Efavirenz

For the long-term management of HIV infection, reducing the risk of viral drug resistance and improving patients' medication adherence have always been the core clinical demands. As the world's first approved non-nucleoside reverse transcriptase inhibitor (NNRTI), efavirenz binds non-competitively to and inhibits the activity of HIV reverse transcriptase, blocking the process of reverse transcription of viral RNA into DNA, and is one of the core components of antiretroviral therapy (ART) regimens. It is mainly used clinically in combination with other antiretroviral drugs to treat HIV-1 infection in adults, adolescents and children over 3 years old, and can also be used as preventive medication after HIV occupational exposure. With its definite efficacy and long-term clinical verification, it is still listed as a first-line recommended drug by many domestic and foreign authoritative guidelines.

At present, the global market size of anti-HIV drugs has exceeded 40 billion US dollars, among which NNRTIs account for about 8%. As a basic variety of this class of drugs, efavirenz has stable demand in public health projects in low- and middle-income countries due to its cost-effectiveness advantage. In terms of the domestic market, this variety has been included in the national centralized drug procurement, the winning bid price has dropped by more than 90% compared with that of the original research drug, the winning enterprises are mainly local generic pharmaceutical enterprises, and the market share of the original research drug is less than 10%. In 2023, the domestic market size of efavirenz preparations was about 210 million yuan, and the annual demand for its API was stable at around 150 tons. All compound patents of efavirenz have expired. At present, 12 domestic enterprises have obtained the production approval documents for efavirenz API, with sufficient production capacity and relatively sufficient market competition.

The original research enterprise of efavirenz is Merck Sharp & Dohme, with the trade name Sustiva®. Its core compound patent expired in the United States in 2013, and the Chinese patent also officially expired in 2014. The main dosage form approved by the original research is tablet, with three specifications of 50mg, 200mg and 600mg. It has been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and is also a reference preparation recognized by the FDA. Up to now, China NMPA has approved 28 efavirenz preparation varieties for marketing, and there are 24 valid registration information in the CDE API registration platform, among which 19 are in status A (already used in marketed preparations), which can meet the needs of domestic preparation production and export. (Data as of June 2025, please refer to the official website of CDE for the latest information)

In response to the R&D and quality control needs related to efavirenz, CATO can provide a full set of impurity reference standards for this API. Most of the products are in stock, and orders for in-stock products placed before 16:00 will be shipped on the same day. The products fully comply with the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can fully support various scenario needs of pharmaceutical enterprises such as API declaration, process optimization and routine quality testing.