Drug intelligence / Profile preview

tenofovir disoproxil fumarate + zidovudine + lamivudine + lopinavir + ritonavir

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

Overview

The drug combination "tenofovir disoproxil fumarate + zidovudine + lamivudine + lopinavir + ritonavir" is a multi-drug antiretroviral regimen used in the treatment of HIV infection. This combination includes nucleoside reverse transcriptase inhibitors (tenofovir disoproxil fumarate, zidovudine, and lamivudine) along with protease inhibitors (lopinavir and ritonavir). ## Mechanism of Action This combination works through multiple mechanisms to suppress HIV replication: - **Nucleoside Reverse Transcriptase Inhibitors (NRTIs)**: Tenofovir disoproxil fumarate, zidovudine, and lamivudine all inhibit HIV reverse transcriptase, preventing viral RNA from being converted to DNA. - **Protease Inhibitors**: Lopinavir and ritonavir block HIV protease, an enzyme necessary for the production of functional viral proteins. Ritonavir also serves as a pharmacokinetic enhancer for lopinavir by inhibiting its metabolism. This multi-drug approach targets different stages of the HIV life cycle, providing a more comprehensive antiviral effect and reducing the risk of viral resistance. ## Administration While the search results don't specifically mention this exact five-drug combination as a single formulation, the individual components are frequently used in various HIV treatment regimens. The medications are typically taken orally, with specific dosing based on patient factors including weight, renal function, and potential drug interactions. ## Important Considerations - **Renal Function**: Tenofovir disoproxil fumarate requires dose adjustment or may be contraindicated in patients with impaired renal function. - **Drug Interactions**: This combination has numerous potential drug interactions due to the ritonavir component, which is a potent inhibitor of cytochrome P450 enzymes. - **Monitoring**: Patients on this regimen should be monitored for renal function, liver function, and potential side effects specific to each medication. - **Not a Cure**: While effective at suppressing viral replication, this combination does not cure HIV infection or prevent transmission to others.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseHIV-2 PR (HIV-2 protease)HIV-2 reverse transcriptasePR (Progesterone receptor)

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