Overview | Erebrin (eribulin) is a halichondrinB derivative of macrolide compounds extracted from marine biological sponge Halichondriaokadai. It is a chemically active substance. Its medicinal mechanism is to inhibit mitosis by directly binding to tubulin, and to inhibit the growth of microtubules and inhibit the growth of cancer cells to play a therapeutic role. The clinical medicinal ingredient of the drug is Erebrin methanesulfonic acid, and the trade name is Halaven. It was developed by Japan's Eisai company. It was first listed in the United States on November 15, 2010. The U.S. Food and Drug Administration (FDA) approved the Halaven (Mesylate). Iribrin) is used to treat patients with metastatic breast cancer who have received at least two chemotherapy for advanced diseases. The drug has subsequently been listed in Singapore, the European Union, Switzerland, Japan and other countries. |
Indications | Erebulin is suitable for metastatic breast cancer patients who have received at least 2 previous chemotherapy (anthracycline and taxane chemotherapy-based chemotherapy regimens). |
Aibulin | Aibulin was originally structurally modified from a soft sponge B extracted and separated from marine organisms. It can be directly combined with tubulin to inhibit mitosis, and play a therapeutic role by inhibiting the growth of microtubules and inhibiting the growth of cancer cells. Erdrin is a synthetic analog of sponge B. In 1986, Japanese scientists Hirata and Uemura isolated a polyether macrocyclic lipid compound containing only C, H, and O atoms from the sponge Halichondria okadai. They named this natural product with extremely complex structure as soft sponge B(Halichondrin B). On November 15, 2010, the U.S. FDA approved the launch of a new drug Iribulin mesylate (trade name Halaven) developed by Japan Eisai Company for the treatment of metastatic breast cancer. This product is a microtubule inhibitor with anti-cancer The mechanism is basically the same as paclitaxel. On July 12, 2019, Eisai Pharmaceutical's application for listing in China (JXHS1700048) was approved by the State Drug Administration (NMPA) for listing. Although the patent for the compound of Aibulin expires on June 19, 2019, there are only a handful of generic drug companies developing Aibulin APIs or preparations around the world, the main reason being the extremely difficult industrial production of Aibulin. Aibulin is the most complex drug with the most complex structure developed and produced by pure chemical synthesis method so far. The molecule contains 19 chiral carbon atoms, which is synthesized from simple industrial raw materials through 62 steps of reaction. |
marketing history | in November 2010, aibulin was launched in the United States for the third-line treatment of metastatic breast cancer. In July 2011, this product was introduced in Japan for inoperable or recurrent breast cancer. In July 2014, this product was introduced in the European Union to treat locally advanced or metastatic breast cancer. It has previously received at least one chemotherapy regimen, including anthracyclines and taxanes, whether adjuvant or metastatic environment; In January 2016, FDA approved this product for previously treated unresectable liposarcoma. In February 2016, Japan approved this product for soft tissue sarcoma. In May 2016, the European Union approved this product for previously treated unresectable liposarcoma. In July 2019, China NMPA was approved for marketing in the treatment of locally recurrent or metastatic breast cancer. |
adverse reactions | the most common adverse reactions (incidence> 25%) are neutropenia, peripheral neuropathy, anemia, fatigue, alopecia, nausea and constipation. Other adverse reactions (incidence rate 5% ~ 10%): increased lacrimation; gastrointestinal symptoms such as dyspepsia, abdominal pain and dry mouth; peripheral edema at the injection site; upper respiratory tract infection; hypokalemia; myasthenia; taste disturbance, dizziness, insomnia and depression; rash. There are no contraindications. |
usage and dosage | 21d is a course of treatment. the product is infused on the 1st and 8d, and the recommended dose for each time is 1.4mg/m2, which is finished in 2~5min. For patients with liver damage and moderate kidney damage (creatinine clearance of 30-50mL/min), dose reduction is required. Recommended dose: 1.1mg/m2 for patients with mild liver damage; Moderate liver damage: 0.7mg/m2; Patients with moderate kidney damage: 1.1mg/m2. The dose should be adjusted for peripheral neuropathy and full blood count before each medication. |