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

“Oliceridine was negative in an in vitro Ames bacterial reverse mutation assay, the in vitro chromosomal aberration assay using human peripheral blood lymphocytes, and the in vivo rat micronucleus assay.”

“Long-term animal studies have not been completed to evaluate the carcinogenic potential of oliceridine.”

“A battery of reproductive toxicity studies identified effects on female fertility (longer estrous cycle, reduced number of implantation sites, increased preimplantation loss, and reduced viable embryos) and postnatal development (reduced live litter size, postnatal survival, and body weight). No effects on male fertility or EFD were observed.”

“oliceridine is a weak hERG inhibitor with an IC50 of 2.2 mcM which is 367 times its binding affinity of 6 nM at the MOR and 43 times the estimated Cmax of the unbound drug at the proposed maximum recommended human dose (MRHD) of 40 mg/day. No consistent effects on QTc interval have been observed in nonclinical studies.”