Table 1 Summary of Pertinent Clinical Characteristics of Available Integrase Strand Transfer Inhibitor (INSTI) Products
INSTI Product Component(s): Drug and Strength | US Trade Name | Dosage form(s) available | FDA-Labeled Indication(s) | Can it be crushed? | Metabolism | Dosing and Administration | Daily Pill Burden | Tablet Size (mm) | Reference(s) |
|---|---|---|---|---|---|---|---|---|---|
BIC 50 mg FTC 200 mg TAF 25 mg | Biktarvy® | Oral FDC tablet Low dose alternative tablet: 30 mg BIC/ 120 mg FTC/ 15 mg TAF | HIV-1 Treatment: Adult and pediatric patients weighing > 25 kg with no ARV treatment history to replace current ARV regimen in those with HIV-1 RNA < 50 copies/mL on a stable ARV regimen with no history of treatment failure and no known resistance to its components | Conflicting evidence Notes: Potentially better to dissolve in water and take immediately rather than to crush | BIC: CYP3A UGT1A1 | Adults and pediatric patients weighing at least 25 kg: 1 tablet (BIC 50 mg/FTC 200 mg/TAF 25 mg) once daily PO with or without food Pediatric patients weighing at least 14 kg and < 25 kg: 1 tablet (BIC 30 mg/FTC 120 mg/TAF 15 mg) once daily PO with or without food | 1 | 15 × 8 | |
CAB 30 mg | Vocabria® | Oral tablet: 30 mg | HIV-1 Treatment: Adults and adolescents 12 years of age and older weighing at least 35 kg with HIV-1 RNA < 50 copies/mL on a stable ARV regimen with no history of treatment failure and with no known or suspected resistance to CAB or RPV; indicated for short-term treatment in combination with RPV HIV-1 Prophylaxis: At-risk adults and adolescents weighing at least 35 kg for PrEP to reduce the risk of sexually acquired HIV-1 infection and who have a negative HIV-1 test prior to initiating | No Notes: Not recommended due to lack of evidence of efficacy and safety. | CAB: UGT1A1 UGT1A9 (minor) | HIV-1 Treatment: Optional oral lead-in: 1 tablet (CAB 30 mg) PO once daily in combination with 1 RPV (25 mg) tablet PO once daily with a meal for at least 28 days HIV-1 Prophylaxis: Optional oral lead-in: 1 tablet (CAB 30 mg) PO once daily for at least 28 days | 1 | 14.3 × 8 | [19] |
CAB LA 200 mg/mL | Apretude® | Extended-release injectable suspension: 600 mg/3 mL | HIV-1 Prophylaxis: At-risk adults and adolescents weighing at least 35 kg for PrEP to reduce the risk of sexually acquired HIV-1 infection and who have a negative HIV-1 test prior to initiating | N/A | Initiation injection: CAB LA 3 mL once (if taking oral lead-in: on last day of oral lead-in or within 3 days thereafter) at month 2 and month 3 Continuation injections: CAB LA 3 mL at month 5 and every 2 months onwards | N/A;every 2-month injection | N/A | [19] | |
CAB LA 200 mg/mL plus RPV 300 mg/mL | Cabenuva® | Extended-release injectable suspension 400 mg/600 mg kit: CAB 400 mg/2 mL RPV 600 mg/2 mL Extended-release injectable suspension 600 mg/900 mg kit: CAB 600 mg/3 mL RPV 900 mg/3 mL | HIV-1 Treatment: Adult and pediatric patients 12 years of age and older weighing > 35 kg to replace current ARV regimen in those with HIV-1 RNA < 50 copies/mL an a stable ARV regimen with no history of treatment failure and no known resistance to its components | N/A | Dosing Schedule for Monthly Injections: Initiation Injections: CAB 600 mg (3 mL) IM and RPV 900 mg (3 mL) IM once given on last day of current ARV therapy OR if oral lead-in is used Continuation injections: CAB 400 mg (2 mL) IM and RPV 600 mg (2 mL) IM once monthly Dosing Schedule for Every-2 Month Injections: Initiation Injections: CAB 600 mg (3 mL) and RPV 900 mg (3 mL) IM at month 1 given on last day of current ARV therapy OR if oral lead-ins used and at month 2 Continuation Injections: CAB 600 mg (3 mL) and RPV 900 mg (3 mL) IM every 2 months onwards (starting at month 4) | N/A;every 2-month injection | N/A | [14] | |
DTG 50 mg | Tivicay® | Oral tablet: 10 mg 25 mg 50 mg Tivicay PD tablets for oral suspension: 5 mg | HIV-1 Treatment: Adults and pediatric patients aged at least 4 weeks and weighing at least 3 kg in combination with other antiretroviral agents | Yes Notes: Add to small amount of semi-solid food or liquid, consume immediately | DTG: UGT1A1 (major), CYP3A (minor) | Adults: 1 tablet (DTG 50 mg) tablet once daily PO with or without food Take twice daily if: INSTI resistance or also taking certain UGT1A or CYP3A inducers Pediatric: Weight based dosing (refer to prescribing information) PO with or without food Take twice daily if: Also taking certain UGT1A or CYP3A inducers | 1 or 2 | 9 × 9 | [20] |
DTG 50 mg 3TC 300 mg | Dovato® | Oral FDC tablet | HIV-1 Treatment: Adults with no ARV treatment history and with no known resistance to its components | Yes Notes: Crushing not recommended in product information, however if crushing is decided based on clinical judgment, add to small amount of semi-solid food or liquid, consume immediately. Study data shows virologic suppression after crushing DTG when suspending it in water or adding to small amount of semi-solid food and consuming immediately | 1 tablet (DTG 50 mg/3TC 300 mg) once daily PO with or without food | 1 | 18.5 × 9.5 | ||
DTG 50 mg RPV 25 mg | Juluca® | Oral FDC tablet | HIV-1 Treatment: Adults to replace current ARV regimen in those with HIV-1 RNA ≤ 50 copies/mL on a stable ARV regimen for at least 6 months with no history of treatment failure and no known resistance to its components | No Notes: If crushing is decided based on clinical judgment, add to small amount of semi-solid food or liquid, consume immediately | 1 tablet (DTG 50 mg/RPV 25 mg) once daily PO with a meal Dose adjustments recommended:Take with an additional 25-mg tablet of RPV PO once daily with a meal if coadministered with rifabutin | 1 | 14 × 7 | [26] | |
DTG 50 mg 3TC 300 mg ABC 600 mg | Triumeq® | Oral FDC tablet Triumeq PD tablets for oral suspension: DTG 5 mg/ABC 60 mg/3TC 30 mg | HIV-1 Treatment: Adult and pediatric patients weighing > 10 kg | Yes Notes: Add to small amount of semi-solid food or liquid, consume immediately | Adults: 1 tablet (DTG 50 mg/ABC 600 mg/3TC 300 mg) once daily PO with or without food Pediatric: Weight based dosing (refer to prescribing information) PO with or without food DTG dose adjustments recommended: - Also taking certain UGT1A or CYP3A inducers | 1 | 22 × 11 | ||
EVG 150 mg COBI 150 mg FTC 200 mg TAF 10 mg | Genvoya® | Oral FDC tablet | HIV-1 Treatment: Adult and pediatric patients weighing > 25 kg with no ARV treatment history or to replace current ARV regimen in those with HIV-1 RNA < 50 copies/mL on a stable ARV regimen for at least 6 months with no history of treatment failure and no known resistance to its components | Yes Notes: Crushing not recommended in product information, however study data shows no significant effect on pharmacokinetics when crushed and administered with food or drip feed | EVG: CYP3A (major), UGT1A1/3 (minor) | 1 tablet (EVG 150/COBI 150/FTC 200/TAF 10 mg) once daily PO with food | 1 | 19 × 8.5 | |
EVG 150 mg COBI 150 mg FTC 200 mg TDF 300 mg | Stribild® | Oral FDC tablet | HIV-1 Treatment: Adult and pediatric patients 12 years of age and older weighing > 35 kg with no ARV treatment history or to replace current ARV regimen in those with HIV-1 RNA < 50 copies/mL on a stable ARV regimen for at least 6 months with no history of treatment failure and no known resistance to its components | Yes Notes: Crushing not recommended in product information, however study data shows no significant effect on pharmacokinetics when crushed and administered with food or with drip feed | 1 tablet (EVG 150/COBI 150/FTC 200/TDF 300 mg) once daily PO with food | 1 | 20 × 10 | ||
RAL 400 mg | Isentress® | Oral tablet: 400 mg Chewable tablet: 25 mg 100 mg this is a third available dosage form for this product | HIV-1 Treatment: Adults and pediatric patients weighing > 2 kg in combination with other antiretroviral agents | Yes Notes: Crushing not recommended in product information, however study data shows acceptable plasma concentrations; important to note that alternative dosage forms available that may ease administration. Pediatric 25 mg chewable tablets may be crushed if swallowing is difficult | RAL: UGT1A1 | Adults: 1 tablet (RAL 400 mg) twice daily PO with or without food Pediatric: Weight based dosing (refer to prescribing information) | 2 | 16 × 8.8 | [33] |
RAL HD 600 mg | Isentress HD® | Oral tablet: 600 mg | HIV-1 Treatment: Adults and pediatric patients weighing > 40 kg in combination with other antiretroviral agents | No | 2 tablets (RAL 600 mg × 2) once daily PO with or without food | 2 | 19 × 9.7 | [33] |