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saquinavir + zidovudine + zalcitabine

Development stage
Discontinued
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is a **triple combination antiretroviral regimen** for HIV infection, composed of saquinavir (a protease inhibitor), zidovudine (a nucleoside reverse transcriptase inhibitor, NRTI), and zalcitabine (another NRTI). - **Saquinavir** inhibits HIV-1 protease, preventing cleavage of Gag-Pol polyproteins, thereby inhibiting viral maturation. - **Zidovudine** and **zalcitabine** are converted intracellularly to their active triphosphate forms, which inhibit HIV reverse transcriptase by acting both as competitive inhibitors and as chain terminators of viral DNA synthesis. Clinical trials showed this triple regimen **reduced HIV-1 replication, increased CD4+ counts,** and lowered immune activation markers more than two-drug regimens. The combination generally uses the oral forms of all three drugs. The regimen has historical significance but is no longer commonly used since zalcitabine's withdrawal and due to advances in more potent, safer therapies[1][2][3][5].

Brand names
Invirase + Retrovir + HividFortovase + Retrovir + Hivid
Other names
saquinavir + AZT + ddCsaquinavir + ZDV + ddC
02

Targets

Human immunodeficiency virus type 1 reverse transcriptasePR (Progesterone receptor)

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