Table 6. Characteristics of Integrase Strand Transfer Inhibitors.

	Dolutegravir (Tivicay ®)	Elvitegravir	Raltegravir (Isentress ®)
Abbreviation	DTG	EVG	RAL
US FDA Approval Year	2013	2012	2007
US FDA Indication(s) for HIV-infected adults	antiretroviral (ART) naïve and experienced patients	ART naïve patients	ART naïve and experienced patients
US FDA Indication(s) for HIV-infected children	12 years of age and older	Not recommended for children	4 weeks and older
Generic Formulation	t:h="c"No	No	No
Usual Dose (Adult)	50mg po once daily; or 50mg po twice daily for the following situations: -For INSTI-naïve patients given with potent UGT1A1/CYP3A4 inducersa: or -For INSTI-experienced patients with certain INSTI mutations (see product label) or with clinically suspected INSTI resistance	EVG only available in a co-formulated single tablet regimen with cobicistat/ emtricitabine/tenofovir: STRIBILD ® One tablet once daily Not recommended for patients with creatinine clearance (CrCl) < 70 mL/min	400mg po BID
Adjust dose in renal dysfunction	No	Yes	No
Formulations	Oral tablet: 50mg	Single tablet: Elvitegravir 150mg/cobicistat 150mg/emtricitabine 200mg/tenofovir 300mg	Oral tablet: 400mg Chewable tablets: 25mg, 100mg
Daily Pill Burden	1 pill; once daily administration	1 pill; once daily administration (full regimen)	2 pills, twice daily administration
Significant and/or common adverse effects	Insomnia Headache	Nausea Diarrhea Renal impairment (due to cobicistat and tenofovir)	Rash Nausea Insomnia CPK elevations
Major drug interactionsb	Mediated mainly by UGT1A1 and to a lesser extent CYP3A: dosage adjustments required when given concomitantly with UGT1A1/CYP3Aa inducersa Inhibits tubular secretion of creatinine via inhibition of OCT2: use with dofetilide contraindicated; use metformin with caution Chelation: administration should be separated (2 hours) when giving DTG with polyvalent cations containing Mg, Al, Fe, Ca	Mediated mainly by CYP3A and UGT1A1/3 Potent CYP3A4 inhibition (by cobicistat): cautionary use with drugs that are major CYP3A4 substrates Chelation: administration should be separated (2 hours) when giving EVG with polyvalent cations containing Mg, Al, Fe, Ca	Mediated mainly by UGT1A1: cautionary use with drugs which induce UGT1A1 including rifamycins Chelation: administration should be avoided when giving RAL with polyvalent cations containing Mg, Al, Fe. Antacids containing calcium carbonate may be given without dosage adjustment
Primary resistance mutations61	E138A/K, G140S, Q148	T66A/I, E92G/Q, S147G, Q148R, N155H	Y143 C/H/R, Q148H/K/R, N155H
Special Considerations		Should be discontinued in patients with a CrCl <50ml/min while on therapy

^aefavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin

^bPlease refer to http://aidsinfo.nih.gov/guidelines/html/1/adult-and-adolescent-arv-guidelines/32/drug-interactions for a comprehensive list of drug-drug interactions.