FDA

Eribulin Mesylate

Approved 1 Oct 2024IntravenousSolution

The FDA lists this product in 10 strengths and forms.

Indications

Eribulin Mesylate Injection is a microtubule inhibitor indicated for the treatment of patients with:

Metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic disease. Prior therapy should have included an anthracycline and a taxane in either the adjuvant or metastatic setting. (1.1)
Unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen. (1.2)

1.1Metastatic Breast Cancer Eribulin Mesylate

Injection is indicated for the treatment of patients with metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic disease. Prior therapy should have included an anthracycline and a taxane in either the adjuvant or metastatic setting [ see Clinical Studies (14.1) ] .

1.2Liposarcoma Eribulin Mesylate

Injection is indicated for the treatment of patients with unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen [ see Clinical Studies (14.2) ] .

Contraindications

None. None (4)

Warnings and precautions

Neutropenia : Monitor peripheral blood cell counts and adjust dose as appropriate. (5.1)
Peripheral Neuropathy : Monitor for signs of neuropathy. Manage with dose delay and adjustment. (5.2)
Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to the fetus and to use effective contraception. (5.3 , 8.1 , 8.3)
QT Prolongation : Monitor for prolonged QT intervals in patients with congestive heart failure, bradyarrhythmias, drugs known to prolong the QT interval, and electrolyte abnormalities. Avoid in patients with congenital long QT syndrome. (5.4)

5.1Neutropenia In Study

1, severe neutropenia (ANC < 500/mm 3 ) lasting more than one week occurred in 12% (62/503) of patients with metastatic breast cancer, leading to discontinuation in <1% of patients. Febrile neutropenia (fever ≥38.5°C with Grade 3 or 4 neutropenia) occurred in 5% (23/503) of patients; two patients (0.4%) died from complications of febrile neutropenia [ see Adverse Reactions (6.1) ] . In Study 1, patients with alanine aminotransferase (ALT) or aspartate aminotransferase (AST) > 3 × ULN (upper limit of normal) experienced a higher incidence of Grade 4 neutropenia and febrile neutropenia than patients with normal aminotransferase levels.

At a glance

Brand name: Eribulin Mesylate
Route: Intravenous
Dosage form: Solution
Applicant: Baxter Hlthcare Corp
Status: Prescription
FDA approval: 1 Oct 2024
Application: ANDA217250-001

Indications

Eribulin Mesylate Injection is a microtubule inhibitor indicated for the treatment of patients with:

Metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic disease. Prior therapy should have included an anthracycline and a taxane in either the adjuvant or metastatic setting. (1.1)
Unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen. (1.2)

1.1Metastatic Breast Cancer Eribulin Mesylate

1.2Liposarcoma Eribulin Mesylate

Injection is indicated for the treatment of patients with unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen [ see Clinical Studies (14.2) ] .

Warnings and precautions

Neutropenia : Monitor peripheral blood cell counts and adjust dose as appropriate. (5.1)
Peripheral Neuropathy : Monitor for signs of neuropathy. Manage with dose delay and adjustment. (5.2)
Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to the fetus and to use effective contraception. (5.3 , 8.1 , 8.3)
QT Prolongation : Monitor for prolonged QT intervals in patients with congestive heart failure, bradyarrhythmias, drugs known to prolong the QT interval, and electrolyte abnormalities. Avoid in patients with congenital long QT syndrome. (5.4)

5.1Neutropenia In Study

Adverse reactions

The most common adverse reactions (≥25%) in metastatic breast cancer were neutropenia, anemia, asthenia/fatigue, alopecia, peripheral neuropathy, nausea, and constipation. (6.1) The most common adverse reactions (≥25%) in liposarcoma and leiomyosarcoma were fatigue, nausea, alopecia, constipation, peripheral neuropathy, abdominal pain, and pyrexia. The most common (≥5%) Grade 3-4 laboratory abnormalities in liposarcoma and leiomyosarcoma were neutropenia, hypokalemia, and hypocalcemia.

(6.1) To report SUSPECTED ADVERSE REACTIONS, contact Baxter Healthcare Corporation at 1-866-888-2472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, the adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in other clinical trials and may not reflect the rates observed in clinical practice. The following adverse reactions are discussed in detail in other sections of the labeling:

Neutropenia [ see Warnings and Precautions (5.1) ]
Peripheral neuropathy [ see Warnings and Precautions (5.2) ]
QT prolongation [ see Warnings and Precautions (5.4) ] In clinical trials, Eribulin Mesylate Injection has been administered to 1963 patients including 467 patients exposed to Eribulin Mesylate Injection for 6 months or longer. The majority of the 1963 patients were women (92%) with a median age of 55 years (range: 17 to 85 years). The racial and ethnic distribution was White (72%), Black (4%), Asian (9%), and other (3%). Metastatic Breast Cancer The most common adverse reactions (≥25%) reported in patients receiving Eribulin Mesylate Injection were neutropenia, anemia, asthenia/fatigue, alopecia, peripheral neuropathy, nausea, and constipation. The most common serious adverse reactions reported in patients receiving Eribulin Mesylate Injection were febrile neutropenia (4%) and neutropenia (2%). The most common adverse reaction resulting in discontinuation of Eribulin Mesylate Injection was peripheral neuropathy (5%). The adverse reactions described in Table 2 were identified in 750 patients treated in Study 1 . In Study 1, patients were randomized (2:1) to receive either Eribulin Mesylate Injection (1.4 mg/m on Days 1 and 8 of a 21-day cycle) or single agent treatment chosen by their physician (control group). A total of 503 patients received Eribulin Mesylate Injection and 247 patients in the control group received therapy consisting of chemotherapy [total 97% (anthracyclines 10%, capecitabine 18%, gemcitabine 19%, taxanes 15%, vinorelbine 25%, other chemotherapies 10%)] or hormonal therapy (3%). The median duration of exposure was 118 days for patients receiving Eribulin Mesylate Injection and 63 days for patients receiving control therapy. Table 2 reports the most common adverse reactions occurring in at least 10% of patients in either group. Table 2: Adverse Reactions adverse reactions were graded per National Cancer Institute Criteria for Adverse Events version 4.0. with a Per-Patient Incidence of at Least 10% in Study 1 Adverse Reactions Eribulin Mesylate Injection n=503 Control Group n=247 All Grades ≥ Grade 3 All Grades ≥ Grade 3 Blood and lymphatic system disorders based upon laboratory data. Neutropenia 82% 57% 53% 23% Anemia 58% 2% 55% 4% Nervous system disorders Peripheral neuropathy includes peripheral neuropathy, peripheral sensorimotor neuropathy, peripheral motor neuropathy, polyneuropathy, peripheral sensory neuropathy, and paraesthesia. 35% 8% 16% 2% Headache 19% <1% 12% <1% General disorders Asthenia/Fatigue 54% 10% 40% 11% Pyrexia 21% <1% 13% <1% Mucosal inflammation 9% 1% 10% 2% Gastrointestinal disorders Nausea 35% 1% 28% 3% Constipation 25% 1% 21% 1% Vomiting 18% 1% 18% 1% Diarrhea 18% 0 18% 0 Musculoskeletal and connective tissue disorders Arthralgia/Myalgia 22% <1% 12% 1% Back pain 16% 1% 7% 2% Bone pain 12% 2% 9% 2% Pain in extremity 11% 1% 10% 1% Metabolism and nutrition disorders Decreased weight 21% 1% 14% <1% Anorexia 20% 1% 13% 1% Respiratory, thoracic, and mediastinal disorders Dyspnea 16% 4% 13% 4% Cough 14% 0 9% 0 Skin and subcutaneous tissue disorders Alopecia 45% NA not applicable; (grading system does not specify > Grade 2 for alopecia). 10% NA Infections Urinary Tract Infection 10% 1% 5% 0 Cytopenias : Grade 3 neutropenia occurred in 28% (143/503) of patients who received Eribulin Mesylate Injection in Study 1, and 29% (144/503) of patients experienced Grade 4 neutropenia. Febrile neutropenia occurred in 5% (23/503) of patients; two patients (0.4%) died from complications of febrile neutropenia. Dose reduction due to neutropenia was required in 12% (62/503) of patients and discontinuation was required in <1% of patients. The mean time to nadir was 13 days and the mean time to recovery from severe neutropenia (<500/mm 3 ) was 8 days. Grade 3 or greater thrombocytopenia occurred in 1% (7/503) of patients. G-CSF (granulocyte colony- stimulating factor) or GM-CSF (granulocyte–macrophage colony-stimulating factor) was used in 19% of patients who received Eribulin Mesylate Injection. Peripheral Neuropathy : In Study 1, 17% of enrolled patients had Grade 1 peripheral neuropathy and 3% of patients had Grade 2 peripheral neuropathy at baseline. Dose reduction due to peripheral neuropathy was required by 3% (14/503) of patients who received Eribulin Mesylate Injection. Four percent (20/503) of patients experienced peripheral motor neuropathy of any grade and 2% (8/503) of patients developed Grade 3 peripheral motor neuropathy. Liver Function Test Abnormalities : Among patients with Grade 0 or 1 ALT levels at baseline, 18% of Eribulin Mesylate Injection-treated patients experienced Grade 2 or greater ALT elevation. One Eribulin Mesylate Injection-treated patient without documented liver metastases had concomitant Grade 2 elevations in bilirubin and ALT; these abnormalities resolved and did not recur with re-exposure to Eribulin Mesylate Injection. Less Common Adverse Reactions : The following additional adverse reactions were reported in ≥5% to <10% of the Eribulin Mesylate Injection-treated group:
Eye Disorders: increased lacrimation
Gastrointestinal Disorders: dyspepsia, abdominal pain, stomatitis, dry mouth
General Disorders and Administration Site Conditions: peripheral edema
Infections and Infestations: upper respiratory tract infection
Metabolism and Nutrition Disorders: hypokalemia
Musculoskeletal and Connective Tissue Disorders: muscle spasms, muscular weakness
Nervous System Disorders: dysgeusia, dizziness
Psychiatric Disorders: insomnia, depression
Skin and Subcutaneous Tissue Disorders: rash Liposarcoma The safety of Eribulin Mesylate Injection was evaluated in Study 2, an open-label, randomized, multicenter, active-controlled trial, in which patients were randomized (1:1) to receive either Eribulin Mesylate Injection 1.4 mg/m 2 on Days 1 and 8 of a 21-day cycle or dacarbazine at doses of 850 mg/m 2 (20%), 1000 mg/m 2 (64%), or 1200 mg/m 2 (16%) every 3 weeks. A total of 223 patients received Eribulin Mesylate Injection and 221 patients received dacarbazine. Patients were required to have received at least two prior systemic chemotherapy regimens. The trial excluded patients with pre-existing ≥ Grade 3 peripheral neuropathy, known central nervous system metastasis, elevated serum bilirubin or significant chronic liver disease, history of myocardial infarction within 6 months, history of New York Heart Association Class II or IV heart failure, or cardiac arrhythmia requiring treatment. The median age of the safety population in Study 2 was 56 years (range: 24 to 83 years); 67% female; 73% White, 3% Black or African American, 8% Asian/Pacific Islander, and 15% unknown; 99% received prior anthracycline-containing regimen; and 99% received ≥ 2 prior regimens. The median duration of exposure was 2.3 months (range: 21 days to 26 months) for patients receiv

Our copy of this section ends here. The full text is in the official label at the FDA. Open Drugs@FDA

Eribulin Mesylate

Indications

1.1Metastatic Breast Cancer Eribulin Mesylate

1.2Liposarcoma Eribulin Mesylate

Contraindications

Warnings and precautions

5.1Neutropenia In Study

At a glance

Two medicines in one question?

Eribulin Mesylate

Indications

1.1Metastatic Breast Cancer Eribulin Mesylate

1.2Liposarcoma Eribulin Mesylate

Contraindications

Warnings and precautions

5.1Neutropenia In Study

At a glance

Two medicines in one question?

5.2Peripheral Neuropathy In Study 1, Grade

5.3Embryo-Fetal Toxicity Based

Interactions

7.1Effects of Other Drugs on Eribulin Mesylate Injection

7.2Effects of Eribulin Mesylate Injection on Other Drugs

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary Based

Adverse reactions

6.1Clinical Trials Experience

Composition

Strengths and forms

Official product information