Characteristics of Integrase Inhibitors | Appendix B: Drug Characteristics Tables | Adult and Adolescent ARV | ClinicalInfo

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

The information in the brief version is excerpted directly from the full-text guidelines. The brief version is a compilation of the tables and boxed recommendations.

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 Recommendations^a	Elimination/ Metabolic Pathways	Serum Half-Life	Adverse Events^b
Bictegravir (BIC)	BIC is only available 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
Dolutegravir (DTG) Tivicay	Tivicay: 50 mg 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 mg PO 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 pre-existing psychiatric conditions) Weight gain Hepatotoxicity There is a potential increased risk of NTDs in infants born to individuals who received DTG around the time of conception (see Table 6b 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 10 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 10 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 pre-existing psychiatric conditions)
Raltegravir (RAL) Isentress Isentress HD	Isentress: 400 mg tablet 25 and 100 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 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 pre-existing psychiatric conditions)
^a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 10. When no food restriction is listed, the ARV drug can be taken with or without food. ^b Also see Table 17. ^c See Appendix B, Table 1 for information about these formulations. Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; COBI = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FDC = fixed-dose combination; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HSR = hypersensitivity reaction; 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; UGT = uridine diphosphate glucuronyl transferase

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 Recommendations^a	Elimination/ Metabolic Pathways	Serum Half-Life	Adverse Events^b
Bictegravir (BIC)	BIC is only available 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
Dolutegravir (DTG) Tivicay	Tivicay: 50 mg 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 mg PO 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 pre-existing psychiatric conditions) Weight gain Hepatotoxicity There is a potential increased risk of NTDs in infants born to individuals who received DTG around the time of conception (see Table 6b 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 10 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 10 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 pre-existing psychiatric conditions)
Raltegravir (RAL) Isentress Isentress HD	Isentress: 400 mg tablet 25 and 100 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 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 pre-existing psychiatric conditions)
^a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 10. When no food restriction is listed, the ARV drug can be taken with or without food. ^b Also see Table 17. ^c See Appendix B, Table 1 for information about these formulations. Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; COBI = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FDC = fixed-dose combination; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HSR = hypersensitivity reaction; 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; UGT = uridine diphosphate glucuronyl transferase

Updated

Dec. 18, 2019

Reviewed

Dec. 18, 2019

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