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Emtricitabine and tenofovir alafenamide tablets (Descovy) instruction manual
Common name: Emtricitabine and tenofovir alafenamide tablets
Trade name: Descovy
Full name: Emtricitabine and tenofovir alafenamide tablets, Descovy, Emtricitabine and TenofovirAlafenamide Fumarate Tablets
Indications:
Suitable for use in combination with other antiretroviral drugs to treat human immunodeficiency virus type 1 (HIV-1) infection in adults and adolescents (age 12 years and above and weighing at least 35kg)
Usage and dosage:
One tablet once a day.
Adverse reactions:
Diarrhea, nausea and headache
Contraindications:
Contraindicated for those with hypersensitivity to the active substance or any excipient.
Cautions:
Although the effective virogenic effect of antiretroviral therapy has been shown to significantly reduce the risk of sexual transmission, residual risks cannot be ruled out. Precautions should be taken to prevent spread in accordance with national guidance.
Patients co-infected with HIV and hepatitis B or C virus: Patients with chronic hepatitis B or hepatitis C who receive antiretroviral therapy are at increased risk for severe and potentially fatal hepatic adverse reactions. The safety and efficacy of emtricitabine and tenofovir alafenamide have not been established in patients co-infected with HIV-1 and hepatitis C virus (HCV). Tenofovir alafenamide is active against hepatitis B virus (HBV). In patients co-infected with HIV and HBV, discontinuation of emtricitabine and tenofovir alafenamide therapy may result in severe exacerbations of hepatitis. HIV- and HBV-coinfected patients who discontinue treatment with emtricitabine and tenofovir alafenamide should be closely monitored with clinical and laboratory follow-up for at least several months after discontinuation of treatment.
Liver Disease: The safety and efficacy of emtricitabine and tenofovir alafenamide have not been established in patients with significant underlying liver disease. Patients with pre-existing hepatic impairment, including chronic active hepatitis, have an increased frequency of liver function abnormalities during combination antiretroviral therapy (CART) and should be monitored according to standard practice.
Immune reconstitution inflammatory syndrome: In HIV-infected patients with severe immunodeficiency at the start of CART, an inflammatory response caused by asymptomatic or residual opportunistic pathogenic infection may occur, which may lead to severe clinical symptoms or aggravation of original symptoms. Typically, such reactions are observed within the first weeks or months after starting CART. Examples include cytomegalovirus retinitis, systemic and/or focal mycobacterial infections, and Pneumocystis jiroveci pneumonia. Any inflammatory symptoms should be evaluated and treatment initiated if necessary. Additionally, the development of autoimmune diseases (e.g., Graves' disease) during immune reconstitution has been reported; however, the reported timing of onset is more variable and these events may occur months after initiation of treatment. HIV-1-infected patients carrying mutated genes: Emtricitabine and tenofovir alafenamide should be avoided in HIV-1-infected patients carrying the K65R mutated gene if they have received antiretroviral therapy in the past.
Storage:
Store below 30℃. Avoid light and keep out of reach of children.
Mechanism of action:
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) and a nucleoside analog of 2’-deoxycytidine. Emtricitabine is phosphorylated by cellular enzymes to form emtricitabine triphosphate. Emtricitabine triphosphate uses HIV reverse transcriptase (RT) to integrate into viral DNA (leading to DNA chain termination), thereby inhibiting HIV replication. Emtricitabine is active against HIV-1, HIV-2 and HBV. Tenofovir alafenamide is a nucleotide reverse transcriptase inhibitor (NtRTI) and the phosphoramidite prodrug (2’-deoxyadenosine monophosphate analog) of tenofovir. Tenofovir alafenamide penetrates cells and is more effective than tenofovir disoproxil fumarate in increasing tenofovir concentrations in peripheral blood mononuclear cells (PBMC) or HIV target cells (including lymphocytes and macrophages) due to hydrolysis by cathepsin A, thereby increasing plasma stability and intracellular activation.
Safety and Efficacy:
The approval of emtricitabine and tenofovir alafenamide tablets (Dacova®) was based on 144-week data from two pivotal Phase 3 studies (Study 104 and 111). These two studies were conducted in HIV-1 treatment-naive adult patients and showed that compared with the F/TDF-based treatment regimen (Stribild®; elvitegravir 150 mg/cobicistat 150 mg/emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg, Compared with E/C/F/TDF), the F/TAF-based treatment regimen (Jeflucan®; elvitegravir 150 mg/cobicistat 150 mg/emtricitabine 200 mg/tenofovir alafenamide 10 mg, E/C/F/TAF) achieved the primary endpoint of non-inferiority.
At the same time, another phase 3 study (Study 109) also provided support for the approval of emtricitabine and tenofovir alafenamide tablets (Dacova®). This study evaluated the efficacy of virally suppressed adult patients after switching from an F/TDF-based regimen to an F/TAF-based regimen (Jeflucan®).