||
Alpha-1B adrenergic receptor | GPCR | Ki | 5.83 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 1B | GPCR | Ki | 6.07 | DRUG MATRIX | |||||
Membrane-associated progesterone receptor component 1 | Membrane receptor | Ki | 6.63 | DRUG MATRIX | |||||
Alpha-1A adrenergic receptor | GPCR | IC50 | 5.66 | CHEMBL | |||||
Estrogen receptor | Transcription factor | Ki | 9.43 | CHEMBL | |||||
Estrogen receptor beta | Transcription factor | Ki | 8.56 | CHEMBL | |||||
C-8 sterol isomerase | Enzyme | Ki | 7.18 | CHEMBL | |||||
Cruzipain | Enzyme | IC50 | 4.48 | CHEMBL | |||||
Estrogen receptor | Transcription factor | IC50 | 8.73 | CHEMBL |
ID | Source |
---|---|
4024098 | VUID |
N0000022103 | NUI |
D02217 | KEGG_DRUG |
82640-04-8 | SECONDARY_CAS_RN |
4021080 | VANDF |
4024098 | VANDF |
C0244404 | UMLSCUI |
CHEBI:8772 | CHEBI |
RAL | PDB_CHEM_ID |
CHEMBL81 | ChEMBL_ID |
CHEMBL1116 | ChEMBL_ID |
D020849 | MESH_DESCRIPTOR_UI |
DB00481 | DRUGBANK_ID |
2820 | IUPHAR_LIGAND_ID |
5388 | INN_ID |
YX9162EO3I | UNII |
5035 | PUBCHEM_CID |
166551 | RXNORM |
11500 | MMSL |
5410 | MMSL |
83711 | MMSL |
d04261 | MMSL |
007282 | NDDF |
007283 | NDDF |
109029006 | SNOMEDCT_US |
395856004 | SNOMEDCT_US |
419530003 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Evista | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-4184 | TABLET | 60 mg | ORAL | NDA | 33 sections |
Evista | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-4184 | TABLET | 60 mg | ORAL | NDA | 33 sections |
Evista | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-4184 | TABLET | 60 mg | ORAL | NDA | 33 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-7290 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-7290 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-5295 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 20 sections |
Raloxifene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6902 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 30 sections |
Raloxifene Hydrochloride | Human Prescription Drug Label | 1 | 16714-213 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | Human Prescription Drug Label | 1 | 16714-213 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-256 | TABLET | 60 mg | ORAL | ANDA | 20 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-726 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 31 sections |
Raloxifene Hydrochloride | Human Prescription Drug Label | 1 | 43353-253 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Raloxifene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-505 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 30 sections |
Raloxifene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-505 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 30 sections |
Raloxifene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-3363 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-3866 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-5458 | TABLET | 60 mg | ORAL | ANDA | 27 sections |
Raloxifene hydrochloride | Human Prescription Drug Label | 1 | 50090-6177 | TABLET, COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50228-306 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 30 sections |
Raloxifene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50228-306 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 30 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-694 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Evista | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-4170 | TABLET | 60 mg | ORAL | NDA | 29 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-266 | TABLET | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-266 | TABLET | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-7708 | TABLET | 60 mg | ORAL | ANDA | 27 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-8209 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-057 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-057 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-057 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | Human Prescription Drug Label | 1 | 65862-709 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |