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	Maraviroc is a CCR5 co-receptor antagonist (entry inhibitor) used in combination with other antiretrovirals for ~~'''~~CCR5-tropic HIV-1 only~~'''~~. It is unique among antiretrovirals in targeting a host cell receptor rather than a viral enzyme. A [[HIV - AIDS (main)\|tropism assay]] is required before use.<ref name="SelzentryPI">Selzentry (maraviroc) [prescribing information]. Research Triangle Park, NC: ViiV Healthcare; 2020.</ref>		Maraviroc is a CCR5 co-receptor antagonist (entry inhibitor) used in combination with other antiretrovirals for CCR5-tropic HIV-1 only. It is unique among antiretrovirals in targeting a host cell receptor rather than a viral enzyme. A [[HIV - AIDS (main)\|tropism assay]] is required before use.<ref name="SelzentryPI">Selzentry (maraviroc) [prescribing information]. Research Triangle Park, NC: ViiV Healthcare; 2020.</ref>

	==Administration==		==Administration==
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	==Adult Dosing==		==Adult Dosing==
	Dose depends entirely on concomitant CYP3A medications:<ref name="SelzentryPI"/>		Dose depends entirely on concomitant CYP3A medications:<ref name="SelzentryPI"/>
	*~~'''~~With strong CYP3A inhibitors~~'''~~ (e.g., ritonavir-boosted PIs, ketoconazole): ~~'''~~150 mg PO BID~~'''~~		*With strong CYP3A inhibitors (e.g., ritonavir-boosted PIs, ketoconazole): 150 mg PO BID
	*~~'''~~With strong CYP3A inducers~~'''~~ (e.g., rifampin, carbamazepine, phenytoin, efavirenz): ~~'''~~600 mg PO BID~~'''~~		*With strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, efavirenz): 600 mg PO BID
	*~~'''~~Without strong CYP3A inhibitors or inducers~~'''~~ (e.g., tipranavir/ritonavir, raltegravir, NRTIs): ~~'''~~300 mg PO BID~~'''~~		*Without strong CYP3A inhibitors or inducers (e.g., tipranavir/ritonavir, raltegravir, NRTIs): 300 mg PO BID
	*May take with or without food		*May take with or without food

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	*Adult:<ref name="SelzentryPI"/>		*Adult:<ref name="SelzentryPI"/>
	**Mild to moderate (Child-Pugh A or B): No dose adjustment; monitor closely if moderate impairment + CYP3A inhibitor		**Mild to moderate (Child-Pugh A or B): No dose adjustment; monitor closely if moderate impairment + CYP3A inhibitor
	**Severe (Child-Pugh C): Not studied; ~~'''~~not recommended~~'''~~		**Severe (Child-Pugh C): Not studied; not recommended
	*Pediatric: Not studied		*Pediatric: Not studied

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	==Pharmacology==		==Pharmacology==
	*Half-life: ~14–18 hours<ref name="Abel2009">Abel S, et al. Maraviroc: pharmacokinetics and drug interactions. ''Antivir Ther''. 2009;14(5):607-618.</ref>		*Half-life: ~14–18 hours<ref name="Abel2009">Abel S, et al. Maraviroc: pharmacokinetics and drug interactions. ''Antivir Ther''. 2009;14(5):607-618.</ref>
	*Metabolism: CYP3A4 (primary); also a P-gp substrate. Does ~~'''~~not~~'''~~ inhibit major CYP450 enzymes at therapeutic doses<ref name="Abel2009"/>		*Metabolism: CYP3A4 (primary); also a P-gp substrate. Does not inhibit major CYP450 enzymes at therapeutic doses<ref name="Abel2009"/>
	*Excretion: ~76% feces, ~20% urine<ref name="Abel2009"/>		*Excretion: ~76% feces, ~20% urine<ref name="Abel2009"/>

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	==Comments==		==Comments==
	*Not a first-line ARV; used in treatment-experienced patients with confirmed R5-tropic virus		*Not a first-line ARV; used in treatment-experienced patients with confirmed R5-tropic virus
	*~~'''~~ED hepatotoxicity recognition:~~'''~~ New rash + eosinophilia + liver enzyme elevation → suspect DILI, hold drug, check hepatic panel, consult [[HIV - AIDS (main)\|HIV/ID]]<ref name="LiverTox"/>		*ED hepatotoxicity recognition: New rash + eosinophilia + liver enzyme elevation → suspect DILI, hold drug, check hepatic panel, consult [[HIV - AIDS (main)\|HIV/ID]]<ref name="LiverTox"/>
	*~~'''~~Postural hypotension~~'''~~ may be symptomatic in renal impairment or on CYP3A inhibitors — manage with IV fluids and supine positioning		*Postural hypotension may be symptomatic in renal impairment or on CYP3A inhibitors — manage with IV fluids and supine positioning
	*Maraviroc does not significantly affect levels of other drugs, making it lower risk for interactions when prescribing in the ED<ref name="Abel2009"/>		*Maraviroc does not significantly affect levels of other drugs, making it lower risk for interactions when prescribing in the ED<ref name="Abel2009"/>
	*Overdose: Supportive care; no specific antidote; unlikely removed by dialysis<ref name="SelzentryPI"/>		*Overdose: Supportive care; no specific antidote; unlikely removed by dialysis<ref name="SelzentryPI"/>

Ostermayer: Created page with "Maraviroc is a CCR5 co-receptor antagonist (entry inhibitor) used in combination with other antiretrovirals for '''CCR5-tropic HIV-1 only'''. It is unique among antiretrovirals in targeting a host cell receptor rather than a viral enzyme. A tropism assay is required before use.Selzentry (maraviroc) [prescribing information]. Research Triangle Park, NC: ViiV Healthcare; 2020. ==Administration== *Type: CCR5 co-receptor a..."

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Created page with "Maraviroc is a CCR5 co-receptor antagonist (entry inhibitor) used in combination with other antiretrovirals for '''CCR5-tropic HIV-1 only'''. It is unique among antiretrovirals in targeting a host cell receptor rather than a viral enzyme. A tropism assay is required before use.<ref name="SelzentryPI">Selzentry (maraviroc) [prescribing information]. Research Triangle Park, NC: ViiV Healthcare; 2020.</ref> ==Administration== *Type: CCR5 co-receptor a..."

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Maraviroc is a CCR5 co-receptor antagonist (entry inhibitor) used in combination with other antiretrovirals for '''CCR5-tropic HIV-1 only'''. It is unique among antiretrovirals in targeting a host cell receptor rather than a viral enzyme. A [[HIV - AIDS (main)|tropism assay]] is required before use.<ref name="SelzentryPI">Selzentry (maraviroc) [prescribing information]. Research Triangle Park, NC: ViiV Healthcare; 2020.</ref>

==Administration==
*Type: CCR5 co-receptor antagonist (entry inhibitor)
*Dosage Forms: 25 mg, 75 mg, 150 mg, 300 mg tablets; 20 mg/mL oral solution
*Routes of Administration: Oral
*Common Trade Names: Selzentry (US), Celsentri (EU)

==Adult Dosing==
Dose depends entirely on concomitant CYP3A medications:<ref name="SelzentryPI"/>
*'''With strong CYP3A inhibitors''' (e.g., ritonavir-boosted PIs, ketoconazole): '''150 mg PO BID'''
*'''With strong CYP3A inducers''' (e.g., rifampin, carbamazepine, phenytoin, efavirenz): '''600 mg PO BID'''
*'''Without strong CYP3A inhibitors or inducers''' (e.g., tipranavir/ritonavir, raltegravir, NRTIs): '''300 mg PO BID'''
*May take with or without food

==Pediatric Dosing==
*Approved for patients ≥2 kg; weight-based dosing adjusted for CYP3A interactions<ref name="SelzentryPI"/>
*Consult pediatric ID or prescribing information for weight-based tables

==Special Populations==
===[[Drug pregnancy categories|Pregnancy Rating]]===
*Formerly Category B; no adequate controlled studies in pregnant women<ref name="SelzentryPI"/>
*Animal studies showed no teratogenicity; standard dose appears appropriate in pregnancy<ref name="Colbers2015">Colbers A, et al. Maraviroc pharmacokinetics in HIV-1-infected pregnant women. ''Clin Infect Dis''. 2015;61(10):1582-1589.</ref>

===Lactation risk===
*Secreted into rat milk; unknown in human milk. Women with HIV should not breastfeed (risk of HIV transmission)<ref name="SelzentryPI"/>

===Renal Dosing===
*Adult:<ref name="SelzentryPI"/>
**CrCl ≥30 mL/min: No adjustment needed
**CrCl <30 mL/min or ESRD: '''Contraindicated''' if on potent CYP3A inhibitors or inducers; otherwise no adjustment but reduce to 150 mg BID if postural hypotension occurs
**Hemodialysis has minimal effect on clearance
*Pediatric: Insufficient data

===Hepatic Dosing===
*Adult:<ref name="SelzentryPI"/>
**Mild to moderate (Child-Pugh A or B): No dose adjustment; monitor closely if moderate impairment + CYP3A inhibitor
**Severe (Child-Pugh C): Not studied; '''not recommended'''
*Pediatric: Not studied

==Contraindications==
*Allergy to class/drug
*CXCR4-tropic or dual/mixed-tropic HIV-1 (ineffective)<ref name="SelzentryPI"/>
*Severe renal impairment (CrCl <30 mL/min) or ESRD when coadministered with potent CYP3A inhibitors or inducers<ref name="SelzentryPI"/>

==Adverse Reactions==
===Serious===
*'''Hepatotoxicity''' (Boxed Warning) — may be preceded by rash, fever, eosinophilia, or elevated IgE; discontinue immediately if suspected<ref name="LiverTox">Maraviroc. ''LiverTox''. NCBI Bookshelf. Updated 2019.</ref>
*DRESS syndrome, [[Stevens-Johnson syndrome]], [[toxic epidermal necrolysis]]
*[[Immune reconstitution syndrome|Immune reconstitution inflammatory syndrome (IRIS)]]
*Postural hypotension (dose-limiting; increased risk with renal impairment or CYP3A inhibitors)
*Myocardial ischemia/infarction (reported; causal relationship not established)

===Common===
*Upper respiratory tract infections, cough
*Fever, rash, dizziness
*Abdominal pain, nausea, diarrhea
*Transaminase elevations (~10%, usually mild and asymptomatic)<ref name="LiverTox"/>

==Pharmacology==
*Half-life: ~14–18 hours<ref name="Abel2009">Abel S, et al. Maraviroc: pharmacokinetics and drug interactions. ''Antivir Ther''. 2009;14(5):607-618.</ref>
*Metabolism: CYP3A4 (primary); also a P-gp substrate. Does '''not''' inhibit major CYP450 enzymes at therapeutic doses<ref name="Abel2009"/>
*Excretion: ~76% feces, ~20% urine<ref name="Abel2009"/>

==Mechanism of Action==
Maraviroc is a selective allosteric antagonist of CCR5, a chemokine co-receptor on CD4+ T cells required for entry of R5-tropic HIV-1. It binds within the transmembrane domain of CCR5, altering the extracellular conformation so that viral gp120 cannot recognize the receptor, blocking viral-host membrane fusion and cell entry.<ref name="Dorr2005">Dorr P, et al. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5. ''Antimicrob Agents Chemother''. 2005;49(11):4721-4732.</ref> It has no activity against CXCR4-tropic virus. Resistance occurs primarily through outgrowth of pre-existing CXCR4-using viral populations or gp120 V3 loop mutations.<ref name="SelzentryPI"/>

==Comments==
*Not a first-line ARV; used in treatment-experienced patients with confirmed R5-tropic virus
*'''ED hepatotoxicity recognition:''' New rash + eosinophilia + liver enzyme elevation → suspect DILI, hold drug, check hepatic panel, consult [[HIV - AIDS (main)|HIV/ID]]<ref name="LiverTox"/>
*'''Postural hypotension''' may be symptomatic in renal impairment or on CYP3A inhibitors — manage with IV fluids and supine positioning
*Maraviroc does not significantly affect levels of other drugs, making it lower risk for interactions when prescribing in the ED<ref name="Abel2009"/>
*Overdose: Supportive care; no specific antidote; unlikely removed by dialysis<ref name="SelzentryPI"/>
*Avoid St. John's wort (decreases maraviroc levels)<ref name="SelzentryPI"/>

==See Also==
*[[HIV - AIDS (main)]]
*[[HIV post-exposure prophylaxis]]
*[[Immune reconstitution syndrome]]
*[[Emtricitabine/tenofovir]]

==References==
{{reflist|2}}
[[Category:Pharmacology]]

Maraviroc - Revision history

Danbot: Strip excess bold