Drug Detail:Selzentry (Maraviroc [ ma-rav-i-rok ])
Generic Name: MARAVIROC 25mg
Dosage Form: tablet, film coated
Drug Class: Chemokine receptor antagonist
Testing prior to Initiation of SELZENTRY
Prior to initiation of SELZENTRY for treatment of HIV-1 infection, test all patients for CCR5 tropism using a highly sensitive tropism assay. SELZENTRY is recommended for patients with only CCR5-tropic HIV-1 infection. 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 (12.4), Clinical Studies (14.1)].
Monitor patients for alanine aminotransferase (ALT), aspartate aminotransferase (AST), and bilirubin prior to initiation of SELZENTRY and at other time points during treatment as clinically indicated [see Warnings and Precautions (5.1)].
General Dosing Recommendations
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- SELZENTRY tablets and oral solution are taken twice daily by mouth and may be taken with or without food.
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- SELZENTRY must be given in combination with other antiretroviral medications.
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- The recommended dosage of SELZENTRY differs based on concomitant medications due to drug interactions.
Recommended Dosage in Adult Patients with Normal Renal Function
Table 1 displays oral dosage of SELZENTRY based on different concomitant medications [see Drug Interactions (7.1)].
| Concomitant Medications | Dosage of SELZENTRY |
|---|---|
| a Potent CYP3A inhibitors (with or without a potent CYP3A inducer) including: clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir/ritonavir), telithromycin. b Noninteracting concomitant medications include all medications that are not potent CYP3A inhibitors or inducers such as: dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir/ritonavir. c Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) including: carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin. |
|
|
Potent cytochrome P450 (CYP)3A inhibitors (with or without a potent CYP3A inducer)a |
150 mg twice daily |
|
Noninteracting concomitant medicationsb |
300 mg twice daily |
|
Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)c |
600 mg twice daily |
Recommended Dosage in Pediatric Patients with Normal Renal Function
The recommended dosage of SELZENTRY should be based on body weight (kg) and should not exceed the recommended adult dose. The recommended dosage also differs based on concomitant medications due to drug interactions (Table 2 and Table 3) [see Drug Interactions (7.1), Use in Specific Populations (8.4)].
Before prescribing SELZENTRY tablets, assess children for the ability to swallow tablets. If a child is unable to reliably swallow SELZENTRY tablets, the oral solution formulation should be prescribed.
The recommended oral dosage of SELZENTRY tablets in pediatric patients aged 2 years and older weighing at least 10 kg is presented in Table 2.
| a Potent CYP3A inhibitors (with or without a CYP3A inducer) including: clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir/ritonavir), telithromycin. b Noninteracting concomitant medications including all medications that are not potent CYP3A inhibitors or inducers such as: dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir. c Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) including: carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin. d Insufficient data are available to recommend use. |
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|
Concomitant Medications |
Dosage of SELZENTRY Based on Weight |
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|
10 kg to <14 kg |
14 kg to <20 kg |
20 kg to <30 kg |
30 kg to <40 kg |
≥40 kg |
|
|
Potent CYP3A inhibitors (with or without a CYP3A inducer)a |
50 mg |
50 mg |
75 mg |
100 mg |
150 mg |
|
Noninteracting concomitant medicationsb |
150 mg twice daily |
200 mg |
200 mg |
300 mg |
300 mg |
|
Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)c |
Not recommendedd |
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The recommended oral dosage of SELZENTRY oral solution in pediatric patients weighing at least 2 kg is presented in Table 3.
| a Potent CYP3A inhibitors (with or without a CYP3A inducer) including: clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir/ritonavir), telithromycin. b Insufficient data are available to recommend use. c Noninteracting concomitant medications including all medications that are not potent CYP3A inhibitors or inducers such as: dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir. d Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) including: carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin. |
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Concomitant Medications |
Dosage (Volume of Solution) of SELZENTRY |
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|
2 kg to |
4 kg to |
6 kg to <10 kg |
10 kg to <14 kg |
14 kg to <20 kg |
20 kg to <30 kg |
30 kg to <40 kg |
≥40 kg |
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|
Potent CYP3A inhibitors (with or without a CYP3A inducer)a |
Not recommendedb |
50 mg |
50 mg |
80 mg |
100 mg |
150 mg |
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|
Noninteracting concomitant medicationsc |
30 mg |
40 mg |
100 mg |
150 mg |
200 mg |
200 mg |
300 mg |
300 mg |
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|
Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)d |
Not recommendedb |
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Administer the oral solution using the included press-in bottle adapter and the appropriate oral dosing syringe: for doses of 2.5 mL or less, use the 3-mL syringe; for doses greater than 2.5 mL, use the 10-mL syringe.
Care should be taken when measuring neonate doses due to the small volumes of oral solution required.
Recommended Dosage in Patients with Renal Impairment
Adult Patients
Table 4 provides dosing recommendations for patients based on renal function and concomitant medications.
| CrCl = Creatinine clearance. a Potent CYP3A inhibitors (with or without a CYP3A inducer) including: clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir/ritonavir), telithromycin. b Noninteracting concomitant medications include all medications that are not potent CYP3A inhibitors or inducers such as: dolutegravir, enfuvirtide, nevirapine, all NRTIs, raltegravir, and tipranavir/ritonavir. c Dosage of SELZENTRY should be reduced to 150 mg twice daily if there are any symptoms of postural hypotension [see Contraindications (4), Warnings and Precautions (5.3)]. d Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) including: carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin. |
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|
Concomitant Medications |
Dosage of SELZENTRY Based on Renal Function |
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|
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 |
Contra-indicated |
Contra-indicated |
|
Noninteracting concomitant medicationsb |
300 mg twice daily |
300 mg twice daily |
300 mg twice daily |
300 mg twice daily |
300 mg twice dailyc |
|
Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)d |
600 mg twice daily |
600 mg twice daily |
600 mg twice daily |
Contra-indicated |
Contra-indicated |
Pediatric Patients
There are no data to recommend specific doses of SELZENTRY in pediatric patients with mild or moderate renal impairment [see Use in Specific Populations (8.6)]. Additionally, SELZENTRY is contraindicated for pediatric patients with severe renal impairment or end-stage renal disease (ESRD) on regular hemodialysis who are receiving potent CYP3A inhibitors or inducers [see Contraindications (4)].
