Rescriptor: profile and news

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Other information

Indication
For the treatment of HIV-1 infection in combination with appropriate antiretroviral agents when therapy is warranted

Pharmacology
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.

Mechanism Of Action
Delavirdine binds directly to viral reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site.

Drug Category
Anti-HIV Agents; Nonnucleoside Reverse Transcriptase Inhibitors; ATC:J05AG02

Brand Names/Synonyms
BHAP-U 90152; Bhap Der; DLV; Delavirdine; Rescriptor; SPP

Dosage Forms
caplets

Absorption
rapidly absorbed

Interactions
Antiacid, clarithromycin, Didanosine, Fluconazole, Fluoxetine, Indanavir, Ketoconazole, Phenytoin, Phenobarbitol, carbamazepine, Rifabutin, Rifampin, Ritanovir, Saquinavir.

Chemical IUPAC Name
N-[2-[4-[3-(1-methylethylamino)pyridin-2-yl]piperazin-1-yl]carbonyl-1H-indol-5-yl]methanesulfonamide

Chemical Formula
C22H28N6O3S

Half Life
5.8 hours

Drug Type
Approved Drug

# Accession No
APRD00149

CAS Registry Number
136817-59-9