Proguanil

The continuous spread of drug-resistant Plasmodium has led to a rising demand for long-acting and safe chemoprophylactic drugs for malaria prevention and control. Proguanil is a biguanide anti-Plasmodium drug. As a prodrug, it is metabolized by the liver into the active metabolite cycloguanil after entering the human body. It selectively inhibits dihydrofolate reductase of Plasmodium, blocks the folic acid synthesis pathway, and thus inhibits the schizont proliferation of Plasmodium in erythrocytes. Clinically, it is mainly used for the prevention of falciparum malaria and vivax malaria, and can also be used in combination with atovaquone and other drugs for the treatment of malaria. The applicable population includes travelers in malaria-endemic areas, prevention and control staff, and children without contraindications.

Currently, the annual size of the global antimalarial drug market exceeds 4 billion US dollars, of which prophylactic drugs account for about 22%, with a compound annual growth rate maintained at 5.8%. With a low adverse reaction rate and proven preventive effect, proguanil is a first-line malaria prophylactic drug component recommended by the WHO. At present, the market is mainly supplied by generic drugs, and India and China are the core production areas of proguanil API in the world, accounting for more than 75% of the global supply in total. In terms of the domestic market, with the stable demand for entry-exit prevention and control, the annual growth rate of proguanil preparation procurement has remained at around 11% in the past three years, and the overall supply and demand pattern of API is generally stable.

The original developer of proguanil is GlaxoSmithKline, with the original brand name Paludrine. Its core compound patent expired globally around 1970. At present, the main dosage form of the original marketed product is tablet, with specifications of 100mg and 300mg. The original tablet has been included in the FDA Reference Listed Drug Catalog. Up to now, no valid registration number of proguanil has been found on the domestic CDE API registration platform, and no single-agent proguanil preparation has been approved for marketing in China. Only a few enterprises manufacture and supply API for export in accordance with the requirements for overseas production. (Data as of June 2025, please refer to the official CDE website for the latest information)

For the quality research needs related to proguanil, CATO can provide a full set of impurity reference standards for this API. Most products are available from stock, and stock products ordered before 16:00 can be shipped on the same day. All products meet the compliance requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully meet the needs of pharmaceutical enterprises for impurity qualitative and quantitative research and quality standard establishment.