Drug intelligence / Profile preview

ibuprofen + megestrol acetate

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Ibuprofen + megestrol acetate is an investigational combination therapy consisting of two well-established drugs—ibuprofen, a nonsteroidal anti-inflammatory drug (NSAID), and megestrol acetate, a synthetic progestin. This combination has been studied primarily for the management of cancer cachexia (weight loss and muscle wasting) in patients with advanced gastrointestinal cancers. Megestrol acetate acts as an agonist at the progesterone receptor and also exhibits glucocorticoid activity, leading to increased appetite and weight gain. Ibuprofen reduces inflammation by inhibiting cyclooxygenase enzymes (COX-1 and COX-2), thereby decreasing prostaglandin synthesis. Clinical studies have shown that this combination can reverse weight loss, reduce C-reactive protein levels (a marker of inflammation), improve appetite, and enhance quality of life in affected patients[1][2][6][7][10]. The regimen appears to be well-tolerated without significant toxicity.

02

Targets

PR (Progesterone receptor)GR (Glucocorticoid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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