Kaohsiung Medical University / Prof.  Sung-Pin Tseng

 Pain Points Solved 

• The increasing prevalence of clinically drug-resistant bacteria (such as antibiotic-resistant Klebsiella pneumoniae and Acinetobacter baumannii) has significantly reduced the effectiveness of existing antibiotics.
• AS101-003 possesses a novel and previously unexploited chemical structure (first-in-class), which is expected to slow the development of bacterial resistance.
• The compound demonstrates low toxicity, with a median lethal dose (LD₅₀) of approximately 23.3 mg/kg in mice, indicating a favorable therapeutic safety margin.

 Technology Introduction 

Organic tellurium compound AS101-003 is a novel antibiotic with a chemical structure modification created by the team. It features a unique structure that has not been seen in clinical settings, and it is expected that bacteria will develop resistance to it more slowly. In a mouse model of antibiotic-resistant Klebsiella pneumoniae sepsis, a low dose of AS101-003 (0.33 mg/kg/day) achieved the same therapeutic effect as the currently marketed drug ceftazidime-avibactam (200-50 mg/kg/day) with an 83% survival rate. At intermediate/high doses (1.67/3.33 mg/kg/day), it outperformed the clinical drug, resulting in a 100% survival rate. Similar results were observed in a mouse model of antibiotic-resistant Acinetobacter baumannii sepsis, where the low dose was comparable to clinical drug colistin (20 mg/kg/day) at around 10% survival, while intermediate/high doses performed significantly better, with an approximately 80% survival rate. The median lethal dose for mice was approximately 23.3 mg/kg. In summary, this technology offers a new class of antibiotics with high antibacterial activity, a unique structure (first-in-class), and low toxicity. It is expected to provide a new solution to the clinical problem of antibiotic resistance in bacteria.

Figure 1. MIC distribution of AS101-003 against Gram-negative bacteria.

 Application Examples 

• In a mouse model of antibiotic-resistant Klebsiella pneumoniae sepsis, intermediate and high doses of AS101-003 achieved a 100% survival rate, outperforming currently marketed clinical antibiotics.
• In a mouse model of antibiotic-resistant Acinetobacter baumannii sepsis, intermediate and high doses of AS101-003 showed significantly superior efficacy compared with the clinical drug colistin.
• The compound is suitable for the treatment of severe infections and multidrug-resistant bacterial diseases, demonstrating strong potential for further clinical development and translation.

 Related Links 

None

 Patent Name and Number 

TW 111146379
US 18/715,132
CN 202280079824.5
EP 22903321.2

 Industry-Academia / Tech Transfer Partner 

None

 Honors and Awards  

19th National Innovation Award-Academia & Research Innovation Award

 Technical Contact  

Mr. Hung, Assistant Manager

Kaohsiung Medical University 
Tel: +886 7-3121101 ext. 2360
Email: R121084@kmu.edu.tw