They enabled milestone discoveries in pharmacology and biochemistry ranging from the original formulation of the receptor concept, the first isolation and structural analysis of a receptor protein (the nAChR) to the identification, localization, and differentiation of its diverse subtypes and their validation as a target for therapeutic intervention.
Until recently oral and intravenous formulations of the selective 5HT3 receptor antagonists were available, but a new formulation of a 5HT3 receptor antagonist (granisetron) by transdermal route has now been developed and approved by the US Food and Drug Administration FDAA).
Until now only intravenous and oral formulations of 5HT3 receptor antagonists have been available.
Recently a new formulation of a 5HT3 receptor antagonist, transdermal granisetron, has been developed, and approved by the FDA.
2, 4, 5 The challenge of preventing CINV during multiday regimens prompted the development of a new formulation of the 5-HT3 receptor antagonist granisetron: the Granisetron Transdermal System (GTDS; Sancuso®, ProStrakan Pharmaceuticals, Galashiels, UK).
A novel liposomal formulation of paclitaxel targeting the folate receptor (FR) was synthesized and characterized.
Fosaprepitant (Ivemend®, Merck) is a new intravenous prodrug formulation of the oral neurokinin-1 (NK1) receptor antagonist aprepitant (Emend®, Merck).
An extended-release formulation of the selective α2A-adrenergic receptor agonist guanfacine (GXR; Intuniv®, Shire Pharmaceuticals Inc). became the second nonstimulant approved by the Food and Drug Administration FDAA) for the treatment of ADHD.
Since both oral and intravenous formulations of older 5-HT3 receptor antagonists are effective for the prevention of CINV, an oral palonosetron formulation was developed and compared with the intravenous formulation.
Studies of the CV effects of different formulations of GLP-1 receptor agonists, including an oral formulation, are also justified to determine whether similar results are seen in all members of this drug class [ 80].
