Abstract
Studies on T-1220, a broad-spectrum penicillin derivative, were presented at The 23rd East Section Congress of Chemotherapy (Japan Society of Chemotherapy), New Drug Simposium, Tokyo, 1976.
The results of the fundamental and clinical studies in 106 research laboratories in Japan are summarized as follows.
1) T-1220 had broad antibacterial spectrum against gram-positive and gram-negative bacteria.
2) It was more active than the other broad-spectrum penicillins against gramnegative bacilli, especially Pseudomonas aeruginosa, Klebsiella pneumoniae, Proteus sp. and Serratia marcescens.
3) Therapeutic effect of T-1220 against experimental infections of mice was more effective than that of CBPC and SBPC.
4) The serum levels showed dose response relationship and the half life was approximately 0.6 hr.
5) It was mainly excreted from kidney and most of them were excreted as unchanged form and the transfer to bile was also favorable.
6) It was rapidly absorbed after subcutaneous, intramuscular or intravenous injection, indicating especially higher transfer to kidney, liver and then in order, serum, lung, spleen and muscle.
7) The binding rate of the drug with serum protein was 20-30%.
8) The effective rate in 426 cases of the fields of internal medicine, pediatrics and dermatology was 72.5% and the effective rate in 788 cases of the fields of surgery, orthopedics, urology, obstetrics and gynecology, otorhinolaryngology, ophthalmology and oral surgery was 73.6% and the effective rate in total of 1, 214 cases was 73.2%.
Considering the fact that a number of severe infections were included, the clinical result of the drug was considered to be favorable as broad-spectrum synthetic penicillins.
9) Side effects were observed in 47 cases of 1, 266 cases (3.71%) but severe side effect was not observed. Side effects were mainly eruption, nausea, vomiting and diarrhea. Elevation of GOT and GPT, leukopenia, eosinophilia and pyrexia were observed in some cases.
