Drug intelligence / Profile preview

d-cycloserine

Development stage
Approved
Lead developer
Streptomyces orchidaceus (original natural source)
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

d-Cycloserine is a broad-spectrum antibiotic and a structural analogue of the amino acid D-alanine. It is primarily used as a second-line agent in the treatment of multidrug-resistant tuberculosis (MDR-TB), often in combination with other antitubercular drugs. Its antibacterial activity results from inhibition of bacterial cell wall synthesis by competitively inhibiting two key enzymes involved in peptidoglycan biosynthesis—L-alanine racemase and D-alanyl-D-alanine synthetase—thereby preventing formation and cross-linking of peptidoglycan chains essential for bacterial cell wall integrity[1][5][6]. In addition to its antimicrobial use, d-cycloserine has been investigated as an adjunctive therapy for certain psychiatric conditions due to its partial agonist activity at the NMDA receptor glycine site, which may enhance neural plasticity[5][6]. It is administered orally and rapidly absorbed. Common side effects include neuropsychiatric symptoms such as dizziness, headache, mood changes, seizures, and allergic reactions; it should be used with caution in patients with renal impairment or pre-existing neurological disorders[9][10].

Brand names
Seromycin
Other names
右旋环丝氨酸D-环丝氨酸cycloserineD-4-amino-3-isoxazolidinoneD4-amino-3-isoxazolidinoneD 4-amino-3-isoxazolidinone
02

Targets

Alr (Alanine racemase)GluN1 (N-methyl-D-aspartate receptor subunit zeta-1 (GRIN1))DdlA (D-alanyl-D-alanine Synthetase)Halhy (D-amino acid transaminase)

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