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 AUC: The area under the plot of plasma concentration (AUC) of drug is 270 mcgh/L [1]
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 16 mcg/L [1]
  Absorption Tmax: The time to maximum plasma concentration (Tmax) is 2 h [1]
  Clearance: The clearance of drug is 117 L/h [2]
  Elimination: Tenofovir alafenamide has been registered to present a bile elimination that corresponds to 47% of the administered dose and a renal elimination the represents about 36% [1]
  Half-life: The concentration or amount of drug in body reduced by one-half in 0.51 hours [3]
  Metabolism: The drug is metabolized via the cathepsin A or carboxylesterase 1 [1]
  Vd: The volume of distribution (Vd) of drug is 100 L [4]

References

• [1] Olkkola KT, Brunetto AV, Mattila MJ: Pharmacokinetics of oxicam nonsteroidal anti-inflammatory agents. Clin Pharmacokinet. 1994 Feb;26(2):107-20.
• [2] European Medicines Agency Assessment Report: Tenofovir Alafenamide
• [3] Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Nov;78(17):1817-1828. doi: 10.1007/s40265-018-1010-7.
• [4] Markowitz M, Zolopa A, Squires K, Ruane P, Coakley D, Kearney B, Zhong L, Wulfsohn M, Miller MD, Lee WA: Phase I/II study of the pharmacokinetics, safety and antiretroviral activity of tenofovir alafenamide, a new prodrug of the HIV reverse transcriptase inhibitor tenofovir, in HIV-infected adults. J Antimicrob Chemother. 2014 May;69(5):1362-9. doi: 10.1093/jac/dkt532. Epub 2014 Feb 6.