Updated
Reviewed
Jun. 03, 2021

Appendix B: Drug Characteristics Tables

Characteristics of Integrase Inhibitors

Appendix B, Table 6. Characteristics of Integrase Strand Transfer 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 intramuscular long-acting regimen Cabenuva (CAB IM and RPV IM):

  • 400-mg/2-mL vial
  • 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 DTG:c

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

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 INSTI section 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 EVG:c

  • 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 ARV 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: Drug Characteristics Tables

Characteristics of Integrase Inhibitors

Appendix B, Table 6. Characteristics of Integrase Strand Transfer 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 intramuscular long-acting regimen Cabenuva (CAB IM and RPV IM):

  • 400-mg/2-mL vial
  • 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 DTG:c

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

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 INSTI section 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 EVG:c

  • 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 ARV 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

Download Guidelines