What Is Eribulin Mesylate?

Iribrin mesylate injection is an anti-tumor drug, the specification is 1mg / 2mL injection.

Eribulin mesylate injection

Iribrin mesylate injection is an anti-tumor drug, the specification is 1mg / 2mL injection.

Chinese name

Eribulin mesylate injection

Foreign name

eribulin mesylate

Product name

halavan

Specifications

Injection 1mg / 2mL

It is used to treat patients with metastatic breast cancer who have received at least 2 chemotherapy regimens, and the chemotherapy regimen should include anthracycline or taxane.

Iribrin mesylate is dissolved in a 5% ethanol solution at a concentration of 0.5 g / mL, and the general dose is (with 21 days as a course of treatment): 1.4 mg / day on the 1st and 8th days m2, intravenous injection lasts 2-5 minutes.

Iribrin mesylate injection was developed by Eisai (Japan) and is the first single-agent chemotherapeutic agent to improve overall survival in patients with metastatic breast cancer. Iribrin mesylate alone or Combined with other chemotherapeutic drugs to treat various cancers, including bladder cancer, prostate cancer, pancreatic cancer, head and neck cancer, non-small cell lung cancer, etc. Clinical research is ongoing, and subsequent international multi-center phase III clinical treatment of metastatic breast cancer Research is ongoing. Iribrin mesylate has a very significant effect in the treatment of metastatic breast cancer. The late-developed indications are very wide and it is a very valuable drug ^[1]

The US FDA approved its listing in November 2010 under the trade name HALAVEN . It was launched in Europe in March 2011, and a domestic clinical approval was issued in April 2013. No other applications at this time.

Results of preclinical pharmacokinetic studies show that eribulin mesylate has a fast distribution phase and a long elimination phase, with an average elimination half-life of about 40 h ^[2]

The results of several phase I clinical studies have shown that neutropenia is one of the most common dose-limiting toxicities of this product, with the incidence increasing from 22% (a dose of 1.4 mg · m) to 100% ( The maximum dose is 4 mg · m). The most common adverse reactions reported by Goel et al. In phase I clinical studies were fatigue (53%), followed by nausea (41%) and anorexia (38%). The most common adverse reactions reported by Tan et al. In phase I clinical studies were neutropenia (38%, 33% grade 3-4), fatigue (33%, grade 1-2), and hair loss (33 %, Both grades 1-2). The results of a phase II clinical study reported by Vahdat et al. Showed that the most common grade 3-4 adverse reactions in the treatment of eribulin mesylate were neutropenia (64%) and leukocytopenia (18%). Fatigue (5%), peripheral neuropathy (5%) and febrile neutropenia (5%). Cortes et al reported the results of a phase II clinical study. The most common grade 3-4 adverse reactions in the treatment of this product are neutropenia (54%), leukocytopenia (14%), and fatigue (10%). Wait. In the phase III clinical study (EMBRACE study), except for neutropenia grade 3-4, most adverse reactions were grade 1-2, and the incidence of neutropenia grade 3 was 21.1%. , 4 is 24.1%. Peripheral neuropathy grade 3 was 7.8% and grade 4 was 0.4%. ^[5]

As a tubulin polymerization inhibitor with a new mechanism of action, eribulin mesylate provides a new treatment for patients with locally advanced breast cancer or metastatic breast cancer to improve survival and quality of life.