Drug intelligence / Profile preview

emivirine + didanosine + stavudine + delavirdine mesylate + hydroxyurea

Development stage
Discontinued
Lead developer
Mitsubishi Tanabe Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is an **investigational combination regimen** containing five agents: emivirine, didanosine, stavudine, delavirdine mesylate, and hydroxyurea. These were all studied as part of multi-drug antiretroviral therapy for HIV infection. - **Didanosine** and **stavudine** are nucleoside reverse transcriptase inhibitors (NRTIs) that work by inhibiting HIV reverse transcriptase. - **Delavirdine mesylate** is a non-nucleoside reverse transcriptase inhibitor (NNRTI) targeting the same enzyme via a different binding site. - **Emivirine** is an experimental NNRTI. - **Hydroxyurea** is a ribonucleotide reductase inhibitor that by decreasing deoxynucleotide pools can potentiate NRTI activity. This combination was aimed at achieving greater suppression of HIV replication by using multiple mechanisms of action. However, studies of similar regimens (not always including all five agents) showed increased antiviral activity but also increased toxicity, particularly neuropathy, hepatotoxicity, pancreatitis, and myelosuppression[1][2][3][5][9]. No approved product or unique brand/canonical combination exists for all five together, and emivirine is not an approved antiretroviral therapy.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseRNR (Ribonucleotide reductase)

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