Minireviews
Copyright ©The Author(s) 2016.
World J Hepatol. Apr 28, 2016; 8(12): 557-565
Published online Apr 28, 2016. doi: 10.4254/wjh.v8.i12.557
Table 1 Main pharmacokinetic properties of the new direct-acting antivirals
DrugMolecular weightEffect of food on absorptionCytochrome P450 enzymes interaction
Binding to plasma proteinHalf-life
EnzymeEffect of the drug on the enzymeEffect of the enzyme on the drug
Sofosbuvir529.45 DaIncreased absorption, slower rateNONoneNone85%0.5 h/26 h1
Simeprevir749.93 DaIncreased absorption, slower rateCYP3A4InhibitorAlter AUC> 99.9%10-41 h
Daclatasvir738.98 DaDecreased absorption2CYP3A4Weak inducerAlter AUC> 99%12-15 h
Ledipasvir888.9 DaNo effectCYP3A4Weak inducerNone> 99.8%47 h
ViekiraxOmbitasvir894.1Increased absorptionCYP3A4InhibitorAlter AUC99.9%21-25 h
Paritaprevir765.8 Da98.6%5.5 h
Ritonavir720.9 Da99%4 h
Dasabuvir493.5 DaIncreased absorptionCYPC19InducerNone99.5% (94.5%3)6 h
CYP2C8NoneAlter AUC
CYP3A4NoneAlter AUC3
CYPC19InducerNone
Table 2 Effect of new direct-acting antivirals in pregnancy and Food and Drug Administration Pregnancy Categories
DrugEmbryotoxicity and/or teratogenicity1Dose-escalation2Transfer across placentaTransfer into milkFDA Pregnancy Category3
SofosbuvirNo28-foldYesYesB
SimeprevirYes4-foldYesYesC
DaclatasvirYes4-foldYesYesNA4
LedipasvirNoMaternal toxic dosesYesYesB
ViekiraxOmbitasvirYes4-foldMinimalYesB
Paritaprevir32-fold
Ritonavir8-fold
DasabuvirNo48-foldMinimalYesB