Rimexolone

Summary

Rimexolone (CHEMBL1200617) is an approved small molecule (ATC H02AB12); indicated across 2 conditions including eye disorder and dry eye syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: H02AB12 (+1 more)
• Indications: 2 conditions
• Clinical trials: 1
• Chemistry: 370.5 Da · C24H34O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1200617
Name	Rimexolone
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5311412
ATC	H02AB12, S01BA13
Molecular formula	C24H34O3
Molecular weight	370.5
InChIKey	QTTRZHGPGKRAFB-OOKHYKNYSA-N

SMILES: CCC(=O)[C@]1([C@@H](C[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2CCC4=CC(=O)C=C[C@]34C)O)C)C)C

IUPAC name: (8S,9S,10R,11S,13S,14S,16R,17S)-11-hydroxy-10,13,16,17-tetramethyl-17-propanoyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one

Also known as: ORG 6216, ORG-6216, Rimexolon, Rimexolona, Rimexolone, Vexol, SID56463550, RIMEXOLONE, rimexolone

Patent coverage: 189 distinct patent families (891 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: 6 (assay-derived). Sample: Beta-lactamase, Glucocorticoid receptor, Progesterone receptor, Nuclear receptor subfamily 1 group I member 2, Cannabinoid receptor 1, Nuclear receptor subfamily 1 group I member 2.

Bioactivity

ChEMBL activities: 9 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PGR	8.49	AC50	3.2	nM	CHEMBL_ACT_25223154
NR3C1	8	AC50	10	nM	CHEMBL_ACT_25175993
NR1I2	6.4	EC50	400	nM	CHEMBL_ACT_15455054
Q9R1A7	6.17	EC50	680	nM	CHEMBL_ACT_15463840
NR1I2	5.8	EC50	1600	nM	CHEMBL_ACT_15463808
NR1I2	5.6	EC50	2500	nM	CHEMBL_ACT_15465502
P00811	5.55	Potency	2818	nM	CHEMBL_ACT_4643188
NR1I2	5.4	EC50	4000	nM	CHEMBL_ACT_15463762
CNR1	5.16	AC50	6907	nM	CHEMBL_ACT_25181728

Target pathways

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

Indications & clinical

Indications

2 indications (1 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
eye disorder	4	MONDO:0005328	EFO:0005752
dry eye syndrome	3	MONDO:0006733	EFO:1000906

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00471419	PHASE3	COMPLETED	Phase II Study of AL-2178 (FID 109980) in the Treatment of Dry Eye

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).