Active Ingredient History
Maraviroc (UK-427,857; brand-named Selzentry, or Celsentri outside the U.S) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. Maraviroc is the product of a medicinal chemistry effort initiated following identification of an imidazopyridine CCR5 ligand from a high-throughput screen of the Pfizer compound file. Selzentry, in combination with other antiretroviral agents, is indicated for adult patients infected with only CCR5-tropic HIV-1. This indication is based on analyses of plasma HIV-1 RNA levels in two controlled trials of SELZENTRY in treatment-experienced subjects and one trial in treatment-naive subjects. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc. Antiviral Activity in Cell Culture Maraviroc inhibits the replication of CCR5-tropic laboratory strains and primary isolates of HIV-1 in models of acute peripheral blood leukocyte infection. The mean EC50 value (50% effective concentration) for maraviroc against HIV-1 group M isolates (subtypes A to J and circulating recombinant form AE) and group O isolates ranged from 0.1 to 4.5 nM (0.05 to 2.3 ng per mL) in cell culture. When used with other antiretroviral agents in cell culture, the combination of maraviroc was not antagonistic with NNRTIs (delavirdine, efavirenz, and nevirapine), NRTIs (abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, zalcitabine, and zidovudine), or protease inhibitors (amprenavir, atazanavir, darunavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, and tipranavir). Maraviroc was not antagonistic with the HIV fusion inhibitor enfuvirtide. Maraviroc was not active against CXCR4-tropic and dual-tropic viruses (EC50 value greater than 10 µM). The antiviral activity of maraviroc against HIV-2 has not been evaluated. Maraviroc can cause serious, life-threatening side effects such as, liver problems, skin reactions, and allergic reactions. NCATS
Drug Pricing (per unit)
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| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Acquired Immunodeficiency Syndrome (Phase 4)
AIDS Dementia Complex (Phase 2/Phase 3)
Arthritis, Rheumatoid (Phase 2)
Atherosclerosis (Phase 4)
Cardiovascular Diseases (Phase 3)
CCR5 Receptor Antagonists (Phase 4)
Cognition Disorders (Phase 4)
Colorectal Neoplasms (Phase 1)
COVID-19 (Phase 2)
Cytochrome P-450 CYP3A (Phase 1)
Depression (Phase 2)
Endothelial Cells (Phase 4)
Graft vs Host Disease (Phase 2)
Healthy Volunteers (Phase 4)
Heart Disease Risk Factors (Phase 4)
Hematologic Neoplasms (Phase 2)
Hematopoietic Stem Cell Transplantation (Phase 2)
Hepatitis B (Phase 4)
Hepatitis C (Phase 4)
Hepatitis C, Chronic (Phase 4)
HIV (Phase 4)
HIV-1 (Phase 3)
Hodgkin Disease (Phase 2)
Hypertriglyceridemia (Phase 1)
Inflammation (Phase 4)
Infusions, Intravenous (Phase 2)
Kidney Diseases (Phase 2)
Kidney Transplantation (Phase 4)
Leukemia, Lymphocytic, Chronic, B-Cell (Phase 2)
Leukemia, Myeloid, Acute (Phase 2)
Lymphoma, B-Cell (Phase 2)
Lymphoma, Follicular (Phase 2)
Lymphoma, Large B-Cell, Diffuse (Phase 2)
Mycobacterium (Phase 1)
Myelodysplastic Syndromes (Phase 2)
Pancreatic Neoplasms (Phase 1)
Pharmacokinetics (Phase 1)
Proteinuria (Phase 4)
Steatitis (Phase 2/Phase 3)
Stroke (Phase 2/Phase 3)
Virus Diseases (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
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