Raltegravir

The iteration of antiviral therapeutic drugs in the field of AIDS has always centered on reducing the risk of drug resistance and improving medication safety. Raltegravir, as the world's first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor, inhibits viral replication from the source by blocking the integration process of viral DNA with the host cell genome. Compared with traditional nucleoside and non-nucleoside reverse transcriptase inhibitors, it has a higher drug resistance barrier and a lower incidence of adverse reactions. This drug is mainly used in combination with other antiretroviral drugs to treat HIV-1 infection in adults and children over 2 years old. It is a component of the first-line treatment regimen recommended in current domestic and international AIDS diagnosis and treatment guidelines, and is particularly suitable for treatment-naive patients, elderly infected persons with underlying comorbidities, and people who cannot tolerate other types of antiviral drugs.

At present, the global market size of anti-HIV API has exceeded 9 billion US dollars, among which the proportion of integrase inhibitor APIs has increased year by year to nearly 40%. As a classic variety of this category, raltegravir has an annual growth rate of around 8% stably. In terms of the domestic market, with the expansion of the coverage of AIDS prevention and treatment and the update of the free treatment catalogue, the demand for raltegravir preparations continues to rise. At present, 6 domestic enterprises have obtained the approval documents for generic preparations, and the winning bid price in centralized procurement has dropped by more than 85% compared with the price of the original research drug. There is broad space for domestic substitution of upstream APIs, and there are fewer than 3 existing local API suppliers, so there is no competitive pattern of overcapacity yet.

The original research enterprise of raltegravir is Merck, and the original brand name is Isentress®. The expiration date of its core compound patent in China is October 2023, and the expiration date of the core preparation patent in the United States is 2029. The main dosage forms approved for the original research include film-coated tablets (specification 400mg), dry suspensions (specification 100mg) and chewable tablets (specifications 25mg, 100mg). The original research preparations have been included in the Catalogue of Listed Drugs in China as reference preparations, and are also included in the FDA Reference Preparations List. Up to now, there are 9 registration records of raltegravir API on the API registration platform of the Center for Drug Evaluation of China, among which 5 have obtained A status through joint evaluation with preparations, and there are already multiple approved and marketed generic raltegravir preparation varieties in China. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO can provide a full set of raltegravir impurity reference standards, covering process impurities, degradation impurities and isotope-labeled impurities, which meet the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA. Most of the products are in stock. For in-stock orders placed before 16:00, delivery can be made on the same day, which fully meets the various reference standard needs in the stages of API R&D, quality research and registration declaration.