As the patent expiration of many drugs' core compounds approaches in 2024, the market is expected to become more competitive, which in turn will give rise to new market patterns and development opportunities. In this article, we will focus on a few of these drugs that have excelled in the treatment of a wide range of diseases, including AstraZeneca's olaparib, Novartis' sinimod, AstraZeneca's linaclotide launched in collaboration with Ironwood, and Yiten Pharma's rutabopa in collaboration with Shionogi Pharmaceuticals.
Olaparib - AstraZeneca
Olaparib is the first FDA-approved oral poly ADP ribose polymerase (PARP) inhibitor, which is based on the principle of killing DNA-repair-deficient cancer cells, especially BRCA1/2 mutant cancer cells, through the use of PARP inhibitors. This drug, developed by AstraZeneca, was approved for marketing in the European Union and the United States in December 2014, respectively, and was approved for marketing in China in August 2018, making it the first PARP inhibitor to be marketed in the country. Olaparib has been approved for the treatment of ovarian cancer, breast cancer, desmoplasia-resistant prostate cancer, pancreatic cancer, fallopian tube cancer, peritoneal cancer and other indications. In the domestic market, there are currently five PARP inhibitors, including AstraZeneca's olaparib, Paige Shenzhou's pamiparib, GSK and Zaidin Pharmaceuticals' co-developed niraparib, Hengrui Pharmaceuticals' fludzoparib, and Pfizer's talazoparib.
The core compound patent (ZL200480012878.1) of olaparib will expire on March 12, 2024. Currently, nine domestic pharmaceutical companies, including Hunan Kelun Pharmaceutical, Qilu Pharmaceutical, Shiyao Ouyi, and Zhongmei Huadong Pharmaceutical, have submitted applications for generic listing of olaparib tablets, of which Qilu Pharmaceutical was the first to receive approval, becoming the first domestic generic pharmaceutical company to receive approval. After the expiration of the core patent of Olaparib, the competition in the domestic PARP inhibitor market will enter into white heat.
Sinemode - Novartis
Sinemode tablets (trade name: Vanillen) were approved for marketing in May 2020 through the NMPA's priority approval process for the treatment of adults with relapsing forms of multiple sclerosis, including clinically isolated syndromes, relapsing-remitting disease, and active secondary progressive disease. It was approved for marketing by the FDA as early as March 2019 in the United States. This is the first FDA approval for the treatment of relapsing-remitting multiple sclerosis (RRMS) in 15 years. Multiple sclerosis (MS) is a chronic inflammatory autoimmune disease in which a patient's autoimmune system attacks the myelin sheath that protects the nerves, leading to impairment of nerve function, with the majority of patients experiencing their first symptoms between the ages of 20 and 40, and it is one of the most common causes of neurological disability in young adults.MS is divided into three main clinical courses: primary progressive multiple sclerosis (PPMS), relapsing-remitting multiple sclerosis (RRMS), and secondary progressive multiple sclerosis (SPMS). Since its approval in 2020, sinemode has shown rapid growth in the domestic market, with overall market sales in 2022 reaching 84 million.
However, it is worth paying attention to the fact that the patent (ZL200480013248.6) of the core compound of Sinemode is about to expire on May 19, 2024. At present, the layout of the domestic cinimod generic enterprises are more limited, Colum Pharmaceuticals is the first to submit cinimod tablets generic drug listing application, and is expected to capture the cinimod first generic.
Linaclotide - AstraZeneca/Ironwood
Linaclotide, developed in-house by Ironwood, is an innovative drug that agonizes guanylate cyclase-C (GC-C), endorsed by the American Gastroenterological Association (AGA) guidelines and recommended for the treatment of constipated irritable bowel syndrome (IBS-C), and considered the standard of care for the treatment of this disorder. AstraZeneca has partnered with Ironwood for exclusive rights to develop, manufacture and commercialize the drug in China (except Taiwan). Irritable bowel syndrome (IBS) is a common functional bowel disease, of which IBS-C is a subtype, and its main clinical symptoms include recurrent episodes of constipation as well as symptoms of abdominal pain, bloating and abdominal discomfort accompanying bowel movements. Linaclotide was first approved for marketing by the FDA in August 2012, and subsequently entered the Chinese market on January 15, 2019, filling a gap in the IBS-C market. It has broad prospects in the IBS market as it is widely recognized for its safety and efficacy. In terms of the domestic market, by 2022, its overall sales have exceeded 100 million dollars. As for the global market, the sales in 2022 have exceeded $2 billion.
However, the patent for linaclotide's core compound will expire on January 24, 2024. At present, there are four domestic pharmaceutical companies in the layout of the species, namely, Sichuan Guowei Pharmaceuticals, Shuanghe Pharmaceuticals (Hainan), Shenzhen Hanyu Pharmaceuticals, Qilu Pharmaceuticals (Hainan)
Rutabopa - Yiteng Pharmaceuticals/Shionogi Pharmaceuticals
On June 27, 2023, Yiten Pharma's new drug (Class 5.1), rutrupapa (Stablecoda®), successfully received marketing approval from the National Medicines and Products Administration (NMPA). The drug is indicated for adult patients, suffering from chronic liver disease with thrombocytopenia and scheduled to undergo surgery (including diagnostic operations.) In 2019, Yiten Pharma reached an agreement with Japan's Shionogi Pharmaceuticals for the rights to develop and commercialize Stabilkoda's products in China, Hong Kong and Macau. Although marketing approval for this drug was granted in June, unfortunately, the patent for its core compound is set to expire on August 10, 2024. According to the CDE's official website, Coren Pharmaceuticals has submitted a listing application for rutabopa tablets on August 17, which will be the first generic rutabopa tablets to be declared for marketing in China. This means that rutabopa tablets may enter the competitive market ahead of patent expiration.
In conclusion, these drugs have occupied an important position in the global pharmaceutical market and brought new hope to patients by virtue of their unique pharmacological mechanisms and therapeutic effects. However, with the imminent expiration of the patents of the core compounds of these drugs, many pharmaceutical companies at home and abroad have entered into the research and development and declaration of generic drugs, which signals that the competition in the market will become more and more intense in the future. This will not only push the original drug companies to continuously innovate and improve the level of drug R&D, but also bring more choices and possibilities of medication for the majority of patients. In this surge of market competition, we expect to see more innovative and efficient drugs to meet the growing medical needs of patients.