Newly Approved HIV Medications

Ian Villaluz, PharmD Candidate 2021; Glenn R. Grantner, PharmD, BCPS

US Pharmacist. 2020;45(10):17-25.

Abstract and Introduction

Abstract

The available antiretroviral (ARV) drugs for the treatment of HIV have expanded since 2018. Novel types of ARVs with new mechanisms of action have been approved, including ibalizumab-uiyk and fostemsavir. There have also been approvals of combination tablets of previously available drugs, such as bictegravir/emtricitabine/tenofovir alafenamide and dolutegravir/lamivudine. Finally, there has been an expansion in approved indications for previously available ARVs themselves, such as emtricitabine/tenofovir alafenamide for use in pre-exposure prophylaxis.

Introduction

The mainstays of antiretroviral (ARV) agents for treatment of HIV have largely consisted of the same handful of drug classes for years. HIV treatment was first attempted with nucleoside reverse transcriptase inhibitors (NRTIs), the first FDA-approved class of ARVs. Gradually, more and more classes were discovered and made available for treatment in various, often complex, regimens (Table 1).^[1–3] After the approval of raltegravir in 2007, new HIV drug approvals were largely for repurposed available drugs and new combination drugs. This changed in 2018 with the approval of ibalizumab-uiyk, the first novel ARV in over a decade.^[4] Ibalizumab-uiyk was quickly followed by a new nonnucleoside reverse transcriptase inhibitor (NNRTI), doravirine, later that year and a novel attachment inhibitor, fostemsavir, in 2020 (Table 2).^[5–7]

While novel drugs are often the most exciting new drug approvals, ARVs have improved in other ways. Given the enormous pill burden of many HIV regimens, newly approved combination ARVs (Table 3) can make life much easier for patients. Use of such agents and limiting the necessary pill burden have demonstrated improved adherence and overall outcomes.^[8,9] There have also been expansions in approved indications for previously available ARVs (Table 4), offering new options for certain patient populations and indications.^[10–14]

Although their are many new approvals since 2018, this aricle profiles four of the newly approved medications and one new indication. These approvals were selected to demonstrate a sample of the wide variety of new agents becoming available, as well as emphasize some new options that offer a unique opportunity in the treatment of HIV.

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Table 1. FDA-Approved ARV Classes Before 2018
Drug Class	Mechanism of Action	First Approved Drug	Approval Date
Nucleoside reverse transcriptase inhibitors	Inhibit reverse transcriptase via chain termination	Zidovudine	March 19, 1987
Nonnucleoside reverse transcriptase inhibitors	Inhibit reverse transcriptase via direct binding and inactivation	Nevirapine	June 21, 1996
Protease inhibitors	Inhibit HIV protease, an enzyme necessary for catalytic cleavage of proteins needed for viral replication	Saquinavir	December 6, 1995
Fusion inhibitors	Block entrance of HIV into CD4 cells	Enfuvirtide	March 13, 2003
CCR5 antagonists	Block CCR5 receptors on CD4 cell surfaces, preventing HIV entrance	Maraviroc	August 6, 2007
Integrase inhibitors	Inhibit integrase, an enzyme necessary for integration of viral DNA into host cells	Raltegravir	October 12, 2007

ARV: antiretroviral; CCR5: C-C chemokine receptor type 5; HIV: human immunodeficiency virus.
Source: References 2, 3.

Table 2. ARV Agents Approved Since 2018
Generic Name	Brand Name	Drug Class	Indication	Dosing	Route of Administration	Approval Date
Ibalizumab-uiyk	Trogarzo	Post-attachment inhibitor	In combination with other ARV for the treatment of HIV-1 in HTE adults	2 g IV loading dose, 800 mg IV every 2 weeks	IV	March 6, 2018
Doravirine^a	Pifeltro	NNRTI	In combination with other ARV for the treatment of HIV-1 in adults	100 mg by mouth once daily	Oral	August 30, 2018
Fostemsavir	Rukobia	gp120 attachment inhibitor	In combination with other ARV for the treatment of HTE adults with MDR HIV-1	600 mg by mouth twice daily	Oral	July 2, 2020

^aAlso newly approved in combination with emtricitabine and tenofovir disoproxil fumarate.
ARV: antiretroviral; HIV: human immunodeficiency virus; HTE: heavily treatment-experienced; MDR: multidrug resistant; NNRTI: nonnucleoside reverse transcriptase inhibitor.
Source: Reference 7.

Table 3. New Combination Approvals
Generic Name	Brand Name	Mechanism(s) of Action	Indication	Dosing	Route of Administration	Approval Date
Bictegravir, emtricitabine, and tenofovir alafenamide	Biktarvy	INSTI/NRTI/NRTI	Treatment of HIV-1 infection as a complete regimen	1 tablet by mouth daily	Oral	February 2018
Lamivudine and tenofovir disoproxil fumarate	Cimduo	NRTI/NRTI	In combination with other ARV for the treatment of HIV-1 in adults and pediatric patients weighing ≥35 kg	1 tablet by mouth daily	Oral	February 2018
Efavirenz, lamivudine, and tenofovir disoproxil fumarate	Symfi Lo	NNRTI/NRTI/NRTI	Treatment of HIV-1 infection in adult patients weighing ≥35 kg	1 tablet by mouth daily	Oral	February 2018
Efavirenz, lamivudine, and tenofovir disoproxil fumarate	Symfi	NNRTI/NRTI/NRTI	Treatment of HIV-1 infection in adult patients weighing ≥40 kg	1 tablet by mouth daily	Oral	March 2018
Darunavir, cobicistat, emtricitabine, and tenofovir alafenamide	Symtuza	NNRTI/BOOSTER/NRTI/NRTI	Treatment of HIV-1 infection in adults and pediatric patients ≥40 kg	1 tablet by mouth daily	Oral	July 2018
Doravirine, lamivudine, and tenofovir disoproxil fumarate	Delstrigo	NNRTI/NRTI/NRTI	Treatment of HIV-1 infection in adults	1 tablet by mouth daily	Oral	August 2018
Dolutegravir and lamivudine	Dovato	INSTI/NRTI	Treatment of HIV-1 infection in adults	1 tablet by mouth daily	Oral	April 2018

HIV: human immunodeficiency virus; INSTI: integrase strand transfer inhibitor; NNRTI: nonnucleoside reverse transcriptase inhibitor; NRTI: nucleoside reverse transcriptase inhibitor.
Source: Reference 7.

Table 4. New-Indication Approvals
Generic Name	Brand Name	Mechanism(s) of Action	New Indication	Approval Date
Darunavir	Prezista	Protease inhibitor	Pregnant women with HIV	July 2018
Emtricitabine/tenofovir disoproxil fumarate	Truvada	NRTI/NRTI	PrEP in adolescents weighing at least 35 kg	May 2018
Doravirine/lamivudine/tenofovir disoproxil fumarate	Delstrigo	NNRTI/NRTI/NRTI	A complete regimen to replace the current ARV regimen in adult patients who are virologically suppressed (viral load <50 copies/mL)	September 2019
Doravirine	Pifeltro	NNRTI	In combination with other ARV, to replace the current ARV regimen in adult patients who are virologically suppressed (viral load <50 copies/mL)	September 2019
Emtricitabine/tenofovir alafenamide	Descovy	NRTI/NRTI	HIV PrEP	October 2019
Dolutegravir	Tivicay, Tivicay PD	INSTI	Pediatric patients (treatment-naive or INSTI-naive) aged at least 4 weeks and weighing at least 3 kg	June 2020

ARV: antiretroviral; INSTI: integrase strand transfer inhibitor; HIV: human immunodeficiency virus; NNRTI: nonnucleoside reverse transcriptase inhibitor; NRTI: nucleoside reverse transcriptase inhibitor; PrEP: pre-exposure prophylaxis.
Source: References 6, 10–14.

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Newly Approved HIV Medications

Abstract and Introduction

Abstract

Introduction

Tables

Tables

Tables

Tables

References

Authors and Disclosures

Authors and Disclosures

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