Details of the Drug

General Information of Drug (ID: )

• #Ro5 Violations (Lipinski): 1:
  Molecular Weight (mw)
  Logarithm of the Partition Coefficient (xlogp)
  Rotatable Bond Count (rotbonds)
  Hydrogen Bond Donor Count (hbonddonor)
  Hydrogen Bond Acceptor Count (hbondacc)
• ADMET Property:
  Absorption Tmax: The time to maximum plasma concentration (Tmax) is 2-4 h [1]
  Clearance: The apparent oral clearance of drug is 53.7 L/h [2]
  Elimination: Following administration of a single radio-labelled dose from the immediate-release formulation, approximately 53% of the total dose was excreted in the feces where 38% of the excreted dose was an unchanged parent drug [3]
  Half-life: The concentration or amount of drug in body reduced by one-half in 8 - 14 hours [1]
  Metabolism: The drug is metabolized via the CYP2D6 [1]
  Vd: The volume of distribution (Vd) of drug is 224 L [3]

References

• [1] FDA Approved Drug Products: RINVOQ (upadacitinib) extended-release tablets, for oral use
• [2] Klunder B, Mittapalli RK, Mohamed MF, Friedel A, Noertersheuser P, Othman AA: Population Pharmacokinetics of Upadacitinib Using the Immediate-Release and Extended-Release Formulations in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I-III Clinical Trials. Clin Pharmacokinet. 2019 Aug;58(8):1045-1058. doi: 10.1007/s40262-019-00739-3.
• [3] Upadacitinib Summary Review - FDA