Drug intelligence / Profile preview

zidovudine + lamivudine + delavirdine

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

Overview

**Zidovudine + lamivudine + delavirdine** is a combination regimen used in the treatment of HIV/AIDS. This drug regimen contains three active antiretroviral ingredients: zidovudine (a nucleoside reverse transcriptase inhibitor, NRTI), lamivudine (also an NRTI), and delavirdine (a non-nucleoside reverse transcriptase inhibitor, NNRTI). - **Mechanism of Action:** - *Zidovudine* and *lamivudine* competitively inhibit HIV-1 reverse transcriptase by acting as nucleoside analogs, leading to premature termination of viral DNA synthesis[1][5]. - *Delavirdine* binds directly to HIV-1 reverse transcriptase at a different site (non-nucleoside binding site), altering enzyme conformation and disrupting viral replication. The combination of two NRTIs and one NNRTI synergistically limits HIV viral replication, reduces the emergence of drug resistance, and decreases HIV viral load in patients. - **Indication:** Primary use is for the treatment of HIV-1 infection, generally in combination with other antiretrovirals. - **Route of administration:** Primarily oral. - **Common side effects:** headache, nausea, diarrhea, malaise, fatigue, fever, anemia, neutropenia, myopathy, hepatic toxicity[1][2][5]. Severe reactions include lactic acidosis and hepatomegaly with steatosis[4]. - **Note:** Fixed-dose combinations of zidovudine + lamivudine (Combivir) are marketed, while the addition of delavirdine would require separate administration as there is no known fixed-dose product for the three together.

Other names
zidovudine + lamivudine + delavirdine
02

Targets

Human immunodeficiency virus type 1 reverse transcriptase

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