Overview of antiretroviral and other drugs for HIV infection in adults

The classes of antiretroviral drugs used for treatment or prevention of HIV infection are included in Antiretroviral and other drugs for HIV infection in adults.

Figure 1. Antiretroviral and other drugs for HIV infection in adults

Commonly used drug classes:

nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) – abacavir, emtricitabine, lamivudine, tenofovir alafenamide, tenofovir disoproxil fumarate, tenofovir disoproxil maleate, tenofovir disoproxil phosphate, tenofovir disoproxil succinate and zidovudine
integrase strand transfer inhibitors (INSTIs) – bictegravir, cabotegravir, dolutegravir, elvitegravir and raltegravir.

Less commonly used drug classes:

non-nucleoside reverse transcriptase inhibitors (NNRTIs) – doravirine, efavirenz, etravirine, nevirapine and rilpivirine
protease inhibitors (PIs) – atazanavir, darunavir, fosamprenavir, lopinavir, ritonavir and saquinavir

Additional drug classes with a role in cases with treatment failure:

fusion inhibitors – enfuvirtide
entry inhibitors – maraviroc
attachment inhibitors – fostemsavir
capsid inhibitors – lenacapavir
post-attachment CD4 monoclonal antibody – ibalizumab.

Boosting drugs:

cytochrome P450 inhibitors – cobicistat and ritonavir [NB1].

Note:

NB1: Cytochrome P450 inhibitors are used to increase the plasma concentrations of PIs, and the INSTI elvitegravir.

The antiretrovirals used for initial therapy are described in Initial antiretroviral therapy for HIV infection in adults. Other antiretrovirals are reserved for use in resistant HIV infection or when patients are unable to tolerate standard therapy.

At least 2 antiretroviral drugs are needed for initial therapy; however, most regimens include 3 active agents. Single-tablet once-daily combination products containing the complete antiretroviral regimen improve adherence; products currently available in Australia are listed in Single-tablet once-daily combination products containing 3 antiretroviral drugs. Products that do not contain the complete regimen (listed in Commonly used combination products containing 1 or 2 antiretroviral drugs) need to be taken in combination for initial therapy and are not as convenient for the patient.

Once viral suppression is achieved, carefully selected patients who started a 3-drug regimen can change to a 2-drug maintenance regimen – seek expert adviceLlibre, 2018. Some products listed in Commonly used combination products containing 1 or 2 antiretroviral drugs can be used for this 2-drug maintenance regimen.

The antiretroviral regimens listed in Antiretroviral and other drugs not routinely used for treatment of HIV infection in adults in Australia are not routinely used for treatment of HIV infection due to pill burden, adverse effects or drug resistance. Seek expert advice for management of patients on these regimens.

Practice points for initial antiretroviral therapy are listed in Practice points for initial antiretroviral therapy. For information about changing antiretroviral therapy, see Changing antiretroviral therapy for HIV infection.

Table 1. Single-tablet once-daily combination products containing 3 antiretroviral drugs
[NB1]
Brand name examples	Antiretroviral drugs
NRTI plus INSTI products
Biktarvy	tenofovir alafenamide+emtricitabine+bictegravir
Genvoya	tenofovir alafenamide+emtricitabine+elvitegravir+cobicistat [NB2]
Stribild	tenofovir disoproxil fumarate+emtricitabine+elvitegravir+cobicistat [NB2]
Triumeq	dolutegravir+abacavir+lamivudine
NRTI plus NNRTI products
Tenofovir Disoproxil/Emtricitabine/Efavirenz Mylan 300/200/600 Tenofovir Disoproxil/Emtricitabine/Efavirenz Viatris 300/200/600	tenofovir disoproxil fumarate+emtricitabine+efavirenz
Eviplera	tenofovir disoproxil fumarate+emtricitabine+rilpivirine
Odefsey	emtricitabine+rilpivirine+tenofovir alafenamide
NRTI plus PI products
Symtuza	tenofovir alafenamide+emtricitabine+cobicistat+darunavir [NB2]
Note: INSTI = integrase strand transfer inhibitor; NNRTI = non-nucleoside reverse transcriptase inhibitor; NRTI = nucleoside/nucleotide reverse transcriptase inhibitor; PI = protease inhibitor NB1: This table includes products available in Australia at the time of writing. Other brands may be available. NB2: Cobicistat is not an antiretroviral drug; it is a cytochrome P450 3A4 inhibitor used to increase the plasma concentration of elvitegravir and darunavir.

Table 2. Commonly used combination products containing 1 or 2 antiretroviral drugs
[NB1]
Brand name examples	Antiretroviral drugs
NRTI plus INSTI products
Dovato [NB3]	lamivudine+dolutegravir
Dual-NRTI products
Descovy	emtricitabine+tenofovir alafenamide
Kivexa	abacavir+lamivudine
Tenofovir/Emtricitabine 300/200 APOTEX	tenofovir disoproxil fumarate+emtricitabine [NB2]
Tenofovir Disoproxil Emtricitabine Mylan 300/200	tenofovir disoproxil maleate+emtricitabine [NB2]
Tenofovir EMT GH	tenofovir disoproxil phosphate+emtricitabine [NB2]
Tenofovir/Emtricitabine Sandoz 301/200	tenofovir disoproxil succinate+emtricitabine [NB2]
INSTI plus NNRTI products
Cabenuva [NB3]	cabotegravir+rilpivirine
Juluca [NB4]	dolutegravir+rilpivirine
PI plus cobicistat products [NB5]
Evotaz	atazanavir+cobicistat
Prezcobix	darunavir+cobicistat
Note: INSTI = integrase strand transfer inhibitor; NNRTI = non-nucleoside reverse transcriptase inhibitor; NRTI = nucleoside/nucleotide reverse transcriptase inhibitor; PI = protease inhibitor NB1: This table includes products available in Australia that contain 1 or 2 antiretroviral drugs. Other combination products and brands may be available. These products are usually taken in combination with other antiretrovirals to ensure that 3-drugs are used for initial therapy. NB2: Cabenuva and Dovato may be used as a complete antiretroviral regimen in carefully selected patients. For more information, see Initial antiretroviral therapy for HIV infection in adults. NB3: Tenofovir disoproxil salts (tenofovir disoproxil fumarate, tenofovir disoproxil maleate, tenofovir disoproxil phosphate and tenofovir disoproxil succinate) are bioequivalent. NB4: Juluca can be used as a 2-drug maintenance regimen (ie the complete regimen) in select patients with a suppressed viral load. NB5: Cobicistat is not an antiretroviral drug; it is a cytochrome P450 3A4 inhibitor used to increase the plasma concentration of atazanavir and darunavir.

Table 3. Antiretroviral and other drugs not routinely used for treatment of HIV infection in adults in Australia
Antiretroviral drugs	Combination products (brand name examples)
NRTIs
didanosine stavudine zidovudine	abacavir+lamivudine+zidovudine (Trizivir) lamivudine+zidovudine (Combivir)
PIs
fosamprenavir indinavir lopinavir saquinavir tipranavir	lopinavir+ritonavir (Kaletra)
Entry inhibitors
maraviroc	–
Fusion inhibitors
enfuvirtide	–
Attachment inhibitors
fostemsavir	–
Long-acting capsid inhibitor
lenacapavir	–
Post-attachment CD4 monoclonal antibody
ibalizumab	–
Note: NRTIs = nucleoside/nucleotide reverse transcriptase inhibitors; PIs = protease inhibitors