Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents With HIV

Cabenuva 600-mg/900-mg Kit:

• CAB 600-mg/3-mL vial and RPV 900-mg/3-mL vial

Cabenuva 400-mg/600-mg Kit:

• CAB 400-mg/2-mL vial and RPV 600-mg/2-mL vial

Optional Lead-In With Oral CAB and RPV

• CAB 30 mg PO and RPV 25 mg PO once daily with food for 4 weeks

Monthly IM CAB and RPV

• Loading dose: CAB 600 mg/3 mL IM for 1 dose and RPV 900 mg/‌3 mL IM for 1 dose 
• Continuation phase: CAB 400 mg/2 mL IM monthly and RPV 600 mg/2 mL IM monthly

Every 2-Month IM CAB and RPV

• Loading dose: CAB 600 mg/3 mL IM and RPV 900 mg/3 mL IM once monthly for 2 doses 
• Continuation phase: CAB 600 mg/3 mL IM and RPV 900 mg/3 mL IM every 2 months

Tenofovir Disoproxil Fumarate/Emtricitabine
(TDF/FTC)
Truvada

Note: Generic product available.

^a For dose adjustments in people with renal or hepatic insufficiency, see Appendix B. All FDC tablets listed in this table can be taken without regard to food.

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; FDC = fixed-dose combination; FTC = emtricitabine; PO = orally; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate

• One tablet PO once daily

See Appendix A, Table 1 for dosing information.

CYP3A4 substrate

UGT1A1-mediated glucuronidation

Diarrhea

Nausea

Headache

Weight gain

Depression

Copackaged IM Regimen

• Cabenuva (CAB plus RPV)

Also available in oral tablet formulation Vocabria (CAB PO)

• 30-mg tablet
• Must be obtained from manufacturer for oral lead-in and oral bridging during administration of Cabenuva (CAB IM/RPV IM)

PO: 41 hours

IM: 6–12 weeks

CAB Plus RPV

• Headache
• Nausea
• Abnormal dreams
• Anxiety
• Insomnia
• Depressive disorders
• Hepatotoxicity

IM Formulation Only

• Injection site reactions (e.g., pain, induration, swelling, nodules)

Tivicay

• 50-mg tablet

STRs That Contain DTG^c

• Dovato (DTG/3TC)
• Juluca (DTG/RPV)
• Triumeq (DTG/ABC/3TC)

In People Without Prior ARV Treatment or ARV-Experienced People Who Had Never Received INSTIs

• DTG 50 mg PO once daily

In People Without Prior ARV Treatment or ARV-Experienced People Who Had Never Received INSTIs When Coadministered With EFV, FPV/r, TPV/r, or Rifampin

• DTG 50 mg PO twice daily

In INSTI-Experienced People With Certain INSTI Mutations (See Product Label) or With Clinically Suspected INSTI Resistance

• DTG 50 mg PO twice daily

See Appendix A, Table 1 for dosing information for STRs that contain DTG.

UGT1A1-mediated glucuronidation

Minor substrate of CYP3A4

Insomnia

Headache

Depressive disorders and suicidal ideation (rare; usually occurs in people with preexisting psychiatric conditions)

Weight gain

Hepatotoxicity

HSRs, including rash, constitutional symptoms, and organ dysfunction (including liver injury), have been reported.

EVG is only available as a component of STR tablets that also contain COBI, FTC, and either TDF or TAF.

STRs That Contain EVG^c

• Genvoya (EVG/c/TAF/FTC)
• Stribild (EVG/c/TDF/FTC)

Genvoya and Stribild

• One tablet PO once daily with food.
• See Appendix A, Table 1 for dosing information

Genvoya 

• See Appendix B for recommendations on dosing in persons with renal insufficiency.

Stribild

• Not recommended for people with baseline CrCl <70 mL/min (see Appendix B).

EVG

• CYP3A and UGT1A1/3 substrate

COBI

• CYP3A inhibitor and substrate
• CYP2D6 inhibitor

Nausea

Diarrhea

Depression and suicidal ideation (rare; usually occurs in people with preexisting psychiatric conditions)

Isentress

• 400-mg tablet
• 100-mg single-use packet for oral suspension

Isentress HD

• 600-mg tablet

Isentress

• 400 mg PO twice daily

With Rifampin

• 800 mg PO twice daily

Isentress HD

In People Without Prior ARV Treatment or ARV-Experienced People With Virologic Suppression on a Regimen Containing RAL 400 mg Twice Daily

• 1,200 mg (two 600-mg tablets) PO once daily

With Rifampin

• Not recommended

Rash, including Stevens-Johnson syndrome, HSR, and toxic epidermal necrolysis

Nausea

Headache

Diarrhea

Pyrexia

CPK elevation, muscle weakness, and rhabdomyolysis

Weight gain

Insomnia

Depression and suicidal ideation (rare; usually occurs in people with preexisting psychiatric conditions)

^a For dose adjustments in people with hepatic insufficiency, see Appendix B. When no food restriction is listed, the antiretroviral drug can be taken with or without food.

^b Also see Table 20.

^c See Appendix A, Table 1 for information about these formulations.

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; CAB = cabotegravir; COBI = cobicistat; CrCl = creatinine clearance; CYP = cytochrome P450; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HD = high dose; HSR = hypersensitivity reaction; IM = intramuscular; INSTI = integrase strand transfer inhibitor; PO = orally; RAL = raltegravir; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; TPV/r = tipranavir/ritonavir; UGT1 = uridine diphosphate glucuronyl transferase 1 family

• 300-mg tablet
• Single-dose 463.5-‍mg/‌‌‌‌‍‌‌‍‌1.5-‍mL vial for injection

Initiation Option 1

• Day 1: 927 mg SQ x 1 dose + 600 mg PO x 1 dose
• Day 2: 600 mg PO x 1 dose

Initiation Option 2

• Day 1: 600 mg PO x 1 dose 
• Day 2: 600 mg PO x 1 dose 
• Day 8: 300 mg PO x 1 dose
• Day 15: 927 mg SQ x 1 dose

Maintenance Dosing

• 927 mg by SQ injection every 6 months from the date of the last injection (+/-‍2 weeks)

Note: Each SQ dose requires two injections. 

PO: 10–12 days

SQ: 8–12 weeks

Substrate of P-‍gp, CYP3A (minor), UGT1A1 (minor)

CYP3A4 inhibitor (moderate) and P-gp inhibitor

Injection site reactions, including nodules, induration, and necrosis

Serious injection site reactions (e.g., necrosis and ulcer) may occur when LEN is improperly administered intradermally instead of subcutaneously.

Nausea, diarrhea, headache

• 600-mg extended-release tablets

• FTR 600 mg PO twice daily

Nausea

Transaminase elevation; transient bilirubin elevation

Sleep disturbance, dizziness

QTc prolongation was seen at four times the recommended dose. Use with caution in people with preexisting heart disease, QTc prolongation, or concomitant use of medications that may prolong QTc interval.

• Single-dose 2‑mL vial containing IBA 200 mg/1.33 mL (150 mg/mL)

• Administer a single loading dose of IBA 2,000-‍mg IV infusion over 30 minutes, followed by a maintenance dose of IBA 800-mg IV infusion over 15 minutes or
• Undiluted IBA solution can be given as IV push: over 90 seconds for loading dose and over 30 seconds every 2 weeks for maintenance dose.
• See prescribing information for additional instructions for preparing, storing, and administering IBA, and for monitoring people who are receiving IBA. 

Diarrhea

Dizziness

Nausea

Rash

HSRs, including anaphylaxis and infusion-related reactions, have been reported.

Maraviroc
(MVC)
Selzentry

Note: Generic products are available.

Selzentry

• 150-mg and 300‑mg tablets
• 20-mg/1-mL oral solution 

Generic

• 150-mg and 300‑mg tablets

• MVC 150 mg PO twice daily when given with drugs that are strong CYP3A inhibitors (with or without CYP3A inducers), including PIs (except TPV/r)
• MVC 300 mg PO twice daily when given with NRTIs, RAL, and other drugs that are not strong CYP3A inhibitors or inducers
• MVC 600 mg PO twice daily when given with drugs that are CYP3A inducers, including EFV, ETR, etc. (without a CYP3A inhibitor)

Take MVC without regard to food.

Abdominal pain

Cough

Dizziness

Musculoskeletal symptoms

Pyrexia

Rash

Upper respiratory tract infections

Hepatotoxicity, which may be preceded by severe rash or other signs of systemic allergic reactions

Orthostatic hypotension, especially in people with severe renal insufficiency