Drug intelligence / Profile preview

nelfinavir + antiretroviral therapy

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Nelfinavir + antiretroviral therapy** refers to the combined use of nelfinavir, a small molecule HIV-protease inhibitor, together with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection. Nelfinavir acts as a competitive inhibitor of HIV-1 protease by reversibly binding to the enzyme’s active site, blocking cleavage of the gag-pol polyprotein, and preventing maturation of infective HIV particles, thereby reducing viral load[4][6][1][7][3]. The combination is used to slow disease progression and lower the risk of AIDS-related and opportunistic infections, though it is not curative[1][3][7]. Nelfinavir was developed by Agouron Pharmaceuticals and is marketed under the brand name Viracept, principally by Pfizer[5]. In clinical practice, nelfinavir is always administered alongside other antiretroviral drugs such as nucleoside reverse transcriptase inhibitors (e.g., zidovudine, lamivudine) or other combination regimens[5]. Its mechanism further includes inducing lipid bilayer stress and disruption of mitochondrial respiration, drug efflux transport (ABCB1), and broad cellular metabolic rewiring[2].

Other names
nelfinavir mesylate
02

Targets

ABCB1 (P-glycoprotein)ADIPOR2 (Adiponectin receptor 2)PR (Progesterone receptor)

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