Hawra Al Lawati M.D.

11/2021 HIV ART Quick Guide @HawraAllawati

1st Line= 3 drug regimen = NRTI + NRTI + INSTI

Common First Line Regimens in the U.S. :
TAF + FTC + BIC [Co-formulated in a single pill regimen: Biktarvy]
TAF + FTC + DTG [Co-formulated in a 2 pill regimen: Descovy (TAF+FTC) & Tivicay (DTG)]
TDF + FTC + DTG [Co-formulated in a 2 pill regimen:Truvada (TDF+FTC) & Tivicay (DTG)]

NRTI INSTI
(Nucleoside Reverse Transcriptase Inhibitor) (Integrase Strand Transfer Inhibitors)

Overall well tolerated drugs High barrier to resistance

Interact with rifampin
Decrease in drug levels when taken with mul:valent ca:ons
Emtricitabine (FTC) Ca2+, Mg2+, Fe (tell pa:ents to avoid antacids!)
Lamivudine (3TC)
Very similar in structure and are considered interchangeable- they Bictegravir (BIC)
are not used together. Choose ONE of them to combine with a BIKTARVY (with TAF/FTC)
separate NRTI. Typically [Emtricitabine with Tenofovir] & Available in single tablet regimen Kg
[Lamivudine with Abacavir]. Emerging data on weight gain
Emtricitabine in rare circumstances can cause Not much data/ experience of its use in pregnancy
hyperpigmenta:on

Dolutegravir (DTG)
TRIUMEQ (with ABC/3TC)
JULUCA (with RPV)
DOVATO (with 3TC)
Kg
Higher barrier to resistance than EVG or RAL
If using rifamycins, preferred over BIC
Tenofovir (TAF)/(TDF) Emerging data on weight gain
Typically combined with FTC. TDF is a prodrug of TAF. Overall TAF Interacts with meOormin- can’t exceed 1g meOormin per day
used more frequently as it is less likely to cause renal & bone No co-formula:ons with TAF/TDF
toxicity compared to TDF. NOTE: Use at concep:on & in very early pregnancy has been associated with a
slightly higher prevalence of neural tube defects. However, the overall prevalence
was low & when compared to other ARTs, it was not meaningfully different (Zash et
Circumstances where TDF preferred: when also using rifampin (TAF al., 2019). Dolutegravir based regimens are s:ll considered first line in pregnancy.
interacts with rifamycins) & PreP as TDF is the only formulaOon
that’s FDA approved for PrEP Elvitegravir (EVG) + c
Ac:ve against HBV GENVOYA (with TAF/FTC)
Renal toxicity (Avoid TDF if GFR <50, TAF if GFR <30) STRIBLID (with TDF/FTC)
Decreased bone density Available in single tablet regimen with TAF/FTC
Possible weight gain with TAF Kg Low barrier to resistance (compared to BIC or DTG)
Needs boos:ng with Cobicistat (c) which increases drug
interac:ons (e.g. Cobicistat increases systemic flu:casone levels
when flu:casone used as nasal spray)

Abacavir (ABC) Raltegravir (RAL)

Typically combined with 3TC
More data on its safety in pregnancy
Not nephrotoxic
Low barrier to resistance (compared to BIC or DTG)
Contraindicated in pa:ents with HLA-B*5701 allele due to Virologic failure may lead to two-class resistance (INSTI plus NRTI)
hypersensi:vity reac:on (must have nega:ve result before No coformula:ons. Need to use BID dosing in pregnancy
star:ng)
Some reports of rhabdomyolysis
May increase risk of CVD events. Avoid in pa:ents with
CAD
Cabotegravir (CAB)
Comes as a long ac:ng injectable with rilpivirine
 Hawra Al Lawati M.D.
11/2021 HIV ART Quick Guide @HawraAllawati

PI NNRTI
(Protease Inhibitors) (NON- Nucleoside Reverse Transcriptase Inhibitors)

High barrier to resistance Low barrier to resistance (especially 1st genera:on: EFV,
Side effects: metabolic syndrome (DM, HLD, NVP)
lipodystrophy) Not ac:ve against HIV-2
Interact with many medica:ons. Avoid coadministra:on
of rifampin. Can co-administer with rifabu:n Efavirenz (EFV)
ATRIPLA (with TDF/FTC)
Single pill coformula:on with TDF/FTC
Neuropsychiatric side effects (vivid dreams + may increase suicide
risk + “hungover feeling”)
Darunavir (DRV) Increase LFTs with risk of fulminant hepa::s (Child Pugh B and C)
SYMTUZA (with TAF/FTC/cobcistat) CYP450 inducer – > decreases methadone levels (may precipitate
Best tolerated PI opiod withdrawal when ini:ated)
Needs boos:ng with Ritonavir(r) or Cobicistat (c) Prolongs QT
Avoid in severe liver disease
Can increase risk of CVD
Rilpivirine (RPV)
ODEFSEY (with TAF/FTC)
COMPLERA (with TDF/FTC)
JULUCA (with DTG)
Less metabolic syndrome effects
Needs food (400 calorie meal) for op:mal absorp:on.
Needs gastric acid for op:mal absorp:on. Cau:on with H2
Atazanavir (ATV) blockers, avoid PPIs.
less metabolic syndrome effects Not as good at a higher viral load. Use in PLWH with CD4 T-cell
Needs boos:ng with Ritonavir(r) or Cobicistat (c) counts >200 cells/μL and HIV RNA <100,000 copies/mL
Needs gastric acid and food for op:mal absorp:on. Can’t use Neuropsychiatric side effects (vivid dreams + may increase suicide
PPI >20 mg omeprazole with it risk)
Increased risk of kidney stones and AKI Prolongs QT
Can cause indirect hyperbilirubinemia
Avoid in severe liver disease
Avoid in higher viral
load

Doravirine (DOR)
DELSTRIGO (with TDF/FTC)
BEST IN CLASS
Ritonavir (r) Unique resistance pathway from other NNRTIs
used as a booster

Etravirine (ETR)
One of the common meds used in the sewng of drug resistance
Rash (can be mild, but SJS also reported)
Drug interac:ons

Emerging Data on Two Drug regimens, now approved for first line therapy: Non-inferior to 3 drug regimen but in
very specific circumstances. Dolutegravir ad lamivudine (DTG/3TC) are coformulated as Dovato. Can use this
only if the HIV load is <500,000 copies/mL, there is no chronic HBV infec:on, and there is no transmimed
resistance to NRTIs or INSTIs.
(Cahn, Pedro et al. 2019, GEMINI-1 & GEMINI-2 Trials)
 Hawra Al Lawati M.D.
11/2021 HIV ART Quick Guide @HawraAllawati
Factors to consider when deciding on a regimen:
• Resistance pamern
• HLA-B*5701 allele status (for Abacavir)
• Concomitant HBV infec:on (if HbSag +, include TAF/TDF in regimen)
• Concomitant treatment for TB/LTBI (check drug-drug interac:ons especially when using
rifampin)
• Cardiovascular risk factors
• Comorbid condi:ons (e.g. kidney disease, liver disease, osteoporosis, psychiatric illness, concern for
weight gain, cancer/autoimmune disease)
• Interac:on with other medica:ons (see table in DHHS guideline or Liverpool rug interac:on
website included below)
• Pill burden (single tablet regimen vs. other regimens vs. long ac:ng injectable)
• Woman of child bearing age/ pregnancy

Helpful links
• Tool to assist on deciding on a regimen: hmps://www.hivassist.com/tool
• Drug-Drug interacYons: hmps://www.hiv-druginterac:ons.org/checker
• Brochure with coformulaYons, brand names and pill pictures: hmps://aidsetc.org/sites/
default/files/resources_files/HIV%20Med%20Chart_June%202019.pdf
• DHHS 2021 guidelines on management of HIV : hmps://clinicalinfo.hiv.gov/en/guidelines/adult-
and-adolescent-arv/whats-new-guidelines?view=brief
• JAMA IAS USA guidelines hmps://jamanetwork.com/journals/jama/ar:cle-abstract/2771873
• Stanford tool to look up genotype muta:ons and resistance: hmps://hivdb.stanford.edu/hivdb/
by-muta:ons/

References & Acknowledgements

Created by Dr. Hawra Al Lawa:. Reviewed by Dr. Rajesh
Gandhi and Dr. Robert Goldstein (MGH ID)

• Paul Sax M.D. Selec:ng an:retroviral regimens for the

treatment-naïve HIV-infected pa:ent. Post TW, ed.
UpToDate. Waltham, MA: UpToDate Inc. hmps://
www.uptodate.com (Accessed on Aug, 2021)

• Courtney Fletcher, PharmD. Overview of an:retroviral

agents used to treat HIV. Post TW, ed. UpToDate.
Waltham, MA: UpToDate Inc. hmps://
www.uptodate.com (Accessed on Aug 2021)

• John E. Bennem, Raphael Dolin, Mar:n J. Blaser.

Mandell, Douglas, and Bennem's Principles and Prac:ce
of Infec:ous Diseases. Philadelphia, PA :Elsevier/
Saunders, 2015.

• Spec, Andrej, et al. Comprehensive Review of Infec:ous

Diseases. Elsevier, 2020

Figure 1Gandhi M, Gandhi RT. Single-pill combinaOon regimens for treatment of

HIV-1 infecOon. N Engl J Med. 2014;371:248-59.