Nonclinical safety of tildrakizumab, a humanized anti-IL-23p19 monoclonal antibody, in nonhuman primates

Regul Toxicol Pharmacol. 2019 Nov:108:104476. doi: 10.1016/j.yrtph.2019.104476. Epub 2019 Sep 16.

Abstract

Tildrakizumab (also known as MK-3222), is a high-affinity, humanized, immunoglobin G1κ monoclonal antibody targeting the p19 subunit of interleukin-23 recently approved for the treatment of moderate to severe plaque psoriasis in the US, Europe, and Australia. The safety profile of tildrakizumab was characterized in nonclinical studies using a pharmacologically relevant cynomolgus monkey model. In repeat-dose toxicity studies, cynomolgus monkeys were chronically treated with subcutaneous (SC) injections of 100 mg/kg of tildrakizumab every 2 weeks up to 9 months. Tildrakizumab was well tolerated, with no toxicological findings (including assessment of reproductive organs; hormonal effects; and cardiovascular, respiratory, and central nervous system function) at systemic exposures approximately 90 times higher than the recommended human dose of 100 mg. An embryofetal developmental study conducted in pregnant monkeys revealed no treatment-related effects to the developing fetus following SC administration of tildrakizumab 100 mg/kg. In a pre- and postnatal development study, 2 neonatal deaths due to potential viral infection at 100 mg/kg were considered of uncertain relationship to the treatment based on a lack of historical data on the occurrence of viral infection in neonate cynomolgus monkeys. The results of this comprehensive nonclinical safety program support the safe use of tildrakizumab.

Keywords: Animal model; Interleukin-23; Monoclonal antibody; Pre- and postnatal development; Psoriasis.

MeSH terms

  • Animals
  • Antibodies, Monoclonal, Humanized / blood
  • Antibodies, Monoclonal, Humanized / pharmacokinetics
  • Antibodies, Monoclonal, Humanized / toxicity*
  • Embryonic Development / drug effects
  • Female
  • Fetal Development / drug effects
  • Interleukin-23 Subunit p19 / blood
  • Interleukin-23 Subunit p19 / immunology
  • Macaca fascicularis
  • Male
  • Maternal-Fetal Exchange
  • Milk / chemistry
  • Pregnancy
  • Psoriasis / drug therapy
  • Toxicity Tests, Chronic

Substances

  • Antibodies, Monoclonal, Humanized
  • Interleukin-23 Subunit p19
  • tildrakizumab