Repositioning Candidate Details
| Candidate ID: | R0533 |
| Source ID: | DB14126 |
| Source Type: | experimental; investigational |
| Compound Type: | small molecule |
| Compound Name: | Tenofovir |
| Synonyms: | |
| Molecular Formula: | C9H14N5O4P |
| SMILES: | C[C@H](CN1C=NC2=C1N=CN=C2N)OCP(O)(O)=O |
| Structure: |
|
| DrugBank Description: | Tenofovir is an acyclic nucleotide diester analog of adenosine monophosphate.[A37693] In the most strict sense and due to the fact that it presents a phosphate group bound to the nitrogenous base, it is determined as an actual nucleotide analog.[A37693] The antiviral activities of tenofovir were first reported in 1993 and this agent was commercially available since 2008 in the form of [tenofovir disoproxil] and [tenofovir alafenamide] in order to obtain oral bioavailability.[A18473, A178360] |
| CAS Number: | 147127-20-6 |
| Molecular Weight: | 287.2123 |
| DrugBank Indication: | Tenofovir has been shown to be effective against HIV, herpes simplex virus-2, and hepatitis B virus.[A178330] To know more about the specific product indications, please visit the information in the orally available forms of tenofovir, [tenofovir alafenamide] and [tenofovir disoproxil]. |
| DrugBank Pharmacology: | Tenofovir has been shown to be highly effective in patients that have never had an antiretroviral therapy and it seemed to have lower toxicity than other antivirals such as [stavudine]. In phase 3 clinical trials, tenofovir presented a similar efficacy than [efavirenz] in treatment-naive HIV patients.[A178330] In hepatitis B infected patients, after one year of tenofovir treatment, the viral DNA levels were undetectable.[A178360] |
| DrugBank MoA: | Once tenofovir is activated by a bi-phosphorylation it acts as an antiviral acyclic nucleoside phosphonate. It is a potent inhibitor of the viral reverse transcriptase with an inhibitory constant of approximately 0.022 micromolar.[A18473] Once activated, tenofovir acts with different mechanisms including the inhibition of viral polymerase causing chain termination and the inhibition of viral synthesis.[L6241] All these activities are attained by its competition with deoxyadenosine 5'-triphosphate in the generation of new viral DNA. Once tenofovir is incorporated in the chain, it induces a chain termination which in order inhibits viral replication.[A178330] The safety of tenofovir relies on its low affinity towards the cellular DNA polymerase including the mitochondrial DNA polymerase gamma.[T324] |
| Targets: | Reverse transcriptase/RNaseH; Reverse transcriptase; DNA polymerase |
| Inclusion Criteria: |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class |
|---|