Recently, the listing application of Amgen's multiple myeloma drug "Carfilzomib for Injection" (relevant acceptance number is JXHS1900150) has been changed to "under approval" in China's NMPA, and it is expected to be formally approved soon.

Carfilzomib (Kyprolis) is a proteasome inhibitor. The proteasome can break down damaged or no longer needed proteins, and it plays an important role in the normal function and growth of cells. Studies have found that multiple myeloma cells will produce a large number of abnormal proteins, and inhibiting the proteasome will make them overwhelmed and collapse and die.

Carfilzomib was developed by Proteolix and then acquired by Onyx Pharmaceuticals. In 2013, Amgen acquired the drug when it acquired Onyx Pharmaceuticals for $10.4 billion. Since being accelerated by the FDA in July 2012, Kyprolis has been approved for multiple indications, including:

(1) Single drug for MM patients who have previously received at least 2 drug treatments but relapsed (including Velcade and Thalomid);

(2) Combine Revlimid (lenalidomide, lenalidomide) and dexamethasone (KRd combination) for recurrent MM patients who have previously received 1-3 lines of treatment;

(3) Combine Darzalex (daratumumab, daratumumab) and dexamethasone for R/R MM adult patients who have previously received 1-3 therapies.

Moreover, in October 2018, the FDA also approved a new Kyprolis once-a-week regimen, that is, a once-a-week 70mg/m2 dose of Kyprolis combined with dexamethasone for the treatment of R/R MM. In addition, Kyprolis combined Darzalex and dexamethasone (the (DKd) regimen) supplementary new drug application for the treatment of R/R MM is currently under review in the United States.

According to Amgen’s financial report, Kyprolis’s sales have risen year by year since its listing, and it has become a blockbuster product in 2019, which exceeded $1 billion. However, in 2020, the sales growth of the drug has slowed down significantly. I don't know if it is affected by the new crown epidemic.

In China, Kyprolis's listing application was accepted by CDE in November 2019. Now the listing application has entered the administrative approval stage and is expected to be formally approved soon. It is worth mentioning that in November 2019, Amgen and BeiGene reached a strategic cooperation, granting BeiGene to develop and commercialize Xgeva (desulumab), Kyprolis (carfilzomib) and Blincyto in China. Lintuoli) rights, of which both disulumab and belintuoli have been officially approved in China. According to relevant statistics, at present, domestic companies have begun to deploy the carfilzomi generic drug market, and most of them have been approved for clinical trials. Tigermed is progressing rapidly and is in the phase III clinical stage.

Carfilzomib and bortezomib are both proteasome inhibitors (PI), used for the treatment of relapsed/refractory multiple myeloma (MM). Compared with bortezomib, carfilzomib has stronger proteasome inhibitory activity and fewer off-target effects. As a new generation of highly selective irreversible proteasome blocking drugs, multiple clinical studies have confirmed that carfilzomib alone or in combination with other drugs has a strong anti-MM effect with low toxicity, especially the incidence of peripheral neuropathy. Low, good patient tolerance, high safety, and long-term clinical use. The industry expects it may replace bortezomib, and the market prospects are promising.

At present, the patent of Carfilzomib compound expires in 2025, and it has not been listed in China. There is no approval for imported and domestic raw materials. TOSUN PHARM can provide imported raw materials for R&D and production with excellent quality and complete qualifications.