ATC Group: J05AF Nucleoside and nucleotide reverse transcriptase inhibitors

The World Health Organization's ATC classification organizes medical drugs based on therapeutic properties, chemical composition, and anatomy. It helps make essential medicines readily available globally and is widely used in the pharmaceutical industry.

Position of J05AF in the ATC hierarchy

Level Code Title
1 J Antiinfectives for systemic use
2 J05 Antivirals for systemic use
3 J05A Direct acting antivirals
4 J05AF Nucleoside and nucleotide reverse transcriptase inhibitors

Group J05AF contents

Code Title
J05AF01 Zidovudine
J05AF02 Didanosine
J05AF03 Zalcitabine
J05AF04 Stavudine
J05AF05 Lamivudine
J05AF06 Abacavir
J05AF07 Tenofovir disoproxil
J05AF08 Adefovir dipivoxil
J05AF09 Emtricitabine
J05AF10 Entecavir
J05AF11 Telbivudine
J05AF12 Clevudine
J05AF13

Active ingredients in J05AF

Active Ingredient Description
Abacavir

Abacavir is a NRTI. It is a potent selective inhibitor of HIV-1 and HIV-2. Abacavir is metabolised intracellularly to the active moiety, carbovir 5'-triphosphate (TP). In vitro studies have demonstrated that its mechanism of action in relation to HIV is inhibition of the HIV reverse transcriptase enzyme, an event which results in chain termination and interruption of the viral replication cycle.

Adefovir dipivoxil

Adefovir dipivoxil is an oral prodrug of adefovir, an acyclic nucleotide phosphonate analogue of adenosine monophosphate, which is actively transported into mammalian cells where it is converted by host enzymes to adefovir diphosphate. Adefovir diphosphate inhibits viral polymerases by competing for direct binding with the natural substrate (deoxyadenosine triphosphate) and, after incorporation into viral DNA, causes DNA chain termination.

Didanosine

Didanosine belongs to a class of medicines called nucleoside analogues or nucleoside reversetranscriptase inhibitors (NRTIs). Intracellularly, didanosine is converted by cellular enzymes to the active metabolite, dideoxyadenosine 5'-triphosphate. Dideoxyadenosine 5'-triphosphate inhibits the activity of HIV-1 reverse transcriptase both by competing with the natural substrate, deoxyadenosine 5'-triphosphate, and by its incorporation into viral DNA causing termination of viral DNA chain elongation.

Emtricitabine

Emtricitabine is a synthetic nucleoside analogue of cytidine with activity that is specific to HIV-1, HIV-2 and HBV. Emtricitabine is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate, which competitively inhibits HIV-1 reverse transcriptase, resulting in DNA chain termination. Emtricitabine is a weak inhibitor of mammalian DNA polymerase α, β and ε and mitochondrial DNA polymerase γ.

Entecavir

Entecavir, a guanosine nucleoside analogue with activity against HBV polymerase, is efficiently phosphorylated to the active triphosphate (TP) form, which has an intracellular half-life of 15 hours. By competing with the natural substrate deoxyguanosine TP, entecavir-TP functionally inhibits the 3 activities of the viral polymerase: (1) priming of the HBV polymerase, (2) reverse transcription of the negative strand DNA from the pregenomic messenger RNA, and (3) synthesis of the positive strand HBV DNA.

Lamivudine

Lamivudine is a nucleoside analogue which has activity against human immunodeficiency virus (HIV) and hepatitis B virus (HBV). Its main mode of action is as a chain terminator of viral reverse transcription.

Stavudine

Stavudine, a thymidine analogue, is phosphorylated by cellular kinases to stavudine triphosphate which inhibits HIV reverse transcriptase by competing with the natural substrate, thymidine triphosphate. It also inhibits viral DNA synthesis by causing DNA chain termination due to a lack of the 3'-hydroxyl group necessary for DNA elongation. Cellular DNA polymerase γ is also sensitive to inhibition by stavudine triphosphate, while cellular polymerases α and β are inhibited at concentrations 4,000-fold and 40-fold higher, respectively, than that needed to inhibit HIV reverse transcriptase.

Telbivudine

Telbivudine is a synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase. It is efficiently phosphorylated by cellular kinases to the active triphosphate form. Incorporation of telbivudine-5'-triphosphate into viral DNA causes DNA chain termination, resulting in inhibition of HBV replication.

Tenofovir disoproxil

Tenofovir disoproxil is absorbed and converted to the active substance tenofovir, which is a nucleoside monophosphate analogue. Tenofovir is then converted to the active metabolite, tenofovir diphosphate, an obligate chain terminator, by constitutively expressed cellular enzymes. Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and the HBV polymerase by direct binding competition with the natural deoxyribonucleotide substrate and, after incorporation into DNA, by DNA chain termination.

Zalcitabine

Zalcitabine is a nucleoside analog reverse-transcriptase inhibitor (NRTI).

Zidovudine

Zidovudine is an antiviral agent which is highly active in vitro against retroviruses including the Human Immunodeficiency Virus (HIV).

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