"The U.S. Food and Drug Administration today approved Tivicay (dolutegravir), a new drug to treat HIV-1 infection.
Tivicay is an integrase strand transfer inhibitor that interferes with one of the enzymes necessary for HIV to multiply. "...
This indication is based on analyses of plasma HIV-1 RNA levels in 2 controlled trials of SELZENTRY in treatment-experienced subjects and one trial in treatment-naive subjects. Both trials in treatment-experienced subjects were conducted in clinically advanced, 3-class antiretroviral-experienced (nucleoside reverse transcriptase inhibitor [NRTI], non-nucleoside reverse transcriptase inhibitor [NNRTI], protease inhibitor [PI], or enfuvirtide) adults with evidence of HIV-1 replication despite ongoing antiretroviral therapy.
The following points should be considered when initiating therapy with SELZENTRY:
- Adult patients infected with only CCR5-tropic HIV-1 should use SELZENTRY.
- Tropism testing must be conducted on a current sample with a highly sensitive tropism assay that has demonstrated the ability to identify patients appropriate for use of SELZENTRY. Outgrowth of pre-existing low-level CXCR4-or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on SELZENTRY [see Microbiology, Clinical Studies].
- Use of SELZENTRY is not recommended in subjects with dual/mixed-or CXCR4-tropic HIV-1 as efficacy was not demonstrated in a Phase 2 trial of this patient group.
- The safety and efficacy of SELZENTRY have not been established in pediatric patients.
- In treatment-naive subjects, more subjects treated with SELZENTRY experienced virologic failure and developed lamivudine resistance compared with efavirenz [see Microbiology, Clinical Studies].
DOSAGE AND ADMINISTRATION
Dose Recommendations For Patients With Normal Renal Function
The recommended dose of SELZENTRY differs based on concomitant medications due to drug interactions (see Table 1). SELZENTRY can be taken with or without food. SELZENTRY must be given in combination with other antiretroviral medications.
Table 1 gives the recommended dose adjustments [see DRUG INTERACTIONS].
Table 1: Recommended Dosing Regimen
|Concomitant Medications||Dose of SELZENTRY|
|Potent CYP3A inhibitors (with or without a potent CYP3A inducer) including:
||150 mg twice daily|
|Other concomitant medications, including tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, and enfuvirtide||300 mg twice daily|
|Potent CYP3A inducers (without a potent CYP3A inhibitor) including:
||600 mg twice daily|
Dose Recommendations For Patients With Renal Impairment
Table 2 provides dosing recommendations for patients based on renal function and concomitant medications.
Table 2: Recommended Dosing
Regimens Based on Renal Function
|Concomitant Medicationsa||Dose of SELZENTRY Based on Renal Function|
|Normal (CrCl > 80 mL/min)||Mild (CrCl > 50 and ≤ 80 mL/min)||Moderate (CrCl ≥ 30 and ≤ 50 mL/min)||Severe (CrCl < 30 mL/min)||End-Stage Renal Disease On Regular Hemodialysis|
|Potent CYP3A inhibitors (with or without a CYP3A inducer)a||150 mg twice daily||150 mg twice daily||150 mg twice daily||NR||NR|
|Other concomitant medicationsa||300 mg twice daily||300 mg twice daily||300 mg twice daily||300 mg twice dailyb||300 mg twice dailyb|
|Potent CYP3A Inducers (without a potent CYP3A inhibitor)a||600 mg twice daily||600 mg twice daily||600 mg twice daily||NR||NR|
|NR = Not recommended.
aSee Table 1 for the list of concomitant medications.
bThe dose of SELZENTRY should be reduced to 150 mg twice daily if there are any symptoms of postural hypotension [see WARNINGS AND PRECAUTIONS].
Dosage Forms And Strengths
- 150-mg blue, oval, film-coated tablets debossed with “MVC 150” on one side and plain on the other.
- 300-mg blue, oval, film-coated tablets debossed with “MVC 300” on one side and plain on the other.
Storage And Handling
SELZENTRY film-coated tablets are available as follows: 150-and 300-mg tablets are blue, biconvex, oval, film-coated tablets debossed with “MVC 150” or “MVC 300” on one side and plain on the other.
Bottle packs 150-mg tablets: 60 tablets (NDC 49702-223-18).
Bottle packs 300-mg tablets: 60 tablets (NDC 49702-224-18).
SELZENTRY film-coated tablets should be stored at 25°C (77°F); excursions permitted between 15°C and 30°C (59°F-86°F) [see USP Controlled Room Temperature].
Manufactured for: Healthcare Research Triangle Park, NC 27709. by: Pfizer Manufacturing Deutschland GmbH Freiburg, Germany. March 2014
Last reviewed on RxList: 4/11/2014
This monograph has been modified to include the generic and brand name in many instances.
Additional Selzentry Information
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
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