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Maraviroc – HIV Drug & CCR5 Antagonist

Maraviroc is an antiretroviral medication used to treat HIV-1 infection. It blocks the entry of the virus into human immune cells and is used specifically against CCR5-tropic HIV-1.

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Things worth knowing about "Maraviroc"

Maraviroc is an antiretroviral medication used to treat HIV-1 infection. It blocks the entry of the virus into human immune cells and is used specifically against CCR5-tropic HIV-1.

What is Maraviroc?

Maraviroc is an antiretroviral drug belonging to the class of CCR5 antagonists, also known as entry inhibitors or coreceptor antagonists. It is used in the treatment of infection with Human Immunodeficiency Virus type 1 (HIV-1). In the European Union, the drug is marketed under the brand name Celsentri, and in the United States under Selzentry. It is used as part of a combined antiretroviral therapy (cART) regimen and was the first CCR5 antagonist to receive global regulatory approval.

Mechanism of Action

Maraviroc works by selectively binding to the CCR5 coreceptor found on the surface of human CD4-positive T cells (immune cells). HIV-1 requires two binding points to enter a cell: the CD4 receptor and a coreceptor – either CCR5 or CXCR4. By binding to CCR5, maraviroc alters its conformation, preventing the virus from attaching to the cell and thus blocking viral entry before infection can occur.

Because maraviroc is only effective against CCR5-tropic HIV-1, a tropism test must be performed prior to initiating therapy to confirm that the patient harbors CCR5-tropic virus and not CXCR4-tropic or dual/mixed-tropic virus, which would not respond to treatment.

Indications and Use

Maraviroc is indicated for:

Adults and children (from a body weight of 2 kg) with confirmed CCR5-tropic HIV-1 infection
Treatment-experienced patients who have had prior antiretroviral therapy failure
In selected cases, treatment-naive patients (without prior antiretroviral treatment)

It must always be used in combination with other antiretroviral agents and is never used as monotherapy.

Dosage

The standard adult dose is 300 mg twice daily orally. However, the dose may vary depending on concomitant medications, as maraviroc is a substrate of the CYP3A4 enzyme and is subject to significant drug interactions:

When combined with strong CYP3A4 inhibitors (e.g., protease inhibitors): dose reduction to 150 mg twice daily
When combined with strong CYP3A4 inducers (e.g., efavirenz): dose increase to 600 mg twice daily

Pediatric dosing is calculated individually based on body weight and concomitant medications.

Side Effects

Maraviroc is generally well tolerated. Commonly reported side effects include:

Increased susceptibility to respiratory tract infections
Nausea and abdominal pain
Dizziness and headache
Fatigue and weakness
Skin rash

Less common but clinically important side effects include:

Hepatotoxicity (liver damage), particularly in patients with pre-existing liver disease or co-infection with hepatitis B or C
Orthostatic hypotension (a drop in blood pressure upon standing)
Rarely, severe allergic or hypersensitivity reactions

Contraindications and Drug Interactions

Maraviroc is contraindicated in patients with CXCR4-tropic or dual/mixed-tropic HIV-1. Caution is required in patients with:

Severe renal impairment when combined with strong CYP3A4 inhibitors
Pre-existing liver damage or hepatic impairment
Concurrent use of St. John's Wort (Hypericum perforatum), which can significantly reduce the effectiveness of maraviroc

Due to the range of potential drug interactions, therapy with maraviroc should always be supervised by a physician experienced in HIV treatment.

Clinical Significance

Maraviroc represented a major milestone in HIV therapy as the world's first approved CCR5 antagonist. Unlike older antiretroviral drug classes that interfere with the viral replication cycle inside the cell, maraviroc prevents viral entry into the host cell entirely. This novel mechanism of action makes it particularly valuable for patients who have developed resistance to other antiretroviral medications, offering a new therapeutic option when conventional regimens have failed.

References

European Medicines Agency (EMA): Celsentri (Maraviroc) – Product Information and EPAR. Available at: https://www.ema.europa.eu
Panel on Antiretroviral Guidelines for Adults and Adolescents, U.S. Department of Health and Human Services: Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV (2023). Available at: https://clinicalinfo.hiv.gov
Dorr P et al.: Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity. Antimicrobial Agents and Chemotherapy, 2005; 49(11): 4721–4732.

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