ATC Group: J05A Direct acting antivirals

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 J05A in the ATC hierarchy

Level Code Title
1 J Antiinfectives for systemic use
2 J05 Antivirals for systemic use
3 J05A Direct acting antivirals

Group J05A contents

Code Title
J05AA Thiosemicarbazones
J05AB Nucleosides and nucleotides excl. reverse transcriptase inhibitors
J05AC Cyclic amines
J05AD Phosphonic acid derivatives
J05AE Protease inhibitors
J05AF Nucleoside and nucleotide reverse transcriptase inhibitors
J05AG Non-nucleoside reverse transcriptase inhibitors
J05AH Neuraminidase inhibitors
J05AJ Integrase inhibitors
J05AL Συνδυασμοί αναστολέων πρωτεάσης
J05AP Antivirals for treatment of HCV infections
J05AR Antivirals for treatment of HIV infections, combinations
J05AX Other antivirals

Active ingredients in J05A

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.

Aciclovir

Acyclovir is an antiviral agent with activity against herpes simplex virus and varicella-zoster virus. Acyclovir inhibits the DNA polymerase of the virus, preventing further proliferation.

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.

Amenamevir
Amprenavir

Amprenavir is a competitive inhibitor of HIV-1 protease. Amprenavir binds to the active site of HIV-1 protease and thereby prevents the processing of viral gag and gag-pol polyprotein precursors, resulting in the formation of immature non-infectious viral particles.

Asunaprevir

Asunaprevir is an orally bioavailable inhibitor of the nonstructural protein 3 (NS3), with potential activity against hepatitis C virus (HCV). Upon administration, asunaprevir binds to the active center of the HCV NS3 and prevents NS3 protease-mediated polyprotein maturation. This disrupts the processing of viral proteins required for HCV replication.

Atazanavir

Atazanavir is an azapeptide HIV-1 protease inhibitor (PI). The compound selectively inhibits the virus-specific processing of viral Gag-Pol proteins in HIV-1 infected cells, thus preventing formation of mature virions and infection of other cells.

Baloxavir marboxil

Baloxavir marboxil is a prodrug that is converted by hydrolysis to baloxavir, the active form that exerts anti-influenza activity. Baloxavir acts on the cap-dependent endonuclease (CEN), an influenza virus-specific enzyme in the polymerase acidic (PA) subunit of the viral RNA polymerase complex and thereby inhibits the transcription of influenza virus genomes resulting in inhibition of influenza virus replication.

Boceprevir

Boceprevir is an inhibitor of the HCV NS3 protease. Boceprevir covalently, yet reversibly, binds to the NS3 protease active site serine (Ser139) through a (alpha)-ketoamide functional group to inhibit viral replication in HCV-infected host cells.

Brivudine

Brivudine is a thymidine analogue with antiviral activity, indicated for the early treatment of acute herpes zoster in adult patients. Brivudine is incorporated into the viral DNA and blocks the action of DNA polymerases, thus inhibiting viral replication.

Bulevirtide

Bulevirtide blocks the entry of HBV and HDV into hepatocytes by binding to and inactivating NTCP, a bile salt liver transporter serving as essential HBV/HDV entry receptor.

Cabotegravir

Cabotegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle.

Cidofovir

Cidofovir suppresses HCMV replication by selective inhibition of viral DNA synthesis. Biochemical data support selective inhibition of HSV-1, HSV-2 and HCMV DNA polymerases by cidofovir diphosphate, the active intracellular metabolite of cidofovir.

Daclatasvir

Daclatasvir is an inhibitor of nonstructural protein 5A (NS5A), a multifunctional protein that is an essential component of the HCV replication complex. Daclatasvir inhibits both viral RNA replication and virion assembly.

Darunavir

Darunavir is an inhibitor of the dimerisation and of the catalytic activity of the HIV-1 protease (KD of 4.5 × 10-12 M). It selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in virus infected cells, thereby preventing the formation of mature infectious virus particles.

Darunavir and Cobicistat

Darunavir is an inhibitor of the dimerisation and of the catalytic activity of the HIV-1 protease. It selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in virus infected cells, thereby preventing the formation of mature infectious virus particles. Cobicistat is a mechanism-based inhibitor of cytochromes P450 of the CYP3A subfamily. Inhibition of CYP3A-mediated metabolism by cobicistat enhances the systemic exposure of CYP3A substrates, such as darunavir, where bioavailability is limited and half-life is shortened due to CYP3A-dependent metabolism.

Dasabuvir

Dasabuvir is a non-nucleoside inhibitor of the HCV RNA-dependent RNA polymerase encoded by the NS5B gene, which is essential for replication of the viral genome. Co-administration of dasabuvir with ombitasvir/paritaprevir/ritonavir combines three direct-acting antiviral medicinal products with distinct mechanisms of action and non-overlapping resistance profiles to target HCV at multiple steps in the viral lifecycle.

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.

Dolutegravir

Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral Deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle.

Dolutegravir and Rilpivirine
Doravirine

Doravirine is a pyridinone non-nucleoside reverse transcriptase inhibitor of HIV-1 and inhibits HIV-1 replication by non-competitive inhibition of HIV-1 reverse transcriptase (RT). Doravirine does not inhibit the human cellular DNA polymerases α, β, and mitochondrial DNA polymerase γ.

Efavirenz

Efavirenz is a NNRTI of HIV-1. Efavirenz is a non-competitive inhibitor of HIV-1 reverse transcriptase (RT) and does not significantly inhibit HIV-2 RT or cellular DNA polymerases (α, β, γ or δ).

Elbasvir
Elbasvir and Grazoprevir

Elbasvir/grazoprevir combines two direct-acting antiviral agents with distinct mechanisms of action and nonoverlapping resistance profiles to target HCV at multiple steps in the viral lifecycle. Elbasvir is an inhibitor of HCV NS5A, which is essential for viral RNA replication and virion assembly. Grazoprevir is an inhibitor of the HCV NS3/4A protease which is necessary for the proteolytic cleavage of the HCV encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication.

Elvitegravir

Elvitegravir, is a type of antiviral agent called an ‘integrase inhibitor’. It blocks an enzyme called integrase, which is involved in a step in the reproduction of HIV. When the enzyme is blocked, the virus cannot reproduce normally, slowing down the spread of infection.

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.

Emtricitabine and Tenofovir alafenamide

Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) and nucleoside analogue of 2'-deoxycytidine. Tenofovir alafenamide is a nucleotide reverse transcriptase inhibitor (NtRTI) and phosphonamidate prodrug of tenofovir (2'-deoxyadenosine monophosphate analogue). They both inhibit HIV replication through incorporation into viral DNA by the HIV RT, which results in DNA chain-termination. They have activity against HIV-1, HIV-2, and HBV.

Emtricitabine, Tenofovir alafenamide and Bictegravir
Emtricitabine, Tenofovir disoproxil and Efavirenz

Efavirenz is an NNRTI of HIV-1. Efavirenz non-competitively inhibits HIV-1 reverse transcriptase (RT) and does not significantly inhibit human immunodeficiency virus-2 (HIV-2) RT or cellular deoxyribonucleic acid (DNA) polymerases (α, β, γ, and δ). Emtricitabine is a nucleoside analogue of cytidine. Tenofovir disoproxil is converted in vivo to tenofovir, a nucleoside monophosphate (nucleotide) analogue of adenosine monophosphate. Emtricitabine and tenofovir are phosphorylated by cellular enzymes to form emtricitabine triphosphate and tenofovir diphosphate, respectively, which competitively inhibit HIV-1 reverse transcriptase, resulting in DNA chain termination.

Emtricitabine, Tenofovir disoproxil and Rilpivirine

Emtricitabine is a nucleoside analogue of cytidine. Tenofovir disoproxil is converted in vivo to tenofovir, a nucleoside monophosphate (nucleotide) analogue of adenosine monophosphate. Both emtricitabine and tenofovir have activity that is specific to HIV-1, HIV-2 and, HBV. Rilpivirine is a diarylpyrimidine NNRTI of HIV-1. Rilpivirine activity is mediated by non-competitive inhibition of HIV-1 reverse transcriptase (RT).

Enfuvirtide

Enfuvirtide is a member of the therapeutic class called fusion inhibitors. It is an inhibitor of the structural rearrangement of HIV-1 gp41 and functions by specifically binding to this virus protein extracellularly thereby blocking fusion between the viral cell membrane and the target cell membrane, preventing the viral RNA from entering into the target cell.

Ensitrelvir
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.

Etravirine

Etravirine is an non-nucleoside reverse transcriptase inhibitors (NNRTI) of human immunodeficiency virus type 1 (HIV-1). Etravirine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme’s catalytic site.

Famciclovir

Famciclovir is the oral prodrug of penciclovir. Famciclovir is rapidly converted in vivo into penciclovir, which has in vitro activity against herpes simplex viruses (HSV types 1 and 2), varicella zoster virus (VZV), Epstein-Barr virus and cytomegalovirus.

Favipiravir

Favipiravir is metabolized in cells to a ribosyl triphosphate form (favipiravir RTP) and that favipiravir RTP selectively inhibits RNA polymerase involved in influenza viral replication.

Fosamprenavir

Fosamprenavir after oral administration, is rapidly and almost completely hydrolysed to amprenavir and inorganic phosphate prior to reaching the systemic circulation. Amprenavir binds to the active site of HIV-1 protease and thereby prevents the processing of viral gag and gag-pol polyprotein precursors, resulting in the formation of immature noninfectious viral particles.

Foscarnet

Foscarnet is an antiviral agent with a broad spectrum inhibiting all known human viruses of the herpes group. Foscarnet exerts its antiviral activity by a direct inhibition of viral specific DNA polymerase a reverse transcriptase at concentrations that do not affect cellular DNA polymerases.

Fostemsavir

Fostemsavir is an HIV-1 antiretroviral agent. It used in combination with other antiretroviral(s) for the treatment of human immunodeficiency virus type 1 (HIV-1) infection,

Ganciclovir

Ganciclovir, 9-(1,3-dihydroxy-2-propoxymethyl)guanine or DHPG, is a broadspectrum virustatic agent which inhibits the replication of viruses, including viruses of the herpes group, both in vivo and in vitro: herpes simplex types 1 and 2 (HSV), cytomegalovirus (CMV), Epstein-Barr virus (EBV), herpes zoster (HZV).

Glecaprevir
Glecaprevir and Pibrentasvir

Glecaprevir/Pibrentasvir is a fixed-dose combination of two pan-genotypic, direct-acting antiviral agents, glecaprevir (NS3/4A protease inhibitor) and pibrentasvir (NS5A inhibitor), targeting multiple steps in the HCV viral lifecycle.

Grazoprevir
Ibalizumab

Ibalizumab, a humanized monoclonal antibody of immunoglobulin G type 4 (IgG4), is a CD4 domain 2-directed HIV-1 inhibitor. Ibalizumab blocks HIV-1 from infecting CD4+ T cells by binding to domain 2 of CD4 and interfering with the post-attachment steps required for the entry of HIV-1 virus particles into host cells and preventing the viral transmission that occurs via cell-cell fusion.

Indinavir

Indinavir inhibits recombinant HIV-1 and HIV-2 protease with an approximate tenfold selectivity for HIV-1 over HIV-2 proteinase. Indinavir binds reversibly to the protease active site and inhibits competitively the enzyme, thereby preventing cleavage of the viral precursor polyproteins that occurs during maturation of the newly formed viral particle.

Inosine pranobex

Inosine pranobex is a synthetic purine derivative with immunomodulatory and antiviral properties, which result from an apparent in vivo enhancement of host immune responses due to the drug.

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.

Lamivudine and Abacavir

Abacavir and lamivudine are NRTIs, and are potent selective inhibitors of HIV-1 and HIV-2 (LAV2 and EHO) replication. Both abacavir and lamivudine are metabolised sequentially by intracellular kinases to the respective 5'-triphosphate (TP) which are the active moieties. Their main antiviral activity is through incorporation of the monophosphate form into the viral DNA chain, resulting in chain termination.

Lamivudine and Dolutegravir

Lamivudine and dolutegravir combination is indicated for the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in adults and adolescents. Dolutegravir inhibits HIV integrase and lamivudine, via its active metabolite 5'-triphosphates (TP) (an analogue for cytidine), inhibits reverse transcriptase of HIV-1 and HIV-2.

Lamivudine, Abacavir and Dolutegravir

Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral Deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle. Abacavir and lamivudine are potent selective inhibitors of HIV-1 and HIV-2.

Lamivudine, Tenofovir disoproxil and Doravirine

Lamivudine is a nucleoside analogue. Intracellularly, lamivudine is phosphorylated to its active 5'-triphosphate metabolite, lamivudine triphosphate (3TC-TP). The principal mode of action of 3TC-TP is inhibition of HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleotide analogue. Tenofovir diphosphate inhibits the activity of HIV-1 RT by competing with the natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, by DNA chain termination. Doravirine is a pyridinone non-nucleoside reverse transcriptase inhibitor of HIV-1 and inhibits HIV-1 replication by non-competitive inhibition of HIV-1 RT.

Laninamivir
Lenacapavir

Lenacapavir is a multistage, selective inhibitor of HIV-1 capsid function that directly binds to the interface between capsid protein (CA) subunits. Lenacapavir inhibits HIV-1 replication by interfering with multiple, essential steps of the viral lifecycle, including capsid-mediated nuclear uptake of HIV-1 proviral DNA, virus assembly and release, and capsid core formation.

Letermovir

Letermovir inhibits the CMV DNA terminase complex which is required for cleavage and packaging of viral progeny DNA. Letermovir affects the formation of proper unit length genomes and interferes with virion maturation. Letermovir is indicated for prophylaxis of cytomegalovirus (CMV) reactivation and disease.

Lopinavir and Ritonavir

Lopinavir provides the antiviral activity of lopinavir/ritonavir. Lopinavir is an inhibitor of the HIV-1 and HIV-2 proteases. Inhibition of HIV protease prevents cleavage of the gag-pol polyprotein resulting in the production of immature, non-infectious virus.

Lysozyme

Lysozyme is a naturally occurring enzyme found in bodily secretions such as tears, saliva, and milk. It functions as an antimicrobial agent by cleaving the peptidoglycan component of bacterial cell walls, which leads to cell death.

Maraviroc

Maraviroc is a member of a therapeutic class called CCR5 antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5, preventing CCR5-tropic HIV-1 from entering cells.

Maribavir

Maribavir is a competitive inhibitor of the UL97 protein kinase. UL97 inhibition occurs at the viral DNA replication phase, inhibiting UL97 serine/threonine kinase by competitively inhibiting the binding of ATP to the kinase ATP-binding site, without affecting the concatemer maturation process, abolishing phosphotransferase inhibiting CMV DNA replication and maturation, CMV DNA encapsidation, and CMV DNA nuclear egress.

Molnupiravir

Molnupiravir is indicated for treatment of mild to moderate coronavirus disease 2019 (COVID-19) in adults with a positive SARS-COV-2 diagnostic test and who have at least one risk factor for developing severe illness. Molnupiravir is a prodrug that is metabolised to the ribonucleoside analogue N-hydroxycytidine (NHC) which distributes into cells where it is phosphorylated to form the pharmacologically active ribonucleoside triphosphate (NHC-TP).

Nelfinavir

Nelfinavir reversibly binds to the active site of HIV protease and prevents cleavage of the polyproteins resulting in the formation of immature non-infectious viral particles.

Nevirapine

Nevirapine is a NNRTI of HIV-1. Nevirapine is a non-competitive inhibitor of the HIV-1 reverse transcriptase, but it does not have a biologically significant inhibitory effect on the HIV-2 reverse transcriptase or on eukaryotic DNA polymerases α, β, γ, or δ.

Ombitasvir, Paritaprevir and Ritonavir

Ombitasvir/paritaprevir/ritonavir, when co-administered with dasabuvir, combines three direct-acting antiviral medicinal products with distinct mechanisms of action and non-overlapping resistance profiles to target HCV at multiple steps in the viral lifecycle. Ombitasvir is an inhibitor of HCV NS5A which is essential for viral replication. Paritaprevir is an inhibitor of HCV NS3/4A protease which is necessary for the proteolytic cleavage of the HCV encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication. Ritonavir is not active against HCV. Ritonavir is a CYP3A inhibitor that increases the systemic exposure of the CYP3A substrate paritaprevir.

Oseltamivir

Oseltamivir (oseltamivir carboxylate) is a selective inhibitor of influenza virus neuraminidase enzymes, which are glycoproteins found on the virion surface. Viral neuraminidase enzyme activity is important both for viral entry into uninfected cells and for the release of recently formed virus particles from infected cells, and for the further spread of infectious virus in the body.

Penciclovir

Penciclovir has demonstrated in vivo and in vitro activity against herpes simplex viruses (types 1 and 2) and varicella zoster virus. Penciclovir triphosphate persists in infected cells for more than 12 hours where it inhibits replication of viral DNA and has a half-life of 9, 10 and 20 hours in cells infected with varicella zoster virus, herpes simplex virus type 1 and herpes simplex virus type 2 respectively.

Peramivir

Peramivir is an inhibitor of influenza virus neuraminidase, an enzyme that releases viral particles from the plasma membrane of infected cells and is also important for viral entry into uninfected cells, which causes further spread of infectious virus in the body.

Pibrentasvir

Pibrentasvir is a pan-genotypic inhibitor of HCV nonstructural protein 5A (NS5A), which is essential for viral RNA replication and virion assembly.

Raltegravir

Raltegravir is an integrase strand transfer inhibitor active against the Human Immunodeficiency Virus (HIV-1). Raltegravir inhibits the catalytic activity of integrase, an HIV-encoded enzyme that is required for viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of the HIV genome into the host cell genome.

Ribavirin

Ribavirin is a synthetic nucleoside analogue which has shown in vitro activity against some RNA and DNA viruses. The mechanism by which ribavirin in combination with other medicinal products exerts its effects against HCV is unknown.

Rilpivirine

Rilpivirine is a diarylpyrimidine NNRTI of HIV-1. Rilpivirine activity is mediated by non-competitive inhibition of HIV-1 reverse transcriptase (RT). Rilpivirine does not inhibit the human cellular DNA polymerases α, β and γ.

Ritonavir

Ritonavir is an orally active peptidomimetic inhibitor of the HIV-1 and HIV-2 aspartyl proteases. Inhibition of HIV protease renders the enzyme incapable of processing the gag-pol polyprotein precursor which leads to the production of HIV particles with immature morphology that are unable to initiate new rounds of infection. Ritonavir has selective affinity for the HIV protease and has little inhibitory activity against human aspartyl proteases. Pharmacokinetic enhancement by ritonavir is based on ritonavir’s activity as a potent inhibitor of CYP3A-mediated metabolism.

Saquinavir

Saquinavir selectively inhibits the HIV protease, thereby preventing the creation of mature infectious virus particles. The HIV protease is an essential viral enzyme required for the specific cleavage of viral gag and gag-pol polyproteins.

Simeprevir

Simeprevir is a specific inhibitor of the hepatitis C virus (HCV) NS3/4A serine protease, which is essential for viral replication. In a biochemical assay, simeprevir inhibited the proteolytic activity of recombinant genotype 1a and 1b HCV NS3/4A proteases, with median Ki values of 0.5 nM and 1.4 nM, respectively.

Sofosbuvir

Sofosbuvir is a pan-genotypic inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is essential for viral replication. Sofosbuvir is a nucleotide prodrug that undergoes intracellular metabolism to form the pharmacologically active uridine analog triphosphate (GS-461203), which can be incorporated into HCV RNA by the NS5B polymerase and acts as a chain terminator.

Sofosbuvir and Ledipasvir

Sofosbuvir is a pan-genotypic inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is essential for viral replication. Ledipasvir is a HCV inhibitor targeting the HCV NS5A protein, which is essential for both RNA replication and the assembly of HCV virions.

Sofosbuvir and Velpatasvir

Sofosbuvir is a pan-genotypic inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is essential for viral replication. Velpatasvir is a HCV inhibitor targeting the HCV NS5A protein, which is essential for both RNA replication and the assembly of HCV virions.

Sofosbuvir, Velpatasvir and Voxilaprevir

Sofosbuvir/velpatasvir/voxilaprevir combination is indicated for the treatment of chronic hepatitis C virus (HCV) infection. Sofosbuvir is a pan-genotypic inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is required for viral replication. Velpatasvir is a pan-genotypic HCV inhibitor targeting the HCV NS5A protein, which is required for viral replication. Voxilaprevir is a pan-genotypic inhibitor of the HCV NS3/4A protease. Voxilaprevir acts as a noncovalent, reversible inhibitor of the NS3/4A protease.

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.

Tecovirimat

Tecovirimat is an antiviral drug against variola (smallpox) virus. Tecovirimat inhibits the activity of the orthopoxvirus VP37 protein, which is encoded by a highly conserved gene in all members of the orthopoxvirus genus. Tecovirimat blocks the interaction of VP37 with cellular Rab9 GTPase and TIP47, which prevents the formation of egress competent enveloped virions necessary for cell-to-cell and long-range dissemination of virus.

Telaprevir

Telaprevir is an inhibitor of the HCV NS3•4A serine protease, which is essential for viral replication.

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.

Tenofovir disoproxil and Emtricitabine

Emtricitabine is a nucleoside analogue of cytidine. Tenofovir disoproxil is converted in vivo to tenofovir, a nucleoside monophosphate (nucleotide) analogue of adenosine monophosphate. Both emtricitabine and tenofovir have activity that is specific to human immunodeficiency virus (HIV-1 and HIV-2) and hepatitis B virus.

Tipranavir

Tipranavir is a non-peptidic inhibitor of the HIV-1 protease that inhibits viral replication by preventing the maturation of viral particles.

Tromantadine

Tromantadine is an antiviral medicine used to treat herpes simplex virus.

Valaciclovir

Valaciclovir, an antiviral, is the L-valine ester of aciclovir. Valaciclovir is rapidly and almost completely converted in man to aciclovir and valine. Aciclovir is a specific inhibitor of the herpes viruses with in vitro activity against herpes simplex viruses (HSV) type 1 and type 2, varicella zoster virus (VZV), cytomegalovirus (CMV), Epstein-Barr Virus (EBV), and human herpes virus 6 (HHV-6).

Valganciclovir

Valganciclovir is an L-valyl ester (prodrug) of ganciclovir. Ganciclovir is a synthetic analogue of 2'-deoxyguanosine and inhibits replication of herpes viruses in vitro and in vivo.

Vidarabine
Voxilaprevir

Voxilaprevir is a pan-genotypic inhibitor of the HCV NS3/4A protease. Voxilaprevir acts as a noncovalent, reversible inhibitor of the NS3/4A protease.

Zalcitabine

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

Zanamivir

Zanamivir is a selective inhibitor of neuraminidase, the influenza virus surface enzyme. Neuraminidase inhibition occurred in vitro at very low zanamivir concentrations (50% inhibition at 0.64nM–7.9nM against influenza A and B strains).

Zidovudine

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

Zidovudine and Lamivudine

Lamivudine and zidovudine are nucleoside analogues which have activity against HIV. Additionally, lamivudine has activity against hepatitis B virus (HBV). Both medicinal products are metabolised intracellularly to their active moieties, lamivudine 5'-triphosphate (TP) and zidovudine 5'-TP respectively. Their main modes of action are as chain terminators of viral reverse transcription.

Zidovudine, Lamivudine and Abacavir

Abacavir, lamivudine and zidovudine are all NRTIs, and are potent selective inhibitors of HIV-1 and HIV-2.All three medicinal products are metabolised sequentially by intracellular kinases to the respective 5′-triphosphate (TP). Lamivudine-TP, carbovir-TP (the active triphosphate form of abacavir) and zidovudine-TP are substrates for and competitive inhibitors of HIV reverse transcriptase (RT). However, their main antiviral activity is through incorporation of the monophosphate form into the viral DNA chain, resulting in chain termination. Abacavir, lamivudine and zidovudine triphosphates show significantly less affinity for host cell DNA polymerases.

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EPIVIR Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
EVIPLERA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
EXVIERA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
FAMVIR Film-coated tablets Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
FOSCAVIR Solution for infusion Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
Fuzeon 90 mg/ml powder and solvent for solution for injection Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
FUZEON Powder and solvent for solution for injection European Medicines Agency (EU) MPI, EU: SmPC
HARVONI Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
HEPCLUDEX Powder for solution for injection European Medicines Agency (EU) MPI, EU: SmPC
Hepsera 10 mg tablets Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
HEPSERA Tablet European Medicines Agency (EU) MPI, EU: SmPC
IMUNOVIR Tablet Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
INTELENCE Tablet European Medicines Agency (EU) MPI, EU: SmPC
INVIRASE Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
ISENTRESS Chewable tablet European Medicines Agency (EU) MPI, EU: SmPC
ISENTRESS Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
ISENTRESS Granules for oral suspension European Medicines Agency (EU) MPI, EU: SmPC
JULUCA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
KALETRA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
KALETRA Oral solution European Medicines Agency (EU) MPI, EU: SmPC
KIVEXA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
KOVATRAX Film-coated tablet Health Products Regulatory Authority (ZA) MPI, Generic
LAGEVRIO Hard capsule Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
Lamivudine 3TC Tablets Health Products and Food Branch (CA) MPI, CA: SPM
LANOGRAV Film-coated tablet Health Products Regulatory Authority (ZA) MPI, Generic
LIVTENCITY Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
MAVIRET Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
MEDOVIR Cream Υπουργείο Υγείας (CY) MPI, EU: SmPC
MEDOVIR Powder for solution for infusion Υπουργείο Υγείας (CY) MPI, EU: SmPC
MEDOVIR Tablet Υπουργείο Υγείας (CY) MPI, EU: SmPC
NATFLU Hard capsule Health Sciences Authority (SG) MPI, Generic
NEVIRAPINE TEVA Tablet European Medicines Agency (EU) MPI, EU: SmPC
NORVIR Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
ODEFSEY Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
OSELFLU Gelatin capsule Health Products Regulatory Authority (ZA) MPI, Generic
PIFELTRO Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
PREVYMIS Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
PREZCOBIX Film-coated tablet FDA, National Drug Code (US) MPI, US: SPL/PLR
Prezista 75 mg, 150 mg, 400 mg, 600 mg film-coated tablets and Oral suspension 100mg/ml Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
REBETOL Hard capsule European Medicines Agency (EU) MPI, EU: SmPC
REKAMBYS Prolonged-release suspension for injection European Medicines Agency (EU) MPI, EU: SmPC
RELENZA Inhalation powder, pre-dispensed Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
RETROVIR Capsules, hard Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
RETROVIR Concentrate for solution for infusion Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
RETROVIR Oral solution/syrup Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
REYATAZ Hard capsules European Medicines Agency (EU) MPI, EU: SmPC
REYDIN Film-coated tablet Health Products Regulatory Authority (ZA) MPI, Generic
REZOLSTA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
RILOVIA Film-coated tablet Health Products Regulatory Authority (ZA) MPI, Generic
RITONAVIR MYLAN Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
RIZENE Film-coated tablet Health Products Regulatory Authority (ZA) MPI, EU: SmPC
RUKOBIA Extended-release tablet FDA, National Drug Code (US) MPI, US: SPL/PLR
SEBIVO Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
SELZENTRY Film-coated tablet / Oral solution FDA, National Drug Code (US) MPI, US: SPL/PLR
SITAVIG Delayed-release tablet FDA, National Drug Code (US) MPI, US: SPL/PLR
SOVALDI Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
STOCRIN Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
SUNLENCA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
SUNLENCA Solution for injection European Medicines Agency (EU) MPI, EU: SmPC
SYNTOVIR Tablet Υπουργείο Υγείας (CY) MPI, EU: SmPC
TAMIFLU Hard capsule European Medicines Agency (EU) MPI, EU: SmPC
TAMIFLU Powder for oral suspension European Medicines Agency (EU) MPI, EU: SmPC
TELATRI Film-coated tablet Health Products Regulatory Authority (ZA) MPI, Generic
TELZIR Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
TIVICAY Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
TRIUMEQ Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
TRIZIVIR Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
TROGARZO Solution for injection FDA, National Drug Code (US) MPI, US: SPL/PLR
TRUVADA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
VALACICLOVIR Film-coated tablet Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
VALGANCICLOVIR Film-coated tablets Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
VALTREX Film-coated tablet FDA, National Drug Code (US) MPI, US: SPL/PLR
VEKLURY Powder for concentrate for solution for infusion European Medicines Agency (EU) MPI, EU: SmPC
VEMLIDY Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
Videx EC 125mg, 200mg, 250mg and 400mg Gastro-resistant Capsules Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
VIEKIRAX Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
VIRAZOLE Inhalation solution FDA, National Drug Code (US) MPI, US: SPL/Old
VIREAD Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
VISTIDE Concentrate for solution for infusion Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
VOCABRIA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
VOCABRIA Film-coated tablet FDA, National Drug Code (US) MPI, US: SPL/PLR
VOCABRIA Prolonged-release suspension for injection European Medicines Agency (EU) MPI, EU: SmPC
VOLUTRIP Film-coated tablet Health Products Regulatory Authority (ZA) MPI, Generic
VOSEVI Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
XOFLUZA Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
XOFLUZA Film-coated tablet FDA, National Drug Code (US) MPI, US: SPL/PLR
ZELITREX Tablet Health Products Regulatory Authority (ZA) MPI, Generic
ZEPATIER Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
ZERIT Hard capsule European Medicines Agency (EU) MPI, EU: SmPC
ZERIT Powder for oral solution European Medicines Agency (EU) MPI, EU: SmPC
ZIAGEN Film-coated tablet European Medicines Agency (EU) MPI, EU: SmPC
ZIAGEN Oral solution European Medicines Agency (EU) MPI, EU: SmPC
ZOVIRAX Cream Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
ZOVIRAX Dispersible film-coated tablets Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
Zovirax Eye Ointment Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC
Zovirax Intravenous injection Medicines & Healthcare Products Regulatory Agency (GB) MPI, EU: SmPC