Letrofam

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Letrofam

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Letrofam

What is Letrofam? (Overview)

This section provides a concise, authoritative summary of the drug entity Letrofam, focusing on its identity, composition, and core purpose without detailing specific clinical uses or administration protocols.

Property Description
Active Ingredient Letrozole (INN)
Form Film-coated tablets
Pharmacological Class Nonsteroidal Aromatase Inhibitor (Third-Generation)
General Purpose Hormone-action modifier; suppresses estrogen synthesis
Origin Synthetic, C17H11N5 Triazole derivative

Letrofam: Defining the Drug Entity and Pharmacological Class

Letrofam is a medicinal product containing the active substance Letrozole, which is pharmacologically classified as a highly selective nonsteroidal aromatase inhibitor. This category places it within the broader group of Antineoplastic agents used in hormone-action therapy. Letrozole is a synthetic compound derived from the triazoles chemical family, and its chemical identity is defined by the formula C17H11N5. The drug is available only with a doctor's prescription (Rx-only).

Composition and Form: The Active Ingredient and Delivery Type

The composition of Letrofam consists of Letrozole as the single active ingredient, formulated into a film-coated tablet for oral administration. The compound represents a third-generation inhibitor, a status reflecting its drug selectivity and potency. This formulation provides systemic delivery of the pure chemical entity through a non-invasive route.

High-Level Purpose: Understanding its Role as an Aromatase Inhibitor

The general purpose of this medicine is to modify the hormonal environment by reducing the body's estrogen supply. Letrozole achieves this by selectively and competitively inhibiting the aromatase enzyme, thereby blocking the metabolic process that converts androgens into estrogens in peripheral tissues. This specific action on the enzyme makes it a modifier of endocrine signaling, supporting its role in hormone-action therapy.

Regulatory References

  1. NIH LiverTox Letrozole Entry

What side effects are possible with Letrofam?

Possible Side Effects and Safety Information

The safety profile of Letrofam (Letrozole) is formally classified by health authorities based on the frequency of documented adverse reactions, which primarily stem from the drug's mechanism of suppressing estrogen production. These reactions are grouped by System-Organ Class (SOC) in regulatory documents.


Official Frequency Classifications

Side effects are categorized by how often they appeared in clinical trials, ranging from very common to rare:

  • Very Common (ge 1 in 10): Reactions include hot flushes, arthralgia (joint pain), fatigue, and hypercholesterolaemia (elevated cholesterol levels).
  • Common (ge 1 in 100 to < 1 in 10): Documented effects include nausea, headache, peripheral oedema, bone pain, and weight increase.
  • Rare (ge 1 in 10,000 to < 1 in 1,000): Serious adverse events such as thromboembolic events, including pulmonary embolism and arterial thrombosis, are officially listed.

Serious Safety Considerations

The established safety profile includes long-term risks associated with sustained estrogen deprivation. The risk of developing osteoporosis and subsequent bone fracture is a defined safety concern documented in labeling. Rare but clinically serious reactions, such as severe dermatologic events like Toxic Epidermal Necrolysis, are also noted.


Population-Specific Regulatory Notes

Letrofam is contraindicated for use in pre-menopausal women. Cautionary statements are specified for patients with pre-existing conditions; for instance, increased systemic exposure has been noted in patients with severe hepatic impairment, requiring careful assessment. The product is also restricted for individuals with rare hereditary problems, such as galactose intolerance, due to the presence of excipients in the tablet formulation.

Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory documents state that clinical experience with acute overdosage of Letrofam (Letrozole) is limited. A specific, defined toxic syndrome has not been established in the official prescribing information, even in documented cases of overexposure. This limited data means that any suspected overdosage must be treated as a medical emergency requiring immediate professional medical attention.

Required Emergency Actions

It is a regulatory requirement to seek immediate medical attention for a suspected Letrofam overdose. The official guidance instructs contacting emergency services immediately for severe manifestations, such as when an individual has collapsed, experienced a seizure, has trouble breathing, or cannot be awakened. These actions are mandated due to the recognized potential for severe outcomes.

Official Management Profile

The regulatory documentation explicitly states that no specific antidote is known for Letrofam overdosage. Therefore, the management protocol consists entirely of symptomatic and supportive treatment. This mandated approach includes close patient observation and monitoring of vital signs as integral procedural steps. The official profile for Letrofam is defined by the need for prompt external intervention and procedural support, underscoring that the focus is on stabilization and monitoring rather than treatment with a specific reversal agent.

Therapeutic Uses of Letrofam

Letrofam: Quick Facts

  • Approved for use: Postmenopausal women.
  • Primary domain: Hormone receptor-positive breast cancer.
  • Therapeutic use: Adjuvant and advanced treatment settings.

Letrofam is a medication approved for the management of certain types of breast cancer in women who have completed menopause. Its primary therapeutic domains include both early and advanced stages of the disease, provided the cancer is hormone receptor-positive.

The drug is an option for the adjuvant treatment of hormone receptor-positive early breast cancer. This use is intended to reduce the risk of the cancer recurring following initial treatments, such as surgery. It is also utilized for extended adjuvant treatment in women who have already completed a five-year course of tamoxifen therapy.

In cases of locally advanced or metastatic breast cancer, Letrofam is used as a first-line treatment. Additionally, it may be used to manage advanced breast cancer if the disease has worsened after a patient has received other antiestrogen therapies.

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Letrofam — Official Regulatory Information


Eligibility Scope

Classification Eligible Population Non-Eligible/Restricted Population
Hormonal Status Postmenopausal women (confirmed status required) Premenopausal women (Contraindicated)
Reproductive Status Women of non-reproductive potential Pregnancy and Lactation (Contraindicated)
Hypersensitivity No known allergies Known hypersensitivity to letrozole or excipients (Contraindicated)
Age Group Adults, including geriatric patients (no dose adjustment needed) Children and adolescents (Use not established/not recommended)
Organ Function Mild-to-moderate hepatic impairment (no dose change) Severe hepatic impairment (Conditional use, dose reduction recommended)
Comorbidity None specified Severe renal impairment (Use not sufficiently investigated)

Eligibility Classifications (High-Level)

Eligibility severity classification (as defined in official documents):

  • Contraindicated: Pregnancy, Lactation, Premenopausal Status, Hypersensitivity.
  • Restricted/Conditional Use: Severe Hepatic Impairment.
  • Use Not Established/Not Recommended: Pediatric and Adolescent Patients.

Eligibility-context constraints (as defined in official documents): Use is dependent on the patient having a confirmed postmenopausal endocrine status and lacking other absolute contraindications. Women of child-bearing potential must use effective contraception during and for a period after treatment.


Resulting Eligibility Structure

Official eligibility statements:

  • Contraindicated in women with a premenopausal endocrine status.
  • Contraindicated during pregnancy and lactation.
  • Contraindicated in patients with known hypersensitivity to the drug substance.
  • Use is not recommended in children and adolescents.
  • Patients with severe hepatic impairment require close supervision and a dose reduction is recommended.

Connection to the overall eligibility profile: The regulatory documents define eligibility primarily by hormonal status, making the medicine officially limited to postmenopausal women. The profile establishes absolute prohibitions for individuals who are pregnant, breastfeeding, or hypersensitive, and requires conditional use or monitoring for patients with severe organ dysfunction, such as severe hepatic or renal impairment.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Letrofam must not be used concurrently with estrogen-containing medicines, including hormone replacement therapy (HRT) or certain oral contraceptives. The official regulatory classification for this combination is contraindicated due to pharmacological antagonism, which would be expected to reverse the product's therapeutic effect.

Co-administration with tamoxifen is also a contraindicated combination, as clinical data show it reduces the plasma levels of Letrofam. This interaction is classified as highly clinically significant and requires the avoidance of concurrent use.

Interacting Product Category Official Constraint
Strong CYP3A4 Inducers (e.g., rifampin, phenytoin) Avoid or Use with Caution; may decrease Letrofam exposure, leading to reduced efficacy.
Strong CYP3A4 Inhibitors (e.g., ketoconazole, clarithromycin) Use with Caution/Monitor Closely; may increase Letrofam exposure, requiring careful clinical monitoring.
CYP2A6 Substrates Use with Caution/Monitor Closely; Letrofam may increase the concentration of co-administered drugs that are substrates of the CYP2A6 enzyme.

Additionally, the use of St. John’s wort should be avoided as it may alter the drug's metabolism via the CYP450 enzyme system. Patients with severe hepatic impairment or certain pre-existing conditions like osteoporosis or hypercholesterolemia may face interaction-related constraints and require cautious prescribing and close monitoring.

Mechanism of Action

Molecular Targeting and Selective Enzyme Inhibition

Letrofam works by targeting and competitively inhibiting the aromatase enzyme (CYP19A1). The drug binds with high specificity to the enzyme's active site, halting the final, rate-limiting step in the steroidogenesis pathway. The mechanism's high selectivity results in minimal or negligible interaction with the biosynthesis of other adrenal steroids, such as cortisol and aldosterone.

Extensive Modulation of Estrogen Biosynthesis

The inhibition of the aromatase enzyme dramatically interrupts the conversion of androgens into estrogens (estrone and estradiol) within peripheral tissues. This molecular action triggers a mechanistic cascade that leads to a state of extensive systemic estrogen deprivation, typically suppressing circulating estradiol levels by over 98%. The resultant physiological change is the removal of a primary hormonal stimulus, which dictates the biological response characteristic of the drug's mechanism.

Mechanistic Constraints and Limitations

The functional physiological effect of the mechanism is most pronounced where peripheral aromatization is the dominant source of estrogen, constraining the drug's action to specific biological contexts. However, the physiological effect is mitigated if the target system develops acquired resistance by activating alternative, non-hormonal growth-signaling pathways (e.g., the MAPK cascade), which bypass the molecular signal.

Dosage and Administration Information

How to Use Letrofam

Letrofam is a systemic medication administered by the oral route as a film-coated tablet. The usage protocol is characterized by a fixed daily dose, specific instructions for intake, and clearly defined duration patterns related to the clinical context.


Standard Dosing and Administration

The standard, fixed dose for all approved indications is 2.5 mg. This dose is administered once daily (Q.D.), establishing a non-titrated approach to therapy. The tablet can be taken without regard to meals, meaning administration is permissible with or without food.

Procedurally, the film-coated tablet must be swallowed whole and must not be split, crushed, or chewed.

Usage Constraint Standard Specification
Frequency Once daily (2.5 mg)
Food Relationship With or without food
Tablet Integrity Swallow whole; do not crush

Treatment Duration and Adjustments

The duration of use is context-dependent. For adjuvant treatment, the medication is typically used for a planned course of up to five years. In the setting of advanced or metastatic disease, treatment continues until there is evidence of disease progression.

Dose modification is necessary only in specific populations. No adjustment is required for elderly patients or those with mild-to-moderate renal or hepatic impairment. However, for patients diagnosed with severe hepatic impairment, the frequency is reduced, with the fixed 2.5 mg dose administered every other day. If a dose is missed, it should be taken as soon as remembered; if it is near the next scheduled time, the missed dose must be skipped.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Letrofam

This section summarizes the structure of the official research and clinical studies conducted on Letrofam (Letrozole) and provides an overview of the types of outcomes that have been observed, according to regulatory and scientific sources. The text focuses only on research structure and reported patterns.


Evidence for Extended Adjuvant Treatment in Early Breast Cancer

Studies exploring this use were conducted as large, randomized, placebo-controlled trials (RCTs). Research focused on postmenopausal women who were disease-free after completing prior tamoxifen therapy. The main outcomes that researchers examined were long-term results related to the observed incidence of cancer recurrence, specifically measuring Disease-Free Survival (DFS) and Overall Survival (OS). Findings describe patterns in DFS compared to those who received a placebo.

Evidence for First-Line Treatment in Advanced Breast Cancer

Research included Phase III Comparative Trials against other standard hormonal treatments, such as tamoxifen, for postmenopausal women with advanced hormone receptor-positive disease. The studies monitored outcomes related to the progression of the cancer, including Time to Progression (TTP) and the Objective Response Rate (RR) (tumor activity). Research examined patterns related to Overall Survival over the duration of the data collection.

Evidence for Second-Line Treatment in Advanced Breast Cancer

Letrofam was also evaluated in randomized comparative trials involving women whose advanced breast cancer had progressed after they received prior antiestrogen therapy. The key outcomes monitored were those reflecting tumor activity, primarily the Objective Response Rate (RR) and Time to Progression (TTP). The consistency of findings varies across the studies that used different hormonal agents as the comparator.

Understanding Long-Term Outcomes and Follow-Up

The core studies for Letrofam were designed to track outcomes over many years. Long-term follow-up reports tracked patterns related to survival. Complex statistical methods were used to account for changes, such as patient crossover between treatment groups, which can affect the analysis of Overall Survival results.

Evidence in Specific Patient Populations

Primary research was evaluated in studies involving postmenopausal women. Data for patients who were premenopausal or perimenopausal, as well as those with specific comorbidities, remain insufficient or limited in published regulatory summaries.

Evidence Gaps and Areas of Scientific Uncertainty

The research provides context but does not determine whether an individual will respond similarly. Certainty around final long-term Overall Survival measurements remains lower than for Disease-Free Survival due to trial complexities. Data for certain subgroups remain limited.

Key Studies & References

  1. Ten-year Update: NRG Oncology/NSABP B-42 Randomized Trial: Extended Letrozole Therapy in Early-stage Breast Cancer

Frequently Asked Questions (FAQ)

Common questions about Letrofam (FAQ)


Q: What is the main reason Letrofam is prescribed?

According to official regulatory documents, Letrofam is approved to treat hormone receptor-positive breast cancer in women who have experienced menopause. The official indications include first-line treatment, as well as use in adjuvant and extended adjuvant settings.


Q: How does Letrofam relate to other similar treatments people talk about online?

Letrofam is classified pharmacologically as a nonsteroidal, third-generation Aromatase Inhibitor. This means it belongs to a specific class of hormone-action modifying drugs designed to suppress estrogen synthesis in the body.


Q: Can Letrofam be used for anything besides its main approved purpose?

Official regulatory indications for Letrofam are restricted to the treatment of hormone receptor-positive breast cancer in postmenopausal women. Any use for conditions outside of those specified in the label is considered off-label use and is not described in the official prescribing information.


Q: How long does it usually take to notice any effect from Letrofam?

Studies described in official documentation indicate that the drug is absorbed quickly after administration. For its systemic effects to reach a steady level in the body, known as 'steady-state plasma concentration,' it typically takes between two to six weeks of consistent daily dosing.


Q: What happens if I stop taking Letrofam suddenly?

Due to the way the body processes the drug, some temporary side effects may begin to improve within a week to 10 days after stopping treatment. However, long-term effects related to estrogen deprivation, such as changes in cholesterol or bone density, may take many months to diminish or stabilize after cessation.


Q: Do most people experience side effects from Letrofam?

Clinical trial data summarized in regulatory documents indicate that adverse reactions are generally observed, with approximately 80% to 81% of patients in the adjuvant setting reporting at least one adverse event. These documented reactions in trials were most frequently reported as being mild or moderate.


Q: Is it possible for Letrofam to cause mood changes or depression?

Regulatory documents list low mood and depression as common side effects associated with Letrofam. Additionally, uncommon psychological side effects, such as increased anxiety, irritability, or somnolence (sleepiness), have been reported in the safety profile.


Q: Does Letrofam cause hair loss?

Yes, the official product safety information lists hair loss, medically known as alopecia, or general hair thinning as a common adverse reaction observed during clinical trials.


Q: Are there any specific supplements or vitamins that interact with Letrofam?

Letrofam is processed by the body’s CYP450 enzyme system. Due to the potential for interactions that could alter how the body handles the drug, consultation with a healthcare professional regarding all supplements and vitamins is recommended.


Q: Can Letrofam interact with herbal remedies?

Official documents state that the use of certain herbal remedies, such as St. John’s wort, should be avoided as they may alter the drug's metabolism via the CYP450 enzyme system. Consultation with a healthcare professional regarding all herbal remedies is generally recommended.


Q: Can I take pain relievers like Tylenol or Advil while using Letrofam?

The official regulatory label does not list common over-the-counter (OTC) pain relievers as specific contraindications or prohibited interactions. The official guidance recommends consulting a healthcare professional before combining any over-the-counter medications with this treatment.


Q: Is it safe to consume alcohol while taking Letrofam?

The official prescribing information does not specify an absolute prohibition on alcohol consumption. However, regulatory information notes that modifying alcohol consumption may be helpful in managing certain common side effects of the medication, such as hot flashes.


Q: Are there any dietary restrictions I need to follow while on Letrofam?

Official prescribing information states that Letrofam tablets can be taken either with or without food. There are no specific food or dietary restrictions listed in the regulatory documents that must be followed while using this medication.


Q: Can I take other prescription medications with Letrofam?

The official product information specifies that several prescription medications are either contraindicated (e.g., estrogens, tamoxifen) or require caution. Due to the potential for interaction, certain categories of co-administered drugs, like strong CYP3A4 inhibitors, are associated with a need for increased clinical oversight.


Q: Is Letrofam approved for use in men?

The official approved indications for Letrofam are restricted to the treatment of breast cancer in postmenopausal women. The regulatory label does not include specific indications for use in men, although its use in combination therapy for male breast cancer has been examined in some studies.


Q: What research evidence supports the use of Letrofam?

Studies and official information indicate that the evidence for the use of Letrofam is based on large, randomized clinical trials. These trials demonstrated superior Disease-Free Survival (DFS) when compared to placebo or other common treatments in the specified postmenopausal breast cancer populations.


Q: Where can I find reliable, official information about studies on Letrofam?

Reliable and official prescribing information, including summaries of the clinical studies that support its use, is available through government-run regulatory websites. These include resources like the FDA DailyMed in the United States or the EMA and MHRA websites internationally.


Q: Is Letrofam a newly approved drug, or has it been around for a while?

Letrofam (Letrozole) is not a newly approved drug; it was initially approved for medical use by the FDA in 1996. It belongs to the class of medications known as third-generation aromatase inhibitors.


Q: Is Letrofam known to cause any long-term effects after stopping treatment?

Official documents indicate that long-term risks associated with sustained estrogen deprivation, such as high cholesterol or decreased bone mineral density (osteoporosis), may persist or take many months to diminish or stabilize after cessation.


Q: Do I need to get blood tests while taking Letrofam?

Regulatory documents state that frequent medical monitoring is typically required during treatment with Letrofam. Your healthcare team may periodically check your cholesterol levels and bone mineral density to monitor for potential changes.


Q: Is it true that Letrofam is sometimes used for fertility purposes?

The official regulatory indications for Letrofam are restricted to the treatment of breast cancer in postmenopausal women. The drug is not officially approved for use for other purposes outside of these indications.


Q: Is there a generic version of Letrofam available?

Yes, the active ingredient in Letrofam is Letrozole, which is available in a generic oral tablet formulation.


Q: Does the time of day I take Letrofam matter?

Letrofam is administered once daily. Regulatory information recommends taking the dose at approximately the same time each day to help maintain consistent drug levels in the body.


Q: What is Letrofam's safety classification?

Letrofam is officially classified as contraindicated in pregnancy and in women who are premenopausal. Its safety profile is defined by long-term risks associated with sustained estrogen deprivation, including the potential for osteoporosis and thromboembolic events.


Q: Is it common for people to switch from a different medicine to Letrofam?

Yes, one of the official approved uses for Letrofam is known as extended adjuvant treatment. This use is specifically indicated for postmenopausal women who have completed five years of prior standard adjuvant therapy with tamoxifen.


Q: How does Letrofam affect sleep?

The product's safety information lists difficulty sleeping, or insomnia, as an uncommon side effect. Additionally, reports of somnolence (sleepiness) have been included in the official adverse reaction summaries.


Q: Does Letrofam affect blood pressure?

Yes, regulatory documents report that high blood pressure, known as hypertension, has been listed as a serious side effect that may be caused or worsened by the drug.


Q: Is there any evidence about the effectiveness of Letrofam in different ethnic groups?

Regulatory summaries of the clinical data generally do not contain specific information about the effectiveness or differences in the pharmacokinetics (how the body processes the drug) due to race or ethnicity.

How should Letrofam be stored and disposed of?

Letrofam (Letrozole Tablets) requires specific conditions to preserve its stability and must be handled and disposed of according to official regulatory guidelines.

Storage Conditions

Requirement Details
Temperature Store at Controlled Room Temperature: 20 C to 25 C (68 F to 77 F). Temporary variations up to 30 C (86 F) are permitted.
Protection Keep away from excessive heat, moisture, and direct light.
Container Keep the medication in the original container, and ensure it is tightly closed.
Safety Must be kept out of the sight and reach of children.

Disposal Instructions

Unused or expired Letrofam must be disposed of according to local regulations. Do not dispose of the tablets via household wastewater or flush them down the toilet. Consult a healthcare professional or pharmacist regarding local take-back programs or appropriate methods for discarding the medicine to protect the environment.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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