Enfuvirtide (T-20; Fuzeon Trimeris/Roche), the first in a new class of HIV drugs known as fusion inhibitors, has received accelerated approval from the FDA for use with other antiretrovirals in adults and children with viral replication despite ongoing antiretroviral therapy. This review describes the mechanism of action and pharmacokinetics of the new drug, and outlines the results of the 2 clinical studies that led to its approval. Sections on adverse effects, development of resistance, and dosage and cost are also included. The review concludes with an overall assessment of the...

Bortezomib (PS341; Velcade Millenium), the first proteasome inhibitor, has received accelerated approval from the FDA for treatment of refractory multiple myeloma. This review includes descriptions of the mechanism of action, pharmacokinetics, adverse effects, and dosage and cost of bortezomib, outlines the results of clinical studies, and concludes with an overall assessment of the drug's effectiveness.

Acetaminophen (paracetamol; Tylenol, and others) taken in overdosage can cause severe hepatic injury and death. Acetaminophen poisoning is treated with (N-)acetylcysteine. Available for many years in the US as a solution for inhalation therapy (Mucomyst, and others), it subsequently became available for oral use and was recently marketed in the US for intravenous (IV) use as Acetadote (Cumberland).

Nelarabine (Arranon - GlaxoSmithKline), a prodrug of the deoxyguanosine analog 9-β-D-arabinofuranosylguanine (ara-G), has been approved by the FDA for treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL) that has not responded to, or has relapsed following, treatment with at least two chemotherapy regimens.

An extended-release formulation of the centrally-acting muscle relaxant cyclobenzaprine (Amrix - Cephalon) has been approved by the FDA for treatment of muscle spasms. Immediate-release (IR) cyclobenzaprine (Flexeril, and others) has been available since 1977.

Sapropterin (Kuvan - BioMarin) has been approved by the FDA to reduce phenylalanine plasma concentrations in patients with phenylketonuria (PKU). PKU is a rare genetic disorder (it occurs in 1 in 8000 Caucasian and 1 in 50,000 African-American newborns) caused by a deficiency of phenylalanine hydroxylase (PAH) the resulting high levels of the amino acid in blood and urine lead to cognitive, behavioral and other neurological complications.

Linagliptin (Tradjenta – Boehringer Ingelheim/Lilly), a third oral dipeptidyl peptidase-4 (DPP-4) enzyme inhibitor, was recently approved by the FDA for treatment of type 2 diabetes, either alone or in combination with metformin, a sulfonylurea or pioglitazone

The FDA has approved a fixed-dose combination of the integrase strand transfer inhibitor (INSTI) elvitegravir, the pharmacokinetic enhancer cobicistat, and the nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) emtricitabine and tenofovir disoproxil fumarate (Stribild – Gilead) for treatment of HIV-1 infection in antiretroviral treament-naïve adults. Elvitegravir is the second INSTI to be approved by the FDA for use in HIV treatment; raltegravir (Isentress) was the first.

The FDA has approved two new oral kinase inhibitors for treatment of unresectable or metastatic melanoma: dabrafenib (Tafinlar – GSK) for melanomas with BRAF V600E mutations and trametinib (Mekinist – GSK) for melanomas with either BRAF V600E or V600K mutations. Dabrafenib is not recommended for patients with wild-type BRAF (BRAF-negative) melanoma, and trametinib is not recommended for patients who have received prior BRAF-inhibitor therapy.

The FDA has approved vortioxetine (vor" tye ox' e teen; Trintellix – Takeda/Lundbeck), a new serotonergic drug, for treatment of major depressive disorder. Like vilazodone (Viibryd), another serotonergic antidepressant, it has been claimed to have a low incidence of sexual side effects and no significant effect on weight.