Lorapitant API

Name	Lorapitant
Chinese name	罗拉吡坦
Cas Number	552292-08-7
Source	India
Qualifications	USDMF/-/-/-/-

On September 1, 2015, the U.S. FDA approved Tesaro's new drug lorapitan tablets for the market. Lorapitant is an oral long-acting neurokinin NK-1 antagonist. By blocking the combination of NK-1 and SP, it can improve the vomiting symptoms of patients receiving chemotherapy. It has the characteristics of fast absorption and slow clearance, and its plasma half-life Up to 7 days, it can cover 90% of the receptors in the cerebral cortex and lasts for 5 days. It can significantly reduce the occurrence of chemotherapy-related vomiting and control it for several days. Compared with other NK-1 receptor antagonists including aprepitant, lorapitan has more obvious advantages, for example: it can selectively bind to human NK-1 receptor and has the advantages of high affinity; at the same time, Unlike other NK-1 receptor antagonists (such as aprepitant and netupitant), lorapitan does not inhibit and induce CYP3A4, and it is compatible with drugs that are mainly or partially metabolized by CYP3A4 (such as midazolam, The combined use of dansetron and dexamethasone does not have potential risks and can effectively avoid drug interactions. In 2018, the sales of terminal antiemetics in public hospitals in key provinces and cities in China were 2.389 billion yuan, an increase of 1.61% year-on-year. The overall domestic market has exceeded 8 billion yuan. The market prospect of lorapitant is very broad.

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