Complete Antiretroviral Regimen: This single tablet contains a fixed-dose combination of three active ingredients: Tenofovir Disoproxil Fumarate (TDF) (A) 300 mg, Lamivudine (B) 300 mg, and Dolutegravir (C) 50 mg.
Three-Drug Class Combination: It combines two nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs/NtRTIs) with a potent integrase inhibitor, providing a complete and robust antiretroviral regimen in a single pill.
Once-Daily Dosing: The formulation is designed for once-daily administration, which is a major advantage for patients and significantly simplifies HIV treatment.
Broad Spectrum: This combination is highly effective against both the Human Immunodeficiency Virus (HIV) and the Hepatitis B virus (HBV), making it suitable for co-infected patients.
Advantages
High Efficacy and Potency: The combination of three different drug classes in a single tablet provides a potent and highly effective means of suppressing HIV viral replication, leading to rapid and sustained reductions in viral load.
Improved Adherence: The single-pill, once-daily regimen significantly reduces the pill burden and complexity of treatment, which is a major factor in improving patient adherence and long-term treatment success.
Favorable Resistance Profile: Dolutegravir has a high barrier to resistance, and when combined with two NRTIs, the risk of developing viral resistance is very low, even with some missed doses.
Dual Indication: The presence of TDF and lamivudine allows for the treatment of both HIV and chronic HBV, which is a significant advantage for patients who are co-infected.
Uses
HIV-1 Infection: This combination is a recommended first-line treatment for HIV-1 infection in adults and adolescents, providing a complete and effective regimen without the need for additional pills.
Treatment-Naïve Patients: It is widely used in patients who are new to antiretroviral therapy due to its high efficacy, good tolerability, and simplified dosing.
Chronic Hepatitis B (HBV) Infection: The TDF and lamivudine components provide effective treatment for chronic HBV, making this a suitable choice for patients coinfected with both HIV and HBV.
Pregnant Patients: Dolutegravir is a preferred agent for HIV treatment in pregnancy, and this combination can be used as part of a regimen for pregnant individuals with HIV.
Nature
Drug Classes: The tablet contains drugs from two different classes: NRTIs (lamivudine) and NtRTIs (TDF), and an integrase inhibitor (dolutegravir).
Mechanism of Action:Dolutegravir works by inhibiting integrase, a viral enzyme essential for integrating HIV’s DNA into the host cell’s DNA. TDF and lamivudine work by inhibiting reverse transcriptase, which is responsible for converting HIV’s RNA into DNA.
Dual-Target Inhibition: By targeting two distinct steps in the HIV replication cycle (reverse transcription and integration), the combination provides a powerful and broad-spectrum attack on the virus.
Renal Excretion: All three drugs are primarily eliminated by the kidneys. Therefore, dose adjustments or a change in therapy may be necessary for patients with significant renal impairment.
Storage
Temperature: Store the tablets at controlled room temperature, typically between 20∘C to 25∘C (68∘F to 77∘F).
Protection: Keep the tablets in their original, tightly closed container, protected from light and moisture.
With or Without Food: The medication can be taken with or without food.
Patient Warning (HBV): Patients with HBV should be educated that abruptly stopping the medication can lead to a severe flare-up of their hepatitis, so they should not discontinue it without consulting their doctor.
