Version May 2024
Hepatotoxicity has been reported with use of maraviroc. Severe rash or evidence of a systemic allergic reaction (eg, eosinophilia, elevated immunoglobulin E [IgE], fever) prior to the development of hepatotoxicity may occur. Patients with signs or symptoms of hepatitis or allergic reaction following use of maraviroc should be immediately evaluated.
HIV-1 infection, treatment: Note: Only recommended for patients with CCR5-tropic HIV-1; prior to therapy, conduct tropism assay to exclude presence of CXCR4-tropic or mixed/dual tropic HIV (maraviroc should not be used).
Oral: 300 mg twice daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥30 mL/minute: No dosage adjustment necessary.
CrCl <30 mL/minute:
Concomitant potent CYP3A inhibitors (with or without a CYP3A inducer) or concomitant potent and moderate CYP3A inducers (without a potent CYP3A inhibitor): Use is contraindicated.
Other concomitant medications (eg, tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, enfuvirtide, dolutegravir, and other medications that are not potent CYP3A inhibitors or inducers): No dosage adjustment necessary, unless postural hypotension occurs; then, reduce dose to 150 mg twice daily.
End-stage renal disease requiring intermittent hemodialysis (IHD): Note: Hemodialysis has minimal effect on clearance.
Concomitant potent CYP3A inhibitors (with or without a CYP3A inducer) or concomitant potent and moderate CYP3A inducers (without a potent CYP3A inhibitor): Use is contraindicated.
Other concomitant medications (eg, tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, enfuvirtide, dolutegravir, and other medications that are not potent CYP3A inhibitors or inducers): No dosage adjustment necessary, unless postural hypotension occurs; then, reduce dose to 150 mg twice daily.
Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer's labeling; however, maraviroc concentrations are increased in mild to moderate impairment; use caution.
Moderate impairment (with concomitant potent CYP3A inhibitor): There are no dosage adjustments provided in the manufacturer's labeling; however, maraviroc concentrations are increased in moderate impairment; use caution and monitor closely for adverse events.
Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
(For additional information see "Maraviroc: Pediatric drug information")
HIV-1 infection, treatment: Note: Only recommended for patients with CCR5-tropic HIV-1; prior to therapy, conduct tropism assay to exclude presence of CXCR4-tropic or mixed/dual tropic HIV (maraviroc should not be used). Gene mutation and antiretroviral resistance patterns should be evaluated (refer to https://www.iasusa.org/ for more information) when necessary.
Infants, Children, and Adolescents: Oral:
2 to <4 kg: Oral solution: 30 mg twice daily.
4 to <6 kg: Oral solution: 40 mg twice daily.
6 to <10 kg: Oral solution: 100 mg twice daily.
10 to <14 kg: Oral solution, tablet: 150 mg twice daily.
14 to <30 kg: Oral solution, tablet: 200 mg twice daily.
≥30 kg: Oral solution, tablet: 300 mg twice daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Infants, Children, and Adolescents weighing ≥2 kg:
Mild or moderate impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied in pediatric patients with kidney impairment).
Severe impairment and receiving potent CYP3A inhibitors: Use is contraindicated.
End-stage renal disease (ESRD) on intermittent hemodialysis and receiving potent CYP3A inhibitors: Use is contraindicated.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied in pediatric patients with any degree of hepatic impairment); however, maraviroc serum concentrations are increased in hepatic impairment; use with caution; monitor closely for adverse events.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Includes data from both treatment-naive and treatment-experienced patients. Unless otherwise noted, frequency of adverse events is as reported in adults receiving combination antiretroviral therapy.
>10%:
Dermatologic: Skin rash (11%)
Gastrointestinal: Vomiting (children and adolescents: 12%; may be more common with oral solution)
Infection: Infection (55%)
Respiratory: Bronchitis (7% to 13%), cough (14%), upper respiratory tract infection (23% to 32%)
Miscellaneous: Fever (13%)
1% to 10%:
Cardiovascular: Acute myocardial infarction (<2%), cardiac failure (<2%), cerebrovascular accident (<2%), coronary artery disease (<2%), coronary occlusion (<2%), endocarditis (<2%), hypertension (3%), ischemic heart disease (<2%), portal vein thrombosis (<2%), septic shock (<2%), unstable angina pectoris (<2%)
Dermatologic: Acne vulgaris (3%), alopecia (2%), condyloma acuminatum (2%), erythema of skin (2%), folliculitis (4%), nail disease (6%; nail and nail bed disorder [excluding infection and infestation]), pruritus (4%), sweat gland disease (apocrine and eccrine gland disorders: 5%), tinea (4%)
Endocrine & metabolic: Lipodystrophy (3% to 4%)
Gastrointestinal: Abdominal distension (≤10%), abdominal pain (children and adolescents: 4%; may be more common with oral solution), bloating (≤10%), carcinoma in situ of esophagus (<2%), change in appetite (8%), Clostridioides difficile colitis (<2%), constipation (6%; may be more common with oral solution), decreased gastrointestinal motility (9%), diarrhea (children and adolescents: 4%; may be more common with oral solution), flatulence (≤10%), increased serum amylase (4%), nausea (children and adolescents: 4%; may be more common with oral solution)
Genitourinary: Ejaculatory disorder (≤3%), erectile dysfunction (≤3%), urinary tract abnormality (bladder/urethral/urinary signs and symptoms: ≤5%)
Hematologic & oncologic: Anemia (8%), basal cell carcinoma of skin (<2%), benign skin neoplasm (3%), bone marrow depression (<2%), carcinoma (nasopharyngeal: <2%), cutaneous squamous cell carcinoma in situ (<2%), hypoplastic anemia (<2%), liver metastases (<2%), malignant lymphoma (including diffuse large B-cell and anaplastic large cell lymphomas T- and null-cell types: <2%), malignant neoplasm (anal: <2%), malignant neoplasm of the bile duct (cholangiocarcinoma: <2%), malignant neoplasm of tongue (<2%; malignant stage unspecified), neoplasm (<2%; includes abdominal and unspecified malignant endocrine neoplasm), neutropenia (4% to 6%), squamous cell carcinoma (<2%), squamous cell carcinoma of skin (<2%)
Hepatic: Cholestatic jaundice (<2%), hepatic cirrhosis (<2%), hepatic failure (<2%), increased serum alanine aminotransferase (>5 x ULN: 4%), increased serum aspartate aminotransferase (>5 x ULN: 4% to 5%), increased serum bilirubin (>2.5 x ULN: 6%), jaundice (<2%)
Infection: Bacterial infection (6%; including treponema), herpes virus infection (7% to 8%), herpes zoster infection (≤5%), influenza (2%), meningococcal infection (3%), varicella zoster infection (≤5%), viral infection (3%)
Nervous system: Abnormal sensory symptoms (3% to 4%; includes body temperature perception disorder), anxiety (4%), depression (4%), dizziness (≤9%), dysesthesia (≤5%), epilepsy (<2%), facial nerve paralysis (<2%), impaired consciousness (4%), insomnia (8%), loss of consciousness (<2%), malaise (≤4%), memory impairment (3%), meningitis (<2%, including viral), orthostatic dizziness (≤9%), paresthesia (≤5%), peripheral neuropathy (4%), pain (≤4%), seizure (<2%)
Neuromuscular & skeletal: Arthropathy (6% to 7%), myalgia (3%), myositis (infective: <2%), increased creatine phosphokinase in blood specimen (4%), osteonecrosis (<2%), rhabdomyolysis (<2%), tremor (<2%; excluding congenital)
Ophthalmic: Conjunctivitis (2%), eye infection (≤2%), hemianopia (<2%), ophthalmic inflammation (≤2%), visual field defect (<2%)
Otic: Ear disease (3%), otitis media (2%)
Respiratory: Irregular breathing (4%), lower respiratory tract infection (≤3%), nasal congestion (≤4%), paranasal sinus disease (3%), pneumonia (<2%), pulmonary infection (≤3%), rhinitis (≤4%), sinusitis (7%), upper respiratory system symptoms (6% to 9%)
Frequency not defined:
Hepatic: Hepatitis, hepatotoxicity
Hypersensitivity: Hypersensitivity reaction
Immunologic: Immune reconstitution syndrome
Postmarketing:
Dermatologic: Stevens-Johnson syndrome, toxic epidermal necrolysis
Immunologic: Drug rash with eosinophilia and systemic symptoms
Patients with severe renal impairment (CrCl <30 mL/minute) or end-stage renal disease (ESRD) who are taking concomitant potent CYP3A inhibitors or inducers
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to maraviroc or any component of the formulation
Concerns related to adverse effects:
• CNS effects: May cause dizziness. If this occurs, patients should avoid driving or operating machinery.
• Hepatotoxicity: [US Boxed Warning]: Possible drug-induced hepatotoxicity with allergic type features has been reported; hepatotoxicity may be preceded by severe rash or other signs of systemic allergic reactions (eg, pruritic rash, eosinophilia, fever, increased IgE) and/or hepatic adverse events (transaminase increases or signs/symptoms of hepatitis); some cases have been life-threatening; immediately evaluate patients with signs and symptoms of allergic reaction or hepatitis (with or without allergy symptoms). Use with caution in patients with pre-existing hepatic dysfunction or coinfection with HBV and/or HCV, however symptoms have occurred in the absence of pre-existing hepatic conditions. Monitor hepatic function at baseline and as clinically indicated during treatment. Consider discontinuation in any patient with possible hepatitis or with elevated transaminases combined with systemic allergic events. Rechallenge with maraviroc is not recommended (HHS [pediatric] 2019).
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
• Infections: Monitor closely for signs/symptoms of developing infections; use associated with a small increase of certain upper respiratory tract infections and herpes virus infections during clinical trials.
• Malignancy: May affect immune surveillance and lead to an increased risk of malignancy due to pharmacologic mechanism of action. No increase in malignancy has been observed. Long term follow up needed to assess this risk.
• Postural hypotension: Symptomatic postural hypotension has occurred; use caution in patients at risk due to concomitant medication or history of condition. An increased risk of postural hypotension may occur in patients with severe renal insufficiency or in those with ESRD. Patients with severe renal dysfunction or ESRD who experience postural hypotension should have dose reduced.
• Skin and hypersensitivity reactions: Severe and life-threatening skin and hypersensitivity reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis and drug rash with eosinophilia with systemic symptoms (DRESS), have been reported with use, predominately in patients also receiving concomitant agents associated with these reactions. Rash and constitutional findings (eg, fever, muscle aches, conjunctivitis, oral lesions), with or without organ dysfunction (including hepatic failure), have also accompanied these reports. Discontinue maraviroc and any other suspected agent immediately if symptoms or signs of hypersensitivity occur. Monitor liver function tests and clinical status as appropriate.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease, or in patients with a history of or current cardiac risk factors for postural hypotension, or receiving concomitant medication known to lower blood pressure. Patients who have cardiovascular comorbidities could be at risk for cardiac adverse events prompted by postural hypotension. During trials, a small increase in cardiovascular events (myocardial ischemia and/or infarction) occurred in treated patients compared to placebo, although a contributory relationship relative to therapy is unknown. Of note, patients experiencing events generally had cardiac disease/risk factors prior to therapy.
• Hepatic impairment: Use caution in patients with HBV and/or HCV coinfection or with mild-to-moderate hepatic impairment; maraviroc concentrations are increased. Maraviroc concentrations are further increased in patients with moderate hepatic impairment receiving concomitant potent CYP3A inhibitors; monitor closely for adverse events. Use in patients with severe hepatic impairment has not been studied.
• Renal impairment: Renal impairment may increase maraviroc concentrations. Use with caution in patients with mild-to-moderate renal impairment. An increased risk of postural hypotension may occur in patients with severe renal impairment or in those with ESRD. Patients with severe renal dysfunction or ESRD who experience postural hypotension should have dose reduced. Use in patients with severe renal impairment or ESRD who are receiving potent CYP3A inhibitors or potent and moderate CYP3A inducers is contraindicated.
Dosage form specific issues:
• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol and/or sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggest that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol and/or benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.
Other warnings/precautions:
• Appropriate use: Prior to therapy, coreceptor tropism testing should be performed for presence of CCR5-tropic only virus HIV-1 infection. Therapy not recommended for use in patients with CXCR4- or dual/mixed tropic HIV-1 infection; efficacy not demonstrated in this population. In studies with treatment-naive patients, virologic failure and emergent lamivudine resistance was more common in maraviroc-treated patients compared to patients receiving efavirenz.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Oral:
Selzentry: 20 mg/mL (230 mL [DSC]) [contains sodium benzoate; strawberry flavor]
Selzentry: 20 mg/mL (230 mL) [latex free; contains sodium benzoate; strawberry flavor]
Tablet, Oral:
Selzentry: 25 mg [DSC], 75 mg [DSC], 150 mg, 300 mg [contains fd&c blue #2 (indigo carm) aluminum lake, soybean lecithin]
Generic: 150 mg, 300 mg
May be product dependent
Solution (Selzentry Oral)
20 mg/mL (per mL): $4.61
Tablets (Maraviroc Oral)
150 mg (per each): $29.39
300 mg (per each): $29.39
Tablets (Selzentry Oral)
150 mg (per each): $34.60
300 mg (per each): $34.60
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Celsentri: 150 mg, 300 mg [contains fd&c blue #2 (indigo carm) aluminum lake, soybean lecithin]
Oral: Administer without regards to meals. Stable immunologic parameters and virologic suppression have been reported following administration of crushed tablets (Ref). However, an oral solution is commercially available.
Oral: May administer without regards to meals.
An FDA-approved patient medication guide, which is available with the product information and at https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022128s019,208984s002lbl.pdf#page=43, must be dispensed with this medication.
HIV-1 infection: Treatment of only CCR5-tropic HIV-1 infection in adult and pediatric patients weighing ≥2 kg, in combination with other antiretroviral agents.
Substrate of CYP3A4 (major), OATP1B1/1B3 (SLCO1B1/1B3), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Betibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Betibeglogene Autotemcel. Risk X: Avoid combination
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Maraviroc. Management: Increase maraviroc adult dose to 600 mg twice/day, but only if not receiving a strong CYP3A4 inhibitor. Not recommended for pediatric patients not also receiving a strong CYP3A4 inhibitor. Contraindicated in patients with CrCl less than 30 mL/min. Risk D: Consider therapy modification
CYP3A4 Inducers (Strong): May decrease the serum concentration of Maraviroc. Management: Increase maraviroc adult dose to 600 mg twice/day, but only if not receiving a strong CYP3A4 inhibitor. Not recommended for pediatric patients not also receiving a strong CYP3A4 inhibitor. Contraindicated in patients with CrCl less than 30 mL/min. Risk D: Consider therapy modification
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Maraviroc. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Maraviroc. Management: Reduce maraviroc to 150mg twice/day in adult and pediatrics weighing 40kg or more. See full interaction monograph for dose adjustments in pediatrics weighing 10 to less than 40kg. Do not use if CrCl less than 30mL/min or in those weighing less than 10 kg. Risk D: Consider therapy modification
Elivaldogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Elivaldogene Autotemcel. Management: Avoid use of antiretroviral medications for at least one month, or for the amount of time required for elimination of the retroviral medication, prior to stem cell mobilization and until the all apheresis cycles are finished Risk X: Avoid combination
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Lovotibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Lovotibeglogene Autotemcel. Risk X: Avoid combination
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy
St John's Wort: May decrease the serum concentration of Maraviroc. Risk X: Avoid combination
Contraception is not required to initiate or continue antiretroviral therapy (ART).
The Health and Human Services perinatal HIV guidelines do not recommend maraviroc (except in special circumstances) for patients with HIV who are not yet pregnant but are trying to conceive.
Maximum viral suppression sustained below the limits of detection prior to conception is recommended for all persons with HIV who are planning a pregnancy. Optimization of the health of the person who will become pregnant is recommended. Selection of or changes to a specific antiretroviral regimen prior to pregnancy should be done as part of a shared decision-making process. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Health care providers caring for couples planning a pregnancy when one or both partners are diagnosed with HIV may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal 2023]).
Maraviroc has moderate transfer across the human placenta.
Data collected by the antiretroviral pregnancy registry are insufficient to evaluate human teratogenic risk. Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm birth, low birth weight, and small for gestational age infants. Actual risks may be influenced by maternal factors, such as disease severity, gestational age at initiation of therapy, and specific ART regimen; therefore, close fetal monitoring is recommended. Because there is clear benefit to appropriate treatment, maternal ART should not be withheld due to concerns for adverse neonatal outcomes. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children not diagnosed with HIV but who were exposed to ART in utero or as a neonate and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential metabolic dysfunction.
The Health and Human Services perinatal HIV guidelines do not recommend maraviroc for pregnant patients with HIV who are antiretroviral naive; maraviroc is not recommended (except in special circumstances) in pregnant patients who have had ART therapy in the past but are restarting, or who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen). Patients who become pregnant while taking maraviroc may continue if viral suppression is effective and the regimen is well tolerated. Standard adult doses can be used during pregnancy.
ART is recommended for all pregnant people with HIV to maximize their health, maintain the viral load below the limit of detection, and reduce the risk of perinatal transmission. Selection of or changes to a specific antiretroviral regimen during pregnancy should be done as part of a shared decision-making process. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitoring of patients who are pregnant is more frequent than in patients who are not pregnant. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Health care providers should enroll all patients exposed to antiretroviral medications during pregnancy in the Antiretroviral Pregnancy Registry (1-800-258-4263). Enrollment should be done as early in pregnancy as possible.
Health care providers caring for pregnant patients with HIV and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).
It is not known if maraviroc is present in breast milk.
Maintaining maximum viral suppression during pregnancy and postpartum decreases but does not eliminate the risk of HIV transmission via breast milk. In addition, multiclass-resistant virus has been detected in breastfeeding infants who acquire HIV despite maternal therapy. In the United States, where formula is usually accessible, affordable, safe, and sustainable, and the risk of infant mortality due to diarrhea and respiratory infections is low, the Health and Human Services perinatal HIV guidelines do not recommend breastfeeding for patients with HIV when safer infant feeding options are available. Persons with HIV who maintain an undetectable viral load while taking antiretroviral therapy (ART) should evaluate infant feeding options (formula, banked donor milk, or breastfeeding) as part of a shared decision-making process (if breastfeeding is being considered, see guidelines for measures to reduce the risk of HIV transmission). When the HIV status at delivery is not known, breast milk may be expressed and stored until a negative test is available. If HIV infection is diagnosed after breastfeeding has been initiated, breastfeeding should be discontinued immediately. Breastfeeding is not recommended for persons with HIV who are not taking ART and/or who do not have sustained viral suppression.
Information is available for counseling and managing patients with HIV who are considering breastfeeding (1-888-448-8765). In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth (HHS [perinatal] 2023).
Viral load, CD4 count, transaminases and bilirubin (prior to initiation and periodically during treatment); signs/symptoms of infection, rash, severe skin reactions, hepatitis and/or allergic reaction; postural hypotension; tropism testing (prior to initiation)
Maraviroc, a CCR5 antagonist, selectively and reversibly binds to the chemokine (C-C motif receptor 5 [CCR5]) coreceptors located on human CD4 cells. CCR5 antagonism prevents interaction between the human CCR5 coreceptor and the gp120 subunit of the viral envelope glycoprotein, thereby inhibiting gp120 conformational change required for CCR5-tropic HIV-1 fusion with the CD4 cell and subsequent cell entry.
Note: Maraviroc pharmacokinetic parameters in pediatric patients were similar to those observed in adults.
Distribution: Vd: ~194 L.
Protein binding: ~76%.
Metabolism: Hepatic, via CYP3A to inactive metabolites.
Bioavailability: 23% to 33% (maraviroc is a substrate for the efflux transporter P-gp).
Half-life elimination: 14 to 18 hours.
Time to peak, plasma: 0.5 to 4 hours.
Excretion: Urine (~20%, 8% as unchanged drug); feces (76%, 25% as unchanged drug).
Altered kidney function: In a single 300 mg dose study in patients with severe renal impairment (CrCl <30 mL/minute) and ESRD, Cmax and AUC were 2.4- and 3.2-fold higher, respectively, for patients with severe renal impairment, and 1.7- and 2-fold higher, respectively, for ESRD patients.
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