에리불린메실레이트

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P301+P312：삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

에리불린메실레이트 화학적 특성, 용도, 생산

• 용도

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

• 정의

  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+).

• Clinical Use

  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.

• Clinical Use

  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.

• 부작용

  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.

• Mode of action

  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.

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