anastrozole indications/contra

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

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • anastrozole
  • anastrazole
  • anastrol
  • arimidex
trade name; aromatase inhibitor; structure given in first source
  • Molecular weight: 293.37
  • Formula: C17H19N5
  • CLOGP: 1.48
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 78.29
  • ALOGS: -3.65
  • ROTB: 4

Drug dosage:

DoseUnitRoute
1 mg O

Approvals:

DateAgencyCompanyOrphan
Dec. 27, 1995 FDA ASTRAZENECA

FDA Adverse Event Reporting System

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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
Arthralgia 900.48 27.52 345 3407 60516 3321591
Hot flush 568.92 27.52 149 3603 7352 3374755
Malignant neoplasm progression 352.57 27.52 126 3626 17667 3364440
Metastases to bone 346.96 27.52 84 3668 2977 3379130
Bone pain 262.61 27.52 87 3665 9674 3372433
Breast cancer 257.56 27.52 82 3670 8035 3374072
Fatigue 233.08 27.52 169 3583 107071 3275036
Metastases to liver 211.75 27.52 60 3692 3936 3378171
Myalgia 209.27 27.52 103 3649 31972 3350135
Breast cancer metastatic 195.80 27.52 48 3704 1785 3380322
Organising pneumonia 185.75 27.52 44 3708 1411 3380696
Pseudocirrhosis 179.61 27.52 27 3725 51 3382056
Carpal tunnel syndrome 164.27 27.52 44 3708 2335 3379772
Trigger finger 163.63 27.52 33 3719 487 3381620
Breast cancer recurrent 162.31 27.52 34 3718 611 3381496
Disease progression 148.31 27.52 82 3670 32177 3349930
Alopecia 144.94 27.52 68 3684 18918 3363189
Pain in extremity 142.80 27.52 93 3659 49119 3332988
Nausea 129.35 27.52 131 3621 129514 3252593
Osteopenia 126.04 27.52 35 3717 2125 3379982
Joint stiffness 123.50 27.52 41 3711 4561 3377546
Acute myeloid leukaemia 122.69 27.52 42 3710 5131 3376976
Headache 116.26 27.52 106 3646 91874 3290233
Depression 114.86 27.52 75 3677 39695 3342412
Metastases to lung 112.61 27.52 33 3719 2431 3379676
Osteoporosis 110.32 27.52 38 3714 4727 3377380
Asthenia 105.80 27.52 87 3665 65578 3316529
Hair growth abnormal 105.23 27.52 24 3728 648 3381459
Arthritis 102.64 27.52 45 3707 10673 3371434
Paraesthesia 102.34 27.52 61 3691 27487 3354620

Pharmacologic Action:

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SourceCodeDescription
ATC L02BG03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Aromatase inhibitors
FDA EPC N0000175563 Aromatase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
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 D006730 Hormones, Hormone Substitutes, and Hormone Antagonists
MeSH PA D065088 Steroid Synthesis Inhibitors

Drug Use (View source of the data)

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

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Aromatase Enzyme INHIBITOR IC50 6.22 WOMBAT-PK CHEMBL

External reference:

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IDSource
5137 IUPHAR_LIGAND_ID
4020948 VUID
N0000148427 NUI
C0290883 UMLSCUI
D00960 KEGG_DRUG
2Z07MYW1AZ UNII
7274 INN_ID
2187 PUBCHEM_CID
4020948 VANDF
N0000007441 NDFRT
N0000148427 NDFRT
173198 MMSL
005094 NDDF
d03873 MMSL
4200 MMSL
84857 RXNORM
108774000 SNOMEDCT_US
386910003 SNOMEDCT_US
CHEMBL1399 ChEMBL_ID
CHEBI:2704 CHEBI
DB01217 DRUGBANK_ID
C090450 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 0054-0164 TABLET 1 mg ORAL ANDA 16 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 0093-7536 TABLET, FILM COATED 1 mg ORAL ANDA 17 sections
ANASTROZOLE HUMAN PRESCRIPTION DRUG LABEL 1 0179-0068 TABLET 1 mg ORAL ANDA 17 sections
ARIMIDEX HUMAN PRESCRIPTION DRUG LABEL 1 0310-0201 TABLET 1 mg ORAL NDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 0781-5356 TABLET, FILM COATED 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 0904-6195 TABLET 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 16571-421 TABLET 1 mg ORAL ANDA 16 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 16729-035 TABLET 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 21695-990 TABLET 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 42254-161 TABLET 1 mg ORAL ANDA 18 sections
ANASTROZOLE HUMAN PRESCRIPTION DRUG LABEL 1 43063-383 TABLET 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 50090-2005 TABLET, FILM COATED 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 50090-2453 TABLET 1 mg ORAL ANDA 17 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 17 sections
ARIMIDEX HUMAN PRESCRIPTION DRUG LABEL 1 54868-5000 TABLET 1 mg ORAL NDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 54868-6130 TABLET 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 55111-647 TABLET, FILM COATED 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60429-286 TABLET, FILM COATED 1 mg ORAL ANDA 16 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60505-2985 TABLET, FILM COATED 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60687-112 TABLET, COATED 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 60763-376 TABLET 1 mg ORAL ANDA 16 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 62033-0376 TABLET, COATED 1 mg ORAL Export only 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 62175-710 TABLET, FILM COATED 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 63187-080 TABLET 1 mg ORAL ANDA 16 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 63323-129 TABLET 1 mg ORAL ANDA 16 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 63629-5269 TABLET 1 mg ORAL ANDA 17 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 63672-0015 TABLET, FILM COATED 1 mg ORAL ANDA 19 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 65841-743 TABLET, COATED 1 mg ORAL ANDA 18 sections
Anastrozole HUMAN PRESCRIPTION DRUG LABEL 1 66336-533 TABLET 1 mg ORAL ANDA 17 sections