Review on the clinical pharmacology of hydroxychloroquine sulfate for the treatment of COVID-19.

Cui, Cheng; Tu, Siqi; En, Valerie Sia Jie; Li, Xiaobei; Yao, Xueting; Li, Haiyan; Liu, Dongyang

BACKGROUND As the number of severe acute respiratory syndrome coronavirus 2 (SARS-COV-2) infected people is skyrocketing worldwide, the international medical situation becomes very serious. Potential therapeutic drugs, vaccine and stem cell replacement methods are emerging, it is urgent to find specific therapeutic drugs and the best treatment regimens. After the publication of hydroxychloroquine (HCQ) with anti-SARS-COV-2 activity in vitro, a small, non-randomized, open-label clinical trial showed that HCQ treatment was significantly associated with reduced viral load in patients with coronavirus disease-19 (COVID-19). Meanwhile, a large prophylaxis study of HCQ sulfate for COVID-19 has been initiated in the United States. HCQ offered a promising efficacy in the treatment of COVID-19, but the optimal administration is still being explored. METHODS Use the keyword 'Hydroxychloroquine' to conduct a literature search in PubMed to collect relevant literature on the mechanism of action of HCQ, clinical efficacy and safety, pharmacokinetic characteristics, precautions for clinical use and drug interactions, and extract and organize information. RESULTS This paper reviews the mechanism, clinical efficacy and safety, pharmacokinetic characteristics, exposure-response relationship and precautions and drug interactions of HCQ, and summarized dosage recommendations for HCQ sulfate. CONCLUSION It has been proved that HCQ, which has an established safety profile, is effective against SARS-CoV-2 with sufficient pre-clinical rationale and evidence. Data from high-quality clinical trials are urgently needed worldwide.