Related Experiment Video
Updated: Dec 22, 2025
Chronic, Acute, and Reactivated HIV Infection in Humanized Immunodeficient Mouse Models
Published on: December 3, 2019
Single- and repeated-dose toxicity studies on the novel HIV maturation inhibitor QF-036 in Sprague-Dawley rats
Rong-Tian Cui1, Hong-Hong He2, Dong-An Yu3
1State Key Laboratory of Innovative Natural Medicine and TCM Injections, Jiangxi Qingfeng Pharmaceutical Co. Ltd., Ganzhou, Jiangxi, China; Jiangsu Mabwell Health Pharmaceutical R&D Co., Ltd., Taizhou, Jiangsu, China.
Abstract:
QF-036 is a novel human immunodeficiency virus (HIV) maturation inhibitor that is a lupine triterpenoid derivative. The objective of this study was to evaluate the safety of QF-036. A single oral toxicity and a 4-week repeated oral toxicity were investigated in Sprague-Dawley (SD) rats. The single oral toxicity study of QF-036 in SD rats showed that no mortality or visible pathological changes were noted at doses of 100, 300, and 1000 mg/kg. QF-036 exhibited a non-linear toxicokinetic profile over the dose range of 100-1000 mg/kg in the single dose study, and a saturation trend appeared at doses of 100 and 300 mg/kg. In the 4-week oral toxicity and toxicokinetic study, SD rats were given 0, 50, 100, and 200 mg/kg QF-036 once daily for 4 weeks, followed by a 4-week recovery period. No mortality or significant effects on food consumption, body weight, or behavior were observed. In addition, there were no test article-related changes in hematology, clinical biochemistry and histopathology. The no observed adverse effect level (NOAEL) was 200 mg/kg. The toxicokinetic study demonstrated a dose-dependent increase in the systemic exposure to QF-036 after 4 weeks of oral administration. There were no marked sex differences or drug accumulation observed for repeated doses of QF-036.
Insights
This study evaluated the safety of QF-036, a novel HIV maturation inhibitor, in rats. QF-036 demonstrated a good safety profile with no observed adverse effects at doses up to 200 mg/kg.
Area of Science:
- Pharmacology
- Toxicology
- Virology
Background:
- QF-036 is a novel lupine triterpenoid derivative investigated as a human immunodeficiency virus (HIV) maturation inhibitor.
- Evaluating the safety of potential therapeutic agents is crucial before clinical application.
Purpose of the Study:
- To assess the safety and toxicokinetic profile of QF-036 in Sprague-Dawley (SD) rats.
- Determine the no observed adverse effect level (NOAEL) for QF-036.
Main Methods:
- Single oral toxicity study with doses of 100, 300, and 1000 mg/kg in SD rats.
- 4-week repeated oral toxicity study with doses of 0, 50, 100, and 200 mg/kg, followed by a 4-week recovery period.
- Toxicokinetic analysis was performed in both studies.
Main Results:
- No mortality or pathological changes were observed in the single oral toxicity study.
- The 4-week study showed no adverse effects on body weight, food consumption, behavior, hematology, clinical biochemistry, or histopathology up to 200 mg/kg.
- The NOAEL was determined to be 200 mg/kg, with dose-dependent systemic exposure and no drug accumulation.
Conclusions:
- QF-036 exhibits a favorable safety profile in SD rats.
- The established NOAEL supports further investigation of QF-036 as a potential HIV treatment.
