Fosmidomycin

Summary

Fosmidomycin (CHEMBL203125) is a phase-3 clinical-stage small-molecule antimicrobial agent; indicated across 2 conditions including malaria and plasmodium falciparum malaria.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 5
• Chemistry: 183.1 Da · C4H10NO5P

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL203125
Name	Fosmidomycin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	572
ChEBI	CHEBI:443725
Molecular formula	C4H10NO5P
Molecular weight	183.1
InChIKey	GJXWDTUCERCKIX-UHFFFAOYSA-N

SMILES: C(CN(C=O)O)CP(=O)(O)O

IUPAC name: 3-[formyl(hydroxy)amino]propylphosphonic acid

ChEBI definition: Propylphosphonic acid in which one of the hydrogens at position 3 is substituted by a formyl(hydroxy)amino group. An antibiotic obtained from Streptomyces lavendulae, it specifically inhibits DXP reductoisomerase (EC 1.1.1.267), a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis.

Pharmacological roles (ChEBI): antimicrobial agent, EC 1.1.1.267 (1-deoxy-D-xylulose-5-phosphate reductoisomerase) inhibitor.

Other ChEBI roles (chemical / environmental): bacterial metabolite.

Also known as: Fosmidomicina, Fosmidomycin, Fosmidomycine, fosmidomycin, FOSMIDOMYCINE, SID174006643, FOSMIDOMYCIN

Parent form; salt/anhydrous children: CHEMBL2164257

Patent coverage: 427 distinct patent families (1,550 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase		6.43

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: 1-deoxy-D-xylulose 5-phosphate reductoisomerase, 1-deoxy-D-xylulose 5-phosphate reductoisomerase, chloroplastic, 1-deoxy-D-xylulose 5-phosphate reductoisomerase, 1-deoxy-D-xylulose 5-phosphate reductoisomerase, 1-deoxy-D-xylulose 5-phosphate reductoisomerase, apicoplastic, 1-deoxy-D-xylulose 5-phosphate reductoisomerase.

Bioactivity

ChEMBL activities: 20 potent at pChembl ≥ 5 of 20 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P45568	7.7	IC50	19.95	nM	CHEMBL_ACT_1510911
Q55663	7.68	Ki	21	nM	CHEMBL_ACT_1461156
P45568	7.52	IC50	30	nM	CHEMBL_ACT_1703865
P45568	7.52	IC50	30	nM	CHEMBL_ACT_5155394
P45568	7.5	IC50	32	nM	CHEMBL_ACT_15061786
P45568	7.5	IC50	32	nM	CHEMBL_ACT_15114434
P9WNS1	7.4	Kd	40	nM	CHEMBL_ACT_13390210
P45568	7.32	IC50	48	nM	CHEMBL_ACT_1702792
Q8IKG4	7.2	IC50	63	nM	CHEMBL_ACT_26012405
A0QVH7	7.1	IC50	80	nM	CHEMBL_ACT_10841692
P9WNS1	7.1	IC50	80	nM	CHEMBL_ACT_13390189
P9WNS1	7.1	IC50	80	nM	CHEMBL_ACT_2199546
P9WNS1	7.1	IC50	80	nM	CHEMBL_ACT_6274911
P9WNS1	7.1	IC50	80	nM	CHEMBL_ACT_6339433
Q9XFS9	7	IC50	100	nM	CHEMBL_ACT_12570367
P9WNS1	6.85	Ki	140	nM	CHEMBL_ACT_6274895
P9WNS1	6.64	IC50	230	nM	CHEMBL_ACT_13457012
P9WNS1	6.36	IC50	440	nM	CHEMBL_ACT_13888030
P9WNS1	6.36	IC50	440	nM	CHEMBL_ACT_26012451
A0QVH7	6.29	IC50	510	nM	CHEMBL_ACT_10841693

Target pathways

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

Indications & clinical

Indications

2 indications (0 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
malaria	3	MONDO:0005136	EFO:0001068
Plasmodium falciparum malaria	2	MONDO:0005920	EFO:0007444

Clinical trials

Total trials: 5.

Phase distribution

Phase	Trials
PHASE2	4
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00214643	PHASE3	COMPLETED	Efficacy of Fosmidomycin-Clindamycin for Treating Malaria in Gabonese Children
NCT01002183	PHASE2	WITHDRAWN	Fosmidomycin With Clindamycin or With Clindamycin Plus Artesunate
NCT01361269	PHASE2	UNKNOWN	Evaluation of Fosmidomycin and Clindamycin in the Treatment of Acute Uncomplicated Plasmodium Falciparum Malaria
NCT01464125	PHASE2	UNKNOWN	Fosmidomycin and Azithromycin for Acute Uncomplicated Plasmodium Falciparum Malaria (P. Malaria) in Adults
NCT01464138	PHASE2	COMPLETED	Evaluation of Fosmidomycin and Clindamycin in the Treatment of Acute Uncomplicated P.Falciparum Malaria in Children

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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