icotrokinra (Icotyde)

Structure

• cyclic peptide

Indications

• treatment of moderate-severe plaque psoriasis in adults & adolescents >= 12 years
• ulcerative colitis (investigational)

Dosage

• 200 mg once daily
  • taken upon waking on an empty stomach, at least 30 minutes before food
  • must be swallowed whole

Tablet: 200 mg

Dosage adjustment in renal failure

• none*

* monitor for potential adverse reactions when ICOTYDE is used in patients with eGFR <60 mL/min

Pharmacokinetics

• median (min, max) time to maximum plasma concentration (Tmax) is 2 (0.25, 8) hours
• steady state is reached in ~3 days
• food decreases absorption 43%
• 52% bound to plasma protein
• apparent volume of distribution is 92,800 L
• median elimination half-life is 12 hours
• metabolized by peptide catabolism
• excreted in feces, very little excreted in urine
• no significant age differences in pharmacokinetics 12-87 years

Adverse effects

• common
  • headache, nausea, cough, & fatigue

• drug adverse effects of immunosuppressive agents
• drug adverse effects of biologic immunosuppressive agents

Mechanism of action

• 1st IL-23 antagonist
  • high skin clearance rates comparable to injectables

More general terms

• IL-23 antagonist
• dermatologic agent

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=162462321
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=171390009