Eribulin Mesylate

Использование

Eribulin Mesylate is a synthetic analog of the marine natural product halichondrin B.

Определение

ChEBI: Eribulin mesylate is a methanesulfonate salt obtained by reaction of eribulin with one equivalent of methanesulfonic acid. A fully synthetic macrocyclic ketone analogue of marine sponge natural products. Inhibits growth phase of microtubules via tubulin-based antimitotic mechanism, which leads to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage. It has a role as an antineoplastic agent and a microtubule-destabilising agent. It contains an eribulin(1+).

Клиническое использование

Eribulin is a highly potent cytotoxic agent approved in the U.S. for the treatment of metastatic breast cancer for patients who have received at least two previous chemotherapeutic regimens. Eribulin was discovered and developed by Eisai and it is currently undergoing clinical evaluation for the treatment of sarcoma (PhIII) and non-small cell lung cancer which shows progression after platinumbased chemotherapy and for the treatment of prostate cancer (PhII). Early stage clinical trials are also underway to evaluate eribulin’s efficacy against a number of additional cancers. Eribulin is a structural analog of the marine natural product halichondrin B. Its mechanism of action involves the disruption of mitotic spindle formation and inhibition of tubulin polymerization which results in the induction of cell cycle blockade in the G2/M phase and apoptosis.

Клиническое использование

Eribulin mesylate, a nontaxane, completely synthetic microtubule inhibitor, has recently been approved by the U.S. Food and Drug Administration as third-line treatment of metastatic breast cancer refractory to anthracyclines and taxanes.

Побочные эффекты

Eribulin Mesylate (Halaven) may cause serious side effects including:hives; difficulty breathing; swelling of your face, lips, tongue, or throat; chest pain; severe dizziness; fast or pounding heartbeats, numbness, tingling, or burning pain in your hands or feet; pain or burning when you urinate; confusion; uneven heart rate; extreme thirst; increased urination; leg discomfort; muscle weakness; limp feeling; fever; chill; painful mouth sores; pain when swallowing; cough; trouble breathing; pale skin; easy bruising; sore throat; skin pain followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Способ действия

Eribulin Mesylate is the mesylate salt of a synthetic analogue 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.