ABSTRACT
Objective To review pharmacological mechanism, pharmacokinetics, clinical research progress and prospects of pradefovir, a liver targeted medicine for hepatitis B.Methods The studies of pradefovir were summarized by searching literature databases of Web of Science,Elsevier ScienceDirect,Springer Link,Wiley Online Library, Pubmed, CNKI, Wanfang and VIP datebase.Results Pradefovir is a prodrug that targets to the liver, which absorbs rapidly by oral administration.Pradefovir could be quickly converted to adefovir with hepatic drug metabolizing enzyme CYP3A4. Compared with adefovir dipivoxil, it has shown smaller nephrotoxicity and larger liver targeting.Conclusion Pradefovir has shown favorable safety and effectiveness in the clinical study and has no durg resistance to be found.The approval Ⅲ clinical trial has been acquired of pradefovir in USA and has enteredⅠ clinical trial currently in our country, which has good prospects for clinical application in future.
ABSTRACT
El tratamiento de hepatitis B está en fase de experimentación en espera de obtener medicamentos con mayor eficiencia y menor resistencia. La mayoría de los medicamentos, en experimentación, son análogos de nucleósidos y nucleóticos que inhiben competitivamente la polimerasa HBV. La emtricitrabina es un medicamento que potencialmente se podría utilizar en pacientes coinfectados con HIV con el inconveniente de la resistencia cruzada a lamivudina. El tenofovir es un medicamento prometedor en los pacientes coinfectados con HIV tanto los Hbe Ag negativo como los resistentes a lamivudina. Prodrogas como el pradefovir se visualizan como medicamentos más efectivos y con menos efectos adversos que la droga original. La mayoría de estos medicamentos requieren de más estudios para definir su rol en el tratamiento de la hepatitis B crónica.
Hepatitis B treatment is in the experimentation stage expecting to obtain more effective and less resistant treatments. Most treatments under experimentation are nucleoside and nucleotide analogues that competitively inhibit HBV polymerase. Emtricitabine is a drug that could be used in con-infected HIV patients with the inconvenience of cross-resistance to lamivudine. Tenofovir is a promising drug for co-infected HIV patients, not only for the HbeAg negative but also for those resistant to lamuvidine. Pro-drugs such as pradefovir are considered more effective and with less adverse effects than the original drug. Most of these drugs require more studies to define its role in the treatment of chronic hepatitis B.