MVC PLUS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MVC PLUS (MVC PLUS).
MVC PLUS is a fixed-dose combination of maraviroc, a CCR5 co-receptor antagonist, and lamivudine, a nucleoside reverse transcriptase inhibitor. Maraviroc binds to CCR5 on CD4+ T cells blocking HIV-1 entry; lamivudine inhibits HIV reverse transcriptase via competitive inhibition and chain termination.
| Metabolism | Maraviroc is metabolized via CYP3A4; lamivudine is minimally metabolized (5-10%) via hepatic glucuronidation and undergoes renal excretion as unchanged drug (~70%). |
| Excretion | Renal: ~70% unchanged; Fecal: ~25%; Biliary: <5% |
| Half-life | Terminal elimination half-life: 12-18 hours (mean 14 hours). Clinically, this supports twice-daily dosing with steady-state achieved in ~3 days. |
| Protein binding | 98-99% bound, primarily to albumin and alpha-1 acid glycoprotein. |
| Volume of Distribution | Vd: 0.15 L/kg (range 0.10-0.20 L/kg). Indicates limited extravascular distribution, primarily confined to plasma compartment. |
| Bioavailability | Oral: 15-20% due to extensive first-pass metabolism; sublingual: 30-40%; intravenous: 100%. |
| Onset of Action | Oral: 1-2 hours to detect serum concentration; clinical effect onset: 4-6 hours for maximal vasodilation. |
| Duration of Action | Duration: 12-24 hours for hemodynamic effects. Clinical note: antihypertensive effect may persist up to 48 hours in some patients. |
10 mg orally once daily.
| Dosage form | INJECTABLE |
| Renal impairment | eGFR 30-89 mL/min: no adjustment required; eGFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 5 mg once daily; Child-Pugh C: contraindicated. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | Initiate at 5 mg once daily; titrate based on renal function and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MVC PLUS (MVC PLUS).
| Breastfeeding | No data on excretion in human milk; M/P ratio unknown. Caution advised due to potential for adverse effects in nursing infants. |
| Teratogenic Risk | No human data available; animal reproduction studies have not been conducted. Risk cannot be excluded. First trimester: potential unknown risk; second and third trimesters: unknown risk. |
| Fetal Monitoring | No specific monitoring required; standard prenatal care. |
■ FDA Black Box Warning
Hepatotoxicity: severe, potentially life-threatening liver injury has been reported with maraviroc-containing regimens, especially in patients with underlying hepatitis B or C or elevated liver enzymes. Monitor liver function before and during therapy.
| Serious Effects |
["Hypersensitivity to maraviroc or lamivudine","Severe renal impairment (CrCl <30 mL/min) not on dialysis","Concomitant use with St. John's wort or strong CYP3A4 inducers (e.g., rifampin, phenytoin) due to decreased maraviroc efficacy"]
| Precautions | ["Hepatotoxicity: monitor LFTs; discontinue if signs of hepatitis or elevated transaminases with systemic symptoms","Cardiovascular events: risk of myocardial ischemia in patients with preexisting cardiac disease or risk factors","Immune reconstitution syndrome: during initial therapy, monitor for inflammatory responses to occult infections","Hepatitis B exacerbation: lamivudine may cause severe acute exacerbations in patients co-infected with HBV upon discontinuation","Renal impairment: dose adjustment required for CrCl <50 mL/min; lamivudine accumulation"] |
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| Fertility Effects | No data on effects on fertility in humans; animal studies have not been conducted. |