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{{VP}}


<!--Overview-->


{{drugbox
|genericName=
| IUPAC_name = 4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile
 
| image = Letrozole.svg
 
| CAS_number = 112809-51-5
 
| ATC_prefix = L02
|aOrAn=
| ATC_suffix = BG04
 
| ATC_supplemental =  
an
| PubChem = 3902
 
| DrugBank = APRD01066
|drugClass=
| C = 17 | H = 11 | N = 5
 
| molecular_weight = 285.303 g/mol
aromatase inhibitor
| bioavailability = 99.9%
 
| protein_bound = 60%, mainly to albumin
|indication=
| metabolism =  
 
| elimination_half-life = 2 days
adjuvant treatment of early [[breast cancer]], extended adjuvant treatment of early [[breast cancer]], first and second-line treatment of advanced [[breast cancer]]
| pregnancy_category =  
 
| legal_status =  
|hasBlackBoxWarning=
| routes_of_administration =  
 
}}
|adverseReactions=
{{SI}}
 
'''Letrozole''' ([[International Nonproprietary Name|INN]], trade name '''Femara®''') is an oral non-steroidal [[aromatase inhibitor]] that has been introduced for the adjuvant treatment of hormonally-responsive [[breast cancer]]
[[hot flashes]], [[arthralgia]], [[flushing]], [[asthenia]], [[edema]], [[arthralgia]], [[headache]], [[dizziness]], [[hypercholesterolemia]], sweating increased, and [[bone pain]]
 
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<!--Adult Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Adult)-->
 
|fdaLIADAdult=
 
=====Adjuvant Treatment of Early Breast Cancer=====
 
Letrozole tablets, USP are indicated for the adjuvant treatment of postmenopausal women with hormone receptor positive early breast cancer.
 
The recommended dose of letrozole tablets is one 2.5 mg tablet administered once a day, without regard to meals.
 
=====Extended Adjuvant Treatment of Early Breast Cancer=====
 
Letrozole tablets, USP are indicated for the extended adjuvant treatment of early breast cancer in postmenopausal women, who have received 5 years of adjuvant tamoxifen therapy. The effectiveness of letrozole in extended adjuvant treatment of early breast cancer is based on an analysis of disease-free survival in patients treated with letrozole tablets for a median of 60 months [see Clinical Studies (14.2, 14.3)].
 
=====First and Second-Line Treatment of Advanced Breast Cancer=====
 
Letrozole tablets, USP are indicated for first-line treatment of postmenopausal women with hormone receptor positive or unknown, locally advanced or metastatic breast cancer. Letrozole tablets are also indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.
 
<!--Off-Label Use and Dosage (Adult)-->
 
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=====Special Senses=====
 
 
 
 
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* ®<ref>{{Cite web | title =  | url =  }}</ref>


[[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.
<!--Look-Alike Drug Names-->


==FDA-approved use==
|lookAlike=
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]].


==Off-label use==
* A® — B®<ref name="www.ismp.org">{{Cite web  | last = | first = | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
It has been in use for the use of ovulation induction by fertility doctors since 2001; having less side-effects than [[clomiphene]] citrate ('''Clomid®''') for the patient. A Canadian study presented at the [[American Society of Reproductive Medicine]] 2005 Conference suggests that it may increase the risk of birth defects compared with a control group, however a more detailed follow-up study found no basis for concern when letrozole is used for ovulation induction.<ref>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 Apr 28. PMID 16650422</ref>  


The manufacturer, [[Novartis]], has issued letters to doctors in Canada and the United States reiterating that it is not approved for such a use and is not safe to use with pregnant women or women who may become pregnant.
<!--Drug Shortage Status-->


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 [[bodybuilder]]s 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.
|drugShortage=
}}


Letrozole has also been shown to delay the fusing of the [[epiphyseal plate|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.
<!--Pill Image-->


A related agent is [[anastrozole]].
{{PillImage
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Letrozole has also been used to treat [[endometriosis]].<ref>http://www.endometriosis.org/ESHRE2005-abbamonte.html</ref>
<!--Label Display Image-->


==References==
{{LabelImage
<references/>
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
}}
 
{{LabelImage
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
}}


==See also==
<!--Category-->
*[[Aromatase inhibitor]]
==External links==
*[http://www.femara.com Femara website]
{{Sex hormones}}


[[Category:Aromatase inhibitors]]
[[Category:Drug]]
[[Category:Endocrinology]]
[[es:Femara]]
{{WikiDoc Help Menu}}
{{WikiDoc Sources}}

Revision as of 15:22, 29 December 2014

Letrozole
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Vignesh Ponnusamy, M.B.B.S. [2]

Disclaimer

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Overview

Letrozole is an aromatase inhibitor that is FDA approved for the {{{indicationType}}} of adjuvant treatment of early breast cancer, extended adjuvant treatment of early breast cancer, first and second-line treatment of advanced breast cancer. Common adverse reactions include hot flashes, arthralgia, flushing, asthenia, edema, arthralgia, headache, dizziness, hypercholesterolemia, sweating increased, and bone pain.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Adjuvant Treatment of Early Breast Cancer

Letrozole tablets, USP are indicated for the adjuvant treatment of postmenopausal women with hormone receptor positive early breast cancer.

The recommended dose of letrozole tablets is one 2.5 mg tablet administered once a day, without regard to meals.

Extended Adjuvant Treatment of Early Breast Cancer

Letrozole tablets, USP are indicated for the extended adjuvant treatment of early breast cancer in postmenopausal women, who have received 5 years of adjuvant tamoxifen therapy. The effectiveness of letrozole in extended adjuvant treatment of early breast cancer is based on an analysis of disease-free survival in patients treated with letrozole tablets for a median of 60 months [see Clinical Studies (14.2, 14.3)].

First and Second-Line Treatment of Advanced Breast Cancer

Letrozole tablets, USP are indicated for first-line treatment of postmenopausal women with hormone receptor positive or unknown, locally advanced or metastatic breast cancer. Letrozole tablets are also indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Letrozole in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Letrozole in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Letrozole in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Letrozole in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Letrozole in pediatric patients.

Contraindications

  • Condition1

Warnings

  • Description

Precautions

  • Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Letrozole in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Letrozole in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Letrozole in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Letrozole during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Letrozole with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Letrozole with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Letrozole with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Letrozole with respect to specific gender populations.

Race

There is no FDA guidance on the use of Letrozole with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Letrozole in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Letrozole in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Letrozole in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Letrozole in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

There is limited information regarding Monitoring of Letrozole in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Letrozole in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Letrozole in the drug label.

Pharmacology

There is limited information regarding Letrozole Pharmacology in the drug label.

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Letrozole in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Letrozole in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Letrozole in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Letrozole in the drug label.

How Supplied

Storage

There is limited information regarding Letrozole Storage in the drug label.

Images

Drug Images

{{#ask: Page Name::Letrozole |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Letrozole |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Letrozole in the drug label.

Precautions with Alcohol

  • Alcohol-Letrozole interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ Empty citation (help)
  2. ↑ "http://www.ismp.org". External link in |title= (help)


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