Lostar

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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 Lostar

Quick Facts

Property Description
Active ingredient Letrozole (INN)
Form Oral, film-coated tablet
Pharmacological class Third-generation Aromatase Inhibitor (AI)
Common purpose Systemic estrogen level reduction
Origin Synthetic, nonsteroidal

Lostar: Definition and Pharmacological Classification

Lostar is a pharmaceutical product whose active substance is the International Nonproprietary Name (INN) compound Letrozole. It is classified as a third-generation nonsteroidal Aromatase Inhibitor (AI). This drug belongs to the broader class of antineoplastic agents, meaning it is designed to address abnormal cellular growth by intervening in hormonal pathways.

Letrozole possesses an exceptionally high selectivity, achieving one of the most potent inhibitions of the aromatase enzyme system available. This advanced design minimizes off-target effects on the synthesis of other necessary adrenal hormones, a key differentiator from older generation inhibitors.

Composition, Origin, and Dosage Form

The core component of Lostar is the single active ingredient, Letrozole, which is a synthetic triazole derivative. The drug is supplied for patient use as an oral, film-coated tablet, a solid dosage form intended for systemic administration. This oral bioavailability is a factor for patient adherence and consistent systemic delivery.

Each tablet is formulated using standard pharmaceutical excipients, such as lactose monohydrate, combined with the active compound to ensure stability and reliable delivery. The precise, nonsteroidal chemical design allows for efficient absorption and targeted action against its specific biological target.

General Purpose of an Aromatase Inhibitor

The general purpose of Lostar is to achieve a profound, systemic reduction of estrogen levels in the body, typically utilized for postmenopausal women where estrogen is primarily produced peripherally. This is accomplished by the Letrozole actively and competitively inhibiting the aromatase enzyme. This medicine serves as an agent for lowering estrogen levels.

This physiological action prevents the final, critical step in the biosynthesis of estrogen, stopping the conversion of precursor androgens into active hormones like estradiol. The resulting low level of circulating estrogen effectively removes the primary hormonal stimulus for cells classified as estrogen-dependent.

Regulatory References

  1. MedlinePlus Letrozole Patient Information

What side effects are possible with Lostar?

Possible Side Effects and Safety Information

Lostar's official safety profile, as documented in regulatory sources like the EMA Summary of Product Characteristics (SmPC) and FDA prescribing information, organizes adverse reactions by frequency and affected body system. Most documented effects are associated with the drug's mechanism of reducing systemic estrogen levels.


Adverse Reaction Scope

The most frequently reported adverse reactions are classified as Very Common (1/10) or Common (1/100 to < 1/10).

Frequency Category Representative Adverse Reactions
Very Common Hot flashes, Hypercholesterolaemia (high cholesterol), Arthralgia (joint pain), Fatigue, Hyperhidrosis (increased sweating).
Common Headache, Nausea, Vomiting, Constipation, Osteoporosis, Bone fractures, Peripheral oedema, Vaginal haemorrhage.

These effects primarily involve Musculoskeletal and connective tissue disorders, Vascular disorders, and Metabolism and nutrition disorders.


Serious Adverse Reactions and Restrictions

Serious concerns highlighted in regulatory labeling include Thromboembolic events (like pulmonary embolism), Ischaemic cardiac events (including myocardial infarction), and the increased risk of Bone fractures related to long-term use and decreased bone mineral density (BMD).

Population-Specific Safety: Lostar is formally contraindicated in women with a premenopausal endocrine status, and in those who are pregnant or breastfeeding. Patients with severe hepatic impairment are identified as requiring close supervision due to reduced drug clearance.

Safety Monitoring: Official documents state that monitoring of both BMD and serum cholesterol should be considered during the course of treatment. The risk of bone fracture and the elevation of cholesterol are among the most serious documented safety concerns associated with extended exposure.

Overdose and Emergency Response

Overdose and when to seek help

The regulatory profile for Lostar (Letrozole) overdose is based on limited available human data and explicit emergency instructions. Official documents state that a reported case of high-dose oral ingestion, specifically up to 62.5 mg, was not associated with serious adverse reactions.

Classification Official Regulatory Statement
Severity Not associated with serious adverse reactions in documented cases.
Antidote No specific antidote is known for this medication.

Immediate Actions and Management

If a suspected overdose occurs, or if someone accidentally takes the tablets, individuals must seek immediate medical attention and contact a doctor or hospital for advice immediately. If the individual collapses, has a seizure, or has trouble breathing, emergency services must be called.

Management of the situation should consist of symptomatic and supportive treatment. This includes close medical supervision and monitoring of vital signs until the patient is stable. Procedural interventions, such as gastric lavage, are considered only if medically indicated by a healthcare professional.

Therapeutic Uses of Lostar

What Lostar Treats: Main Uses and Benefits

Lostar is commonly used in therapeutic domains addressing the management of hormone receptor-positive breast cancer, primarily in postmenopausal women. The medication is applied across several clinical contexts: as an adjuvant treatment following primary therapy, in extended adjuvant therapy after prior antiestrogen use, as first-line systemic therapy for advanced disease, and in the neoadjuvant setting to achieve tumor shrinkage. The medication is relevant for easing the symptoms related to systemic imbalance associated with hormone-sensitive conditions and addressing the long-term risk of recurrence following initial treatment. The benefit contributes to improved comfort during symptomatic periods and supports the patient's ability to maintain a sense of stability.

“The therapeutic intent is relevant for conditions marked by increased physiological stress associated with hormone-sensitive disease.”


Quick Fact: Support for Disease Management Context Main Therapeutic Benefit
Adjuvant Use Supports the patient during difficult episodes by easing distress related to recurrence risk.
Metastatic Use Assists with maintaining functional stability in advanced contexts.
Neoadjuvant Use Provides supportive relief when symptoms interfere with routine activities related to pre-surgical preparation.

Regulatory References

  1. official FDA label information on Letrozole

Eligibility and Restrictions for Use

Lostar (Letrozole) is officially approved for use exclusively in women of confirmed postmenopausal endocrine status. Eligibility for the medicine is strictly defined by regulatory authorities based on reproductive status, organ function, and specific comorbidities.

Populations Who Must Not Use Lostar (Contraindications)

Classification Population Status
Reproductive Status Premenopausal Women Contraindicated
Physiological State Pregnancy or Lactation Contraindicated
Allergy Known Hypersensitivity Contraindicated

Eligibility Conditions and Restrictions

  • Organ Function: Use is permitted in mild to moderate liver impairment, but patients with severe hepatic impairment (Child-Pugh C) require close supervision. Use in severe renal impairment ( CrCl < 10 mL/ min) is not established due to insufficient data.
  • Age: The medicine is not recommended for use in children and adolescents as safety and efficacy have not been established. No dose adjustment is required for older adults.
  • Comorbidities: Women with a history of osteoporosis or at risk of bone fractures must have their bone mineral density (BMD) assessed and monitored during treatment. Cholesterol monitoring may also be considered.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The following medically significant interactions are officially documented for Lostar, strictly based on regulatory guidance. These interactions may affect the efficacy of Lostar or the co-administered medication, and in some cases, increase the risk of adverse effects.

Documented Interaction Domains

Interacting Product Category Regulatory Requirement/Constraint
Potassium-Sparing Agents (e.g., potassium supplements, triamterene, spironolactone) Concomitant use increases the documented risk of hyperkalemia (high serum potassium levels). Avoid these products.
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) May reduce the blood pressure-lowering effect of Lostar. Co-administration increases the documented risk of worsening kidney function, particularly in older or volume-depleted individuals.
Lithium Lostar decreases the documented renal clearance of lithium, leading to increased lithium concentrations. Close monitoring of serum lithium levels is required.
Other RAS Blockers (e.g., Aliskiren) Concomitant use with Aliskiren is officially contraindicated in patients with diabetes or moderate-to-severe kidney impairment (GFR < 60 ml/min/1.73m^2).
Rifampin (Rifampicin) This medication may decrease the concentration of the active form of Lostar, potentially reducing its effectiveness.

Official Monitoring and Constraints

Official regulatory information emphasizes that the combination of Lostar with other agents affecting the Renin-Angiotensin System (RAS) or potassium balance carries a risk of additive effects, mandating specific avoidance rules and careful laboratory supervision. Close monitoring of kidney function and potassium levels is required when co-administering with NSAIDs or potassium-sparing agents. Additionally, strict monitoring of serum lithium is necessary due to altered drug excretion.

Mechanism of Action

Selective Angiotensin II Receptor Blockade

The mechanism operates within the Renin-Angiotensin System (RAS). The compound and its active metabolite, EXP3174, achieve their effect by acting as a highly selective, competitive antagonist at the AT1 receptor site.


Modulating Key Vasoconstrictive Pathways

By preventing the hormone angiotensin II from binding to the AT1 receptor on smooth muscle, the drug interrupts the signaling sequence that typically causes blood vessel tightening (vasoconstriction). This engagement of receptor-mediated signaling pathways results in vascular smooth muscle relaxation and vessel widening.


Systemic Hemodynamic and Fluid Regulation

Blocking the AT1 receptor also suppresses other angiotensin II-mediated effects, including the stimulation of aldosterone release from the adrenal glands. This disruption of the hormonal cascade alters the downstream physiological consequences involving sodium and water retention.


Influencing End-Organ Cellular Signaling

The mechanism influences processes within organs like the heart and kidneys that are subject to chronic AT1 receptor activation. The compound engages mechanisms that influence cellular hypertrophy (enlargement) and hyperplasia, modulating the structural changes associated with overactive or dysregulated signaling processes.

Dosage and Administration Information

How Lostar is Administered

Lostar is an oral medication with a standardized usage protocol, defined by its formulation as a 2.5 mg film-coated tablet. This strength is the standard recommended daily dose for all major approved indications.

Dosing and Schedule

The official regimen specifies that the tablet must be taken once daily, a frequency designed for continuous systemic delivery. The medication may be taken with or without food, providing flexibility in daily scheduling. Proper administration requires the tablet to be swallowed whole, as crushing or chewing is not indicated in the administration guidelines.

Duration and Adjustments

The duration of use is explicitly tied to the therapeutic context. For adjuvant and extended adjuvant therapy, administration is typically continued for a period of up to five years. Conversely, use in advanced or metastatic disease is typically maintained until disease progression is confirmed.

A specific dose adjustment is mandated for certain patient populations. For individuals with severe hepatic impairment, the official protocol requires a reduced frequency to 2.5 mg every other day to manage exposure. No change to the standard regimen is needed for elderly patients or those with mild-to-moderate renal impairment.

Handling Missed Doses

The established protocol for a missed dose is to resume the normal schedule. If the time until the next scheduled dose is less than approximately 2 to 3 hours, the missed dose should be skipped to avoid doubling the daily intake.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Lostar

Evidence for Use as Initial Therapy in Advanced Cancer

This section summarizes the types of high-level studies that have investigated Lostar as the first systemic treatment for postmenopausal women with advanced, hormone receptor-positive breast cancer. Researchers designed large, multi-site Randomized Controlled Trials (RCTs) to examine what outcomes were observed for patients in this situation.

The research examined several core outcomes related to the course of the condition. Studies monitored the Time to Disease Progression (TTP), and documented the Objective Response Rate (RR), which involves measuring tumor shrinkage. Furthermore, studies monitored Overall Survival (OS) of the participants. Studies report how TTP and survival measurements evolved in the observed populations, with specific measurements documented over the observation period.

Evidence for Use in Adjuvant Treatment for Early-Stage Cancer

This block details the structure of the research base, including large-scale clinical trials, which focused on using Lostar after initial treatment (like surgery) for early-stage hormone receptor-positive breast cancer. These long-term, international RCTs were applied in studies examining patient experiences over many years.

The main outcomes studied focused on measuring Disease-Free Survival (DFS), which tracks recurrence events, and Overall Survival (OS). Studies report how DFS and OS rates evolved in the observed populations over follow-up periods that often extended to eight years or more. A key limitation for some of the longest studies is that a certain number of patients sometimes discontinue the study medication early, which may be a factor in the final outcomes analysis.

What Is Still Uncertain About the Research for Lostar

The evidence quality varies across studies, with some indications supported by large Randomized Controlled Trials (RCTs), while others rely on smaller or shorter-term trials. Long-term effects are not fully established for all outcomes, particularly in the extended adjuvant setting where patient crossover was documented. Also, there is limited information for certain groups. The results apply only to the specific populations studied, and findings describe group patterns, not individual predictions. This section highlights what is known—and what is still uncertain—about the existing research.

Key Studies & References

  1. Letrozole Oral Tablet Official FDA Label Information
  2. Pharmacological Classification and Mechanism of Action: Aromatase Inhibitors (General)

Frequently Asked Questions (FAQ)

Common questions about Lostar (FAQ)


Q: What is the main condition or problem that Lostar is intended to treat?

According to official regulatory labeling, Lostar (Letrozole) is indicated for the treatment of hormone receptor-positive breast cancer in women who are confirmed to be postmenopausal. This includes its use as both an initial therapy (first-line) and as subsequent treatment (adjuvant or extended adjuvant).


Q: Is Lostar in the same group of medicines as common blood pressure drugs?

No, Lostar is not classified with common blood pressure medications. Its classification is a nonsteroidal Aromatase Inhibitor, which works by reducing estrogen levels in the body. Its chemical composition and pharmacological action are fundamentally different from drugs used to manage hypertension.


Q: How is Lostar different from other similar medicines used for the same purpose?

Official documents describe Lostar (Letrozole) as a highly selective, nonsteroidal Aromatase Inhibitor. The medicine is recognized for achieving highly selective and potent inhibition of the aromatase enzyme, a feature that differentiates it from some older classes of hormone-blocking therapies.


Q: Is it normal to feel dizzy or lightheaded when first taking Lostar?

Yes, official drug labeling lists dizziness as a common adverse reaction. Due to the potential for dizziness, fatigue, and somnolence (drowsiness), official warnings state that caution is required when driving or operating machinery.


Q: Do the side effects of Lostar generally go away after the first few weeks?

Patient information states that these effects are typically mild to moderate and may improve or resolve after a few days to a few weeks of continuous treatment. Most adverse events are associated with the drug's mechanism of reducing systemic estrogen levels.


Q: Does Lostar cause weight gain or weight loss?

Regulatory-based patient information lists changes in weight as a potential side effect. While clinical trial data indicates that both weight gain and weight loss have been reported, these changes were observed in a minority of the study population.


Q: What does official guidance say about consuming alcohol while taking Lostar?

Official patient guidance states there is no specific evidence that drinking alcohol causes problems with Lostar. However, official guidance states that alcohol should be avoided if it is found to worsen side effects, such as hot flashes or dizziness.


Q: How quickly should a person expect Lostar to start showing its effects?

Lostar (Letrozole) acts quickly to suppress the aromatase enzyme once administered. However, it typically takes approximately 2 to 6 weeks of consistent daily dosing for the medicine to reach a stable, steady concentration in the blood, which is necessary for the continuous maintenance of the full pharmacological effect.


Q: How long does it typically take to reach the full or maximum effect of Lostar?

The maximum reduction in circulating estrogen levels—the drug's intended pharmacological action—is generally seen once the stable drug concentration is achieved. According to regulatory pharmacokinetics data, this steady state occurs in about 2 to 6 weeks after starting the standard daily regimen.


Q: Is there a Black Box Warning or a similar high-level safety alert associated with Lostar?

Lostar (Letrozole) does not carry an FDA Black Box Warning. However, the official drug labeling does include specific Warnings and Precautions sections regarding important risks, such as a possible decrease in bone mineral density and increases in cholesterol levels.


Q: Are there different brand names for Lostar, and are they medically the same?

Yes, the active ingredient in Lostar is the compound Letrozole, which is also marketed under the brand name Femara®. The FDA has approved generic versions, and these are considered to be therapeutically equivalent to the brand product.


Q: Why are there different strengths (milligrams) of Lostar available?

Regulatory documents define the standard recommended daily dose for approved cancer indications as 2.5 mg. While other doses were studied during development, the 2.5 mg strength is the only standard approved strength listed by the FDA for oncology use, as it has been shown to achieve maximum estrogen suppression.


Q: Is Lostar considered a generic drug, and what does that mean?

Yes, Lostar (Letrozole) is available as a generic drug. Being generic means the medicine contains the identical active ingredient, strength, and dosage form as the original brand name product, and it is usually available at a lower cost.


Q: Does Lostar cause a persistent cough, unlike some other similar medications?

Official lists of adverse reactions and patient information indicate that cough has been reported as a possible side effect of Lostar (Letrozole). While not one of the most common events, it is a reaction that has been documented in clinical settings.


Q: Does Lostar affect sleep or cause insomnia?

Yes, regulatory-based patient information lists difficulty falling asleep or staying asleep (insomnia) as a potential side effect. This is noted along with other central nervous system effects such as dizziness and fatigue.


Q: What is the risk of stopping Lostar treatment suddenly?

Regulatory sources emphasize that the use of Lostar is typically continuous and long-term. Abrupt discontinuation of the treatment is not recommended in official guidelines, as the medication is a key part of the therapeutic plan.


Q: Why is Lostar often used as a first-line treatment for certain conditions?

Lostar (Letrozole) is explicitly approved by regulatory authorities for use as a first-line treatment for postmenopausal women with hormone receptor-positive advanced or metastatic breast cancer. This approval is based on the evidence presented in pivotal clinical trials.


Q: Is it common for people to switch from a different drug to Lostar?

Yes, one of the official approved indications for Lostar is for use in women who have already completed five years of prior adjuvant therapy with another hormone drug, such as tamoxifen. This means the drug is documented and approved for use in a switching scenario.


Q: Does Lostar have any known effects on libido or sexual function?

Official drug monographs mention that the hormonal mechanism can affect the endocrine system. Animal studies have reported effects on fertility and related hormonal parameters.


Q: What is the general information about overdosing on Lostar?

Regulatory patient information states that in case of a suspected overdose of Lostar (Letrozole), immediate contact with the Poison Control Helpline or emergency services is the required protocol.


Q: Does taking Lostar affect one's ability to drive or operate machinery?

Yes, Lostar (Letrozole) may cause side effects like fatigue, dizziness, and somnolence (drowsiness). Official warnings state that caution is required when driving or operating machinery because of these potential side effects.


Q: Are there any specific vitamins, minerals, or supplements that interact with Lostar?

The official product information notes that using potassium-sparing agents or estrogen-containing supplements is a potential interaction. Regulatory documents emphasize the importance of communicating all supplements, vitamins, and herbal products being taken.


Q: What does the term 'contraindication' mean when discussing Lostar?

A contraindication defines specific conditions or patient populations for whom the risk of taking the medicine is known to outweigh any potential benefit. For Lostar, official documents state that premenopausal women and those who are pregnant are formally listed as being contraindicated.


Q: Is it necessary to take Lostar at the exact same time every day?

Lostar is prescribed to be taken once daily to maintain a consistent level of the medicine in the body. Patient resources recommend taking the tablet around the same time every day to support this continuous effect.


Q: Can Lostar be taken with other medicines that are also prescribed for high blood pressure?

The official interaction information specifically details interactions with certain classes of blood pressure-related drugs, such as NSAIDs and other Renin-Angiotensin System (RAS) blockers. These combinations require careful consideration due to potential effects on blood pressure control and kidney function.


Q: What does the research say about Lostar's impact on cardiovascular outcomes?

Data from clinical trials reports that thromboembolic events (blood clots) and ischemic cardiac events (heart-related issues) are listed as serious adverse reactions associated with Lostar (Letrozole) use. These findings are included in regulatory documents as a key safety consideration for the medication.

How should Lostar be stored and disposed of?

Storage and Disposal Requirements

Lostar (Letrozole) must be stored according to specific regulatory requirements to maintain its stability. The tablets should be kept at controlled room temperature, typically 25 C (77 F) , with permitted excursions between 15 C and 30 C.

Storage Rule Protection Mandate
Store in original container Protect from moisture
Keep container tightly closed Keep out of reach of children

Storage must be in a dry place and away from excessive heat. Do not use the medicine past the expiry date printed on the packaging. Disposal of unused or expired Lostar must follow local regulatory instructions for pharmaceutical waste. To protect privacy, all personal information must be scratched out from the prescription label before the container is discarded.

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

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