Qilu Pharmaceutical Submits NDA for Regorafenib Tablets as No Domestic Generic Approved Yet

On September 23, the official website of the CDE indicated that Qilu Pharmaceutical's Class 4 generic drug 「Regorafenib Tablets」 has been filed for marketing approval (Acceptance No.: CYHS2101768).

Data source: CDE official website

Regorafenib is a novel oral multi-kinase inhibitor and represents the next-generation oral multi-target tyrosine kinase inhibitor developed by Bayer following sorafenib. In addition to inhibiting the KIT and PDGFRα kinase targets, regorafenib also acts on targets including RET, BRAF, RAF1, VEGFR, FGFR, and PDGFR. By blocking multiple enzymes that promote tumor growth, regorafenib inhibits tumorigenesis, angiogenesis, and tumor microenvironment formation through its action on multiple kinases in tumor cells, endothelial cells, and pericytes.

On September 27, 2012, the FDA approved it for the treatment of patients with metastatic colorectal cancer (CRC) who have previously received fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, anti-VEGF therapy, and anti-EGFR therapy (if KRAS wild-type).

On February 25, 2013, the FDA approved it for the treatment of patients with locally advanced, unresectable, or metastatic gastrointestinal stromal tumors (GIST) who had previously been treated with imatinib and sunitinib.

On April 28, 2017, the FDA approved it as a second-line treatment for patients with hepatocellular carcinoma (HCC) who had previously been treated with Nexavar® (sorafenib).

On March 24, 2013, the former CFDA approved its marketing for the treatment of patients with metastatic colorectal cancer (mCRC) who have previously received fluorouracil-, oxaliplatin-, and irinotecan-based chemotherapy and anti-EGFR therapy (RAS wild-type), as well as patients with locally advanced, unresectable, or metastatic gastrointestinal stromal tumors (GIST) who have previously been treated with imatinib mesylate and sunitinib malate.

In May 2017, the former CFDA approved it for the treatment of metastatic colorectal cancer (mCRC) and gastrointestinal stromal tumors (GIST).

On December 12, 2017, the former CFDA approved it for the treatment of liver cancer.

In 2018, regorafenib was included in the Class B National Reimbursement Drug List through negotiation, with a reimbursement standard of RMB 196 (40 mg/tablet); upon expiration in 2020, it successfully renewed its listing through negotiations at a modest 12% price reduction to RMB 172.48 (40 mg/tablet), valid until December 31, 2022, for the second-line treatment of hepatocellular carcinoma, third-line treatment of metastatic colorectal cancer, and third-line treatment of gastrointestinal stromal tumors.

According to the Insight database, global sales of regorafenib have risen year by year since its market launch in 2012 (with the exception of 2016), reaching USD 545 million in 2020.

Global Sales of Regorafenib

Source: Insight Database (http://db.dxy.cn/v5/home/)

Currently, in addition to the originator company Bayer, 21 other pharmaceutical companies are developing regorafenib. The three most advanced companies are Yangtze River Pharmaceutical, Nanjing Chia Tai Tianqing, and Qilu Pharmaceutical, which have successively filed for marketing approval. Additionally, four companies—Shuanglu Pharmaceutical, Kelun Pharmaceutical, Hansoh Pharmaceutical, and Shanghai Chuangnuo Pharmaceutical—are currently conducting bioequivalence (BE) studies.

Competitive Landscape of Regorafenib in China

Source: Insight Database (http://db.dxy.cn/v5/home/)