Drug intelligence / Profile preview

cycloserine

Development stage
Approved
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Cycloserine (specifically D-cycloserine) is a small molecule drug that serves a dual role as a broad-spectrum antibiotic and a cognitive enhancer in neuropsychiatric research. Originally developed by Eli Lilly and Merck in 1954 and marketed under the brand name Seromycin, cycloserine is FDA-approved as a second-line treatment for active pulmonary and extrapulmonary tuberculosis (including multidrug-resistant strains) and urinary tract infections. It exerts its antibacterial effect by inhibiting bacterial cell wall synthesis through the competitive inhibition of alanine racemase and D-alanine—D-alanine ligase. In the central nervous system, D-cycloserine acts as a partial agonist at the glycine-binding site of the NMDA receptor (specifically the GluN1 subunit). This glutamatergic activity facilitates fear extinction and enhances emotional learning, leading to its investigation as an adjunctive therapy to augment exposure-based cognitive behavioral therapy. In a pilot clinical trial (NCT01996644) conducted by the Washington University School of Medicine, D-cycloserine (referred to in the trial registry under the name "Setraline") was investigated for its ability to reduce food anxiety and facilitate weight gain in patients with anorexia nervosa, bulimia nervosa, and eating disorder not otherwise specified (EDNOS).

Brand names
MyserNovaserinePamserineSeromycin
Other names
D-cycloserineDCSSetraline
02

Targets

Alr (Alanine racemase)DdlA (D-alanyl-D-alanine Synthetase)GRIN1 (NMDA receptor subunit 1)

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