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

“The genotoxicity of momelotinib was evaluated in a battery of in vitro and in vivo tests (bacterial reverse mutation assay, in vitro mammalian cytogenetic test using human lymphocytes, and in vivo micronucleus assay). Overall, momelotinib was not genotoxic under the test conditions.”

“Oral administration of the top dose of 15 mg/kg/day of momelotinib (17-times the MRHD) for 2 years significantly increased the incidence of testicular Leydig cell tumors in male rats (11/60 versus 2/60 in control males, Table 32).”

“MMB, when administered orally to pregnant rats and rabbits during organogenesis showed evidence of embryo-fetal toxicities, but no teratogenicity.”

“The cardiovascular in vitro studies showed that MMB was a weak inhibitor of hERG channel K+ current (IC50>10 µM), with no clinical relevance.”