Exblifep: genotox, carcinogenicity and repro: done or skipped?

“Enmetazobactam was negative for genetic toxicity in vitro in a bacterial reverse mutation assay and a chromosomal aberration assay in Chinese Hamster ovary cells, and in vivo in a mouse micronucleus assay in bone marrow cells.”

“Carcinogenicity studies of enmetazobactam have not been conducted and are not planned based on the intended duration of therapy (≤ 14 days).”

“In embryo-fetal development (EFD) studies in rats and rabbits, enmetazobactam was not associated with fetal malformations, but did cause maternal toxicity in the form of reduced body weight gain and fetal toxicity as reduced fetal body weights in both studies.”

“The hERG study revealed an IC50 -value of 1,254.22 µg/mL, corresponding to 3,990.30 μM, for enmetazobactam which translates into a 63-fold safety margin compared to the Cmax level of 19.8 µg/ml at the MRHD. Thereby, the potential risk for QT prolongation in humans is low.”