Lenacapavir

The clinical treatment of chronic hepatitis C (HCV) has long relied on the regimen of interferon combined with ribavirin, which has many adverse reactions and a cure rate of less than 50%. This situation was completely changed until the advent of direct-acting antiviral drugs (DAAs). Ledipasvir is an HCV NS5A inhibitor class of DAA. By targeting and binding to the dimer interface of the NS5A protein, it blocks the assembly of viral replication complexes and the release of progeny viruses, and is currently one of the core components of global anti-HCV compound preparations. In clinical practice, it is usually used in combination with NS3/4A protease inhibitors or NS5B polymerase inhibitors, and is suitable for the treatment of adult patients with genotype 1 and genotype 4 chronic hepatitis C, including those with compensated cirrhosis. The sustained virological response rate of the combination regimen can be increased to more than 95%, which greatly reduces the risk of cirrhosis progression and liver cancer occurrence.

The global HCV DAA market exceeded USD 23 billion at its peak in 2015. Subsequently, with the popularization of high-cure-rate products and the reduction of the stock of patients, the market size has gradually declined, but ledipasvir, as a basic combination component, has always maintained a stable market demand. At present, the global supply of ledipasvir is dominated by the original research enterprises, and generic drug manufacturers are mainly concentrated in major generic drug exporting countries such as India and Bangladesh, and there are no compliant generic drugs on the market in China; as of 2023, the overall market size of anti-HCV DAAs at the terminal of domestic public medical institutions is approximately RMB 1.8 billion, and the market share of ledipasvir-related compound preparations is approximately 12%.

The original research enterprise of ledipasvir is Gilead Sciences, and the original research trade name is Harvoni (i.e. ledipasvir/sofosbuvir compound preparation). The expiration date of its core compound patent in the United States is 2030, and the compound patent in China will expire in 2031. The main dosage form approved by the original research is tablet, with the specification of ledipasvir 90mg/sofosbuvir 400mg. This compound preparation has been included in the FDA Reference Listed Drug Catalog, and has also entered China's *Catalog of Reference Preparations for Chemical Drugs (Third Batch)*. At present, there are no marketed ledipasvir single-drug preparations in China, and no valid registration number of ledipasvir has been found on the CDE API registration platform for the time being. Only the original research imported ledipasvir/sofosbuvir compound preparation was approved for marketing in China in 2018. (Data as of October 2024, please refer to the official website of CDE for the latest information.)

In response to the R&D and quality control needs of ledipasvir, CATO can provide a full set of impurity reference standards for this API. Most of the products are in stock, and in-stock products ordered before 16:00 will be shipped on the same day. They meet the compliance requirements of multiple regulations including the Chinese Pharmacopoeia and FDA, and can fully meet the reference substance use needs of pharmaceutical enterprises in the whole process from API synthesis, preparation R&D to quality consistency evaluation.