Eribulin

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Eribulin

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

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 Eribulin

Property Description
Active ingredient Eribulin mesylate (INN)
Form Solution for injection (clear, colorless)
Pharmacological class Antineoplastic agent, Microtubule dynamics inhibitor
Common use Systemic treatment for advanced cancer
Origin Synthetic analog of the marine natural product Halichondrin B

Eribulin mesylate is a specialized chemotherapy medication that belongs to the antineoplastic agent class, functioning as a unique microtubule dynamics inhibitor to fight cancer cell growth. The drug is classified as a cytotoxic agent, meaning its primary action is to disrupt and kill rapidly dividing cells within the body.


What Type of Medicine is Eribulin Mesylate?

Eribulin mesylate is a laboratory-produced compound, designated as a synthetic analog of the potent natural substance Halichondrin B, which was originally isolated from marine sponges. This means the chemical structure was carefully synthesized to achieve a stable and potent pharmaceutical product. The medication is formulated as a sterile solution for injection for intravenous (IV) administration and is structurally recognized as a non-taxane inhibitor. This distinct chemical profile is clinically recognized for providing therapeutic benefits in patients whose disease has progressed despite prior treatment regimens.


Understanding Eribulin's Function and General Purpose

The general purpose of Eribulin in oncology is directly linked to its capacity to halt cell replication, thus serving to slow the progression of the disease and reduce the overall tumor burden. The mechanism is rooted in the drug's unique ability to bind to the cell's internal 'scaffolding' proteins, known as microtubules, preventing their necessary growth. By forcing cells to undergo apoptosis, or programmed cell death, Eribulin provides systemic treatment for advanced stages of the disease when other options may be limited, focusing on stabilizing patient condition and mitigating tumor growth.

Regulatory References

  1. NIH: Eribulin Drug Review

What side effects are possible with Eribulin?

Eribulin: Possible Side Effects and Safety Information

This section describes the officially documented adverse reactions and safety characteristics of eribulin mesylate as classified by government regulatory authorities.


Official Adverse Reaction Scope

The safety profile is primarily defined by effects on the Blood and Lymphatic System Disorders and Nervous System Disorders. Adverse reactions are categorized by frequency based on clinical study data:

  • Very Common (May affect more than 1 in 10 people): Includes Neutropenia (low white blood cell count), Anemia, Asthenia/Fatigue, Alopecia (hair loss), Peripheral Neuropathy (numbness or tingling), and common Gastrointestinal Disorders (nausea, constipation).
  • Common (May affect up to 1 in 10 people): Includes Febrile Neutropenia, Thrombocytopenia, Vomiting, Diarrhea, and increases in liver enzymes (AST/ALT increased).

Serious Safety Considerations

The official labeling highlights several serious adverse reactions. Severe Neutropenia is a prominent safety concern, associated with the potential for life-threatening infections, including fatal neutropenic sepsis. Eribulin is also formally associated with dose-dependent QT Interval Prolongation, which increases the risk of severe ventricular arrhythmias. Due to the mechanism of action, the drug is expected to cause Embryo-Fetal Toxicity.

Population and Cumulative Safety Notes

Specific safety considerations exist for certain populations. Patients with Hepatic Impairment and Renal Impairment may experience a higher incidence of severe neutropenia, which may necessitate a lower starting dose as specified in regulatory documents. Furthermore, Peripheral Neuropathy is noted to be associated with the cumulative dose of the drug received over the course of treatment. The use of eribulin must be avoided in individuals with congenital long QT syndrome.

Overdose and Emergency Response

Eribulin Overdose and When to Seek Help

The information regarding Eribulin overdose is primarily derived from non-clinical data, as controlled human overdose studies are not available. This section reflects the guidance provided in official regulatory documents concerning the management of potential overexposure.


Documented Overdose Considerations

Consideration Official Regulatory Statement
Anticipated Manifestations Non-clinical studies identified dose-related mortality associated with severe myelosuppression (low white blood cell and platelet counts), ataxia (loss of muscle control), and paralysis following high exposure.
Physiological Systems Affected Primarily the hematopoietic system (bone marrow suppression) and the nervous system. Cardiac monitoring is also generally advised due to the drug's known risk for QTc prolongation.

Required Emergency Action

There is no specific antidote for Eribulin overdose.

In the event of a suspected overdose, the patient must be kept under close observation. Treatment is strictly supportive and symptomatic. Immediate medical attention is necessary to manage anticipated complications such as life-threatening myelosuppression and potential cardiotoxicity. Supportive measures involve frequent monitoring of complete blood cell counts and symptomatic management of any arising toxicities, including neurological changes.

Therapeutic Uses of Eribulin

What Eribulin Treats: Main Uses and Benefits

Eribulin is commonly used to help with specific advanced or metastatic cancers. The primary therapeutic purpose of Eribulin is relevant for easing symptoms linked to organ-specific functional stress associated with these conditions characterized by periods of heightened symptoms.

The medicine is considered relevant for two main therapeutic areas: locally advanced or metastatic breast cancer (after progression from previous treatment) and advanced or metastatic liposarcoma, a type of soft-tissue cancer, in adult patients who have received prior chemotherapy.

Eribulin may assist with maintaining a sense of stability when symptoms are more noticeable, especially in clinical settings that involve acute or unstable symptom patterns. This approach contributes to easing the overall symptom load associated with systemic or localized discomfort, supporting patients during episodes of heightened discomfort.


Quick Fact: Relief for Symptoms that Create Noticeable Physiological Strain

Regulatory References

  1. European Medicines Agency (EMA) overview of Halaven's uses

Eligibility and Restrictions for Use

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

Regulatory agencies strictly define the populations eligible to use Eribulin mesylate.


Eligibility Scope

Classification Population Rule (As Stated in Label)
Populations Contraindicated Women who are breastfeeding and patients with known hypersensitivity to Eribulin or its excipients.
Absolute Avoidance Patients with congenital long QT syndrome [FDA Label].
Age-Related Rules Approved for Adult patients only. Use is not recommended in the pediatric population (children and adolescents) as efficacy and safety have not been established.
Pregnancy Status Not recommended during pregnancy due to expected fetal harm (embryo-fetal toxicity). Women of childbearing potential and men must use effective contraception.

Condition-Specific Requirements

Condition Type Required Restriction or Pre-treatment Status
Organ Function Lower initial starting doses are recommended for patients with mild-to-moderate hepatic impairment or moderate-to-severe renal impairment.
Pre-treatment Status Treatment initiation is conditional upon meeting specific baseline blood cell counts (Absolute Neutrophil Count ge 1.5 imes 10^9/ L and platelets > 100 imes 10^9/ L).

The regulatory structure clearly defines Eribulin as an adult-only medicine, establishing absolute exclusions based on reproductive status and hypersensitivity. Eligibility is conditional on the patient's baseline hematological status and organ function, ensuring use only in populations meeting the specific health thresholds documented in the official prescribing information.

What should I know about interactions with other medicines?

Eribulin Interactions with other medicines and products

The official regulatory documents define the interaction profile of Eribulin around specific administration rules and the potential for a pharmacodynamic (PD) risk. A key restriction is the incompatibility with certain solutions: Eribulin must not be diluted in or administered with dextrose-containing solutions. Furthermore, it must not be administered concurrently with any other medicinal products in the same intravenous line.

From a metabolic and enzyme standpoint, Eribulin exposure is largely unaffected by co-administration with strong inhibitors or inducers of the CYP3A4 enzyme (such as ketoconazole or rifampicin), suggesting that no clinically relevant pharmacokinetic interaction is expected through these major pathways. However, Eribulin is classified as a mild inhibitor of CYP3A4 in vitro, leading to a formal caution when used with other medicines that are predominantly cleared via CYP3A4 and possess a narrow therapeutic window.

A primary pharmacodynamic interaction risk involves the cardiac system. Co-administration with agents known to prolong the QT interval, including Class Ia and Class III antiarrhythmics, increases the risk of additive QT prolongation. Due to this risk, use is formally advised to be avoided where possible, and pre-existing electrolyte abnormalities, such as hypokalemia or hypomagnesemia, must be corrected before starting therapy. Use is also advised to be avoided in patients with congenital long QT syndrome.

The profile includes population-specific findings: Eribulin exposure is officially documented to be increased in patients with mild or moderate hepatic impairment and moderate or severe renal impairment, a finding that requires a modified starting dose. The label states no known interactions with food or drinks.

Mechanism of Action

Eribulin mesylate functions as a non-taxane microtubule dynamics inhibitor. Its primary biological target is the beta-tubulin subunit. The drug binds selectively to the high-affinity site located at the positive (+) ends of the growing microtubules. This interaction type suppresses the growth phase of the microtubules without affecting the shortening phase.

This molecular action causes the formation of non-productive tubulin aggregates within the cell. The subsequent intracellular cascade involves the arrest of the cell cycle at the G2/ M phase checkpoint, ultimately triggering the programmed cell death pathway, known as apoptosis.

Beyond its core antimitotic activity, Eribulin modulates the tumor microenvironment. This includes the system-level physiological consequence of modulating tumor vasculature. The drug also mediates the reversal of the mesenchymal phenotype to an epithelial-like phenotype, a process referred to as Mesenchymal-to-Epithelial Transition (MET), by influencing gene expression profiles.

Dosage and Administration Information

Eribulin mesylate is administered solely by the intravenous (IV) route as a solution for injection, typically infused over a brief period of 2 to 5 minutes. The standard approach to its use is based on a 21-day treatment cycle.

The initial dose is precisely calculated based on the individual's body surface area (BSA), with the standard starting dose being 1.4 mg/m^2 (eribulin mesylate salt basis) or 1.23 mg/m^2 (eribulin base, used in European guidelines). This dose is administered on Day 1 and Day 8 of the cycle, followed by a rest period.

The official instructions detail specific preparation requirements. The solution may be given undiluted or, if necessary, diluted in 100 mL of 0.9% Sodium Chloride Injection, USP; it must not be administered in or mixed with any solutions containing dextrose. Furthermore, the drug must not be administered concurrently with other medicinal products in the same IV line.

The regimen requires strict procedural adherence. A complete blood cell count must be assessed prior to each dose to determine eligibility for treatment. For ongoing treatment, the dosage is permanently reduced if necessary due to specific clinical events, and there is an explicit rule that the dose must not be re-escalated after it has been lowered. Population-specific dose adjustments are mandatory for patients with hepatic or renal impairment. Treatment continues under this structured cyclic regimen until permanent discontinuation is required.

Recent Clinical Evidence

Eribulin: Recent Clinical Evidence

Clinical evidence for Eribulin, a synthetic analogue of a natural product, has focused on its use in treating metastatic breast cancer (mBC) and liposarcoma (LPS).


Metastatic Breast Cancer (mBC)

The Phase III EMBRACE trial was a key study that investigated Eribulin in women with heavily pretreated mBC. The study results suggested an improvement in overall survival (OS) when compared to treatment of physician's choice (TPC). In an updated analysis, the median OS for the Eribulin group was observed to be longer than that of the TPC group, providing data on the drug's use after previous lines of chemotherapy that typically included an anthracycline and a taxane.

Further analyses have investigated the effects of Eribulin in specific subgroups, such as patients with Triple-Negative Breast Cancer (TNBC), where the agent showed favorable outcomes in some cohorts.


Liposarcoma (LPS)

The use of Eribulin in treating unresectable or metastatic liposarcoma was evaluated in a Phase III trial comparing it to dacarbazine. This study generally focused on patients who had previously received an anthracycline-containing regimen. The findings indicated a longer median overall survival in patients with liposarcoma who received Eribulin compared to the control group.

Subgroup analysis from this trial suggested a greater effect in certain types of liposarcoma, such as dedifferentiated and pleomorphic subtypes.


General Safety Findings in Studies

Across the major clinical trials, Eribulin's safety profile has been documented. Common adverse events observed in the research included neutropenia (low white blood cell count) and peripheral neuropathy (nerve damage), with the majority being Grade 1 or 2 in severity. Monitoring for these conditions was a standard part of the trial protocols.

Frequently Asked Questions (FAQ)

Common questions about Eribulin (FAQ)

Q: Why is Eribulin sometimes referred to by its brand name, Halaven?

A: Eribulin is often referred to by the brand name Halaven. Halaven is the registered commercial name for the medicine that contains the active substance Eribulin mesylate. This is a common practice in medicine, where the generic name is the active substance and the brand name is the product's trademark.

Q: What is the typical duration of Eribulin-related fatigue or weakness?

A: Fatigue (asthenia) is listed in official documents as a very common side effect. Regulatory sources do not provide a specific timeline for how long this tiredness lasts. However, clinical information suggests that fatigue may continue for a period even after the treatment regimen is complete.

Q: What are the signs of a low white blood cell count related to Eribulin?

A: Eribulin treatment can be associated with severe neutropenia, which is a significant drop in infection-fighting white blood cells. Official regulatory documents advise that patients should be aware of signs such as fever or other indications of infection, as monitoring for these is necessary due to the risk of severe neutropenia (low white blood cell count).

Q: Is hair loss (alopecia) permanent after stopping Eribulin?

A: Hair loss, or alopecia, is a very common side effect noted in official product information. While the sources do not explicitly state if the hair loss is permanent, general patient information suggests that hair often begins to regrow after Eribulin therapy is discontinued.

Q: What common side effects of Eribulin are generally described as "manageable"?

A: The drug's safety profile, based on regulatory data, documents common adverse reactions such as fatigue, nausea, and peripheral neuropathy. These events are often described in trials as mild-to-moderate (Grade 1 or 2), which suggests they are often addressed with supportive care.

Q: What are the signs of a mineral or electrolyte imbalance that may be caused by Eribulin?

A: Eribulin has been associated with imbalances, specifically low potassium (hypokalemia) and low magnesium (hypomagnesemia). Official documents advise that these imbalances are typically corrected before starting therapy because they can increase the risk of serious heart rhythm changes, even if the specific symptoms of the imbalance are not detailed.

Q: Is joint or muscle pain a known side effect of Eribulin?

A: Yes, both joint pain (arthralgia) and muscle pain (myalgia) are reported as common side effects in the official regulatory documents for Eribulin.

Q: Can Eribulin cause changes in taste or loss of appetite?

A: Changes in taste, known as dysgeusia, and a loss of appetite, or anorexia, are listed as common side effects in the official product information for Eribulin.

Q: Are there any known lung problems or breathing issues associated with Eribulin?

A: Official product information reports common respiratory side effects such as cough and dyspnea (shortness of breath). These effects, if they occur, are typically managed by a healthcare provider.

Q: Is it true that Eribulin can cause dizziness or vertigo?

A: Yes, dizziness is listed as a common side effect of Eribulin in regulatory documents. This type of effect is documented under the nervous system disorders.

Q: How long after the last infusion do people typically see improvement in numbness and tingling?

A: Peripheral neuropathy (numbness and tingling) is a common side effect that may be linked to the total amount of drug received over time. Regulatory documents indicate that while symptoms may slowly lessen after treatment is stopped, neuropathy has been noted to persist for an extended duration in certain instances.

Q: Are there any specific non-prescription supplements that should be avoided with Eribulin?

A: Official product information states that concomitant use of St John’s wort is not recommended. This is because this non-prescription supplement may potentially reduce the amount of Eribulin in the body.

Q: Is it necessary to limit alcohol intake while on Eribulin?

A: The Eribulin solution does contain a very small amount of ethanol (alcohol) in its formulation. However, official regulatory documents state that the amount of alcohol present is generally too small to have any noticeable or relevant effect.

Q: What is the recommended period for women to use contraception after stopping Eribulin?

A: Official information advises that females who can become pregnant should use effective birth control throughout the treatment period. This effective contraception should be continued for at least 2 weeks following the final dose of Eribulin.

Q: What is the recommended period for men to use contraception after stopping Eribulin?

A: Official information advises that males with female partners who can become pregnant should use effective birth control throughout the treatment period. This effective contraception should be continued for 3.5 months following the last dose of Eribulin.

Q: How soon after starting treatment might a patient notice any effect, based on research themes?

A: Official clinical trial data provides a measure of how long patients in the study lived without their disease worsening (Progression-Free Survival, or PFS). For example, the median PFS in the key metastatic breast cancer trial was reported as 3.7 months.

Q: Is there ongoing research into new uses for Eribulin?

A: Yes, official summaries and publicly available databases indicate that Eribulin continues to be investigated. Ongoing clinical studies are examining its use in various cancer types, different combination therapies, and alternative dosing approaches.

Q: Why is Eribulin sometimes discussed in the context of different dosing standards (mg vs mg/m2)?

A: The dose is precisely calculated based on the individual's body surface area ( mg/m^2). The differences in dose numbers, such as 1.4 mg/m^2 versus 1.23 mg/m^2, are due to the use of different regulatory reference standards—one referring to the mesylate salt basis and the other to the eribulin base.

Q: Does Eribulin have any potential effects on the kidneys?

A: Official product information indicates that Eribulin exposure in the body is higher for patients with moderate or severe kidney (renal) impairment. Due to this finding, which may require a lower initial starting dose as determined by a healthcare provider.

Q: What makes a patient generally eligible for Eribulin treatment for metastatic breast cancer?

A: According to official regulatory documents, eligibility for metastatic breast cancer ( mBC) is generally defined as patients who have previously received chemotherapy. This prior treatment typically includes an anthracycline and a taxane, unless those therapies were deemed unsuitable.

Q: Is Eribulin used to treat all types of liposarcoma?

A: Official labeling indicates Eribulin for patients with unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen. The treatment is approved for this general population based on clinical trial evidence.

Q: What is the reported average difference in overall survival for Eribulin vs. comparison drugs in clinical studies?

A: Studies and official documents quantify the effect in clinical trials. For example, in the Phase 3 EMBRACE trial for metastatic breast cancer, the median Overall Survival ( OS) was reported as 13.1 months in the Eribulin group versus 10.6 months in the control group.

Q: What are the reasons why a doctor might need to delay an Eribulin dose?

A: Official product information states that a dose may need to be delayed in certain circumstances. Specifically, the Day 8 dose may be postponed for up to a week if the patient is experiencing specific toxicities, particularly if blood cell counts (like neutrophils or platelets) are lower than required thresholds.

How should Eribulin be stored and disposed of?

How to Store and Dispose of Eribulin?

Eribulin mesylate injection vials must be stored in their original cartons for protection from light. The required storage temperature for the unopened product is 25°C (77°F), with permitted excursions between 15°C and 30°C. Unopened vials must not be refrigerated or frozen.

Stability After Preparation

Once prepared, the stability window changes. Both the undiluted solution drawn into a syringe and the diluted solution may be stored for up to 4 hours at room temperature or up to 24 hours under refrigeration (4°C or 40°F).

Disposal and Handling

As a cytotoxic drug, Eribulin requires special handling. Procedures for the proper handling and disposal of anticancer drugs must be followed. Any unused portions of the single-use vial must be discarded, and the product must not be disposed of via wastewater or household trash. The medication must be kept out of the sight and reach of children.

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

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