Repositioning Candidate Details
| Candidate ID: | R0254 |
| Source ID: | DB00879 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Emtricitabine |
| Synonyms: | |
| Molecular Formula: | C8H10FN3O3S |
| SMILES: | NC1=NC(=O)N(C=C1F)[C@@H]1CS[C@H](CO)O1 |
| Structure: |
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| DrugBank Description: | Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) indicated for the treatment of HIV infection in adults[L9019] or combined with [tenofovir alafenamide] for the prevention of HIV-1 infection in high risk adolescents and adults.[L9010] Emtricitabine is a cytidine analogue.[L9019] The drug works by inhibiting HIV reverse transcriptase, preventing transcription of HIV RNA to DNA.[L9019] Emtricitabine was granted FDA approval on 2 July 2003.[L9019] |
| CAS Number: | 143491-57-0 |
| Molecular Weight: | 247.247 |
| DrugBank Indication: | Emtricitabine is indicated in combination with other medications for the treatment of HIV-1 infections;[L9019,L9836] treatment of HIV-1 infections in pediatric patients 25-35kg, treatment of HIV-1 infections in adult patients ≥35kg, for pre exposure prophylaxis of HIV-1 in adolescent and adult patients excluding those who have receptive vaginal sex;[L4388,L9010] treatment of HIV-1 infections in pediatric and adult patients ≥17kg, pre exposure prophylaxis in adolescents and adults ≥35kg;[L9833] treatment of HIV-1 in patients ≥12 years and ≥35kg;[L9587] treatment of HIV-1 in patients weighing ≥35kg;[L9839,L9842] treatment of HIV-1 in patients weighing ≥25kg;[L9647,L9845] and treatment of HIV-1 in patients weighing ≥40kg.[L9848] |
| DrugBank Pharmacology: | Emtricitabine is a cytidine analog that competes with the natural substrate of HIV-1 reverse transcriptase to be incorporated into newly formed DNA, terminating its transcription.[L9019] It is administered once daily so it has a long duration of action. Patients should be counselled regarding the risk of lactic acidosis and hepatomegaly with steatosis.[L9019] |
| DrugBank MoA: | Emtricitabine is a cytidine analog which, when phosphorylated to emtricitabine 5'-triphosphate, competes with deoxycytidine 5'-triphosphate for HIV-1 reverse transcriptase.[L9019] As HIV-1 reverse transcriptase incorporates emtricitabine into forming DNA strands, new nucleotides are unable to be incorporated, leading to viral DNA chain termination.[L9019] Inhibition of reverse transcriptase prevents transcription of viral RNA into DNA, therefore the virus is unable to incorporate its DNA into host DNA and replicate using host cell machinery. This reduces viral load.[A187688] |
| Targets: | Reverse transcriptase/RNaseH |
| Inclusion Criteria: |
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