Drug intelligence / Profile preview

adefovir dipivoxil + didanosine + efavirenz + lamivudine

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination antiretroviral regimen** comprising four active pharmaceutical ingredients: adefovir dipivoxil (a prodrug of adefovir), didanosine, efavirenz, and lamivudine. All four drugs are reverse transcriptase inhibitors used primarily in the treatment of **HIV-1 infection**. - **Adefovir dipivoxil** is a nucleotide reverse transcriptase inhibitor (NtRTI) active primarily against hepatitis B virus but also has weak activity against HIV-1 by inhibiting viral reverse transcriptase and causing DNA chain termination. - **Didanosine** is a nucleoside reverse transcriptase inhibitor (NRTI) converted intracellularly to its active form, dideoxyadenosine triphosphate, which inhibits **HIV reverse transcriptase** and causes chain termination[1][3][5][7][9]. - **Lamivudine** is another NRTI that inhibits HIV-1 reverse transcriptase via incorporation into viral DNA, leading to chain termination. - **Efavirenz** is a non-nucleoside reverse transcriptase inhibitor (NNRTI), which binds to and allosterically inhibits HIV-1 reverse transcriptase, disrupting viral replication[2][4][6]. The combination disrupts HIV replication at multiple points of the reverse transcriptase enzyme pathway, reducing viral load and slowing immunosuppression and disease progression. These agents are taken orally and require combination with other antiretrovirals for maximal efficacy and to reduce the emergence of resistance.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseHBV Pol (Hepatitis B virus polymerase)

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