Identification

Name
Letrozole
Accession Number
DB01006  (APRD01066)
Type
Small Molecule
Groups
Approved, Investigational
Description

Letrozole (INN, trade name Femara®) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast cancer

Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Letrozole blocks production of estrogens in this way by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of mineralo- or corticosteroids. In contrast, the antiestrogenic action of tamoxifen, the major medical therapy prior to the arrival of aromatase inhibitors, is due to its interfering with the estrogen receptor, rather than inhibiting estrogen production. Letrozole is approved by the United States Food and Drug Administration (FDA) for the treatment of local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status in postmenopausal women. Side effects include signs and symptoms of hypoestrogenism. There is concern that long term use may lead to osteoporosis, which is why prescriptions of Letrozole are often accompanied by prescriptions of osteoporosis-fighting medication such as Fosamax. Letrozole has shown to reduce estrogen levels by 98 percent while raising testosterone levels. The anti-estrogen action of letrozole is preferred by athletes and bodybuilders for use during a steroid cycle to reduce bloating due to excess water retention and prevent the formation of gynecomastia related breast tissue that is a side effect of some anabolic steroids. Usage above 2.5 mg/day is known to potentially temporarily kill sex drive. Above 5mg/day for extended periods may cause kidney problems.

Letrozole has also been shown to delay the fusing of the growth plates in adolescents. This may boost the effectiveness of growth hormone, and thus Letrozole is used to treat adolescents and children with short stature.

Structure
Thumb
Synonyms
  • Letrozol
External IDs
CGS 20267 / CGS-20267
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Accel-letrozole Tablets USPTablet2.5 mgOralAccel Pharma IncNot applicableNot applicableCanada
Ach-letrozoleTablet2.5 mgOralAccord Healthcare Limited2010-05-03Not applicableCanada
Ag-letrozoleTablet2.5 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Auro-letrozoleTablet2.5 mgOralAuro Pharma Inc2013-06-12Not applicableCanada
Bio-letrozoleTablet2.5 mgOralBiomed Pharma2013-02-12Not applicableCanada
Ccp-letrozoleTablet2.5 mgOralCellchem Pharmaceuticals Inc.2017-07-24Not applicableCanada
Co LetrozoleTablet2.5 mgOralCobalt LaboratoriesNot applicableNot applicableCanada
Dom-letrozoleTablet2.5 mgOralDominion PharmacalNot applicableNot applicableCanada
FemaraTablet, film coated2.5 mg/1OralPhysicians Total Care, Inc.2005-02-10Not applicableUs
FemaraTablet, film coated2.5 mg/1OralNovartis1997-07-31Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-letrozoleTablet2.5 mgOralApotex Corporation2012-06-11Not applicableCanada
LetrozoleTablet, film coated2.5 mg/1OralLannett Company, Inc.2014-10-292017-08-02Us
LetrozoleTablet, film coated2.5 mg/1OralArab Pharmaceutical Manufacturing Co. Psc Ltd2016-06-03Not applicableUs
LetrozoleTablet, film coated2.5 mg/1OralAPP Pharmaceuticals, Inc.2011-06-04Not applicableUs
LetrozoleTablet, film coated2.5 mg/1OralKaiser Foundations Hospitals2015-02-05Not applicableUs16729 0034 10 nlmimage10 a140d0a6
LetrozoleTablet, film coated2.5 mg/1OralAv Kare, Inc.2015-01-02Not applicableUs
LetrozoleTablet, film coated2.5 mg/1OralSun Pharmaceutical Industries Limited2015-09-092019-03-31Us62756 0511 83 nlmimage10 bd445ef2
LetrozoleTablet, film coated2.5 mg/1OralDr Reddy's Laboratories2011-06-03Not applicableUs
LetrozoleTablet2.5 mg/1OralWest Ward Pharmaceutical2011-06-032019-01-30Us00054 0269 13 nlmimage10 7c3bbe5d
LetrozoleTablet, film coated2.5 mg/1OralCadila Pharnmaceuticals2011-06-03Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Kisqali Femara Co-packLetrozole + RibociclibKitNovartis2017-05-04Not applicableUs
Kisqali Femara Co-packLetrozole + RibociclibKitNovartis2017-05-04Not applicableUs
Kisqali Femara Co-packLetrozole + RibociclibKitNovartis2017-05-04Not applicableUs
Categories
UNII
7LKK855W8I
CAS number
112809-51-5
Weight
Average: 285.3027
Monoisotopic: 285.101445377
Chemical Formula
C17H11N5
InChI Key
HPJKCIUCZWXJDR-UHFFFAOYSA-N
InChI
InChI=1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H
IUPAC Name
4-[(4-cyanophenyl)(1H-1,2,4-triazol-1-yl)methyl]benzonitrile
SMILES
N#CC1=CC=C(C=C1)C(N1C=NC=N1)C1=CC=C(C=C1)C#N

Pharmacology

Indication

For the extended adjuvant treatment of early breast cancer in postmenopausal women who have received 5 years of adjuvant tamoxifen therapy. Also for first-line treatment of postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer. Also indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.

Structured Indications
Pharmacodynamics

Letrozole is an aromatase inhibitor used in the treatment of breast cancer. Aromatase inhibitors work by inhibiting the action of the enzyme aromatase, which converts androgens into estrogens by a process called aromatization. As breast tissue is stimulated by estrogens, decreasing their production is a way of suppressing recurrence of the breast tumor tissue.

Mechanism of action

Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system; it inhibits the conversion of androgens to estrogens. In adult nontumor- and tumorbearing female animals, letrozole is as effective as ovariectomy in reducing uterine weight, elevating serum Leuteinizing hormone (LH), and causing the regression of estrogen-dependent tumors. In contrast to ovariectomy, treatment with letrozole does not lead to an increase in serum (folicile stimulating hormone (FSH). Letrozole selectively inhibits gonadal steroidogenesis but has no significant effect on adrenal mineralocorticoid or glucocorticoid synthesis.

TargetActionsOrganism
ACytochrome P450 19A1
antagonist
Human
Absorption

Rapidly and completely absorbed. Absorption is not affected by food.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Primarily hepatic via CYP3A4 and CYP2A6. Letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues. It is metabolized slowly to an inactive metabolite whose glucuronide conjugate is excreted renally, representing the major clearance pathway.

Route of elimination
Not Available
Half life

2 days

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Letrozole.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Letrozole.Experimental
AmiodaroneThe metabolism of Letrozole can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Letrozole can be increased when it is combined with Aprepitant.Approved, Investigational
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Letrozole resulting in a loss in efficacy.Approved, Investigational
AtazanavirThe metabolism of Letrozole can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Letrozole can be decreased when combined with Atomoxetine.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Letrozole.Approved, Investigational
BoceprevirThe metabolism of Letrozole can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Letrozole can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Letrozole can be decreased when it is combined with Bosentan.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Letrozole.Approved
CarbamazepineThe metabolism of Letrozole can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Letrozole can be increased when it is combined with Ceritinib.Approved
ClarithromycinThe metabolism of Letrozole can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Letrozole can be decreased when combined with Clemastine.Approved
ClotrimazoleThe metabolism of Letrozole can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Letrozole can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Letrozole can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Letrozole can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Letrozole.Approved, Investigational
CyclosporineThe metabolism of Letrozole can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Letrozole.Experimental
DabrafenibThe serum concentration of Letrozole can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Letrozole can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Letrozole can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Letrozole can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Letrozole can be decreased when combined with Delavirdine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Letrozole.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Letrozole.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Letrozole.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Letrozole.Approved
DihydroergotamineThe metabolism of Letrozole can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Letrozole can be decreased when combined with Diltiazem.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Letrozole.Approved, Investigational
DoxycyclineThe metabolism of Letrozole can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Letrozole can be decreased when combined with Dronedarone.Approved
EnzalutamideThe serum concentration of Letrozole can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Letrozole can be decreased when combined with Erythromycin.Approved, Vet Approved
FluconazoleThe metabolism of Letrozole can be decreased when combined with Fluconazole.Approved
FluvoxamineThe metabolism of Letrozole can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Letrozole can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Letrozole can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Letrozole can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Letrozole can be increased when it is combined with Fusidic Acid.Approved
GitoformateGitoformate may decrease the cardiotoxic activities of Letrozole.Experimental
IdelalisibThe serum concentration of Letrozole can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Letrozole can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Letrozole can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Letrozole can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Letrozole can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Letrozole can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Letrozole can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Letrozole can be decreased when combined with Ketoconazole.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Letrozole.Experimental
LopinavirThe metabolism of Letrozole can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Letrozole can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Letrozole can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Letrozole can be increased when combined with Lumacaftor.Approved
MethadoneThe serum concentration of Methadone can be increased when it is combined with Letrozole.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Letrozole.Experimental
MifepristoneThe serum concentration of Letrozole can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Letrozole can be decreased when it is combined with Mitotane.Approved
NefazodoneThe metabolism of Letrozole can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Letrozole can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Letrozole can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Letrozole can be increased when combined with Nevirapine.Approved
NicotineThe metabolism of Letrozole can be decreased when combined with Nicotine.Approved
NilotinibThe metabolism of Letrozole can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Letrozole can be decreased when combined with Olaparib.Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Letrozole.Experimental, Investigational
OsimertinibThe serum concentration of Letrozole can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Letrozole.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Letrozole.Approved, Vet Approved
PalbociclibThe serum concentration of Letrozole can be increased when it is combined with Palbociclib.Approved
PentobarbitalThe metabolism of Letrozole can be increased when combined with Pentobarbital.Approved, Vet Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Letrozole.Experimental
PhenobarbitalThe metabolism of Letrozole can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Letrozole can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Letrozole can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Letrozole can be increased when combined with Primidone.Approved, Vet Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Letrozole.Experimental
RanolazineThe metabolism of Letrozole can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Letrozole can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Letrozole can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Letrozole can be increased when combined with Rifapentine.Approved
SaquinavirThe metabolism of Letrozole can be decreased when combined with Saquinavir.Approved, Investigational
SildenafilThe metabolism of Letrozole can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Letrozole can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Letrozole can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Letrozole can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Letrozole can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Letrozole can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamoxifenThe serum concentration of Letrozole can be decreased when it is combined with Tamoxifen.Approved
TelaprevirThe metabolism of Letrozole can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Letrozole can be decreased when combined with Telithromycin.Approved
TiclopidineThe metabolism of Letrozole can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Letrozole can be decreased when it is combined with Tocilizumab.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Letrozole.Approved, Investigational
VenlafaxineThe metabolism of Letrozole can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Letrozole can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Letrozole can be decreased when combined with Voriconazole.Approved, Investigational
ZiprasidoneThe metabolism of Letrozole can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take without regard to meals. Food slows absorption without decreasing the quantity absorbed.

References

Synthesis Reference

Peter MacDonald, Ettore Bigatti, Pierluigi Rossetto, Zvi Harel, "Process for the preparation of letrozole." U.S. Patent US20070066831, issued March 22, 2007.

US20070066831
General References
  1. Tulandi T, Martin J, Al-Fadhli R, Kabli N, Forman R, Hitkari J, Librach C, Greenblatt E, Casper RF: Congenital malformations among 911 newborns conceived after infertility treatment with letrozole or clomiphene citrate. Fertil Steril. 2006 Jun;85(6):1761-5. Epub 2006 May 2. [PubMed:16650422]
External Links
Human Metabolome Database
HMDB15141
KEGG Drug
D00964
KEGG Compound
C08163
PubChem Compound
3902
PubChem Substance
46504610
ChemSpider
3765
BindingDB
13061
ChEBI
6413
ChEMBL
CHEMBL1444
Therapeutic Targets Database
DAP000626
PharmGKB
PA450196
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Letrozole
ATC Codes
L02BG04 — Letrozole
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (112 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingBasic ScienceNeoplasms, Brain1
0RecruitingBasic ScienceCancer, Breast2
1Active Not RecruitingBasic ScienceTumors, Solid1
1Active Not RecruitingOtherAdvanced Breast Cancer1
1Active Not RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Invasive Ductal Breast Carcinoma / Progesterone Receptor-positive Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
1Active Not RecruitingTreatmentHormone Receptor Positive, HER2-negative, Advanced Breast Cancer1
1Active Not RecruitingTreatmentMetastatic or Locally-advanced Unresectable Breast Cancer1
1CompletedNot AvailableHealthy Volunteers2
1CompletedOtherAdvanced or Metastatic Breast Cancer1
1CompletedPreventionHealthy, no Evidence of Disease / Lobular Breast Carcinoma In Situ1
1CompletedTreatmentCancer, Breast2
1CompletedTreatmentCancer, Breast / Metastatic Breast Cancer, Locally Advanced Breast Cancer1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentMcCune Albright Syndrome / Polyostotic Fibrous Dysplasia / Puberty, Precocious1
1CompletedTreatmentMetastatic Breast Cancer (MBC)1
1RecruitingTreatmentCancer, Advanced / Lung Cancer Non-Small Cell Cancer (NSCLC) / Mesothelioma, Malignant / Metastatic Breast Cancer (MBC) / Metastatic Cancers / Non-Hodgkin's Lymphoma (NHL)1
1RecruitingTreatmentCancer, Breast4
1RecruitingTreatmentCancer, Breast / Carcinoma, Breast / Malignant Neoplasm of Breast1
1RecruitingTreatmentCancer, Breast / Tumors, Solid2
1RecruitingTreatmentNeoplasms, Breast1
1RecruitingTreatmentNeoplasms / Neoplasms, Breast1
1RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL) / Non-Hodgkin's Lymphoma, Solid Cancers / Solid Cancers1
1TerminatedTreatmentCancer, Breast2
1TerminatedTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer1
1WithdrawnTreatmentSymptomatic or Large Uterine Fibroids1
1, 2Active Not RecruitingTreatmentAndrogen Deficiency / BMI >30 kg/m2 / Insulin Resistance / Metabolic Diseases / Type 2 Diabetes Mellitus1
1, 2Active Not RecruitingTreatmentCancer, Breast1
1, 2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1, 2CompletedNot AvailableCancer, Breast1
1, 2CompletedTreatmentCancer, Breast1
1, 2CompletedTreatmentOvarian Stimulation1
1, 2Not Yet RecruitingTreatmentCancer, Breast1
1, 2Not Yet RecruitingTreatmentEstrogen Receptor Positive / HER2/Neu Negative / Invasive Breast Carcinoma / Multifocal Breast Carcinoma / One to five years postmenopausal / Progesterone Receptor Positive / Stage I Breast Carcinoma / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage II Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage III Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1, 2RecruitingTreatmentCancer, Breast2
1, 2TerminatedTreatmentCancer, Breast1
2Active Not RecruitingTreatmentAdvanced, Persistent, or Recurrent Endometrial Cancer1
2Active Not RecruitingTreatmentBreast Cancer Invasive Nos1
2Active Not RecruitingTreatmentCancer of the Breast / Cancer, Breast / Neoplasms, Breast1
2Active Not RecruitingTreatmentCancer, Breast9
2Active Not RecruitingTreatmentEndometrial Cancers2
2Active Not RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Recurrent Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2Active Not RecruitingTreatmentHormone Receptor Positive Breast Cancer1
2Active Not RecruitingTreatmentMalignant Ovarian Mixed Epithelial Tumor / Ovarian Endometrioid Adenocarcinoma / Ovarian Seromucinous Carcinoma / Ovarian Serous Cystadenocarcinoma / Ovarian Serous Surface Papillary Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Ovarian Germ Cell Tumor / Recurrent Primary Peritoneal Carcinoma / Undifferentiated Ovarian Carcinoma1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentNeoadjuvant Operable Breast Cancer1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2Active Not RecruitingTreatmentNeoplasms / Neoplasms, Breast1
2CompletedDiagnosticCancer, Breast1
2CompletedPreventionCancer, Breast4
2CompletedSupportive CareArthralgia / Musculoskeletal Complications / Pain / Recurrent Breast Cancer / Stage I Breast Carcinoma / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2CompletedSupportive CareDuctal Carcinoma In Situ / Estrogen Receptor-Positive Breast Cancer / Progesterone Receptor-positive Breast Cancer / Stage I Breast Carcinoma / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2CompletedTreatmentCancer, Breast14
2CompletedTreatmentEndometrial Cancers2
2CompletedTreatmentEstrogen Receptor-negative Breast Cancer / Estrogen Receptor-Positive Breast Cancer / Her2-Positive Breast Cancer / Progesterone Receptor-negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer1
2CompletedTreatmentLeiomyosarcomas1
2CompletedTreatmentLymphangioleiomyomatosis1
2CompletedTreatmentMetastatic Breast Cancer (MBC)5
2CompletedTreatmentNeoplasms, Breast4
2CompletedTreatmentPostmenopausal Women With Advanced Breast Cancer3
2CompletedTreatmentPregnancy1
2CompletedTreatmentRecurrent and Metastatic Endometrial Cancer1
2CompletedTreatmentSevere and Recurrent Endometriosis1
2Not Yet RecruitingTreatmentAnovulatory cycle / Polycystic Ovaries Syndrome1
2Not Yet RecruitingTreatmentBreast Cancer Metastatic1
2Not Yet RecruitingTreatmentBreast Cancer Stage II / Breast Cancer Stage III / Cancer, Breast1
2Not Yet RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Not Yet RecruitingTreatmentNeoplasms, Breast2
2RecruitingBasic ScienceCancer, Breast1
2RecruitingPreventionBone destruction / Cancer, Breast1
2RecruitingTreatmentCancer of Breast / Cancer, Breast / Carcinoma, Breast1
2RecruitingTreatmentCancer of Breast / Cancer, Breast / Carcinoma, Breast / Malignant Tumor of Breast1
2RecruitingTreatmentCancer, Breast10
2RecruitingTreatmentCancer, Breast / Carcinoma, Breast / Tumors, Breast1
2RecruitingTreatmentCancer, Breast / Hormone Receptor Positive Tumor / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast1
2RecruitingTreatmentCancer, Ovarian / Endometrial Cancers1
2RecruitingTreatmentEarly-Stage Breast Carcinoma / Estrogen Receptor Positive Tumor1
2RecruitingTreatmentEndometrial Cancers1
2RecruitingTreatmentEndometrial Carcinoma / Malignant Neoplasms of Female Genital Organs1
2RecruitingTreatmentEstrogen Receptor Negative / Estrogen Receptor Positive / HER2/Neu Negative / Progesterone Receptor Negative / Progesterone Receptor Positive / Stage IV Breast Cancer / Triple-Negative Breast Carcinoma1
2RecruitingTreatmentEstrogen Receptor Positive / HER2/Neu Negative / One to five years postmenopausal / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
2RecruitingTreatmentEstrogen Receptor Positive / One to five years postmenopausal / RB1 Positive / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Recurrent Uterine Corpus Carcinoma1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)4
2RecruitingTreatmentNeoplasms, Breast2
2RecruitingTreatmentUterine Cervical Neoplasms1
2TerminatedNot AvailableStage I Breast Carcinoma1
2TerminatedTreatmentAdvanced Breast Cancer (Phase 1b) / Early Breast Cancer (Phase 2)1
2TerminatedTreatmentCancer, Breast6
2TerminatedTreatmentCancer, Ovarian / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
2TerminatedTreatmentCarcinoma, Breast1
2TerminatedTreatmentEndocrine Breast Diseases / Neoplasms Metastasis / Neoplasms, Breast1
2TerminatedTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2TerminatedTreatmentHormone-sensitive Metastatic Breast Cancer1
2TerminatedTreatmentLeiomyosarcomas / Uterine Neoplasms1
2TerminatedTreatmentMedical Abortion, Complete or Unspecified, Without Complication1
2TerminatedTreatmentNeoplasms, Breast1
2Unknown StatusPreventionCancer, Breast / One to five years postmenopausal1
2Unknown StatusTreatmentCancer, Breast1
2Unknown StatusTreatmentCancer, Breast / Hormone-Sensitive Breast Cancer1
2WithdrawnTreatmentCancer, Breast1
2WithdrawnTreatmentCancer, Ovarian / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
2, 3Active Not RecruitingNot AvailableHealthy Volunteers / Idiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia1
2, 3Active Not RecruitingTreatmentConstitutional Delay of Growth and Puberty1
2, 3Active Not RecruitingTreatmentUterine Cancers1
2, 3CompletedTreatmentAbortions spontaneous1
2, 3CompletedTreatmentCancer, Breast1
2, 3CompletedTreatmentComplete Miscarriage1
2, 3CompletedTreatmentMetastatic Breast Cancer (MBC)1
2, 3RecruitingTreatmentInfertilities2
2, 3RecruitingTreatmentInflammatory carcinoma of the breast / Invasive Ductal Breast Carcinoma / Mucinous Breast Cancer / Tubular Breast Carcinoma1
2, 3RecruitingTreatmentLow Grade Ovarian Serous Adenocarcinoma / Micropapillary Serous Carcinoma / Ovarian Serous Adenocarcinoma / Primary Peritoneal Serous Adenocarcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
3Active Not RecruitingPreventionCancer, Breast1
3Active Not RecruitingPreventionBrca1 Mutation Carrier / Brca2 Mutation Carrier / Cancer, Breast / Hereditary Breast/Ovarian Cancer (brca1, brca2)1
3Active Not RecruitingTreatmentAdvanced, Metastatic Breast Cancer2
3Active Not RecruitingTreatmentBreast Adenocarcinoma / Estrogen Receptor and/or Progesterone Receptor Positive / HER2/Neu Negative / Stage IA Breast Cancer / Stage IA Breast Cancer AJCC v7 / Stage IB Breast Cancer / Stage IB Breast Cancer AJCC v7 / Stage IIA Breast Cancer / Stage IIA Breast Cancer AJCC v6 and v7 / Stage IIB Breast Cancer / Stage IIB Breast Cancer AJCC v6 and v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v71
3Active Not RecruitingTreatmentCancer, Breast9
3Active Not RecruitingTreatmentEstrogen Receptor Positive / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IV Breast Cancer1
3Active Not RecruitingTreatmentNeoplasms, Breast2
3CompletedPreventionBone destruction / Neoplasms, Breast1
3CompletedSupportive CareBone destruction / Cancer, Breast1
3CompletedTreatmentAzoospermia, Nonobstructive / Oligozoospermia1
3CompletedTreatmentBMI >30 kg/m2 / Hypogonadotrophic Hypogonadism1
3CompletedTreatmentBone Loss / Cancer, Breast1
3CompletedTreatmentCancer, Breast8
3CompletedTreatmentHormone Sensitive Resected Primary Breast Cancer in Postmenopausal Women1
3CompletedTreatmentIdiopathic Short Stature (ISS)1
3CompletedTreatmentInfertilities2
3CompletedTreatmentMalignant Neoplasm of Female Breast1
3CompletedTreatmentNeoplasms, Breast / Neoplasms, Hormone-Dependent1
3CompletedTreatmentPolycystic Ovarian Syndrome1
3CompletedTreatmentPolycystic Ovaries Syndrome / Pregnancy1
3CompletedTreatmentPregnancy / Unexplained Infertility1
3CompletedTreatmentUnexplained Infertility1
3CompletedTreatmentBone destruction / One to five years postmenopausal1
3No Longer AvailableNot AvailableAdvanced Breast Cancer (Female)1
3Not Yet RecruitingPreventionOvarian Hyperstimulation Syndrome1
3Not Yet RecruitingTreatmentCancer, Breast1
3RecruitingOtherCancer, Breast1
3RecruitingTreatmentAdvanced Breast Cancer (Female) / Advanced Breast Cancer Female1
3RecruitingTreatmentAdvanced Metastatic Breast Cancer1
3RecruitingTreatmentBreast Cancer Metastatic1
3RecruitingTreatmentCancer, Breast6
3RecruitingTreatmentDuctal Breast Carcinoma In Situ / Estrogen Receptor and/or Progesterone Receptor Positive / HER2/Neu Negative / Invasive Breast Carcinoma / Multicentric Breast Carcinoma / Multifocal Breast Carcinoma / Synchronous Bilateral Breast Carcinoma1
3RecruitingTreatmentEstrogen Receptor Positive Breast Cancer / HER-2 Positive Breast Cancer1
3RecruitingTreatmentInfertilities3
3RecruitingTreatmentInfertility, Female1
3RecruitingTreatmentMetastatic Breast Cancer (MBC)1
3RecruitingTreatmentNeoadjuvant Therapy1
3RecruitingTreatmentNeoplasms, Breast1
3RecruitingTreatmentPolycystic Ovaries Syndrome1
3RecruitingTreatmentSubfertility1
3TerminatedTreatmentNeoplasms, Breast / Neoplasms, Hormone-Dependent2
3TerminatedTreatmentOperable Breast Neoplasms1
3Unknown StatusTreatmentCancer, Breast3
3WithdrawnTreatmentCancer, Breast1
4Active Not RecruitingTreatmentHormono-depending Adjuvant Breast Cancer1
4Active Not RecruitingTreatmentLeiomyomas / Uterine Leiomyomas1
4CompletedBasic ScienceFertility1
4CompletedDiagnosticESTROGENS/RIFAMPIN [VA Drug Interaction] / Ovarian Cysts / Ovulatory Dysfunction1
4CompletedPreventionCancer, Breast1
4CompletedPreventionOvarian Hyperstimulation Syndrome1
4CompletedTreatmentCancer, Breast3
4CompletedTreatmentInfertilities1
4CompletedTreatmentInfertilities / Polycystic Ovarian Syndrome1
4CompletedTreatmentInfertility Indicated for ICSI1
4CompletedTreatmentLocally Advanced Breast Cancer (LABC)1
4CompletedTreatmentLocally Advanced Metastatic Breast Cancer / Locally Advanced or Metastatic Breast Cancer / Metastatic Breast Cancer (MBC) / Postmenopausal Women1
4Not Yet RecruitingTreatmentHER2/Neu Negative / Invasive Breast Carcinoma / One to five years postmenopausal / Stage 0 Breast Cancer / Stage IA Breast Cancer1
4RecruitingHealth Services ResearchBMI >30 kg/m21
4RecruitingPreventionFertility / Neoplasms, Breast1
4RecruitingTreatmentAnovulatory cycle1
4RecruitingTreatmentCancer, Breast1
4RecruitingTreatmentInfertilities / Polycystic Ovaries Syndrome1
4RecruitingTreatmentShort Stature1
4TerminatedTreatmentMetastatic Breast Cancer (MBC)2
4TerminatedTreatmentNeoplasms, Breast1
4Unknown StatusNot AvailableArthralgia1
4Unknown StatusTreatmentCancer, Breast2
4Unknown StatusTreatmentIs to Identify Biomarkers That Could Predict the Efficacy of an Adjuvant Letrozol Treatment in Postmenopausal Breast Cancer Patients1
4WithdrawnTreatmentInfertilities1
Not AvailableActive Not RecruitingNot AvailableCancer, Breast1
Not AvailableActive Not RecruitingBasic ScienceCancer, Breast1
Not AvailableActive Not RecruitingTreatmentMale Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer2
Not AvailableActive Not RecruitingTreatmentNeoplasms, Breast1
Not AvailableCompletedNot AvailableArthralgia / BMI >30 kg/m2 / Cancer, Breast1
Not AvailableCompletedNot AvailableArthralgia / Cancer, Breast / Pain1
Not AvailableCompletedNot AvailableBMI >30 kg/m21
Not AvailableCompletedNot AvailableCancer, Breast1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedNot AvailableInfertilities1
Not AvailableCompletedHealth Services ResearchOvarian Follicle1
Not AvailableCompletedHealth Services ResearchPolycystic Ovaries Syndrome1
Not AvailableCompletedOtherInfertilities1
Not AvailableCompletedPreventionBone destruction / Cancer, Breast1
Not AvailableCompletedTreatmentCancer, Breast1
Not AvailableCompletedTreatmentEndometrial Carcinoma1
Not AvailableCompletedTreatmentEndometriosis1
Not AvailableCompletedTreatmentInfertilities1
Not AvailableCompletedTreatmentInfertility Poly Cystic Ovary1
Not AvailableCompletedTreatmentPolycystic Ovaries Syndrome3
Not AvailableCompletedTreatmentPoor Responders1
Not AvailableEnrolling by InvitationNot AvailableCancer, Breast1
Not AvailableNot Yet RecruitingTreatmentInfertilities1
Not AvailableNot Yet RecruitingTreatmentInfertilities / Polycystic Ovaries Syndrome1
Not AvailableRecruitingBasic ScienceCancer, Breast1
Not AvailableRecruitingBasic ScienceNeoplasms1
Not AvailableRecruitingTreatmentCancer, Breast1
Not AvailableRecruitingTreatmentCancer, Breast / Infertilities1
Not AvailableRecruitingTreatmentFemale Infertility Due to Nonimplantation of Ovum1
Not AvailableRecruitingTreatmentNeoplasms Metastasis / Neoplasms, Breast1
Not AvailableRecruitingTreatmentPolycystic Ovarian Syndrome / Subfertility1
Not AvailableSuspendedTreatmentCancer, Breast1
Not AvailableUnknown StatusNot AvailableArterial hypoxia / Cancer, Breast1
Not AvailableUnknown StatusTreatmentComplete Abortion1
Not AvailableUnknown StatusTreatmentInfertilities2
Not AvailableUnknown StatusTreatmentPolycystic Ovarian Syndrome1
Not AvailableUnknown StatusTreatmentPolycystic Ovaries Syndrome2

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
  • Mylan pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
TabletOral2.5 mg
Kit
TabletOral2.5 mg/1
Tablet, film coatedOral2.5 mg/1
Prices
Unit descriptionCostUnit
Femara 2.5 mg tablet16.87USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4978672No1994-06-032011-06-03Us
US8685980No2010-05-252030-05-25Us
US9193732No2011-11-092031-11-09Us
US8415355No2011-02-192031-02-19Us
US8324225No2008-06-172028-06-17Us
US9416136No2009-08-202029-08-20Us
US8962630No2009-12-092029-12-09Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)184-185 °CNot Available
logP2.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0799 mg/mLALOGPS
logP1.86ALOGPS
logP2.94ChemAxon
logS-3.6ALOGPS
pKa (Strongest Basic)2.17ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area78.29 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity94.47 m3·mol-1ChemAxon
Polarizability29.59 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9965
Blood Brain Barrier+0.9737
Caco-2 permeable+0.6347
P-glycoprotein substrateNon-substrate0.8391
P-glycoprotein inhibitor INon-inhibitor0.8087
P-glycoprotein inhibitor IINon-inhibitor0.9147
Renal organic cation transporterNon-inhibitor0.5908
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6843
CYP450 1A2 substrateNon-inhibitor0.8374
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorInhibitor0.8993
CYP450 3A4 inhibitorInhibitor0.6451
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7027
Ames testNon AMES toxic0.6371
CarcinogenicityNon-carcinogens0.8926
BiodegradationNot ready biodegradable0.9864
Rat acute toxicity1.9916 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9261
hERG inhibition (predictor II)Non-inhibitor0.8817
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-0090000000-0fbd577a32ff572f7368
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-0190000000-dfcab9af789387521571
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0006-0390000000-dbc68fd6017abe6e8adc
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00kf-0490000000-c3fc389848a06a012234
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014l-0690000000-38ba597054b02b136ab6
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00kf-1980000000-13a8827cbc5c1b36a14f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-00kf-3940000000-e01d63313ef1cfa7477a
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9410000000-83b93aed0756bd41adaf
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9100000000-d1757f8c218d5dcc4809
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0090000000-791121bd513899b7dfc0
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0090000000-eb3996846ea4f036ccca
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0390000000-a57ce4cfb24ba743c54b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0950000000-303d99867511fe3a013b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0930000000-77e720374927be5113ef
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0920000000-4a93d8e76eb7d0d59481
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03du-0910000000-8ad9f37884e8686ef7ba
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03dr-2900000000-2274a3adb5e486f57001
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03dr-6900000000-74d56231c43250bc65ca
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014i-0490000000-7868daa9f0ec9ebda34a

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Benzonitriles / Triazoles / Heteroaromatic compounds / Nitriles / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Diphenylmethane / Benzonitrile / Heteroaromatic compound / 1,2,4-triazole / Azole / Azacycle / Organoheterocyclic compound / Nitrile / Carbonitrile / Organic nitrogen compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
nitrile, triazoles (CHEBI:6413)

Targets

Details
1. Cytochrome P450 19A1
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Oxygen binding
Specific Function
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name
CYP19A1
Uniprot ID
P11511
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Ebert AD, Bartley J, David M, Schweppe KW: [Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis]. Zentralbl Gynakol. 2003 Jul-Aug;125(7-8):247-51. [PubMed:14505258]
  3. Long BJ, Jelovac D, Handratta V, Thiantanawat A, MacPherson N, Ragaz J, Goloubeva OG, Brodie AM: Therapeutic strategies using the aromatase inhibitor letrozole and tamoxifen in a breast cancer model. J Natl Cancer Inst. 2004 Mar 17;96(6):456-65. [PubMed:15026471]
  4. Murphy MJ Jr: Molecular Action and Clinical Relevance of Aromatase Inhibitors. Oncologist. 1998;3(2):129-130. [PubMed:10388095]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxygen binding
Specific Function
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name
CYP19A1
Uniprot ID
P11511
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:33