anastrozole Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
aromatase inhibitors, imidazole-triazole derivatives 210 120511-73-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • anastrozole
  • anastrazole
  • anastrol
  • arimidex
A nitrile and triazole derivative that acts as a selective nonsteroidal aromatase inhibitor. It is used in the treatment of ESTROGEN NUCLEAR RECEPTOR-positive breast cancer in postmenopausal women.
  • Molecular weight: 293.37
  • Formula: C17H19N5
  • CLOGP: 1.48
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 78.29
  • ALOGS: -3.65
  • ROTB: 4

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.50 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.06 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Dec. 27, 1995 FDA ASTRAZENECA

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
Metastases to bone 923.97 11.41 402 42385 18926 53287353
Malignant neoplasm progression 692.72 11.41 523 42264 71018 53235261
Metastases to liver 504.64 11.41 275 42512 21221 53285058
Metastases to lung 400.29 11.41 193 42594 11511 53294768
Breast cancer 376.74 11.41 314 42473 49044 53257235
Breast cancer metastatic 376.16 11.41 202 42585 15126 53291153
Osteonecrosis 320.00 11.41 222 42565 26353 53279926
Hot flush 273.84 11.41 257 42530 46903 53259376
Breast cancer recurrent 267.41 11.41 107 42680 4058 53302221
Metastases to lymph nodes 210.84 11.41 108 42679 7332 53298947
Bone pain 207.80 11.41 229 42558 50493 53255786
Drug ineffective 196.42 11.41 221 42566 817024 52489255
Disease progression 196.40 11.41 318 42469 101602 53204677
Neoplasm progression 160.23 11.41 156 42631 29763 53276516
Osteonecrosis of jaw 152.89 11.41 166 42621 35980 53270299
Tumour marker increased 149.85 11.41 70 42717 3883 53302396
Arthralgia 139.53 11.41 708 42079 439075 52867204
Neutropenia 138.39 11.41 357 42430 158828 53147451
Rheumatoid arthritis 137.29 11.41 41 42746 314490 52991789
Tooth extraction 131.08 11.41 90 42697 10492 53295787
Ejection fraction decreased 116.72 11.41 109 42678 19739 53286540
Pseudocirrhosis 114.01 11.41 36 42751 671 53305608
Maternal exposure during pregnancy 110.81 11.41 3 42784 155636 53150643
Metastases to spine 104.29 11.41 50 42737 2940 53303339
Metastasis 98.57 11.41 56 42731 4675 53301604
Completed suicide 93.69 11.41 4 42783 138197 53168082
Trigger finger 88.99 11.41 49 42738 3850 53302429
Bone lesion 81.59 11.41 53 42734 5633 53300646
Carbohydrate antigen 15-3 increased 81.21 11.41 32 42755 1164 53305115
Bone disorder 80.55 11.41 91 42696 20592 53285687
White blood cell count decreased 79.59 11.41 250 42537 124225 53182054
Osteopenia 78.82 11.41 85 42702 18270 53288009
Systemic lupus erythematosus 72.43 11.41 8 42779 125406 53180873
Infusion related reaction 70.41 11.41 19 42768 155938 53150341
Therapeutic product effect decreased 70.14 11.41 9 42778 125646 53180633
Osteolysis 69.12 11.41 37 42750 2748 53303531
Neuropathy peripheral 65.72 11.41 207 42580 102980 53203299
Breast cancer female 64.03 11.41 49 42738 6755 53299524
Acute myeloid leukaemia 63.40 11.41 73 42714 16859 53289420
Organising pneumonia 61.54 11.41 43 42744 5153 53301126
Treatment failure 61.14 11.41 14 42773 128389 53177890
Synovitis 59.56 11.41 8 42779 107885 53198394
Retinal toxicity 57.46 11.41 25 42762 1172 53305107
Metastases to pleura 54.77 11.41 25 42762 1314 53304965
Myalgia 54.66 11.41 232 42555 133259 53173020
Tonsillar disorder 54.34 11.41 23 42764 1007 53305272
Lymphoedema 52.91 11.41 51 42736 9602 53296677
Malignant pleural effusion 52.33 11.41 30 42757 2547 53303732
Metastases to central nervous system 52.05 11.41 56 42731 12001 53294278
Pain in jaw 51.61 11.41 106 42681 40563 53265716
Drug hypersensitivity 50.87 11.41 84 42703 265158 53041121
Sequestrectomy 50.39 11.41 22 42765 1040 53305239
Invasive ductal breast carcinoma 49.71 11.41 42 42745 6665 53299614
Debridement 49.18 11.41 24 42763 1467 53304812
Nasal disorder 48.67 11.41 28 42759 2393 53303886
Ascites 48.59 11.41 102 42685 39633 53266646
Toxicity to various agents 48.51 11.41 63 42724 219535 53086744
Lacrimation increased 47.54 11.41 65 42722 17838 53288441
Metastases to the mediastinum 46.94 11.41 17 42770 488 53305791
Osteomyelitis 45.75 11.41 75 42712 24160 53282119
Joint swelling 45.27 11.41 74 42713 234564 53071715
Endometrial hyperplasia 42.94 11.41 18 42769 769 53305510
Drug abuse 40.99 11.41 3 42784 65523 53240756
Fatigue 40.85 11.41 816 41971 729690 52576589
Bone sequestrum 40.72 11.41 22 42765 1664 53304615
Hypotension 39.56 11.41 91 42696 253985 53052294
PIK3CA-activated mutation 39.35 11.41 17 42770 783 53305496
Oestradiol increased 39.28 11.41 10 42777 81 53306198
Peritoneal disorder 38.26 11.41 15 42772 538 53305741
Pleural neoplasm 38.14 11.41 12 42775 221 53306058
Hair growth abnormal 37.70 11.41 25 42762 2750 53303529
Hypersensitivity 37.39 11.41 70 42717 210595 53095684
Glossodynia 37.06 11.41 17 42770 100274 53206005
Intentional overdose 37.04 11.41 5 42782 67200 53239079
Metastases to pelvis 36.47 11.41 13 42774 356 53305923
Metastatic neoplasm 36.24 11.41 28 42759 3914 53302365
Second primary malignancy 35.96 11.41 36 42751 7096 53299183
Vulvovaginal dryness 35.71 11.41 23 42764 2409 53303870
Tendonitis 33.96 11.41 54 42733 16952 53289327
Hypertensive angiopathy 33.84 11.41 9 42778 88 53306191
Oestrogen receptor assay positive 33.79 11.41 13 42774 443 53305836
Carpal tunnel syndrome 33.55 11.41 55 42732 17712 53288567
Pleural effusion 33.22 11.41 150 42637 88429 53217850
Nail disorder 32.94 11.41 40 42747 9765 53296514
Invasive lobular breast carcinoma 32.87 11.41 15 42772 788 53305491
Pathological fracture 32.68 11.41 37 42750 8387 53297892
Pericarditis 30.69 11.41 7 42780 64399 53241880
Abdominal discomfort 30.65 11.41 84 42703 220978 53085301
Joint stiffness 30.56 11.41 72 42715 30211 53276068
Uterine polyp 30.53 11.41 19 42768 1874 53304405
Pancreatic neoplasm 30.38 11.41 14 42773 752 53305527
Off label use 29.93 11.41 239 42548 471973 52834306
Product substitution issue 29.81 11.41 49 42738 15817 53290462
Pneumonia 29.69 11.41 198 42589 406971 52899308
Palmar-plantar erythrodysaesthesia syndrome 29.42 11.41 58 42729 21548 53284731
Musculoskeletal chest pain 29.38 11.41 55 42732 19667 53286612
Acute phase reaction 29.22 11.41 10 42777 242 53306037
Bone density decreased 29.12 11.41 40 42747 11024 53295255
Injection site erythema 28.68 11.41 13 42774 77236 53229043
Metastases to soft tissue 28.59 11.41 9 42778 166 53306113
Chronic inflammatory demyelinating polyradiculoneuropathy 28.18 11.41 11 42776 390 53305889
Dental care 27.97 11.41 15 42772 1118 53305161
Gingivitis 27.49 11.41 33 42754 7962 53298317
Dry skin 27.47 11.41 90 42697 45670 53260609
Wound 27.45 11.41 20 42767 91537 53214742
Leukopenia 27.24 11.41 124 42663 73339 53232940
HER2 negative breast cancer 27.18 11.41 5 42782 5 53306274
Metastases to skin 27.17 11.41 16 42771 1428 53304851
Portal hypertension 26.92 11.41 23 42764 3705 53302574
Human epidermal growth factor receptor negative 26.71 11.41 5 42782 6 53306273
Metastases to peritoneum 26.69 11.41 21 42766 3014 53303265
Metastases to thorax 26.41 11.41 9 42778 215 53306064
Progesterone receptor assay positive 26.35 11.41 10 42777 328 53305951
Metastases to chest wall 25.79 11.41 11 42776 491 53305788
Sinusitis 25.71 11.41 61 42726 168503 53137776
Injection site pain 25.56 11.41 32 42755 113359 53192920
Injection site reaction 25.53 11.41 5 42782 51161 53255118
Fibrous histiocytoma 25.46 11.41 11 42776 507 53305772
Superinfection 25.23 11.41 18 42769 2229 53304050
Tooth loss 25.13 11.41 29 42758 6710 53299569
Breast pain 25.13 11.41 32 42755 8197 53298082
Metastases to retroperitoneum 25.00 11.41 8 42779 156 53306123
Radiation skin injury 24.88 11.41 13 42774 919 53305360
Tooth disorder 24.26 11.41 59 42728 25253 53281026
Intentional product use issue 24.23 11.41 14 42773 72480 53233799
Dysgeusia 23.61 11.41 82 42705 42849 53263430
Recurrent cancer 23.60 11.41 16 42771 1826 53304453
Recall phenomenon 23.60 11.41 11 42776 607 53305672
Exposed bone in jaw 23.36 11.41 20 42767 3230 53303049
Interstitial lung disease 23.28 11.41 101 42686 58521 53247758
Cutaneous vasculitis 23.21 11.41 23 42764 4478 53301801
Injection site pruritus 23.14 11.41 3 42784 41586 53264693
Vitreous detachment 23.13 11.41 16 42771 1887 53304392
Thrombocytopenia 23.01 11.41 190 42597 138537 53167742
Fracture 22.89 11.41 47 42740 17972 53288307
Overdose 22.66 11.41 32 42755 107704 53198575
Periodontal disease 22.58 11.41 15 42772 1655 53304624
Hormone receptor positive breast cancer 22.57 11.41 10 42777 490 53305789
Polyneuropathy 22.38 11.41 39 42748 13194 53293085
Tumour marker decreased 22.35 11.41 6 42781 61 53306218
Antisynthetase syndrome 21.68 11.41 6 42781 69 53306210
Osteoporosis 21.57 11.41 84 42703 46376 53259903
Psoriasis 21.32 11.41 23 42764 87066 53219213
Osteosclerosis 20.87 11.41 20 42767 3738 53302541
Retinal detachment 20.81 11.41 24 42763 5551 53300728
Hepatic lesion 20.65 11.41 21 42766 4216 53302063
Vertebral column mass 20.63 11.41 7 42780 165 53306114
Jaw operation 20.61 11.41 11 42776 812 53305467
Therapeutic product effect incomplete 20.58 11.41 26 42761 91758 53214521
Henoch-Schonlein purpura 20.11 11.41 12 42775 1098 53305181
Condition aggravated 19.90 11.41 148 42639 296986 53009293
Haemorrhoids 19.90 11.41 48 42739 20441 53285838
Cardiomyopathy 19.88 11.41 43 42744 17045 53289234
Anaphylactic reaction 19.87 11.41 11 42776 58315 53247964
Suicide attempt 19.77 11.41 11 42776 58157 53248122
Neoplasm malignant 19.74 11.41 55 42732 25546 53280733
Psoriatic arthropathy 19.70 11.41 7 42780 48183 53258096
Vascular purpura 19.62 11.41 13 42774 1428 53304851
Intraductal proliferative breast lesion 19.59 11.41 17 42770 2797 53303482
Neoplasm recurrence 19.50 11.41 16 42771 2438 53303841
Ischaemic stroke 19.49 11.41 44 42743 17949 53288330
Transient acantholytic dermatosis 19.48 11.41 5 42782 42 53306237
Papilloedema 19.06 11.41 19 42768 3724 53302555
Blood copper increased 18.98 11.41 4 42783 12 53306267
Loss of personal independence in daily activities 18.75 11.41 17 42770 69798 53236481
Carbohydrate antigen 27.29 increased 18.70 11.41 5 42782 50 53306229
Bone debridement 18.65 11.41 8 42779 362 53305917
HER2 positive breast cancer 18.61 11.41 8 42779 364 53305915
Cystoid macular oedema 18.48 11.41 13 42774 1574 53304705
Mouth swelling 18.47 11.41 20 42767 4315 53301964
Irritable bowel syndrome 18.42 11.41 6 42781 43626 53262653
Pyrexia 18.37 11.41 221 42566 402972 52903307
Jaw disorder 18.03 11.41 22 42765 5396 53300883
Borrelia infection 17.98 11.41 6 42781 134 53306145
Arthropathy 17.95 11.41 56 42731 141397 53164882
Uterine leiomyoma 17.86 11.41 28 42759 8684 53297595
Cholestasis 17.72 11.41 57 42730 28638 53277641
Swelling 17.63 11.41 86 42701 191019 53115260
Peripheral sensory neuropathy 17.55 11.41 25 42762 7123 53299156
Tongue neoplasm malignant stage unspecified 17.54 11.41 10 42777 840 53305439
Autoimmune pancreatitis 17.47 11.41 7 42780 266 53306013
Osteitis 17.45 11.41 17 42770 3242 53303037
Autoimmune hepatitis 17.42 11.41 27 42760 8291 53297988
Cardio-respiratory arrest 17.40 11.41 13 42774 58745 53247534
Hair colour changes 17.33 11.41 16 42771 2853 53303426
Alopecia 17.24 11.41 274 42513 234309 53071970
Endometrial hypertrophy 17.23 11.41 7 42780 276 53306003
Paraesthesia 17.21 11.41 167 42620 127348 53178931
Product use issue 17.20 11.41 56 42731 139528 53166751
Gingival swelling 17.12 11.41 19 42768 4213 53302066
Pustule 17.03 11.41 11 42776 1157 53305122
Excessive eye blinking 17.02 11.41 10 42777 889 53305390
Blood alkaline phosphatase increased 16.99 11.41 72 42715 41290 53264989
Bone marrow failure 16.98 11.41 58 42729 30057 53276222
Vitreous adhesions 16.90 11.41 4 42783 23 53306256
Wrong technique in product usage process 16.87 11.41 14 42773 60018 53246261
Heart rate increased 16.76 11.41 25 42762 82290 53223989
Atrial enlargement 16.61 11.41 7 42780 303 53305976
Acute promyelocytic leukaemia 16.54 11.41 10 42777 937 53305342
Hair texture abnormal 16.47 11.41 18 42769 3924 53302355
Metastases to abdominal wall 16.37 11.41 5 42782 83 53306196
Neuroectodermal neoplasm 16.31 11.41 3 42784 3 53306276
Injection site bruising 16.21 11.41 5 42782 37641 53268638
Gene mutation 16.09 11.41 11 42776 1272 53305007
Visual acuity reduced 16.07 11.41 47 42740 22438 53283841
Multiple sclerosis relapse 15.96 11.41 8 42779 44845 53261434
Tremor 15.80 11.41 50 42737 125686 53180593
Pain 15.73 11.41 356 42431 588042 52718237
Septic shock 15.72 11.41 16 42771 62213 53244066
Breast mass 15.69 11.41 23 42764 6728 53299551
Acquired gene mutation 15.66 11.41 9 42778 768 53305511
Stomatitis 15.50 11.41 133 42654 98025 53208254
Oroantral fistula 15.50 11.41 6 42781 208 53306071
Meningioma 15.48 11.41 17 42770 3727 53302552
Actinomycosis 15.38 11.41 10 42777 1064 53305215
Toothache 15.33 11.41 40 42747 17874 53288405
Nasopharyngitis 15.26 11.41 91 42696 192204 53114075
Paratracheal lymphadenopathy 15.24 11.41 4 42783 37 53306242
Oestradiol abnormal 15.24 11.41 4 42783 37 53306242
Jaundice 15.05 11.41 56 42731 30257 53276022
Cardiac arrest 15.00 11.41 33 42754 93634 53212645
Blood oestrogen increased 14.97 11.41 5 42782 112 53306167
Hyperkalaemia 14.82 11.41 13 42774 54243 53252036
Oral surgery 14.70 11.41 10 42777 1147 53305132
Asthenia 14.70 11.41 370 42417 343220 52963059
Muscle injury 14.66 11.41 3 42784 29763 53276516
Purulent discharge 14.54 11.41 19 42768 4991 53301288
Hypoaesthesia teeth 14.53 11.41 4 42783 45 53306234
Benign lymph node neoplasm 14.50 11.41 3 42784 8 53306271
Drug intolerance 14.40 11.41 101 42686 205392 53100887
Dysaesthesia 14.37 11.41 17 42770 4038 53302241
Gamma-glutamyltransferase increased 14.24 11.41 59 42728 33496 53272783
Disease recurrence 14.22 11.41 43 42744 20903 53285376
Carcinoembryonic antigen increased 14.18 11.41 11 42776 1546 53304733
Gastrointestinal disorder 14.17 11.41 32 42755 89972 53216307
Folliculitis 14.04 11.41 4 42783 31705 53274574
Malignant neoplasm of choroid 14.00 11.41 3 42784 10 53306269
Abdominal wall cyst 14.00 11.41 3 42784 10 53306269
Vaginal discharge 13.95 11.41 20 42767 5733 53300546
Dental caries 13.90 11.41 28 42759 10564 53295715
Nail avulsion 13.86 11.41 5 42782 142 53306137
Flushing 13.84 11.41 22 42765 70578 53235701
Hypercholesterolaemia 13.82 11.41 31 42756 12595 53293684
Atypical femur fracture 13.70 11.41 19 42768 5282 53300997
Romberg test positive 13.66 11.41 5 42782 148 53306131
Peripheral swelling 13.62 11.41 103 42684 206005 53100274
Tachycardia 13.61 11.41 43 42744 108169 53198110
Mucosal inflammation 13.53 11.41 69 42718 42715 53263564
Postoperative wound complication 13.49 11.41 9 42778 1000 53305279
Discomfort 13.42 11.41 36 42751 95436 53210843
Radiation pneumonitis 13.38 11.41 10 42777 1330 53304949
Metastases to heart 13.35 11.41 4 42783 62 53306217
Metastases to adrenals 13.28 11.41 8 42779 745 53305534
Bacteriuria 13.22 11.41 8 42779 751 53305528
Chronic hepatic failure 13.21 11.41 7 42780 509 53305770
Urticaria 13.20 11.41 60 42727 135825 53170454
Varicophlebitis 13.20 11.41 3 42784 14 53306265
Blood pressure fluctuation 13.12 11.41 6 42781 35464 53270815
Renal vein thrombosis 13.10 11.41 6 42781 318 53305961
Hyperthyroidism 13.10 11.41 31 42756 13042 53293237
Nail infection 13.08 11.41 12 42775 2122 53304157
Erysipelas 12.98 11.41 22 42765 7279 53299000
Hiccups 12.94 11.41 11 42776 1759 53304520
Left ventricular dysfunction 12.76 11.41 28 42759 11209 53295070
Agitation 12.74 11.41 17 42770 58609 53247670
Breast haemorrhage 12.56 11.41 5 42782 187 53306092
Asthma 12.55 11.41 45 42742 108927 53197352
Breast cancer in situ 12.47 11.41 10 42777 1475 53304804
Acquired porokeratosis 12.43 11.41 3 42784 19 53306260
Hyperparathyroidism primary 12.37 11.41 6 42781 362 53305917
Bronchitis 12.37 11.41 47 42740 111852 53194427
Dyshidrotic eczema 12.36 11.41 7 42780 581 53305698
Chronic hepatitis 12.18 11.41 8 42779 866 53305413
Squamous cell breast carcinoma 12.17 11.41 3 42784 21 53306258
Pelvic mass 12.13 11.41 9 42778 1184 53305095
Retinopathy 12.03 11.41 13 42774 2799 53303480
Subacute cutaneous lupus erythematosus 12.02 11.41 12 42775 2356 53303923
Acute kidney injury 11.98 11.41 138 42649 253730 53052549
Menopause 11.93 11.41 12 42775 2378 53303901
Incorrect dose administered 11.93 11.41 14 42773 51031 53255248
Respiratory failure 11.91 11.41 41 42746 100471 53205808
Respiratory arrest 11.90 11.41 6 42781 33534 53272745
Endometrial stromal sarcoma 11.82 11.41 3 42784 24 53306255
Loose tooth 11.80 11.41 14 42773 3337 53302942
Respiratory tract infection 11.71 11.41 6 42781 33218 53273061
Metabolic acidosis 11.68 11.41 10 42777 42232 53264047
Cardiotoxicity 11.68 11.41 21 42766 7278 53299001
Atrophic vulvovaginitis 11.66 11.41 10 42777 1619 53304660
Keratopathy 11.63 11.41 6 42781 413 53305866
Gingival ulceration 11.62 11.41 8 42779 936 53305343
Excessive granulation tissue 11.60 11.41 8 42779 938 53305341
Blister 11.60 11.41 29 42758 78724 53227555
Drug withdrawal syndrome 11.57 11.41 4 42783 28018 53278261
Intentional self-injury 11.55 11.41 3 42784 25281 53280998
Periodontitis 11.54 11.41 14 42773 3415 53302864
Hepatic enzyme increased 11.51 11.41 57 42730 126138 53180141
Somnolence 11.48 11.41 83 42704 167651 53138628
Glomerulonephritis 11.44 11.41 10 42777 1661 53304618
Red blood cell count decreased 11.42 11.41 58 42729 35845 53270434

FDA Adverse Event Reporting System (Male)

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
Growth retardation 91.87 27.75 20 1387 1719 32510400
Mesenteric vein thrombosis 56.40 27.75 11 1396 547 32511572
Secondary hypogonadism 49.71 27.75 9 1398 298 32511821
Metastases to bone 44.80 27.75 17 1390 10693 32501426
Performance enhancing product use 44.47 27.75 7 1400 97 32512022
Breast cancer recurrent 44.45 27.75 6 1401 25 32512094
Haematocrit increased 43.80 27.75 11 1396 1752 32510367
Off label use 43.11 27.75 59 1348 306261 32205858
Spondylolisthesis 41.02 27.75 9 1398 799 32511320
Glucose tolerance decreased 38.54 27.75 6 1401 77 32512042
Blood testosterone increased 38.51 27.75 9 1398 1060 32511059
Autoimmune thyroiditis 38.36 27.75 9 1398 1078 32511041
Product use issue 37.29 27.75 25 1382 52752 32459367
Portal vein thrombosis 31.45 27.75 10 1397 3725 32508394
Osteonecrosis of jaw 29.33 27.75 15 1392 19151 32492968
Insulin-like growth factor increased 28.15 27.75 7 1400 1069 32511050

Pharmacologic Action:

SourceCodeDescription
ATC L02BG03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Aromatase inhibitors
FDA MoA N0000175080 Aromatase Inhibitors
FDA EPC N0000175563 Aromatase Inhibitor
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:50790 aromatase inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
MeSH PA D047072 Aromatase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D004965 Estrogen Antagonists
MeSH PA D006727 Hormone Antagonists
MeSH PA D065088 Steroid Synthesis Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hormone receptor positive malignant neoplasm of breast indication 417181009
Malignant tumor of ovary off-label use 363443007 DOID:2394
Hypercholesterolemia contraindication 13644009
Pregnancy, function contraindication 289908002
Osteopenia contraindication 312894000
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.56 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
Aromatase Enzyme INHIBITOR IC50 6.22 WOMBAT-PK CHEMBL

External reference:

IDSource
4020948 VUID
N0000148427 NUI
D00960 KEGG_DRUG
262485 RXNORM
C0290883 UMLSCUI
CHEBI:2704 CHEBI
CHEMBL1399 ChEMBL_ID
DB01217 DRUGBANK_ID
D000077384 MESH_DESCRIPTOR_UI
2187 PUBCHEM_CID
5137 IUPHAR_LIGAND_ID
7274 INN_ID
2Z07MYW1AZ UNII
173198 MMSL
4200 MMSL
5599 MMSL
d03873 MMSL
005094 NDDF
108774000 SNOMEDCT_US
386910003 SNOMEDCT_US
4020948 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 0093-7536 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
ARIMIDEX HUMAN PRESCRIPTION DRUG LABEL 1 0310-0201 TABLET 1 mg ORAL NDA 28 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 0781-5356 TABLET, FILM COATED 1 mg ORAL ANDA 29 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 0904-6195 TABLET 1 mg ORAL ANDA 26 sections
Anastrozole Human Prescription Drug Label 1 16571-421 TABLET 1 mg ORAL ANDA 29 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 16729-035 TABLET 1 mg ORAL ANDA 26 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 21695-990 TABLET 1 mg ORAL ANDA 27 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 42254-161 TABLET 1 mg ORAL ANDA 28 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 42291-085 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
ANASTROZOLE HUMAN PRESCRIPTION DRUG LABEL 1 43063-383 TABLET 1 mg ORAL ANDA 31 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 45865-909 TABLET 1 mg ORAL ANDA 27 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 50090-2453 TABLET 1 mg ORAL ANDA 28 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 50090-2453 TABLET 1 mg ORAL ANDA 28 sections
ANASTROZOLE HUMAN PRESCRIPTION DRUG LABEL 1 50090-5002 TABLET 1 mg ORAL ANDA 30 sections
Anastrozole Human Prescription Drug Label 1 50090-5812 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
ANASTROZOLE HUMAN PRESCRIPTION DRUG LABEL 1 50268-075 TABLET 1 mg ORAL ANDA 31 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 51655-638 TABLET 1 mg ORAL ANDA 15 sections
ANASTROZOLE HUMAN PRESCRIPTION DRUG LABEL 1 51991-620 TABLET 1 mg ORAL ANDA 31 sections
ARIMIDEX HUMAN PRESCRIPTION DRUG LABEL 1 54868-5000 TABLET 1 mg ORAL NDA 28 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 54868-6130 TABLET 1 mg ORAL ANDA 27 sections
Testozole HUMAN PRESCRIPTION DRUG LABEL 2 57377-060 PELLET, IMPLANTABLE 4 mg SUBCUTANEOUS unapproved drug other 8 sections
Anastrozole Human Prescription Drug Label 1 59651-236 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60429-286 TABLET, FILM COATED 1 mg ORAL ANDA 27 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60687-112 TABLET, COATED 1 mg ORAL ANDA 28 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60763-376 TABLET 1 mg ORAL ANDA 27 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60763-388 TABLET 1 mg ORAL Export only 27 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 62033-0376 TABLET, COATED 1 mg ORAL Export only 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 62135-490 TABLET 1 mg ORAL ANDA 30 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 62175-710 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
ARIMIDEX HUMAN PRESCRIPTION DRUG LABEL 1 62559-670 TABLET 1 mg ORAL NDA 28 sections