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Evista, Optruma(raloxifene)
Evista, Optruma (raloxifene) is a small molecule pharmaceutical. Raloxifene was first approved as Evista on 1997-12-09. It is used to treat postmenopausal osteoporosis in the USA. It has been approved in Europe to treat postmenopausal osteoporosis. The pharmaceutical is active against estrogen receptor and estrogen receptor beta. In addition, it is known to target G-protein coupled estrogen receptor 1.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
musculoskeletal diseasesD009140
nutritional and metabolic diseasesD009750
Trade Name
FDA
EMA
Evista (generic drugs available since 2014-03-04)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Raloxifene hydrochloride
Tradename
Company
Number
Date
Products
EVISTAEli LillyN-020815 RX1997-12-09
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
evistaNew Drug Application2021-02-22
raloxifene hydrochlorideANDA2023-04-15
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
postmenopausal osteoporosisEFO_0003854D015663—
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
G: Genito urinary system and sex hormones
— G03: Sex hormones and modulators of the genital system
— G03X: Other sex hormones and modulators of the genital system in atc
— G03XC: Selective estrogen receptor modulators
— G03XC01: Raloxifene
HCPCS
No data
Clinical
Clinical Trials
65 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Postmenopausal osteoporosisD015663EFO_0003854——48113
OsteoporosisD010024EFO_0003882M81.02—26313
SchizophreniaD012559EFO_0000692F20—125—8
Psychotic disordersD011618F20.81—123—6
Healthy volunteers/patients—3——1—4
Metabolic bone diseasesD001851HP_0000938——11—2
Depressive disorderD003866EFO_1002014F32.A———1—1
DepressionD003863F33.9———1—1
ComplianceD003187———1—1
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Breast neoplasmsD001943EFO_0003869C50—12—47
Polycystic ovary syndromeD011085EFO_0000660E28.2——1—12
Alzheimer diseaseD000544EFO_0000249F03—21——2
Endometrial hyperplasiaD004714N85.0——1——1
CognitionD003071EFO_0003925——1——1
AgingD000375GO_0007568R41.81——1——1
Cardiovascular diseasesD002318EFO_0000319I98——1——1
Covid-19D000086382U07.1—11——1
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
PostmenopauseD017698—1——12
AdenocarcinomaD000230—1——12
Hot flashesD019584—1———1
Endometrial neoplasmsD016889EFO_0004230—1———1
EndometriosisD004715EFO_0001065N80—1———1
Pelvic painD017699—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Prostatic neoplasmsD011471C611————1
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Rheumatoid arthritisD001172EFO_0000685M06.9————11
Esophageal neoplasmsD004938C15————11
Squamous cell neoplasmsD018307————11
DiarrheaD003967HP_0002014R19.7————11
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameRALOXIFENE
INNraloxifene
Description
Raloxifene is a member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively. It has a role as a bone density conservation agent, an estrogen receptor modulator and an estrogen antagonist. It is a member of phenols, an aromatic ketone, a member of 1-benzothiophenes and a N-oxyethylpiperidine. It is a conjugate base of a raloxifene(1+).
Classification
Small molecule
Drug classantiestrogens of the clomifene and tamoxifen groups
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
O=C(c1ccc(OCCN2CCCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12
Identifiers
PDB1QKN
CAS-ID84449-90-1
RxCUI72143
ChEMBL IDCHEMBL81
ChEBI ID8772
PubChem CID5035
DrugBankDB00481
UNII IDYX9162EO3I (ChemIDplus, GSRS)
Target
Agency Approved
ESR1
ESR1
ESR2
ESR2
Organism
Homo sapiens
Gene name
ESR1
Gene synonyms
ESR, NR3A1
NCBI Gene ID
2099
Protein name
estrogen receptor
Protein synonyms
E2 receptor alpha, ER-alpha, Estradiol receptor, estrogen nuclear receptor alpha, estrogen receptor alpha E1-E2-1-2, estrogen receptor alpha E1-N2-E2-1-2, Nuclear receptor subfamily 3 group A member 1, oestrogen receptor alpha
Uniprot ID
Q9UIS7
Mouse ortholog
Esr1 (13982)
estrogen receptor (Q9QY52)
Alternate
GPER1
GPER1
Organism
Homo sapiens
Gene name
GPER1
Gene synonyms
CEPR, CMKRL2, DRY12, GPER, GPR30
NCBI Gene ID
2852
Protein name
G-protein coupled estrogen receptor 1
Protein synonyms
Chemoattractant receptor-like 2, chemokine receptor-like 2, constitutively expressed peptide-like receptor, FEG-1, Flow-induced endothelial G-protein coupled receptor 1, G protein-coupled estrogen receptor 1, G protein-coupled receptor 30, G-protein coupled receptor 30, GPCR-Br, heptahelix receptor, IL8-related receptor DRY12, LYGPR, Lymphocyte-derived G-protein coupled receptor, Membrane estrogen receptor, mER
Uniprot ID
Q99981
Mouse ortholog
Gper1 (76854)
G-protein coupled estrogen receptor 1 (Q9D392)
Variants
Clinical Variant
No data
Financial
Evista - Eli Lilly
$
€
£
₣
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Tabular view
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 10,692 documents
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Safety
Black-box Warning
Black-box warning for: Evista, Raloxifene hydrochloride
Adverse Events
Top Adverse Reactions
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177,565 adverse events reported
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