C.7 Flashcards
Agents against hepatitis virus
- Recombinant protein: (PEG)-IFN-α
- HBV DNA polymerase inhibitor: Entecavir
- NRTI: Tenofovir
- NS5B Polymerase inhibitor: Sofosbuvir
- Non nucleotide NS5B inhibitor: Dasabuvir, Paritaprevir
- NS3-4A protease inhibitor: Grazoprevir
- NS5A protease inhibitor: Velpatasvir, Elbasavir
(PEG)-interferon-α (IFNα2a, IFNα2b)
MOA: recombinant protein, complex antiviral activity (→ induces more than 20 antiviral proteins);
Kinetics: ROA-s.c, i.m, PEGylation-(PEGylated IFNs are absorbed slower) administered once a week;
IND: chronic HBV, chronic HCV (alone or in combination with Ribavirin), Herpes virus, Papillomavirus, Kaposi’s sarcoma in HIV;
SEs: flu-like symptoms (fever, fatigue, myalgia), suppression of hematopoiesis, neurotoxicity (sleeping, depression), liver dysfunction, alopecia
Entecavir
MOA: Guanosine analog, inhibits HBV DNA-polymerase; IND: HBV infection;
Kinetics: administered p.o, almost no primary resistance;
SEs: well tolerated- headache, dizziness, fatigue, nausea
Tenofovir
MOA: AMP analog+antiretroviral agent (NRTI);
IND: HBV infection;
Kinetics: administered p.o, less primary resistance, higher efficacy;
SEs: can be nephrotoxic
Sofosbuvir
MOA: NS5B polymerase (=RNA dependent RNA polymerase) inhibitor, TMP analog→ causes chain termination;
Kinetics: no resistance;
IND: HCV;
SEs: low toxicity
Dasabuvir, Paritaprevir
MOA: Non-nucleoside NS5B-polymerase inhibitor;
IND: used as a part of a combination for Type1 HCV with Paritaprevir (+Ritonavir booster)
Grazoprevir
MOA: NS3-4A protease (serine protease formed by HCV) inhibitors;
IND: HCV;
Kinetics: administered p.o, hepatic metabolism by CYP3A4 and CYP2C8, resistance develops in short time (→ no monotherapy);
SEs: skin reaction, headache, less common- loss of appetite, trouble sleeping
Velpatasvir, Elbasavir
MOA: NS5A (protease important in viral replication and assembly) inhibitor;
IND: HCV, efficient for all genotypes, in combination; Extra: low genetic barrier
