Sulfadiazine

Summary

Sulfadiazine (CHEMBL439) is an approved small-molecule antimicrobial agent (ATC J01EC02); indicated across 7 conditions including bacterial infectious disease and malaria.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J01EC02
• Indications: 7 conditions
• Clinical trials: 3
• Chemistry: 250.28 Da · C10H10N4O2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL439
Name	Sulfadiazine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5215
ChEBI	CHEBI:9328
ATC	J01EC02
Molecular formula	C10H10N4O2S
Molecular weight	250.28
InChIKey	SEEPANYCNGTZFQ-UHFFFAOYSA-N

SMILES: C1=CN=C(N=C1)NS(=O)(=O)C2=CC=C(C=C2)N

IUPAC name: 4-amino-N-pyrimidin-2-ylbenzenesulfonamide

ChEBI definition: A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.

Pharmacological roles (ChEBI): antimicrobial agent, antiinfective agent, coccidiostat, antiprotozoal drug, EC 2.5.1.15 (dihydropteroate synthase) inhibitor, EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor, drug allergen.

Other ChEBI roles (chemical / environmental): xenobiotic, environmental contaminant.

Also known as: Coco-diazine, Diazyl, NSC-35600, Sulfadiazina, Sulfadiazine, Sulfadiazine component of lantrisul, Sulfadiazine component of neotrizine, Sulfadiazine component of sulfaloid, Sulfadiazine component of sulfose, Sulfadiazine component of terfonyl, Sulfadiazine component of triple sulfoid, Sulfolex

Parent form; salt/anhydrous children: CHEMBL1200351, CHEMBL1382627

Patent coverage: 11,635 distinct patent families (31,545 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Prelamin-A/C, Thyrotropin receptor, Dihydrofolate reductase, Aurora kinase A.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DHFR	6.89	IC50	130	nM	CHEMBL_ACT_25035185
LMNA	6.75	Potency	177.8	nM	CHEMBL_ACT_3642089

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

7 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
bacterial infectious disease	4	MONDO:0005113	EFO:0000771
malaria	4	MONDO:0005136	EFO:0001068
congenital toxoplasmosis	3	MONDO:0005715	EFO:0007220
chorioretinitis	3	MONDO:0004674	HP:0012424
cerebral toxoplasmosis	2	MONDO:0005697	EFO:0007200
burn	2	MONDO:0043519	EFO:0009516
osteomyelitis	0	MONDO:0005246	EFO:0003102

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE4	1
PHASE3	1
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00004317	PHASE4	RECRUITING	Pyrimethamine, Sulfadiazine, and Leucovorin in Treating Patients With Congenital Toxoplasmosis
NCT01189448	PHASE3	COMPLETED	Prevention of Congenital Toxoplasmosis With Pyrimethamine + Sulfadiazine Versus Spiramycine During Pregnancy
NCT00000794	PHASE2	COMPLETED	Phase II Randomized Open-Label Trial of Atovaquone Plus Pyrimethamine and Atovaquone Plus Sulfadiazine for the Treatment of Acute Toxoplasmic Encephalitis

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for aminosalicylic acid, chloramphenicol,	CPIC	G6PD

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).