Delavirdine

226-228 °C

226 - 228 °C

Serum aminotransferase elevations occur in 25% or more of patients on delavirdine therapy, but rise above 5 times the upper limit of normal in 4% or less; this rate is higher in patients who have chronic hepatitis C coinfection. Clinically apparent hepatotoxicity due to delavirdine must be rare, as individual case reports of hepatitis or jaundice have not been published. Nevertheless, cases of hepatitis, jaundice and hepatic failure have been reported to the sponsor and are mentioned in the product label. The liver injury may be immunoallergic and similar in pattern to that attributed to nevirapine and efavirenz. In immunoallergic hepatitis due to nonnucleoside reverse transcriptase inhibitors, injury usually arises within 1 to 8 weeks of starting therapy. Signs of hypersensitivity are common including rash, fever, and eosinophilia and sometimes facial edema, lymphadenoapthy and lymphocytosis. The serum enzyme pattern can be cholestatic, hepatocellular or mixed. Recovery is rapid upon stopping therapy.

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

delavirdine

DILI Negative

Oral

DOI:10.1016/j.drudis.2019.09.022

J - Antiinfectives for systemic use

QJ - Antiinfectives for systemic use

Delavirdine is a non-nucleoside reverse transcriptase inhibitor (nNRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Delavirdine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of Delavirdine does not compete with template or nucleoside triphosphates. HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases alpha, beta, or sigma) are not inhibited by Delavirdine.

Hepatic

Delavirdine has known human metabolites that include N-Desisopropyl delavirdine and N-[2-[4-[6-oxo-3-(propan-2-ylamino)-1H-pyridin-2-yl]piperazine-1-carbonyl]-1H-indol-5-yl]methanesulfonamide.

DOL5F9JD3E

DELAVIRDINE

Established Pharmacologic Class [EPC] - Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor

Non-Nucleoside Analog [EXT]

Mechanisms of Action [MoA] - Non-Nucleoside Reverse Transcriptase Inhibitors

Delavirdine is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of delavirdine is as a Non-Nucleoside Reverse Transcriptase Inhibitor.