INTELENCE

What it is

INTELENCE is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1). INTELENCE (etravirine) is a substituted diarylpyrimidine (DAPY) derivative, with potent in vitro activity against wild-type HIV-1 as well as NNRTI-resistant HIV-1. INTELENCE etravirine is available as 100 mg and 200 mg tablets.

Approved indications —

Treatment of HIV-1 infection in antiretroviral treatment-experienced adults who have evidence of viral replication and resistance to non-nucleoside transcriptase inhibitors and other antiretroviral agents, in combination with other antiretroviral agents.

Dosing overview

INTELENCE must always be given in combination with other antiretroviral medicinal products. The recommended oral dose of INTELENCE is 200 mg (one 200 mg tablet or two 100 mg tablets) taken orally twice daily, following a meal. No dose adjustment is required in patients with mild or moderate hepatic impairment (Child-Pugh score A or B). No dose adjustment is required in patients with renal impairment.

Key safety warnings

Severe, potentially life-threatening, and fatal skin reactions have been reported with INTELENCE; Stevens-Johnson Syndrome and toxic epidermal necrolysis have been rarely (< 0.1%) reported. Hypersensitivity reactions including DRESS (Drug Rash with Eosinophilia and Systemic Symptoms) have also been reported and were characterised by rash, constitutional findings, and infrequently organ dysfunction, including hepatic failure. Discontinue INTELENCE immediately if signs or symptoms of severe skin reactions or hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, eosinophilia). Rash most frequently occurred in the second week of therapy and was infrequent after week 4. Rash was mostly self-limiting and generally resolved within 1 to 2 weeks on continued therapy. The incidence of rash was higher in females. Combination antiretroviral therapy has been associated with redistribution of body fat (lipodystrophy) in HIV infected patients. The long-term consequences of these events are currently unknown. Knowledge about the mechanism is incomplete. A connection between visceral lipomatosis and PIs and lipoatrophy and NRTIs has been hypothesised. In HIV infected patients with severe immune deficiency at the time of institution of CART, an inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise and cause serious clinical conditions, or aggravation of symptoms. Typically, such reactions have been observed within the first weeks or months of initiation of CART. Relevant examples are cytomegalovirus retinitis, generalised and/or focal mycobacterial infections, and Pneumocystis jiroveci pneumonia.

Contraindications

Hypersensitivity to etravirine or to any of the excipients.

PBS listing

INTELENCE 200 mg tablet is listed on the PBS with streamlined restriction at an ex-manufacturer price of A$389.53.

Regulatory history

INTELENCE etravirine 100 mg and 200 mg tablets were registered on the Australian Register of Therapeutic Goods (ARTG) on 19 December 2008 and 22 August 2011 respectively.