Maraviroc

FDA label, ViiV Healthcare Company, oral, effective 2022-09-26. Full label on DailyMed

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Quoted from the FDA label. Product labels differ by manufacturer and change over time; confirm against the label for the product you are using.

Boxed warning

WARNING: HEPATOTOXICITY Hepatotoxicity has been reported with use of SELZENTRY. Severe rash or evidence of a systemic allergic reaction (e.g., fever, eosinophilia, or elevated IgE) prior to the development of hepatotoxicity may occur. Patients with signs or symptoms of hepatitis or allergic reaction following use of SELZENTRY should be evaluated immediately [see Warnings and Precautions ( 5.1 )] . WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. • Hepatotoxicity has been reported which may be preceded by severe rash or other features of a systemic allergic reaction (e.g., fever, eosinophilia, or elevated IgE).

( 5.1 ) • Immediately evaluate patients with signs or symptoms of hepatitis or allergic reaction. ( 5.1 )

CCR5 Co-receptor Antagonist

Dosing in kidney impairment

Recommended Dosage in Adult Patients with Normal Renal Function Table 1 displays oral dosage of SELZENTRY based on different concomitant medications [see Drug Interactions] . [See table below.]

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, Use in Specific Populations] .

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 . [See table below.] The recommended oral dosage of SELZENTRY oral solution in pediatric patients weighing at least 2 kg is presented in Table 3 . [See table below.] 50 mg (2.5 mL) twice daily 50 mg (2.5 mL) twice daily 80 mg (4 mL) twice daily 100 mg (5 mL) twice daily 150 mg (7.5 mL) twice daily Noninteracting concomitant medications c 30 mg (1.5 mL) twice daily 40 mg (2 mL) twice daily 100 mg (5 mL) twice daily 150 mg (7.5 mL) twice daily 200 mg (10 mL) twice daily 200 mg (10 mL) twice daily 300 mg (15 mL) twice daily 300 mg (15 mL) twice daily Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) d Not recommended b 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. [See table below.] Contra-indicated Noninteracting concomitant medications b 300 mg twice daily 300 mg twice daily 300 mg twice daily 300 mg twice daily 300 mg twice daily c 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] .

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] .

Table 4. Recommended Dosage in Adults Based on Renal Function
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.
Concomitant Medications	Dosage of SELZENTRY Based on Renal Function
Concomitant Medications	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 medications^b	300 mg twice daily	300 mg twice daily	300 mg twice daily	300 mg twice daily	300 mg twice daily^c
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

Dosing in liver impairment

Hepatic Impairment Maraviroc is principally metabolized by the liver; therefore, when administering this drug to patients with hepatic impairment, maraviroc concentrations may be increased. Maraviroc concentrations are higher when SELZENTRY 150 mg is administered with a potent CYP3A inhibitor compared with following administration of 300 mg without a CYP3A inhibitor, so patients with moderate hepatic impairment who receive SELZENTRY 150 mg with a potent CYP3A inhibitor should be monitored closely for maraviroc-associated adverse events.

Maraviroc has not been studied in subjects with severe hepatic impairment or in pediatric patients with any degree of hepatic impairment [see Warnings and Precautions, Clinical Pharmacology] .

Preparation and administration

SELZENTRY tablets and oral solution are taken twice daily by mouth and may be taken with or without food. SELZENTRY must be given in combination with other antiretroviral medications. Recommended Dosage in Adult Patients: [See table below.] A more complete list of coadministered drugs is listed in Dosage and Administration .

SELZENTRY tablets and oral solution are taken twice daily by mouth and may be taken with or without food. The recommended dosage also differs based on concomitant medications due to drug interactions ( Table 2 and Table 3 ) [see Drug Interactions, Use in Specific Populations] . 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 . [See table below.] The recommended oral dosage of SELZENTRY oral solution in pediatric patients weighing at least 2 kg is presented in Table 3 . [See table below.] 50 mg (2.5 mL) twice daily 50 mg (2.5 mL) twice daily 80 mg (4 mL) twice daily 100 mg (5 mL) twice daily 150 mg (7.5 mL) twice daily Noninteracting concomitant medications c 30 mg (1.5 mL) twice daily 40 mg (2 mL) twice daily 100 mg (5 mL) twice daily 150 mg (7.5 mL) twice daily 200 mg (10 mL) twice daily 200 mg (10 mL) twice daily 300 mg (15 mL) twice daily 300 mg (15 mL) twice daily Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) d Not recommended b 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.

Table 3. Recommended Dosage in Pediatric Patients Weighing at Least 2 kg (Oral Solution)
^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.
Concomitant Medications	Dosage (Volume of Solution) of SELZENTRY Based on Weight
Concomitant Medications	2 kg to <4 kg	4 kg to <6 kg	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
Potent CYP3A inhibitors (with or without a CYP3A inducer)^a	Not recommended^b			50 mg (2.5 mL) twice daily	50 mg (2.5 mL) twice daily	80 mg (4 mL) twice daily	100 mg (5 mL) twice daily	150 mg (7.5 mL) twice daily
Noninteracting concomitant medications^c	30 mg (1.5 mL) twice daily	40 mg (2 mL) twice daily	100 mg (5 mL) twice daily	150 mg (7.5 mL) twice daily	200 mg (10 mL) twice daily	200 mg (10 mL) twice daily	300 mg (15 mL) twice daily	300 mg (15 mL) twice daily
Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)^d	Not recommended^b

Drug interactions

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Label text (3 paragraphs)

7 DRUG INTERACTIONS • Coadministration with CYP3A inhibitors, including protease inhibitors (except tipranavir/ritonavir), will increase the concentration of SELZENTRY. ( 7.1 ) • Coadministration with CYP3A inducers, including efavirenz, may decrease the concentration of SELZENTRY. ( 7.1 ) • Coadministration with St. John’s wort is not recommended. ( 7.1 )

7.1 Effect of Concomitant Drugs on the Pharmacokinetics of Maraviroc Maraviroc is metabolized by CYP3A and is also a substrate for P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP)1B1, and multidrug resistance-associated protein (MRP)2. The pharmacokinetics of maraviroc are likely to be modulated by inhibitors and inducers of CYP3A and P-gp and may be modulated by inhibitors of OATP1B1 and MRP2. Therefore, a dosage adjustment may be required when maraviroc is coadministered with those drugs [see Dosage and Administration ( 2.3 , 2.4 )] . Concomitant use of maraviroc and St. John's wort ( Hypericum perforatum ) or products containing St. John's wort is not recommended.

Coadministration of maraviroc with St. John's wort is expected to substantially decrease maraviroc concentrations and may result in suboptimal levels of maraviroc and lead to loss of virologic response and possible resistance to maraviroc. Additional drug interaction information is available [see Clinical Pharmacology ( 12.3 )] .

Contraindications

4 CONTRAINDICATIONS SELZENTRY is contraindicated in patients with severe renal impairment or ESRD (creatinine clearance [CrCl] less than 30 mL per minute) who are concomitantly taking potent CYP3A inhibitors or inducers [see Warnings and Precautions ( 5.3 )]. SELZENTRY is contraindicated in patients with severe renal impairment or end-stage renal disease (ESRD) (creatinine clearance [CrCl] less than 30 mL per minute) who are concomitantly taking potent CYP3A inhibitors or inducers. ( 4 )

Pregnancy and lactation

Pregnancy

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to SELZENTRY during pregnancy. Physicians are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Limited data on the use of SELZENTRY during pregnancy from the APR and case reports are not sufficient to inform a drug-associated risk of birth defects and miscarriage. In animal reproduction studies, no evidence of adverse developmental outcomes was observed with maraviroc.

During organogenesis in the rat and rabbit, systemic exposures (AUC) to maraviroc were approximately 20 times (rats) and 5 times (rabbits) the exposure in humans at the recommended 300-mg twice-daily dose. In the rat pre- and post-natal development study, maternal systemic exposure (AUC) to maraviroc was approximately 14 times the exposure in humans at the recommended 300-mg twice-daily dose (see Data). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S.

general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data: Maraviroc was administered orally to pregnant rats (up to 1,000 mg per kg per day) and rabbits (up to 75 mg per kg per day) on gestation Days 6 to 17 and 7 to 19, respectively. No adverse effects on embryo-fetal development were observed at these dose levels, resulting in exposures (AUC) approximately 20 times (rats) and 5 times (rabbits) higher than human exposures at the recommended daily dose.

In the rat pre- and post-natal development study, maraviroc was administered orally at up to 1,000 mg per kg per day on gestation Day 6 to lactation/post-partum Day 20, with development of the offspring (including fertility and reproductive performance) unaffected by maternal administration of maraviroc at an exposure (AUC) approximately 14 times higher than human exposure at the recommended daily dose.

For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.

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