Spegra (tenofovir alafenamide + emtricitabine + dolutegravir), 90 tablets: profile, composition and research

Reference page for Spegra (tenofovir alafenamide + emtricitabine + dolutegravir), 90 tablets. Active substance: Тенофовира алафенамид + Эмтрицитабин + Долутегравир / Tenofovir alafenamide + Emtricitabine + Dolutegravir.

Key facts

What Spegra is

Spegra is a combined antiretroviral medicine that brings three active substances together in a single tablet: dolutegravir, emtricitabine and tenofovir alafenamide. A combination of this kind is called a fixed-dose regimen.

A pack holds 90 tablets. That is a supply for a long period, because the treatment of HIV infection is continuous and does not allow breaks without a physician's instruction.

Each of the three substances acts at a different point in the virus life cycle, which is why they are used together within one treatment regimen.

How the combination works

Dolutegravir - an integrase inhibitor

Integrase is the enzyme that inserts viral DNA into the genome of the host cell. Dolutegravir blocks strand transfer and prevents the provirus from becoming part of human DNA.

Emtricitabine - a nucleoside analogue

Emtricitabine is a cytidine analogue that is incorporated into the growing DNA chain and stops its synthesis. It is active against both HIV-1 and the hepatitis B virus.

Tenofovir alafenamide - a prodrug

This is an improved prodrug of tenofovir. Inside the cell it is converted into its active form and blocks reverse transcriptase, while in the blood it remains more stable.

Approved uses

Combinations built on dolutegravir and tenofovir alafenamide are used in HIV-1 infection in adults as part of antiretroviral therapy. Tenofovir alafenamide and emtricitabine are also active against the hepatitis B virus.

The regimen is chosen by an infectious-disease physician on the basis of tests, including viral load and the CD4 cell count. Regular laboratory monitoring remains essential throughout treatment.

Dosing, the replacement of components and the intervals between check-ups are decided by a specialist. The regimen must not be changed on one's own.

What the research shows

Dolutegravir has been studied as a second-generation integrase inhibitor. Reviews describe it as an agent with a high barrier to the emergence of viral resistance that can be used without pharmacokinetic boosting.

Tenofovir alafenamide has been compared with tenofovir disoproxil in several randomised studies and in a meta-analysis. With comparable antiviral activity, differences in renal and bone parameters were noted.

Large studies of this exact three-component combination are fewer than studies of its individual ingredients. Much of the evidence therefore comes from work on related regimens.

Published research

Primary sources, verified against PubMed:

• Dolutegravir, a second-generation integrase inhibitor for the treatment of HIV-1 infection., PubMed 24259658 (Ann Pharmacother, 2014).
• Dolutegravir, the Second-Generation of Integrase Strand Transfer Inhibitors (INSTIs) for the Treatment of HIV., PubMed 25134686 (Infect Dis Ther, 2014).
• Tenofovir alafenamide versus tenofovir disoproxil fumarate, coformulated with elvitegravir, cobicistat, and emtricitabine, for initial treatment of HIV-1 infection: two randomised, double-blind, phase 3, non-inferiority trials., PubMed 25890673 (Lancet, 2015).
• Efficacy and safety of the regimens containing tenofovir alafenamide versus tenofovir disoproxil fumarate in fixed-dose single-tablet regimens for initial treatment of HIV-1 infection: A meta-analysis of randomized controlled trials., PubMed 31988012 (Int J Infect Dis, 2020).

Listed for reference. Publication of a study is not a claim about this particular product.

Precautions

• This is a prescription medicine. Prescribing and monitoring belong to the physician managing the HIV infection.
• Kidney and liver function and blood parameters are checked before and during treatment.
• If the hepatitis B virus is present, abrupt withdrawal of emtricitabine and tenofovir can lead to a flare. The components are not stopped without a physician's instruction.
• Interactions with other medicines are possible, including antituberculosis agents, antiepileptic drugs and antacids. Every medicine taken should be reported to a doctor.
• In pregnancy and breastfeeding the decision belongs to a specialist.
• Adherence matters: missed doses encourage the emergence of viral resistance.

Frequently asked