Appendix B: Drug Characteristics Tables

Updated Reviewed Sep. 21, 2022

To view a table, please click on the corresponding link:

Appendix B, Table 1. Coformulated and Copackaged Antiretroviral Regimens

The following table includes dose recommendations for U.S. Food and Drug Administration–approved coformulated and copackaged antiretroviral regimens. Please see the class-specific drug characteristics tables (Appendix B, Tables 3, 4, 5, and 6) for details about the individual drugs included in these products, including information on elimination and metabolic pathways, serum and intracellular half-lives, and adverse effects. The products in this table are listed by drug class and arranged in alphabetical order by trade name within each class.

Trade Name
(Abbreviations)
ARV Drugs Included in the Regimen Dosing Recommendationa
INSTI plus Two NRTIs

Biktarvy

(BIC/TAF/FTC)

Bictegravir 50 mg/tenofovir alafenamide 25 mg/emtricitabine 200 mg

One tablet PO once daily

Genvoya

(EVG/c/TAF/FTC)

Elvitegravir 150 mg/cobicistat 150 mg/tenofovir alafenamide 10 mg/emtricitabine 200 mg

One tablet PO once daily with food

Stribild

(EVG/c/TDF/FTC)

Elvitegravir 150 mg/cobicistat 150 mg/tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily with food

Triumeq

Triumeq PD

(DTG/ABC/3TC)

Dolutegravir 50 mg/abacavir 600 mg/lamivudine 300 mg

Dolutegravir 5-mg/abacavir 60-mg/lamivudine 30-mg tablet for oral suspension

One tablet PO once daily

INSTI plus One NRTI

Dovato

(DTG/3TC)

Dolutegravir 50 mg/lamivudine 300 mg

One tablet PO once daily

PI plus Two NRTIs

Symtuza

(DRV/c/TAF/FTC)

Darunavir 800 mg/cobicistat 150 mg/tenofovir alafenamide 10 mg/emtricitabine 200 mg

One tablet PO once daily with food

NNRTI plus Two NRTIs

Atripla

(EFV/TDF/FTC)

Efavirenz 600 mg/tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily on an empty stomach, preferably at bedtime

Complera

(RPV/TDF/FTC)

Rilpivirine 25 mg/tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily with food

Delstrigo

(DOR/TDF/3TC)

Doravirine 100 mg/tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily

Odefsey

(RPV/TAF/FTC)

Rilpivirine 25 mg/tenofovir alafenamide 25 mg/emtricitabine 200 mg

One tablet PO once daily with food

Symfi

(EFV/TDF/3TC)

Efavirenz 600 mg/tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily on an empty stomach, preferably at bedtime

Symfi Lo

(EFV/TDF/3TC)

Efavirenz 400 mg/tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily on an empty stomach, preferably at bedtime

INSTI plus One NNRTI

Cabenuva

(CAB IM and RPV IM)

Cabenuva 600-mg/900-mg kit contains:

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

Cabenuva 400-mg/600-mg kit contains:

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

Optional Lead-in with Oral CAB and RPV

  • CAB 30 mg 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 × 1 dose and RPV 900 mg/3 mL IM × 1 dose
  • Continuation phase: CAB 400 mg/2 mL IM every 4 weeks and RPV 600 mg/2 mL IM every 4 weeks

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

Juluca

(DTG/RPV)

Dolutegravir 50 mg/rilpivirine 25 mg

One tablet PO once daily with food

a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 11. When no food restriction is listed, the product can be taken with or without food.

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; CAB = cabotegravir; DOR = doravirine; DRV = darunavir; DRV/c = darunavir/cobicistat; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FTC = emtricitabine; IM = intramuscular; INSTI = integrase strand transfer inhibitor; NNRTI = non-nucleoside reverse transcriptase inhibitor; NRTI = nucleoside reverse transcriptase inhibitor; PI = protease inhibitor; PO = orally; RPV = rilpivirine; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate

Appendix B, Table 2. Nucleoside Reverse Transcriptase Inhibitor-Based, Fixed-Dose Combination Tablets for Use as Part of an Antiretroviral Regimen

The following table includes dose recommendations for U.S. Food and Drug Administration (FDA)–approved dual nucleoside reverse transcriptase inhibitor fixed-dose combination (FDC) products. These FDC tablets are not complete regimens and must be administered in combination with other antiretroviral drugs. FDC products that contain zidovudine (ZDV) have been removed from this table. Please refer to the FDA product labels for information regarding ZDV-containing FDCs. Please see the class-specific drug characteristics tables (Appendix B, Tables 3, 4, 5, and 6) for details about the individual drugs contained in these FDC products, including information on elimination and metabolic pathways, serum and intracellular half-lives, and adverse effects. The FDC tablets in this table are listed by trade name.

Trade Name
(Abbreviation)
ARV Drugs Included in the FDC Tablet Dosing Recommendationa
TAF or TDF plus an NRTI

Descovy
(TAF/FTC)

Tenofovir alafenamide 25 mg/emtricitabine 200 mg

Tenofovir alafenamide 15 mg/emtricitabine 120 mg

One tablet PO once daily

Cimduo
(TDF/3TC)

Tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily

Truvada
(TDF/FTC)

Tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily

Other NRTI-Based, FDC Tablets

Epzicom
(ABC/3TC)

Note: Generic product is available.

Abacavir 600 mg/lamivudine 300 mg

One tablet PO once daily

a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 11. 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; NRTI = nucleoside reverse transcriptase inhibitor; PO = orally; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate

Appendix B, Table 3. Characteristics of Nucleoside Reverse Transcriptase Inhibitors

The older nucleoside reverse transcriptase inhibitors didanosine (ddI) and stavudine (d4T) have been discontinued in the United States. Zidovudine (ZDV) is no longer used commonly in clinical practice. Therefore, these antiretrovirals have been removed from this table. Please refer to the U.S. Food and Drug Administration product label for ZDV for information regarding this drug.

Table 3. Characteristics of Nucleoside Reverse Transcriptase Inhibitors
   
   
   
   

Appendix B, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

The older non-nucleoside reverse transcriptase inhibitor delavirdine (DLV) has been discontinued in the United States and is not listed in this table.

Appendix B, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
   
   
   
   

Appendix B, Table 5. Characteristics of Protease Inhibitors

The older protease inhibitors indinavir (IDV) and saquinavir (SQV) have been discontinued in the United States; fosamprenavir (FPV), nelfinavir (NFV), and tipranavir (TPV) are no longer used commonly in clinical practice. These agents have been removed from this table. Please refer to the July 10, 2019, version of the guidelines (found in the Adult and Adolescent ARV Archived Guidelines section of Clinical Info) or to the U.S. Food and Drug Administration product labels for information regarding these drugs.

Table 5. Characteristics of Protease Inhibitorsa
   
   
   
   

Appendix B, Table 6. Characteristics of Integrase Inhibitors

Generic Name
(Abbreviation)
Trade Name
Formulations Dosing Recommendationsa Elimination/
Metabolic Pathways
Serum Half-Life Adverse Eventsb

Bictegravir
(BIC)

BIC is available only as a component of the STR Biktarvy (BIC/TAF/FTC).c

Biktarvy

  • One tablet PO once daily

CYP3A4 substrate

UGT1A1-mediated glucuronidation

~17 hours

Diarrhea

Nausea

Headache

Weight gain

Cabotegravir
(CAB)

Available as part of the copackaged IM long-acting regimen Cabenuva (CAB IM and RPV IM)

  • 400-mg/2-mL vial
  • 600-mg/3-mL vial

Also available as an individual product for IM long-acting pre-exposure prophylaxis Apretude (CAB IM)

  • 600-mg/3-mL vial

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)

See Appendix B, Table 1 for dosing information for coformulated and copackaged regimens that contain CAB.

UGT1A1 and UGT1A9-mediated glucuronidation

Oral: 41 hours

IM: 6–12 weeks

Headache

Nausea

Abnormal dreams

Anxiety

Insomnia

Depressive disorders

Hepatotoxicity

IM formulation only: Injection-site reactions (e.g., pain, induration, swelling, nodules)

Dolutegravir
(DTG)
Tivicay

Tivicay

  • 10-mg, 25-mg, and 50-mg tablets
  • 5-mg soluble tablet

STRs that Contain DTGc

  • Dovato (DTG/3TC)
  • Juluca (DTG/RPV)
  • Triumeq and Triumeq PD tablet for oral suspension (DTG/ABC/3TC)

In ARV-Naive or ARV-Experienced, INSTI-Naive Patients

  • DTG 50 mg PO once daily

In ARV-Naive or ARV-Experienced, INSTI-Naive Patients when Coadministered with EFV, FPV/r, TPV/r, or Rifampin

  • DTG 50 PO mg twice daily

In INSTI-Experienced Patients with Certain INSTI Mutations (See Product Label) or with Clinically Suspected INSTI Resistance

  • DTG 50 mg PO twice daily

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

UGT1A1-mediated glucuronidation

Minor substrate of CYP3A4

~14 hours

Insomnia

Headache

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

Weight gain

Hepatotoxicity

Potential for increased risk of NTDs in infants born to individuals who received DTG around the time of conception is lower than previously reported. Refer to Appendix B, Table 6 for more information.

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

Elvitegravir
(EVG)

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

STRs that Contain EVGc

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

Genvoya

  • One tablet PO once daily with food
  • See Appendix B, Table 11 for recommendations on dosing in persons with renal insufficiency.

Stribild

  • One tablet PO once daily with food
  • Not recommended for patients with baseline CrCl <70 mL/min (see Appendix B, Table 11 for the CrCl calculation equation).

EVG

  • CYP3A and UGT1A1/3 substrate

COBI

  • CYP3A inhibitor and substrate
  • CYP2D6 inhibitor

EVG/c: ~13 hours

Nausea

Diarrhea

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

Raltegravir
(RAL)
Isentress
Isentress HD

Isentress

  • 400-mg tablet
  • 25-mg and 10-mg chewable tablets
  • 100-mg single-use packet for oral suspension

Isentress HD

  • 600-mg tablet

Isentress

In ARV-Naive Patients or ARV-Experienced Patients

  • 400 mg PO twice daily

With Rifampin

  • 800 mg PO twice daily

Isentress HD

In ARV-Naive or ARV-Experienced Patients 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

UGT1A1-mediated glucuronidation

~9 hours

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 patients with preexisting psychiatric conditions)

a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 11. When no food restriction is listed, the antiretroviral drug can be taken with or without food.

b Also see Table 20.

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

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; CAB = cabotegravir; COBI = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HSR = hypersensitivity reaction; IM = intramuscular; INSTI = integrase strand transfer inhibitor; NTD = neural tube defect; 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

Appendix B, Table 7. Characteristics of the Fusion Inhibitor

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendation Serum Half-Life Elimination Adverse Eventsa

Enfuvirtide
(T-20)
Fuzeon

Fuzeon

  • Injectable; supplied as lyophilized powder.
  • Each vial contains 108 mg of T-20; reconstitute with 1.1 mL of sterile water for injection for delivery of approximately 90 mg/1 mL.
  • Refer to prescribing information for storage instruction.

Fuzeon

  • T-20 90 mg/1 mL SQ twice daily

3.8 hours

Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.

Local injection site reactions (e.g., pain, erythema, induration, nodules and cysts, pruritus, ecchymosis) in almost 100% of patients

Increased incidence of bacterial pneumonia

HSR occurs in <1% of patients. Symptoms may include rash, fever, nausea, vomiting, chills, rigors, hypotension, or elevated serum transaminases. Re-challenge is not recommended.

a Also see Table 20.

Key: HSR = hypersensitivity reaction; SQ = subcutaneous; T-20 = enfuvirtide

Appendix B, Table 8. Characteristics of the CCR5 Antagonist

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendationsa Serum Half-Life Elimination/
Metabolic Pathway
Adverse Eventsb

Maraviroc
(MVC)
Selzentry

Selzentry

  • 150-mg and 300‑mg tablets

Selzentry

  • 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, T‑20, TPV/r, NVP, 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.

14–18 hours

CYP3A4 substrate

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 patients with severe renal insufficiency

a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 11.

b Also see Table 20.

Key: CYP = cytochrome P; EFV = efavirenz; ETR = etravirine; MVC = maraviroc; NRTI = nucleoside reverse transcriptase inhibitor; NVP = nevirapine; PI = protease inhibitor; PO = orally; RAL = raltegravir; T-20 = enfuvirtide; TPV/r = tipranavir/ritonavir

Appendix B, Table 9. Characteristics of CD4 Post-Attachment Inhibitor

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendations Serum Half-Life Elimination/ Metabolic Pathway Adverse Events

Ibalizumab
(IBA)
Trogarzo

Trogarzo

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

Trogarzo

  • 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 every 2 weeks.
  • See prescribing information for additional instructions for preparing, storing, and administering IBA, and for monitoring patients who are receiving IBA.

~64 hours

Not well defined

Diarrhea

Dizziness

Nausea

Rash

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

Key: IBA = ibalizumab; IV = intravenous

Appendix B, Table 10. Characteristics of the gp120 Attachment Inhibitor

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendations Serum Half-Life Elimination/ Metabolic Pathway Adverse Events

Fostemsavir

(FTR)

Rukobia

  • 600-mg extended-release tablets
  • FTR 600 mg PO twice daily

11 hours

Hydrolysis (esterases), CYP3A4

Nausea

Transaminase elevation; transient bilirubin elevation

Sleep disturbance, dizziness

QTc prolongation was seen at 4 times the recommended dose. Use with caution in patients with preexisting heart disease, QTc prolongation, or concomitant use of medications that may prolong QTc interval.

Key: CYP = cytochrome P; FTR = fostemsavir; PO = orally; QTc = corrected QT interval

Appendix B, Table 11. Antiretroviral Dosing Recommendations in Patients with Renal or Hepatic Insufficiency

The older antiretroviral drugs fosamprenavir (FPV), nelfinavir (NFV), tipranavir (TPV), and zidovudine (ZDV) have been removed from this table. Please refer to the U.S. Food and Drug Administration product labels for these drugs for recommendations on dosing in adults and adolescents with renal or hepatic insufficiency. See the reference section at the end of this table for creatinine clearance calculation formulas and criteria for Child-Pugh classification.

Table 11. Antiretroviral Dosing Recommendations in Persons with Renal or Hepatic Insufficiency
   
   
   
   

To view a table, please click on the corresponding link:

Appendix B, Table 1. Coformulated and Copackaged Antiretroviral Regimens

The following table includes dose recommendations for U.S. Food and Drug Administration–approved coformulated and copackaged antiretroviral regimens. Please see the class-specific drug characteristics tables (Appendix B, Tables 3, 4, 5, and 6) for details about the individual drugs included in these products, including information on elimination and metabolic pathways, serum and intracellular half-lives, and adverse effects. The products in this table are listed by drug class and arranged in alphabetical order by trade name within each class.

Trade Name
(Abbreviations)
ARV Drugs Included in the Regimen Dosing Recommendationa
INSTI plus Two NRTIs

Biktarvy

(BIC/TAF/FTC)

Bictegravir 50 mg/tenofovir alafenamide 25 mg/emtricitabine 200 mg

One tablet PO once daily

Genvoya

(EVG/c/TAF/FTC)

Elvitegravir 150 mg/cobicistat 150 mg/tenofovir alafenamide 10 mg/emtricitabine 200 mg

One tablet PO once daily with food

Stribild

(EVG/c/TDF/FTC)

Elvitegravir 150 mg/cobicistat 150 mg/tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily with food

Triumeq

Triumeq PD

(DTG/ABC/3TC)

Dolutegravir 50 mg/abacavir 600 mg/lamivudine 300 mg

Dolutegravir 5-mg/abacavir 60-mg/lamivudine 30-mg tablet for oral suspension

One tablet PO once daily

INSTI plus One NRTI

Dovato

(DTG/3TC)

Dolutegravir 50 mg/lamivudine 300 mg

One tablet PO once daily

PI plus Two NRTIs

Symtuza

(DRV/c/TAF/FTC)

Darunavir 800 mg/cobicistat 150 mg/tenofovir alafenamide 10 mg/emtricitabine 200 mg

One tablet PO once daily with food

NNRTI plus Two NRTIs

Atripla

(EFV/TDF/FTC)

Efavirenz 600 mg/tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily on an empty stomach, preferably at bedtime

Complera

(RPV/TDF/FTC)

Rilpivirine 25 mg/tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily with food

Delstrigo

(DOR/TDF/3TC)

Doravirine 100 mg/tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily

Odefsey

(RPV/TAF/FTC)

Rilpivirine 25 mg/tenofovir alafenamide 25 mg/emtricitabine 200 mg

One tablet PO once daily with food

Symfi

(EFV/TDF/3TC)

Efavirenz 600 mg/tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily on an empty stomach, preferably at bedtime

Symfi Lo

(EFV/TDF/3TC)

Efavirenz 400 mg/tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily on an empty stomach, preferably at bedtime

INSTI plus One NNRTI

Cabenuva

(CAB IM and RPV IM)

Cabenuva 600-mg/900-mg kit contains:

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

Cabenuva 400-mg/600-mg kit contains:

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

Optional Lead-in with Oral CAB and RPV

  • CAB 30 mg 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 × 1 dose and RPV 900 mg/3 mL IM × 1 dose
  • Continuation phase: CAB 400 mg/2 mL IM every 4 weeks and RPV 600 mg/2 mL IM every 4 weeks

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

Juluca

(DTG/RPV)

Dolutegravir 50 mg/rilpivirine 25 mg

One tablet PO once daily with food

a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 11. When no food restriction is listed, the product can be taken with or without food.

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; CAB = cabotegravir; DOR = doravirine; DRV = darunavir; DRV/c = darunavir/cobicistat; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FTC = emtricitabine; IM = intramuscular; INSTI = integrase strand transfer inhibitor; NNRTI = non-nucleoside reverse transcriptase inhibitor; NRTI = nucleoside reverse transcriptase inhibitor; PI = protease inhibitor; PO = orally; RPV = rilpivirine; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate

Appendix B, Table 2. Nucleoside Reverse Transcriptase Inhibitor-Based, Fixed-Dose Combination Tablets for Use as Part of an Antiretroviral Regimen

The following table includes dose recommendations for U.S. Food and Drug Administration (FDA)–approved dual nucleoside reverse transcriptase inhibitor fixed-dose combination (FDC) products. These FDC tablets are not complete regimens and must be administered in combination with other antiretroviral drugs. FDC products that contain zidovudine (ZDV) have been removed from this table. Please refer to the FDA product labels for information regarding ZDV-containing FDCs. Please see the class-specific drug characteristics tables (Appendix B, Tables 3, 4, 5, and 6) for details about the individual drugs contained in these FDC products, including information on elimination and metabolic pathways, serum and intracellular half-lives, and adverse effects. The FDC tablets in this table are listed by trade name.

Trade Name
(Abbreviation)
ARV Drugs Included in the FDC Tablet Dosing Recommendationa
TAF or TDF plus an NRTI

Descovy
(TAF/FTC)

Tenofovir alafenamide 25 mg/emtricitabine 200 mg

Tenofovir alafenamide 15 mg/emtricitabine 120 mg

One tablet PO once daily

Cimduo
(TDF/3TC)

Tenofovir disoproxil fumarate 300 mg/lamivudine 300 mg

One tablet PO once daily

Truvada
(TDF/FTC)

Tenofovir disoproxil fumarate 300 mg/emtricitabine 200 mg

One tablet PO once daily

Other NRTI-Based, FDC Tablets

Epzicom
(ABC/3TC)

Note: Generic product is available.

Abacavir 600 mg/lamivudine 300 mg

One tablet PO once daily

a For dose adjustments in patients with renal or hepatic insufficiency, see Appendix B, Table 11. 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; NRTI = nucleoside reverse transcriptase inhibitor; PO = orally; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate

Appendix B, Table 3. Characteristics of Nucleoside Reverse Transcriptase Inhibitors

The older nucleoside reverse transcriptase inhibitors didanosine (ddI) and stavudine (d4T) have been discontinued in the United States. Zidovudine (ZDV) is no longer used commonly in clinical practice. Therefore, these antiretrovirals have been removed from this table. Please refer to the U.S. Food and Drug Administration product label for ZDV for information regarding this drug.

Table 3. Characteristics of Nucleoside Reverse Transcriptase Inhibitors
   
   
   
   

Appendix B, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

The older non-nucleoside reverse transcriptase inhibitor delavirdine (DLV) has been discontinued in the United States and is not listed in this table.

Appendix B, Table 4. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
   
   
   
   

Appendix B, Table 5. Characteristics of Protease Inhibitors

The older protease inhibitors indinavir (IDV) and saquinavir (SQV) have been discontinued in the United States; fosamprenavir (FPV), nelfinavir (NFV), and tipranavir (TPV) are no longer used commonly in clinical practice. These agents have been removed from this table. Please refer to the July 10, 2019, version of the guidelines (found in the Adult and Adolescent ARV Archived Guidelines section of Clinical Info) or to the U.S. Food and Drug Administration product labels for information regarding these drugs.

Table 5. Characteristics of Protease Inhibitorsa
   
   
   
   

Appendix B, Table 6. Characteristics of Integrase Inhibitors

Generic Name
(Abbreviation)
Trade Name
Formulations Dosing Recommendationsa Elimination/
Metabolic Pathways
Serum Half-Life Adverse Eventsb

Bictegravir
(BIC)

BIC is available only as a component of the STR Biktarvy (BIC/TAF/FTC).c

Biktarvy

  • One tablet PO once daily

CYP3A4 substrate

UGT1A1-mediated glucuronidation

~17 hours

Diarrhea

Nausea

Headache

Weight gain

Cabotegravir
(CAB)

Available as part of the copackaged IM long-acting regimen Cabenuva (CAB IM and RPV IM)

  • 400-mg/2-mL vial
  • 600-mg/3-mL vial

Also available as an individual product for IM long-acting pre-exposure prophylaxis Apretude (CAB IM)

  • 600-mg/3-mL vial

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)

See Appendix B, Table 1 for dosing information for coformulated and copackaged regimens that contain CAB.

UGT1A1 and UGT1A9-mediated glucuronidation

Oral: 41 hours

IM: 6–12 weeks

Headache

Nausea

Abnormal dreams

Anxiety

Insomnia

Depressive disorders

Hepatotoxicity

IM formulation only: Injection-site reactions (e.g., pain, induration, swelling, nodules)

Dolutegravir
(DTG)
Tivicay

Tivicay

  • 10-mg, 25-mg, and 50-mg tablets
  • 5-mg soluble tablet

STRs that Contain DTGc

  • Dovato (DTG/3TC)
  • Juluca (DTG/RPV)
  • Triumeq and Triumeq PD tablet for oral suspension (DTG/ABC/3TC)

In ARV-Naive or ARV-Experienced, INSTI-Naive Patients

  • DTG 50 mg PO once daily

In ARV-Naive or ARV-Experienced, INSTI-Naive Patients when Coadministered with EFV, FPV/r, TPV/r, or Rifampin

  • DTG 50 PO mg twice daily

In INSTI-Experienced Patients with Certain INSTI Mutations (See Product Label) or with Clinically Suspected INSTI Resistance

  • DTG 50 mg PO twice daily

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

UGT1A1-mediated glucuronidation

Minor substrate of CYP3A4

~14 hours

Insomnia

Headache

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

Weight gain

Hepatotoxicity

Potential for increased risk of NTDs in infants born to individuals who received DTG around the time of conception is lower than previously reported. Refer to Appendix B, Table 6 for more information.

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

Elvitegravir
(EVG)

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

STRs that Contain EVGc

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

Genvoya

  • One tablet PO once daily with food
  • See Appendix B, Table 11 for recommendations on dosing in persons with renal insufficiency.

Stribild

  • One tablet PO once daily with food
  • Not recommended for patients with baseline CrCl <70 mL/min (see Appendix B, Table 11 for the CrCl calculation equation).

EVG

  • CYP3A and UGT1A1/3 substrate

COBI

  • CYP3A inhibitor and substrate
  • CYP2D6 inhibitor

EVG/c: ~13 hours

Nausea

Diarrhea

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

Raltegravir
(RAL)
Isentress
Isentress HD

Isentress

  • 400-mg tablet
  • 25-mg and 10-mg chewable tablets
  • 100-mg single-use packet for oral suspension

Isentress HD

  • 600-mg tablet

Isentress

In ARV-Naive Patients or ARV-Experienced Patients

  • 400 mg PO twice daily

With Rifampin

  • 800 mg PO twice daily

Isentress HD

In ARV-Naive or ARV-Experienced Patients 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

UGT1A1-mediated glucuronidation

~9 hours

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 patients with preexisting psychiatric conditions)

a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 11. When no food restriction is listed, the antiretroviral drug can be taken with or without food.

b Also see Table 20.

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

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; CAB = cabotegravir; COBI = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HSR = hypersensitivity reaction; IM = intramuscular; INSTI = integrase strand transfer inhibitor; NTD = neural tube defect; 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

Appendix B, Table 7. Characteristics of the Fusion Inhibitor

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendation Serum Half-Life Elimination Adverse Eventsa

Enfuvirtide
(T-20)
Fuzeon

Fuzeon

  • Injectable; supplied as lyophilized powder.
  • Each vial contains 108 mg of T-20; reconstitute with 1.1 mL of sterile water for injection for delivery of approximately 90 mg/1 mL.
  • Refer to prescribing information for storage instruction.

Fuzeon

  • T-20 90 mg/1 mL SQ twice daily

3.8 hours

Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.

Local injection site reactions (e.g., pain, erythema, induration, nodules and cysts, pruritus, ecchymosis) in almost 100% of patients

Increased incidence of bacterial pneumonia

HSR occurs in <1% of patients. Symptoms may include rash, fever, nausea, vomiting, chills, rigors, hypotension, or elevated serum transaminases. Re-challenge is not recommended.

a Also see Table 20.

Key: HSR = hypersensitivity reaction; SQ = subcutaneous; T-20 = enfuvirtide

Appendix B, Table 8. Characteristics of the CCR5 Antagonist

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendationsa Serum Half-Life Elimination/
Metabolic Pathway
Adverse Eventsb

Maraviroc
(MVC)
Selzentry

Selzentry

  • 150-mg and 300‑mg tablets

Selzentry

  • 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, T‑20, TPV/r, NVP, 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.

14–18 hours

CYP3A4 substrate

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 patients with severe renal insufficiency

a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 11.

b Also see Table 20.

Key: CYP = cytochrome P; EFV = efavirenz; ETR = etravirine; MVC = maraviroc; NRTI = nucleoside reverse transcriptase inhibitor; NVP = nevirapine; PI = protease inhibitor; PO = orally; RAL = raltegravir; T-20 = enfuvirtide; TPV/r = tipranavir/ritonavir

Appendix B, Table 9. Characteristics of CD4 Post-Attachment Inhibitor

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendations Serum Half-Life Elimination/ Metabolic Pathway Adverse Events

Ibalizumab
(IBA)
Trogarzo

Trogarzo

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

Trogarzo

  • 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 every 2 weeks.
  • See prescribing information for additional instructions for preparing, storing, and administering IBA, and for monitoring patients who are receiving IBA.

~64 hours

Not well defined

Diarrhea

Dizziness

Nausea

Rash

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

Key: IBA = ibalizumab; IV = intravenous

Appendix B, Table 10. Characteristics of the gp120 Attachment Inhibitor

Generic Name
(Abbreviation)
Trade Name
Formulation Dosing Recommendations Serum Half-Life Elimination/ Metabolic Pathway Adverse Events

Fostemsavir

(FTR)

Rukobia

  • 600-mg extended-release tablets
  • FTR 600 mg PO twice daily

11 hours

Hydrolysis (esterases), CYP3A4

Nausea

Transaminase elevation; transient bilirubin elevation

Sleep disturbance, dizziness

QTc prolongation was seen at 4 times the recommended dose. Use with caution in patients with preexisting heart disease, QTc prolongation, or concomitant use of medications that may prolong QTc interval.

Key: CYP = cytochrome P; FTR = fostemsavir; PO = orally; QTc = corrected QT interval

Appendix B, Table 11. Antiretroviral Dosing Recommendations in Patients with Renal or Hepatic Insufficiency

The older antiretroviral drugs fosamprenavir (FPV), nelfinavir (NFV), tipranavir (TPV), and zidovudine (ZDV) have been removed from this table. Please refer to the U.S. Food and Drug Administration product labels for these drugs for recommendations on dosing in adults and adolescents with renal or hepatic insufficiency. See the reference section at the end of this table for creatinine clearance calculation formulas and criteria for Child-Pugh classification.

Table 11. Antiretroviral Dosing Recommendations in Persons with Renal or Hepatic Insufficiency
   
   
   
   

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