Eribulin Mesylate is the mesylate salt of a synthetic analog of halichondrin B, a substance derived from a marine sponge (Lissodendoryx sp.) with antineoplastic activity. Eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and, potentially, tumor regression.
Mechanism of Action of Eribulin Mesylate
Eribulin inhibits the growth phase of microtubules without affecting the shortening phase and sequesters tubulin into nonproductive aggregates. Eribulin exerts its effects via a tubulin-based antimitotic mechanism leading to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after the prolonged mitotic blockage. [FDA]
Indications of Eribulin Mesylate
- For the treatment of patients with metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic cancer.
- HALAVEN is indicated for the treatment of adult patients with locally advanced or metastatic breast cancer who have progressed after at least one chemotherapeutic regimen for advanced disease (see section 5.1). Prior therapy should have included an anthracycline and a taxane in either the adjuvant or metastatic setting unless patients were not suitable for these treatments.
- It is indicated for the treatment of adult patients with unresectable liposarcoma who have received prior anthracycline-containing therapy (unless unsuitable) for advanced or metastatic disease.
- Breast Cancer
- Metastatic Liposarcoma
- Refractory, metastatic Breast cancer
- Unresectable Liposarcoma
- For the treatment of patients with metastatic breast cancer who have previously received at least 2 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.
Dosage of Eribulin Mesylate
Strengths: 1 mg/2 mL
Breast Cancer
- 1.4 mg/m2 IV over 2 to 5 minutes on days 1 and 8 of a 21-day cycle
Side Effects of Eribulin Mesylate
More Common
- Black, tarry stools
- bladder pain
- bloating or swelling of the face, arms, hands, lower legs, or feet
- bloody or cloudy urine
- body aches or pain
- burning, numbness, tingling, or painful sensations
- convulsions
- cough
- decreased urine
- decreased weight
- difficult or labored breathing
- difficult, burning, or painful urination
- dry mouth
- ear congestion
- fever
- frequent urge to urinate
Common
- mouth sores or infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">inflammation
- muscle spasms or weakness
- numbness, tingling or burning in hands and feet
- sensation of spinning (vertigo)
- signs of anemia (low red blood cells; e.g., dizziness, pale skin, unusual tiredness or weakness, shortness of breath)
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- signs of infection (symptoms may include fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache, stiff neck, weight loss, or listlessness)
- signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
- skin rash or itching
- swelling of hands, feet or limbs
Rare
- Acid or sour stomach
- pain: Back pain means pain in the spine, muscles, discs, joints, or nerves of the back. সহজ বাংলা: পিঠ/কোমরের ব্যথা।" data-rx-term="back pain" data-rx-definition="Back pain means pain in the spine, muscles, discs, joints, or nerves of the back. সহজ বাংলা: পিঠ/কোমরের ব্যথা।">back pain
- belching
- bone pain
- change in taste
- cracked lips
- depression
- diarrhea
- difficulty having a bowel movement (stool)
- difficulty with moving
- difficulty with swallowing
- dizziness
- hair loss or thinning of the hair
- heartburn
Drug Interactions of Eribulin Mesylate
Eribulin may interact with following drugs, supplements & may change the efficacy of drugs
- antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- bosutinib
- dasatinib
- domperidone
- dronedarone
- famotidine
- formoterol
- galantamine
- indapamide
- lomitapide
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- nilotinib
- quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, paroxetine, sertraline)
- serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
- serotonin-norepinephrine reuptake inhibitors (SNRIs; e.g., duloxetine, venlafaxine)
- sotalol
- sulfamethoxazole
- sunitinib
- tacrolimus
- tamoxifen
- tolterodine
- trimethoprim
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- vardenafil
Pregnancy Category
FDA Pregnancy Category – D
Pregnancy
This medication may harm a developing fetus if it is used by the mother while pregnant. Eribulin should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
It is not known if eribulin passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should breastfeeding-feeding. The safety and effectiveness of using this medication have not been established for children.
References
