Characteristics of Integrase Inhibitors

Last Updated: October 25, 2018;

Last Reviewed: October 25, 2018

Generic Name (Abbreviation) Trade Name	Formulations	Dosing Recommendations^a	Elimination/ Metabolic Pathways	Serum Half-Life	Adverse Events^b
Bictegravir (BIC) Note: BIC is only available as a component of an FDC. (BIC/TAF/FTC) Biktarvy	Biktarvy: (BIC 50 mg plus TAF 25 mg plus FTC 200 mg) tablet	Biktarvy: 1 tablet once daily	BIC: CYP3A4 substrate UGT1A1 mediated glucuronidation	BIC: ~17 hours	Diarrhea Nausea Headache
Dolutegravir (DTG) Tivicay	Tivicay: 50 mg tablet	In ARV-Naive or ARV-Experienced, INSTI-Naive Patients: 50 mg once daily In ARV-Naive or ARV-Experienced, INSTI-Naive Patients when Coadministered with EFV, FPV/r, TPV/r, or Rifampin: 50 mg BID INSTI-Experienced Patients with Certain INSTI Mutations (See Product Label) or with Clinically Suspected INSTI Resistance: 50 mg BID Take without regard to meals	UGT1A1 mediated glucuronidation Minor contribution from CYP3A4	~14 hours	Insomnia Headache Depression and suicidal ideation (rare; usually in patients with pre-existing psychiatric conditions) Hepatotoxicity Preliminary data suggest increased rate of neural tube defects in infants born to mothers who were taking DTG at the time of conception. HSRs, including rash, constitutional symptoms, and organ dysfunction (including liver injury) have been reported.
(DTG/ABC/3TC) Triumeq	Triumeq: (DTG 50 mg plus ABC 600 mg plus 3TC 300 mg) tablet	Triumeq: 1 tablet once daily
(DTG/RPV) Juluca	Juluca: (DTG 50 mg plus RPV 25 mg) tablet	Juluca: 1 tablet once daily with a meal
Elvitegravir (EVG) Note: EVG is only available as a component of an FDC. (EVG/c/FTC/TAF) Genvoya	Genvoya: (EVG 150 mg plus COBI 150 mg plus FTC 200 mg plus TAF 10 mg) tablet	Genvoya: 1 tablet once daily with food Not recommended for patients with CrCl <30 mL/min (see Appendix B, Table 8 for the equation for calculating CrCl). Not recommended for use with other ARV drugs.	EVG: CYP3A, UGT1A1/3 substrate COBI: CYP3A inhibitor and substrate; CYP2D6 inhibitor	~13 hours (EVG/c)	Nausea Diarrhea Depression and suicidal ideation (rare; usually in patients with pre-existing psychiatric conditions)
(EVG/c/FTC/TDF) Stribild	Stribild: (EVG 150 mg plus COBI 150 mg plus FTC 200 mg plus TDF 300 mg) tablet	Stribild: 1 tablet once daily with food Not recommended for patients with baseline CrCl <70 mL/min (see Appendix B, Table 8 for the equation for calculating CrCl). Not recommended for use with other ARV drugs.
Raltegravir (RAL) Isentress Isentress HD	400 mg tablet 600 mg tablet (HD) 25 and 100 mg chewable tablets 100 mg single packet for oral suspension	In ARV-Naive Patients or ARV-Experienced Patients: Isentress: 400 mg BID In ARV-Naive or ARV-Experienced Patients with Virologic Suppression on a Regimen of RAL 400 mg BID: Isentress HD: 1200 mg (two 600-mg tablets) once daily With Rifampin: Isentress: 800 mg BID Isentress HD: Not recommended Take without regard to meals.	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 Insomnia Depression and suicidal ideation (rare; usually in patients with pre-existing psychiatric conditions)
^a For dosage adjustment in patients with hepatic insufficiency, see Appendix B, Table 8. ^b Also see Table 15. Key to Acronyms: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; BID = twice daily; 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; RAL = raltegravir; RPV = rilpivirine; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; TPV/r = tipranavir/ritonavir; UGT = uridine diphosphate gluconyltransferase