raloxifene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives 2351 84449-90-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • raloxifene
  • keoxifene
  • raloxifene hydrochloride
  • evista
  • raloxifene HCl
A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.
  • Molecular weight: 473.59
  • Formula: C28H27NO4S
  • CLOGP: 6.86
  • LIPINSKI: 1
  • HAC: 5
  • HDO: 2
  • TPSA: 70
  • ALOGS: -5.97
  • ROTB: 7
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
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 µM/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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class AAK1,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK16,CDK19,CDK2,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK4,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT3,FLT4,GAK,GRK2,GSK3A,GSK3B,IKBKB,INSR,IRAK1,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MARK1,MARK4,MELK,MET,MINK1,MTOR,NTRK2,NUAK1,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PRKAA1,PRKAA2,PRKCD,PRKCZ,PRKDC,SGK1,SIK2,SIK3,SRC,STK10,STK17A,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,UHMK1,ULK1,ULK2,ZAP70 118
kinase-selectivity-class ACVR2A,ACVR2B,ALK,AURKB,AURKC,AXL,BLK,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK4,CDK7,CDK9,CHEK1,CLK4,CSF1R,CSK,DDR1,DYRK1B,DYRK3,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,INSR,IRAK1,IRAK3,JAK1,JAK2,KDR,KIT,LRRK2,MAP2K6,MAP3K10,MAP3K11,MAP3K2,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK7,MARK4,MELK,MINK1,MTOR,NUAK1,PDGFRB,PDK4,PDPK1,PIK3CA,PIK3CD,PIM3,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK10,STK33,STK4,SYK,TEK,TNIK,TTK,TYRO3,ULK1,ULK2,ZAP70 81
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Dec. 9, 1997 FDA LILLY
Aug. 5, 1998 EMA ELI LILLY NEDERLAND B.V.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Endometrial cancer 270.05 12.17 77 21511 3535 90603324
Breast cancer 264.98 12.17 163 21425 53598 90553261
Deep vein thrombosis 201.31 12.17 170 21418 91450 90515409
Bone density decreased 188.53 12.17 89 21499 17256 90589603
Pulmonary embolism 162.10 12.17 177 21411 130643 90476216
Retinal vein thrombosis 150.03 12.17 33 21555 510 90606349
Femur fracture 132.10 12.17 100 21488 45982 90560877
Fracture 127.04 12.17 74 21514 22002 90584857
Spinal compression fracture 117.89 12.17 62 21526 15116 90591743
Fall 112.69 12.17 309 21279 481501 90125358
Body height decreased 110.78 12.17 55 21533 11894 90594965
Hip fracture 97.49 12.17 73 21515 33004 90573855
Retinal vein occlusion 87.55 12.17 30 21558 2526 90604333
Cerebral infarction 85.83 12.17 62 21526 26534 90580325
Transient ischaemic attack 84.39 12.17 75 21513 43101 90563758
Off label use 75.82 12.17 91 21497 1102161 89504698
Cerebrovascular accident 72.72 12.17 116 21472 123417 90483442
Pelvic fracture 72.01 12.17 45 21543 15174 90591685
Infusion related reaction 71.32 12.17 8 21580 416772 90190087
Breast cancer female 70.39 12.17 44 21544 14842 90592017
Thoracic vertebral fracture 68.55 12.17 31 21557 5443 90601416
Osteonecrosis of jaw 66.81 12.17 63 21525 39040 90567819
Breast cancer in situ 65.81 12.17 22 21566 1718 90605141
Spinal fracture 65.79 12.17 49 21539 21967 90584892
Compression fracture 65.70 12.17 35 21553 8754 90598105
Visual acuity reduced 65.30 12.17 50 21538 23360 90583499
Systemic lupus erythematosus 61.78 12.17 7 21581 361889 90244970
Oestrogen receptor assay positive 61.25 12.17 16 21572 526 90606333
Product use issue 59.94 12.17 5 21583 329914 90276945
Glossodynia 58.12 12.17 5 21583 321774 90285085
Lumbar vertebral fracture 56.59 12.17 30 21558 7428 90599431
Osteonecrosis 54.11 12.17 47 21541 26194 90580665
Low turnover osteopathy 53.18 12.17 24 21564 4194 90602665
Myocardial infarction 52.33 12.17 92 21496 105880 90500979
Hot flush 49.77 12.17 66 21522 59422 90547437
Pericarditis 49.32 12.17 4 21584 270147 90336712
Drug ineffective 49.07 12.17 168 21420 1384130 89222729
Back pain 48.62 12.17 176 21412 316999 90289860
Ovarian cancer 47.92 12.17 26 21562 6741 90600118
Wrist fracture 47.19 12.17 35 21553 15589 90591270
Treatment failure 46.87 12.17 8 21580 303920 90302939
Endometrial cancer stage I 45.96 12.17 11 21577 251 90606608
Product complaint 44.76 12.17 32 21556 13468 90593391
Postmenopausal haemorrhage 44.45 12.17 18 21570 2412 90604447
Wrist deformity 42.66 12.17 19 21569 3219 90603640
Lower respiratory tract infection 42.38 12.17 5 21583 250654 90356205
Drug intolerance 41.32 12.17 28 21560 447563 90159296
Overweight 39.81 12.17 22 21566 5912 90600947
Helicobacter infection 39.68 12.17 4 21584 226846 90380013
Toxicity to various agents 39.39 12.17 10 21578 287836 90319023
Uterine cancer 39.00 12.17 21 21567 5364 90601495
Cataract 38.75 12.17 65 21523 72027 90534832
Wound 38.73 12.17 12 21576 302968 90303891
Retinal vascular thrombosis 38.59 12.17 9 21579 183 90606676
Carbuncle 38.31 12.17 14 21574 1422 90605437
Intentional product use issue 37.48 12.17 4 21584 216888 90389971
Blindness unilateral 36.91 12.17 23 21565 7713 90599146
Renal cyst 36.86 12.17 28 21560 12922 90593937
Rheumatoid arthritis 34.38 12.17 22 21566 362592 90244267
Therapeutic product effect decreased 33.71 12.17 12 21576 277559 90329300
Uterine polyp 33.66 12.17 15 21573 2545 90604314
Dyslipidaemia 33.61 12.17 24 21564 10083 90596776
Monoclonal immunoglobulin present 33.00 12.17 14 21574 2110 90604749
Ischaemic stroke 32.77 12.17 33 21555 22133 90584726
Alopecia 32.70 12.17 42 21546 495029 90111830
Hepatic steatosis 32.47 12.17 42 21546 36903 90569956
Retinal haemorrhage 32.30 12.17 19 21569 5745 90601114
Stress fracture 32.26 12.17 22 21566 8589 90598270
Hypothalamo-pituitary disorder 32.21 12.17 14 21574 2238 90604621
Joint swelling 31.92 12.17 44 21544 503256 90103603
Hyperlipidaemia 31.85 12.17 33 21555 22883 90583976
Product use in unapproved indication 31.06 12.17 21 21567 336215 90270644
Lumbar spinal stenosis 30.19 12.17 18 21570 5579 90601280
Multiple fractures 30.18 12.17 22 21566 9540 90597319
Muscle spasms 29.86 12.17 129 21459 251754 90355105
Liver injury 29.85 12.17 3 21585 170564 90436295
Rib fracture 29.65 12.17 34 21554 26401 90580458
Endometrial cancer stage II 29.54 12.17 5 21583 16 90606843
Feeling abnormal 29.24 12.17 97 21491 167138 90439721
General physical health deterioration 29.20 12.17 25 21563 355090 90251769
Thrombosis 29.16 12.17 58 21530 73193 90533666
Oedema peripheral 28.99 12.17 130 21458 257785 90349074
Bone pain 28.27 12.17 52 21536 61931 90544928
Therapeutic product effect incomplete 27.98 12.17 6 21582 193890 90412969
Injection site haemorrhage 27.76 12.17 34 21554 28284 90578575
Purpura 27.54 12.17 25 21563 14753 90592106
Peripheral swelling 27.32 12.17 35 21553 413071 90193788
Swelling 26.19 12.17 37 21551 419021 90187838
Synovitis 26.16 12.17 24 21564 329728 90277131
Intestinal pseudo-obstruction 26.14 12.17 10 21578 1153 90605706
Embolism 25.89 12.17 20 21568 9461 90597398
Infection 25.72 12.17 29 21559 362065 90244794
Diverticulum 25.58 12.17 22 21566 12091 90594768
Atrial fibrillation 24.70 12.17 79 21509 133532 90473327
Femoral neck fracture 24.54 12.17 20 21568 10213 90596646
Dementia Alzheimer's type 23.92 12.17 9 21579 992 90605867
Fibromyalgia 23.25 12.17 10 21578 206259 90400600
Coronary artery disease 23.18 12.17 34 21554 33589 90573270
Osteopenia 23.17 12.17 28 21560 22974 90583885
Intramedullary rod insertion 23.15 12.17 11 21577 2161 90604698
Embolism venous 23.14 12.17 13 21575 3607 90603252
Breast cancer recurrent 22.88 12.17 15 21573 5488 90601371
Fibrocystic breast disease 22.23 12.17 9 21579 1205 90605654
Spinal osteoarthritis 22.10 12.17 25 21563 19123 90587736
Vision blurred 22.04 12.17 67 21521 110226 90496633
Oestrogen receptor assay negative 22.03 12.17 3 21585 0 90606859
Irritable bowel syndrome 21.92 12.17 11 21577 207437 90399422
Fibrosis 21.81 12.17 15 21573 5937 90600922
Uterine leiomyoma 21.47 12.17 19 21569 10845 90596014
Foot fracture 21.45 12.17 29 21559 26577 90580282
Hepatic enzyme increased 21.41 12.17 33 21555 360703 90246156
Humerus fracture 21.13 12.17 18 21570 9767 90597092
Nasopharyngitis 20.75 12.17 41 21547 407063 90199796
Endometrial hyperplasia 20.52 12.17 8 21580 971 90605888
Wheezing 20.50 12.17 16 21572 238064 90368795
Osteomyelitis 20.43 12.17 29 21559 27817 90579042
Pleurisy 20.00 12.17 17 21571 9200 90597659
Bone disorder 19.87 12.17 26 21562 23094 90583765
Fracture nonunion 19.63 12.17 10 21578 2282 90604577
Osteoporosis 19.62 12.17 59 21529 96472 90510387
Intervertebral disc protrusion 19.47 12.17 28 21560 27168 90579691
Colitis ischaemic 19.40 12.17 19 21569 12327 90594532
Colon cancer 19.39 12.17 18 21570 10926 90595933
Fractured sacrum 19.09 12.17 10 21578 2417 90604442
Limb injury 19.09 12.17 30 21558 31478 90575381
Pain 18.69 12.17 150 21438 996191 89610668
Type 2 diabetes mellitus 18.35 12.17 13 21575 203231 90403628
Hypersensitivity 18.23 12.17 52 21536 454625 90152234
Acute myocardial infarction 18.13 12.17 31 21557 34859 90572000
Abdominal discomfort 18.12 12.17 56 21532 477272 90129587
Jaw disorder 18.02 12.17 13 21575 5546 90601313
Nephropathy 17.95 12.17 16 21572 9219 90597640
Blood calcium increased 17.91 12.17 18 21570 12040 90594819
Cholelithiasis 17.88 12.17 39 21549 52467 90554392
Kyphosis 17.39 12.17 10 21578 2898 90603961
Thrombotic stroke 17.08 12.17 6 21582 544 90606315
Mobility decreased 16.81 12.17 21 21567 250713 90356146
Radius fracture 16.75 12.17 11 21577 4033 90602826
Breast swelling 16.48 12.17 8 21580 1646 90605213
Endometrial hypertrophy 16.09 12.17 5 21583 309 90606550
Haemorrhage subcutaneous 15.96 12.17 10 21578 3386 90603473
Lung neoplasm malignant 15.95 12.17 24 21564 24249 90582610
Erythema multiforme 15.89 12.17 17 21571 12229 90594630
Glaucoma 15.79 12.17 22 21566 20733 90586126
Large intestine polyp 15.79 12.17 15 21573 9371 90597488
Intervertebral disc degeneration 15.74 12.17 20 21568 17254 90589605
Gait disturbance 15.66 12.17 111 21477 260385 90346474
Atrophic vulvovaginitis 15.48 12.17 8 21580 1879 90604980
Stomatitis 15.47 12.17 26 21562 274672 90332187
Pathological fracture 15.43 12.17 15 21573 9645 90597214
Discomfort 15.42 12.17 26 21562 274309 90332550
Subacute hepatic failure 15.42 12.17 4 21584 128 90606731
Exostosis of jaw 15.31 12.17 7 21581 1260 90605599
Head injury 15.28 12.17 27 21561 31161 90575698
Gastrointestinal tract adenoma 15.11 12.17 5 21583 378 90606481
Visual field defect 15.10 12.17 13 21575 7153 90599706
Insulinoma 15.10 12.17 4 21584 139 90606720
Ligament sprain 15.08 12.17 18 21570 14581 90592278
Altered state of consciousness 15.07 12.17 27 21561 31505 90575354
Sternal fracture 14.83 12.17 9 21579 2878 90603981
Tibia fracture 14.81 12.17 12 21576 6075 90600784
Renal failure 14.67 12.17 66 21522 130941 90475918
Breast calcifications 14.61 12.17 7 21581 1401 90605458
Temporomandibular joint syndrome 14.43 12.17 10 21578 4007 90602852
Blindness 14.33 12.17 24 21564 26544 90580315
Prescribed overdose 14.12 12.17 3 21585 97622 90509237
Vascular headache 14.05 12.17 3 21585 40 90606819
Ill-defined disorder 14.02 12.17 14 21574 184877 90421982
Carotid artery stenosis 14.02 12.17 11 21577 5323 90601536
Dysstasia 14.01 12.17 23 21565 25029 90581830
Wound infection 13.97 12.17 4 21584 106398 90500461
Sarcoma uterus 13.91 12.17 3 21585 42 90606817
Vitreous detachment 13.75 12.17 8 21580 2370 90604489
Aortic aneurysm 13.66 12.17 10 21578 4365 90602494
Condition aggravated 13.40 12.17 85 21503 595460 90011399
Fracture delayed union 13.36 12.17 8 21580 2498 90604361
Chronic obstructive pulmonary disease 13.05 12.17 43 21545 73786 90533073
Osteoporotic fracture 12.95 12.17 10 21578 4726 90602133
Benign vulval neoplasm 12.73 12.17 3 21585 64 90606795
Blister 12.71 12.17 26 21562 254972 90351887
Psoriatic arthropathy 12.50 12.17 22 21566 228313 90378546
Pulmonary infarction 12.31 12.17 8 21580 2884 90603975

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bone density decreased 175.66 13.48 71 15624 15971 110557633
Endometrial cancer 164.11 13.48 43 15652 2433 110571171
Breast cancer 119.18 13.48 72 15623 38470 110535134
Deep vein thrombosis 116.07 13.48 120 15575 139767 110433837
Body height decreased 113.06 13.48 46 15649 10517 110563087
Retinal vein thrombosis 111.74 13.48 25 15670 721 110572883
Spinal compression fracture 106.26 13.48 52 15643 18340 110555264
Femur fracture 93.01 13.48 65 15630 44404 110529200
Thoracic vertebral fracture 81.71 13.48 32 15663 6623 110566981
Pulmonary embolism 79.48 13.48 123 15572 214351 110359253
Fall 77.62 13.48 224 15471 603258 109970346
Oestrogen receptor assay positive 74.85 13.48 16 15679 371 110573233
Fracture 73.27 13.48 45 15650 24743 110548861
Off label use 71.49 13.48 65 15630 1500120 109073484
Hip fracture 70.30 13.48 50 15645 35101 110538503
Breast cancer female 68.30 13.48 34 15661 12434 110561170
Spinal fracture 59.14 13.48 38 15657 22595 110551009
Transient ischaemic attack 58.71 13.48 58 15637 63924 110509680
Lumbar vertebral fracture 56.31 13.48 27 15668 9104 110564500
Pelvic fracture 55.87 13.48 31 15664 14123 110559481
Retinal vein occlusion 55.37 13.48 21 15674 3986 110569618
Endometrial cancer stage I 54.98 13.48 11 15684 182 110573422
Wrist fracture 49.96 13.48 29 15666 14388 110559216
Visual acuity reduced 49.26 13.48 39 15656 32134 110541470
Cerebrovascular accident 48.56 13.48 90 15605 181194 110392410
Product complaint 48.14 13.48 28 15667 13944 110559660
Compression fracture 46.95 13.48 24 15671 9275 110564329
Carbuncle 45.13 13.48 14 15681 1453 110572151
Wrist deformity 45.10 13.48 17 15678 3172 110570432
Breast cancer in situ 43.52 13.48 13 15682 1188 110572416
Overweight 42.57 13.48 20 15675 6444 110567160
Postmenopausal haemorrhage 41.97 13.48 14 15681 1832 110571772
Toxicity to various agents 41.09 13.48 9 15686 480546 110093058
Hot flush 39.83 13.48 48 15647 65988 110507616
Osteonecrosis of jaw 39.43 13.48 41 15654 47976 110525628
Monoclonal immunoglobulin present 37.60 13.48 14 15681 2526 110571078
Back pain 36.77 13.48 126 15569 370870 110202734
Ovarian cancer 36.54 13.48 16 15679 4380 110569224
Multiple fractures 36.43 13.48 20 15675 8920 110564684
Hypothalamo-pituitary disorder 36.05 13.48 14 15681 2832 110570772
Infusion related reaction 34.98 13.48 6 15689 381156 110192448
Injection site haemorrhage 34.18 13.48 32 15663 32996 110540608
Endometrial cancer stage II 34.16 13.48 5 15690 9 110573595
Osteonecrosis 33.60 13.48 32 15663 33709 110539895
Uterine polyp 33.32 13.48 12 15683 1971 110571633
Bone pain 32.38 13.48 43 15652 65090 110508514
Cerebral infarction 31.78 13.48 38 15657 51800 110521804
Feeling abnormal 31.21 13.48 75 15620 180636 110392968
Uterine cancer 30.88 13.48 14 15681 4160 110569444
Myocardial infarction 30.29 13.48 77 15618 192006 110381598
Drug ineffective 30.03 13.48 113 15582 1520427 109053177
Renal cyst 29.92 13.48 23 15672 18149 110555455
Product use issue 28.39 13.48 5 15690 311690 110261914
Ischaemic stroke 28.22 13.48 32 15663 41231 110532373
Osteoporosis 26.82 13.48 46 15649 87106 110486498
Dyslipidaemia 25.83 13.48 20 15675 15945 110557659
Fibrosis 25.49 13.48 15 15680 7627 110565977
Muscle spasms 25.40 13.48 92 15603 278065 110295539
Intentional product use issue 24.83 13.48 3 15692 247903 110325701
Oedema peripheral 24.55 13.48 102 15593 328558 110245046
Treatment failure 24.07 13.48 5 15690 277229 110296375
Drug intolerance 22.55 13.48 15 15680 406497 110167107
Low turnover osteopathy 22.30 13.48 9 15686 2013 110571591
Purpura 22.16 13.48 22 15673 24366 110549238
Blindness unilateral 22.09 13.48 15 15680 9771 110563833
Diverticulum 22.02 13.48 18 15677 15508 110558096
Cataract 21.94 13.48 40 15655 79445 110494159
Product use in unapproved indication 21.63 13.48 19 15676 447358 110126246
Hepatic steatosis 20.91 13.48 30 15665 48801 110524803
Injection site erythema 20.64 13.48 43 15652 94133 110479471
Gait disturbance 20.50 13.48 86 15609 278122 110295482
Nephropathy 19.92 13.48 16 15679 13451 110560153
Hyperlipidaemia 19.90 13.48 25 15670 35823 110537781
Lower respiratory tract infection 19.87 13.48 5 15690 243101 110330503
Intervertebral disc degeneration 19.63 13.48 18 15677 18067 110555537
Foot fracture 19.52 13.48 21 15674 25525 110548079
Osteomyelitis 19.49 13.48 25 15670 36575 110537029
Systemic lupus erythematosus 19.36 13.48 6 15689 254332 110319272
Pericarditis 18.92 13.48 4 15691 219110 110354494
Fractured sacrum 18.86 13.48 8 15687 2028 110571576
Endometrial hyperplasia 18.69 13.48 6 15689 696 110572908
Stress fracture 18.55 13.48 12 15683 7209 110566395
Atrophic vulvovaginitis 18.13 13.48 7 15688 1393 110572211
Intestinal pseudo-obstruction 17.93 13.48 9 15686 3347 110570257
Retinal haemorrhage 17.81 13.48 13 15682 9488 110564116
Uterine leiomyoma 17.71 13.48 12 15683 7788 110565816
Limb injury 17.41 13.48 24 15671 37612 110535992
Glossodynia 17.33 13.48 5 15690 221999 110351605
General physical health deterioration 17.24 13.48 21 15674 425274 110148330
Bone disorder 17.22 13.48 18 15677 21174 110552430
Dementia Alzheimer's type 17.04 13.48 6 15689 923 110572681
Jaw disorder 16.78 13.48 10 15685 5202 110568402
Femoral neck fracture 16.64 13.48 14 15681 12553 110561051
Vision blurred 16.60 13.48 48 15647 128974 110444630
Helicobacter infection 16.37 13.48 3 15692 181874 110391730
Rib fracture 16.33 13.48 22 15673 33748 110539856
Endometrial hypertrophy 16.20 13.48 4 15691 178 110573426
Blood calcium increased 15.89 13.48 16 15679 18024 110555580
Therapeutic product effect incomplete 15.79 13.48 6 15689 223799 110349805
Insulinoma 15.74 13.48 4 15691 200 110573404
Erythema multiforme 15.52 13.48 17 15678 21080 110552524
Foot deformity 15.46 13.48 26 15669 48454 110525150
Wound 15.38 13.48 7 15688 234430 110339174
Vascular headache 15.33 13.48 3 15692 44 110573560
Dysstasia 15.21 13.48 21 15674 32965 110540639
Death 15.01 13.48 50 15645 698819 109874785
Completed suicide 14.75 13.48 8 15687 242373 110331231
Fibrocystic breast disease 14.65 13.48 5 15690 701 110572903
Tibia fracture 14.64 13.48 10 15685 6575 110567029
Colitis ischaemic 14.29 13.48 15 15680 17735 110555869
Benign vulval neoplasm 14.27 13.48 3 15692 64 110573540
Fracture nonunion 14.12 13.48 6 15689 1528 110572076
Thrombotic stroke 14.11 13.48 5 15690 783 110572821
Osteoporotic fracture 14.04 13.48 9 15686 5328 110568276
Breast cancer recurrent 14.03 13.48 8 15687 3838 110569766
Temporomandibular joint syndrome 13.98 13.48 8 15687 3861 110569743
Breast swelling 13.86 13.48 6 15689 1598 110572006
Haemorrhage subcutaneous 13.73 13.48 9 15686 5530 110568074
Therapeutic product effect decreased 13.56 13.48 9 15686 244307 110329297

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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
FDA EPC N0000175826 Estrogen Agonist/Antagonist
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50646 bone density conservation agent
CHEBI has role CHEBI:50739 estrogen receptor modulator
CHEBI has role CHEBI:50837 estrogen antagonist
MeSH PA D004965 Estrogen Antagonists
MeSH PA D006727 Hormone Antagonists
MeSH PA D020845 Selective Estrogen Receptor Modulators
MeSH PA D050071 Bone Density Conservation Agents

Related Drugs by ATC class:

G03XC Selective estrogen receptor modulators 4 drugs
bazedoxifenelasofoxifeneormeloxifeneospemifene

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.13 acidic
pKa2 8.6 acidic
pKa3 9.15 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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
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 Surface antigen 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
Replicase polyprotein 1ab Enzyme IC50 5.25 CHEMBL

External reference:

IDSource
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
YX9162EO3I INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Evista HUMAN PRESCRIPTION DRUG LABEL 1 0002-4184 TABLET 60 mg ORAL NDA 32 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 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 50090-5458 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 50090-7073 TABLET, FILM COATED 60 mg ORAL ANDA 28 sections
Raloxifene Hydrochloride Human Prescription Drug Label 1 50090-7073 TABLET, FILM 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 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 63629-8209 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 27 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 68071-2412 TABLET, FILM COATED 60 mg ORAL ANDA 30 sections
raloxifene hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68462-393 TABLET, FILM COATED 60 mg ORAL ANDA 29 sections
Raloxifene Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 69097-825 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
Raloxifene Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71335-1715 TABLET, FILM COATED 60 mg ORAL ANDA 28 sections
Raloxifene Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71335-2059 TABLET, FILM COATED 60 mg ORAL ANDA 28 sections
Raloxifene hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71610-053 TABLET, FILM COATED 60 mg ORAL ANDA 30 sections
Raloxifene Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71610-504 TABLET, FILM COATED 60 mg ORAL ANDA 30 sections
Raloxifene Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 71610-524 TABLET 60 mg ORAL ANDA 28 sections
Raloxifene hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 72162-2418 TABLET, COATED 60 mg ORAL ANDA 28 sections