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 |
---|---|---|---|
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 | 249.05 | 12.10 | 77 | 19832 | 2806 | 50582409 |
Breast cancer | 221.82 | 12.10 | 162 | 19747 | 42728 | 50542487 |
Deep vein thrombosis | 157.38 | 12.10 | 168 | 19741 | 73136 | 50512079 |
Retinal vein thrombosis | 143.84 | 12.10 | 33 | 19876 | 364 | 50584851 |
Bone density decreased | 142.91 | 12.10 | 75 | 19834 | 11000 | 50574215 |
Pulmonary embolism | 122.22 | 12.10 | 174 | 19735 | 101530 | 50483685 |
Fracture | 104.15 | 12.10 | 71 | 19838 | 16762 | 50568453 |
Spinal compression fracture | 99.42 | 12.10 | 62 | 19847 | 12594 | 50572621 |
Femur fracture | 98.80 | 12.10 | 96 | 19813 | 37368 | 50547847 |
Retinal vein occlusion | 81.83 | 12.10 | 30 | 19879 | 1851 | 50583364 |
Breast cancer female | 81.55 | 12.10 | 44 | 19865 | 6818 | 50578397 |
Hip fracture | 77.04 | 12.10 | 71 | 19838 | 25860 | 50559355 |
Transient ischaemic attack | 69.35 | 12.10 | 74 | 19835 | 32136 | 50553079 |
Body height decreased | 65.85 | 12.10 | 42 | 19867 | 8866 | 50576349 |
Thoracic vertebral fracture | 65.44 | 12.10 | 32 | 19877 | 4041 | 50581174 |
Cerebral infarction | 63.88 | 12.10 | 59 | 19850 | 21545 | 50563670 |
Compression fracture | 62.66 | 12.10 | 35 | 19874 | 5802 | 50579413 |
Breast cancer in situ | 59.22 | 12.10 | 22 | 19887 | 1409 | 50583806 |
Lumbar vertebral fracture | 58.92 | 12.10 | 31 | 19878 | 4566 | 50580649 |
Fall | 58.87 | 12.10 | 274 | 19635 | 334658 | 50250557 |
Pelvic fracture | 58.32 | 12.10 | 43 | 19866 | 11477 | 50573738 |
Drug ineffective | 57.58 | 12.10 | 151 | 19758 | 819182 | 49766033 |
Oestrogen receptor assay positive | 56.50 | 12.10 | 16 | 19893 | 427 | 50584788 |
Spinal fracture | 54.93 | 12.10 | 47 | 19862 | 15526 | 50569689 |
Toxicity to various agents | 52.50 | 12.10 | 10 | 19899 | 212489 | 50372726 |
Cerebrovascular accident | 52.04 | 12.10 | 115 | 19794 | 94565 | 50490650 |
Visual acuity reduced | 48.25 | 12.10 | 49 | 19860 | 20090 | 50565125 |
Osteonecrosis of jaw | 45.56 | 12.10 | 60 | 19849 | 32466 | 50552749 |
Low turnover osteopathy | 43.01 | 12.10 | 24 | 19885 | 3970 | 50581245 |
Ovarian cancer | 42.40 | 12.10 | 26 | 19883 | 5123 | 50580092 |
Endometrial cancer stage I | 42.04 | 12.10 | 11 | 19898 | 216 | 50584999 |
Product use issue | 41.56 | 12.10 | 5 | 19904 | 149470 | 50435745 |
Muscle spasms | 41.53 | 12.10 | 126 | 19783 | 125427 | 50459788 |
Wrist fracture | 41.19 | 12.10 | 35 | 19874 | 11452 | 50573763 |
Off label use | 40.02 | 12.10 | 79 | 19830 | 474347 | 50110868 |
Infusion related reaction | 39.76 | 12.10 | 9 | 19900 | 169548 | 50415667 |
Postmenopausal haemorrhage | 39.31 | 12.10 | 18 | 19891 | 1962 | 50583253 |
Osteonecrosis | 38.67 | 12.10 | 46 | 19863 | 22471 | 50562744 |
Hot flush | 38.19 | 12.10 | 65 | 19844 | 44104 | 50541111 |
Retinal vascular thrombosis | 35.40 | 12.10 | 9 | 19900 | 157 | 50585058 |
Product complaint | 35.23 | 12.10 | 32 | 19877 | 11434 | 50573781 |
Blindness unilateral | 34.57 | 12.10 | 23 | 19886 | 5212 | 50580003 |
Systemic lupus erythematosus | 33.91 | 12.10 | 7 | 19902 | 140615 | 50444600 |
Uterine cancer | 33.28 | 12.10 | 20 | 19889 | 3800 | 50581415 |
Synovitis | 32.40 | 12.10 | 5 | 19904 | 123860 | 50461355 |
Rheumatoid arthritis | 32.13 | 12.10 | 20 | 19889 | 202530 | 50382685 |
Myocardial infarction | 31.95 | 12.10 | 92 | 19817 | 88935 | 50496280 |
Uterine polyp | 31.77 | 12.10 | 15 | 19894 | 1753 | 50583462 |
Treatment failure | 30.90 | 12.10 | 8 | 19901 | 137629 | 50447586 |
Drug intolerance | 30.35 | 12.10 | 25 | 19884 | 219079 | 50366136 |
Glossodynia | 29.47 | 12.10 | 5 | 19904 | 115564 | 50469651 |
Cataract | 28.90 | 12.10 | 60 | 19849 | 47240 | 50537975 |
Endometrial cancer stage II | 28.72 | 12.10 | 5 | 19904 | 10 | 50585205 |
Multiple fractures | 27.58 | 12.10 | 22 | 19887 | 6589 | 50578626 |
Stress fracture | 26.83 | 12.10 | 22 | 19887 | 6853 | 50578362 |
Hyperlipidaemia | 25.63 | 12.10 | 33 | 19876 | 17457 | 50567758 |
Intestinal pseudo-obstruction | 25.48 | 12.10 | 10 | 19899 | 744 | 50584471 |
Oedema peripheral | 25.31 | 12.10 | 126 | 19783 | 157835 | 50427380 |
Retinal haemorrhage | 25.23 | 12.10 | 18 | 19891 | 4563 | 50580652 |
Rib fracture | 24.69 | 12.10 | 34 | 19875 | 19187 | 50566028 |
Therapeutic product effect decreased | 23.63 | 12.10 | 12 | 19897 | 136038 | 50449177 |
Therapeutic product effect incomplete | 23.24 | 12.10 | 4 | 19905 | 91511 | 50493704 |
Alopecia | 23.12 | 12.10 | 38 | 19871 | 245009 | 50340206 |
Embolism | 22.50 | 12.10 | 20 | 19889 | 6948 | 50578267 |
Lower respiratory tract infection | 22.41 | 12.10 | 5 | 19904 | 95196 | 50490019 |
Lumbar spinal stenosis | 22.14 | 12.10 | 16 | 19893 | 4138 | 50581077 |
Injection site haemorrhage | 21.96 | 12.10 | 34 | 19875 | 21312 | 50563903 |
Embolism venous | 21.43 | 12.10 | 13 | 19896 | 2512 | 50582703 |
Femoral neck fracture | 21.26 | 12.10 | 20 | 19889 | 7470 | 50577745 |
Breast cancer recurrent | 21.06 | 12.10 | 15 | 19894 | 3793 | 50581422 |
Oestrogen receptor assay negative | 20.52 | 12.10 | 3 | 19906 | 0 | 50585215 |
Peripheral swelling | 20.30 | 12.10 | 31 | 19878 | 205905 | 50379310 |
Ischaemic stroke | 20.17 | 12.10 | 28 | 19881 | 15920 | 50569295 |
Joint swelling | 19.64 | 12.10 | 42 | 19867 | 245244 | 50339971 |
Dementia Alzheimer's type | 19.28 | 12.10 | 9 | 19900 | 1025 | 50584190 |
Fibrocystic breast disease | 18.87 | 12.10 | 9 | 19900 | 1075 | 50584140 |
Intramedullary rod insertion | 18.80 | 12.10 | 11 | 19898 | 1989 | 50583226 |
Pericarditis | 18.79 | 12.10 | 4 | 19905 | 78685 | 50506530 |
Endometrial hyperplasia | 18.78 | 12.10 | 8 | 19901 | 734 | 50584481 |
Osteopenia | 18.77 | 12.10 | 28 | 19881 | 16990 | 50568225 |
Diverticulum | 18.74 | 12.10 | 22 | 19887 | 10592 | 50574623 |
Back pain | 18.58 | 12.10 | 149 | 19760 | 219881 | 50365334 |
Uterine leiomyoma | 18.53 | 12.10 | 19 | 19890 | 7872 | 50577343 |
Thrombosis | 18.40 | 12.10 | 56 | 19853 | 55777 | 50529438 |
Spinal osteoarthritis | 18.21 | 12.10 | 25 | 19884 | 14067 | 50571148 |
Intentional product use issue | 18.18 | 12.10 | 4 | 19905 | 76914 | 50508301 |
Swelling | 18.15 | 12.10 | 32 | 19877 | 200840 | 50384375 |
Bone pain | 18.10 | 12.10 | 50 | 19859 | 47179 | 50538036 |
Pain | 17.46 | 12.10 | 145 | 19764 | 578758 | 50006457 |
Humerus fracture | 17.27 | 12.10 | 18 | 19891 | 7600 | 50577615 |
General physical health deterioration | 16.52 | 12.10 | 19 | 19890 | 142415 | 50442800 |
Infection | 16.13 | 12.10 | 27 | 19882 | 172927 | 50412288 |
Breast swelling | 15.86 | 12.10 | 8 | 19901 | 1079 | 50584136 |
Colitis ischaemic | 15.67 | 12.10 | 19 | 19890 | 9464 | 50575751 |
Insulinoma | 15.46 | 12.10 | 4 | 19905 | 75 | 50585140 |
Foot fracture | 15.33 | 12.10 | 28 | 19881 | 20063 | 50565152 |
Blood calcium increased | 15.32 | 12.10 | 17 | 19892 | 7702 | 50577513 |
Colon cancer | 15.32 | 12.10 | 18 | 19891 | 8673 | 50576542 |
Feeling abnormal | 15.31 | 12.10 | 93 | 19816 | 125399 | 50459816 |
Hepatic enzyme increased | 15.22 | 12.10 | 19 | 19890 | 137361 | 50447854 |
Gastrooesophageal reflux disease | 15.21 | 12.10 | 65 | 19844 | 76363 | 50508852 |
Lung neoplasm malignant | 15.01 | 12.10 | 24 | 19885 | 15460 | 50569755 |
Kyphosis | 14.95 | 12.10 | 10 | 19899 | 2285 | 50582930 |
Thrombotic stroke | 14.80 | 12.10 | 6 | 19903 | 486 | 50584729 |
Wound | 14.72 | 12.10 | 12 | 19897 | 105782 | 50479433 |
Fractured sacrum | 14.60 | 12.10 | 9 | 19900 | 1789 | 50583426 |
Drug abuse | 14.37 | 12.10 | 3 | 19906 | 59843 | 50525372 |
Pleurisy | 14.30 | 12.10 | 16 | 19893 | 7315 | 50577900 |
Endometrial hypertrophy | 14.22 | 12.10 | 5 | 19904 | 273 | 50584942 |
Coronary artery disease | 13.99 | 12.10 | 34 | 19875 | 29692 | 50555523 |
Breast cancer stage III | 13.94 | 12.10 | 11 | 19898 | 3245 | 50581970 |
Product use in unapproved indication | 13.92 | 12.10 | 15 | 19894 | 115804 | 50469411 |
Intervertebral disc protrusion | 13.80 | 12.10 | 27 | 19882 | 20366 | 50564849 |
Jaw disorder | 13.65 | 12.10 | 13 | 19896 | 4930 | 50580285 |
Subacute hepatic failure | 13.61 | 12.10 | 4 | 19905 | 122 | 50585093 |
Haemorrhage subcutaneous | 13.48 | 12.10 | 10 | 19899 | 2691 | 50582524 |
Gastrointestinal tract adenoma | 13.45 | 12.10 | 5 | 19904 | 321 | 50584894 |
Intentional overdose | 13.34 | 12.10 | 4 | 19905 | 62500 | 50522715 |
Osteomyelitis | 13.23 | 12.10 | 28 | 19881 | 22325 | 50562890 |
Sarcoma uterus | 13.17 | 12.10 | 3 | 19906 | 32 | 50585183 |
Erythema multiforme | 13.14 | 12.10 | 17 | 19892 | 9033 | 50576182 |
Atrophic vulvovaginitis | 12.99 | 12.10 | 8 | 19901 | 1588 | 50583627 |
Fracture nonunion | 12.93 | 12.10 | 9 | 19900 | 2195 | 50583020 |
Bone disorder | 12.90 | 12.10 | 25 | 19884 | 18727 | 50566488 |
Tibia fracture | 12.80 | 12.10 | 12 | 19897 | 4463 | 50580752 |
Vision blurred | 12.76 | 12.10 | 63 | 19846 | 78584 | 50506631 |
Road traffic accident | 12.71 | 12.10 | 29 | 19880 | 24323 | 50560892 |
Breast calcifications | 12.60 | 12.10 | 7 | 19902 | 1148 | 50584067 |
Ligament sprain | 12.60 | 12.10 | 18 | 19891 | 10507 | 50574708 |
Fatigue | 12.40 | 12.10 | 200 | 19709 | 707401 | 49877814 |
Glaucoma | 12.14 | 12.10 | 22 | 19887 | 15664 | 50569551 |
Osteoporotic fracture | 12.14 | 12.10 | 10 | 19899 | 3135 | 50582080 |
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 | 156.48 | 12.66 | 43 | 14153 | 1867 | 64482669 |
Bone density decreased | 131.06 | 12.66 | 57 | 14139 | 9895 | 64474641 |
Breast cancer | 108.66 | 12.66 | 72 | 14124 | 29076 | 64455460 |
Retinal vein thrombosis | 104.91 | 12.66 | 25 | 14171 | 608 | 64483928 |
Deep vein thrombosis | 97.65 | 12.66 | 118 | 14078 | 105064 | 64379472 |
Spinal compression fracture | 95.48 | 12.66 | 52 | 14144 | 14723 | 64469813 |
Breast cancer female | 83.11 | 12.66 | 34 | 14162 | 5069 | 64479467 |
Thoracic vertebral fracture | 79.87 | 12.66 | 32 | 14164 | 4521 | 64480015 |
Femur fracture | 76.47 | 12.66 | 62 | 14134 | 34073 | 64450463 |
Oestrogen receptor assay positive | 72.68 | 12.66 | 16 | 14180 | 270 | 64484266 |
Pulmonary embolism | 71.63 | 12.66 | 121 | 14075 | 146235 | 64338301 |
Body height decreased | 67.31 | 12.66 | 33 | 14163 | 7521 | 64477015 |
Fracture | 64.31 | 12.66 | 44 | 14152 | 18711 | 64465825 |
Hip fracture | 58.13 | 12.66 | 48 | 14148 | 27051 | 64457485 |
Lumbar vertebral fracture | 58.05 | 12.66 | 27 | 14169 | 5475 | 64479061 |
Transient ischaemic attack | 53.60 | 12.66 | 57 | 14139 | 44125 | 64440411 |
Retinal vein occlusion | 52.41 | 12.66 | 21 | 14175 | 2967 | 64481569 |
Endometrial cancer stage I | 52.23 | 12.66 | 11 | 14185 | 149 | 64484387 |
Toxicity to various agents | 51.52 | 12.66 | 9 | 14187 | 363504 | 64121032 |
Spinal fracture | 50.61 | 12.66 | 35 | 14161 | 15139 | 64469397 |
Wrist fracture | 48.00 | 12.66 | 29 | 14167 | 9972 | 64474564 |
Compression fracture | 47.90 | 12.66 | 24 | 14172 | 5728 | 64478808 |
Pelvic fracture | 46.54 | 12.66 | 29 | 14167 | 10534 | 64474002 |
Fall | 42.64 | 12.66 | 193 | 14003 | 416633 | 64067903 |
Breast cancer in situ | 42.00 | 12.66 | 13 | 14183 | 859 | 64483677 |
Product complaint | 40.87 | 12.66 | 28 | 14168 | 11926 | 64472610 |
Postmenopausal haemorrhage | 39.41 | 12.66 | 14 | 14182 | 1421 | 64483115 |
Visual acuity reduced | 38.32 | 12.66 | 38 | 14158 | 27103 | 64457433 |
Cerebrovascular accident | 37.35 | 12.66 | 89 | 14107 | 137494 | 64347042 |
Muscle spasms | 36.97 | 12.66 | 90 | 14106 | 140933 | 64343603 |
Hot flush | 36.68 | 12.66 | 48 | 14148 | 46187 | 64438349 |
Multiple fractures | 35.56 | 12.66 | 20 | 14176 | 6020 | 64478516 |
Endometrial cancer stage II | 34.17 | 12.66 | 5 | 14191 | 4 | 64484532 |
Ovarian cancer | 34.12 | 12.66 | 16 | 14180 | 3303 | 64481233 |
Off label use | 33.43 | 12.66 | 55 | 14141 | 632751 | 63851785 |
Uterine polyp | 32.93 | 12.66 | 12 | 14184 | 1310 | 64483226 |
Osteonecrosis of jaw | 31.06 | 12.66 | 41 | 14155 | 39784 | 64444752 |
Injection site haemorrhage | 30.64 | 12.66 | 32 | 14164 | 24246 | 64460290 |
Uterine cancer | 29.89 | 12.66 | 14 | 14182 | 2884 | 64481652 |
Completed suicide | 26.89 | 12.66 | 8 | 14188 | 224406 | 64260130 |
Osteonecrosis | 26.69 | 12.66 | 32 | 14164 | 28197 | 64456339 |
Bone pain | 25.47 | 12.66 | 41 | 14155 | 47531 | 64437005 |
Death | 24.49 | 12.66 | 43 | 14153 | 482662 | 64001874 |
Drug ineffective | 23.09 | 12.66 | 101 | 14095 | 840146 | 63644390 |
Oedema peripheral | 22.65 | 12.66 | 99 | 14097 | 210218 | 64274318 |
Cerebral infarction | 21.46 | 12.66 | 35 | 14161 | 41009 | 64443527 |
Blindness unilateral | 21.15 | 12.66 | 15 | 14181 | 6746 | 64477790 |
Feeling abnormal | 21.05 | 12.66 | 71 | 14125 | 133531 | 64351005 |
Cataract | 20.68 | 12.66 | 39 | 14157 | 51223 | 64433313 |
Hyperlipidaemia | 20.02 | 12.66 | 25 | 14171 | 22951 | 64461585 |
Low turnover osteopathy | 19.17 | 12.66 | 9 | 14187 | 1864 | 64482672 |
Product use issue | 18.93 | 12.66 | 5 | 14191 | 151710 | 64332826 |
Intestinal pseudo-obstruction | 18.60 | 12.66 | 9 | 14187 | 1991 | 64482545 |
Ischaemic stroke | 18.31 | 12.66 | 27 | 14169 | 29008 | 64455528 |
Endometrial hyperplasia | 18.06 | 12.66 | 6 | 14190 | 498 | 64484038 |
Blood calcium increased | 18.04 | 12.66 | 15 | 14181 | 8527 | 64476009 |
Intervertebral disc degeneration | 17.83 | 12.66 | 18 | 14178 | 13102 | 64471434 |
Acute kidney injury | 17.78 | 12.66 | 46 | 14150 | 449194 | 64035342 |
Diverticulum | 17.75 | 12.66 | 18 | 14178 | 13180 | 64471356 |
Infusion related reaction | 17.73 | 12.66 | 7 | 14189 | 164460 | 64320076 |
Myocardial infarction | 17.04 | 12.66 | 77 | 14119 | 165744 | 64318792 |
Uterine leiomyoma | 17.00 | 12.66 | 12 | 14184 | 5357 | 64479179 |
Insulinoma | 16.87 | 12.66 | 4 | 14192 | 95 | 64484441 |
Back pain | 16.65 | 12.66 | 103 | 14093 | 250068 | 64234468 |
Stress fracture | 16.50 | 12.66 | 12 | 14184 | 5612 | 64478924 |
Foot fracture | 16.21 | 12.66 | 20 | 14176 | 18137 | 64466399 |
Atrophic vulvovaginitis | 16.20 | 12.66 | 7 | 14189 | 1194 | 64483342 |
Femoral neck fracture | 15.74 | 12.66 | 14 | 14182 | 8710 | 64475826 |
Retinal haemorrhage | 15.64 | 12.66 | 13 | 14183 | 7385 | 64477151 |
Injection site erythema | 15.25 | 12.66 | 42 | 14154 | 70758 | 64413778 |
Osteomyelitis | 15.07 | 12.66 | 24 | 14172 | 27563 | 64456973 |
Fractured sacrum | 14.82 | 12.66 | 7 | 14189 | 1468 | 64483068 |
Endometrial hypertrophy | 14.75 | 12.66 | 4 | 14192 | 165 | 64484371 |
Neutropenia | 14.38 | 12.66 | 19 | 14177 | 239605 | 64244931 |
Dementia Alzheimer's type | 14.10 | 12.66 | 6 | 14190 | 986 | 64483550 |
Osteoarthritis | 14.07 | 12.66 | 38 | 14158 | 63298 | 64421238 |
Vascular headache | 13.96 | 12.66 | 3 | 14193 | 45 | 64484491 |
Jaw disorder | 13.88 | 12.66 | 10 | 14186 | 4607 | 64479929 |
Gastrooesophageal reflux disease | 13.82 | 12.66 | 45 | 14151 | 83098 | 64401438 |
Breast swelling | 13.78 | 12.66 | 6 | 14190 | 1042 | 64483494 |
Breast cancer recurrent | 13.72 | 12.66 | 8 | 14188 | 2575 | 64481961 |
Osteoporotic fracture | 13.67 | 12.66 | 9 | 14187 | 3589 | 64480947 |
Tibia fracture | 13.64 | 12.66 | 10 | 14186 | 4735 | 64479801 |
Benign vulval neoplasm | 13.55 | 12.66 | 3 | 14193 | 52 | 64484484 |
General physical health deterioration | 13.55 | 12.66 | 15 | 14181 | 204410 | 64280126 |
Erythema multiforme | 13.55 | 12.66 | 17 | 14179 | 15684 | 64468852 |
Multiple organ dysfunction syndrome | 13.31 | 12.66 | 3 | 14193 | 101410 | 64383126 |
Fibrocystic breast disease | 13.29 | 12.66 | 5 | 14191 | 597 | 64483939 |
Rib fracture | 13.25 | 12.66 | 21 | 14175 | 24017 | 64460519 |
Bone disorder | 12.67 | 12.66 | 17 | 14179 | 16742 | 64467794 |
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 | Nuclear hormone receptor | ANTAGONIST | IC50 | 9.40 | WOMBAT-PK | IUPHAR | |||
Estrogen receptor beta | Nuclear hormone receptor | MODULATOR | EC50 | 8 | WOMBAT-PK | CHEMBL | |||
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 | |||||
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 |
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 | 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 | 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 | 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 | 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 | 65862-709 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | Human Prescription Drug Label | 1 | 66993-661 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68071-2412 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 30 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-825 | TABLET | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-2994 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-3046 | TABLET | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene hydrochloride | Human Prescription Drug Label | 1 | 71209-082 | TABLET, COATED | 60 mg | ORAL | ANDA | 28 sections |
Raloxifene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-1460 | TABLET, FILM COATED | 60 mg | ORAL | ANDA | 29 sections |
Raloxifene Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-1663 | TABLET | 60 mg | ORAL | ANDA | 27 sections |