Diacerein

Summary

Diacerein (CHEMBL41286) is a phase-3 clinical-stage small molecule (ATC M01AX21); indicated across 14 conditions including rheumatic disorder and osteoarthritis, hip.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: M01AX21
• Indications: 14 conditions
• Clinical trials: 34
• Chemistry: 368.3 Da · C19H12O8

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL41286
Name	Diacerein
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	26248
ATC	M01AX21
Molecular formula	C19H12O8
Molecular weight	368.3
InChIKey	TYNLGDBUJLVSMA-UHFFFAOYSA-N

SMILES: CC(=O)OC1=CC=CC2=C1C(=O)C3=C(C2=O)C=C(C=C3OC(=O)C)C(=O)O

IUPAC name: 4,5-diacetyloxy-9,10-dioxoanthracene-2-carboxylic acid

Also known as: AC-201, Ac-203, Artrodar, Diacerein, Diacereina, Diacereine, Diacerhein, Diacetylrhein, Diora, Fisiodar, M-01AX21, M01AX21

Patent coverage: 1,469 distinct patent families (5,090 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 4,949 (97%) of the total. 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: 40 (assay-derived). Sample: Pyruvate kinase PKM, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Ubiquitin carboxyl-terminal hydrolase 2, Nuclear receptor ROR-gamma, Survival motor neuron protein, Fructose-bisphosphate aldolase, Prelamin-A/C, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Female germline-specific tumor suppressor gld-1.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 50 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
NAAA	6.16	IC50	700	nM	CHEMBL_ACT_18449190
NAAA	6.16	IC50	700	nM	CHEMBL_ACT_18449191
NAAA	6.16	IC50	700	nM	CHEMBL_ACT_20637182
Q63921	6.05	AC50	900	nM	CHEMBL_ACT_25174402
SMN1	5.85	Potency	1412	nM	CHEMBL_ACT_3894324
FTO	5.82	IC50	1500	nM	CHEMBL_ACT_26037659
MAPT	5.55	Potency	2818	nM	CHEMBL_ACT_4056423
SLC29A1	5.32	AC50	4800	nM	CHEMBL_ACT_25141542
TTR	5.27	IC50	5400	nM	CHEMBL_ACT_23169660
ABCC4	5.19	IC50	6400	nM	CHEMBL_ACT_18130908
Q17339	5.14	IC50	7308	nM	CHEMBL_ACT_5536907
CASP3	5.1	EC50	7894	nM	CHEMBL_ACT_5342297
PDE4D	5.06	AC50	8800	nM	CHEMBL_ACT_25185332
HSP90AA1	5.04	IC50	9234	nM	CHEMBL_ACT_3684686
MEN1	5	Potency	10000	nM	CHEMBL_ACT_3618631
P51450	5	Potency	10000	nM	CHEMBL_ACT_4947072

Target pathways

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

Indications & clinical

Indications

14 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
rheumatic disorder	4	MONDO:0005554	EFO:0005755
osteoarthritis, hip	3	MONDO:0006629	EFO:1000786
osteoarthritis, knee	3	MONDO:0005416	EFO:0004616
osteoarthritis	3	MONDO:0005178	MONDO:0005178
rheumatoid arthritis	2	MONDO:0008383	EFO:0000685
gout	2	MONDO:0005393	EFO:0004274
thrombocytopenia	2	MONDO:0002049	HP:0001873
type 2 diabetes mellitus	2	MONDO:0005148	MONDO:0005148
epidermolysis bullosa simplex	2	MONDO:0017610	MONDO:0017610
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
bullous pemphigoid	2	MONDO:0019082	EFO:0007187
epidermolysis bullosa	2	MONDO:0006541	EFO:1000690
epidermolysis bullosa dystrophica	1	MONDO:0006543	Orphanet:303
junctional epidermolysis bullosa	1	MONDO:0017612	MONDO:0017612

Clinical trials

Total trials: 34.

Phase distribution

Phase	Trials
PHASE2	15
PHASE4	8
PHASE1	5
PHASE3	4
PHASE2/PHASE3	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07352306	PHASE4	NOT_YET_RECRUITING	Topical Diacerein in Psoriasis Vulgaris
NCT00440661	PHASE4	COMPLETED	Exploration of the Synovial Fluid Inflammation Mediators Under Diacerhein in Knee Osteoarthritis
NCT00445276	PHASE4	COMPLETED	Symptomatic Efficacy of Diacerein in Knee Osteoarthritis
NCT00685542	PHASE4	COMPLETED	Effect of Diacerein on Hand Osteoarthritis
NCT01120015	PHASE4	COMPLETED	Diacerein as Adjuvant to Diclofenac Sodium in Indian Patients of Osteoarthritis (OA) Knee
NCT01906801	PHASE4	COMPLETED	Clinical Efficacy of Glucosamine Plus Diacerein Versus Mono-therapy of Glucosamine
NCT02060552	PHASE4	COMPLETED	Immune Molecular and Inflammatory Cytokines Dysfunction Analysis in Gout Patients With Different Urate Levels
NCT03404479	PHASE4	UNKNOWN	Trial to Evaluate Efficacy and Safety of Combination of Diacerein and Celecoxib Administered in Patients With Knee OA
NCT04318041	PHASE3	RECRUITING	Evaluation of the Structural Modification Effect of Diacerein (Artrodar®) in Knee Osteoarthritic Patients
NCT06073132	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	An International, Multicenter, Randomized, Double-Blind, Parallel Group, Vehicle-Controlled, Phase 2/3 Study With Open-Label Extension Evaluating the Efficacy and Safety of Diacerein 1% Ointment for the Treatment of Generalized Epidermolysis Bullosa Simplex (EBS)
NCT00451360	PHASE3	COMPLETED	Chondromodulating Effect of Diacerein in Osteoarthritis of the Hip
NCT02242149	PHASE3	COMPLETED	Efficacy Study of Diacerein on Glycemic Control and Liver Fat in Type 2 Diabetes Subjects
NCT02688400	PHASE3	COMPLETED	Effect of Diacerein vs Celecoxib on Symptoms and Structural Changes in Symptomatic Knee Osteoarthritis
NCT01264211	PHASE2	COMPLETED	Safety and Efficacy of the Combination of Diacerein 100 mg Daily and MTX Versus MTX Alone in the Treatment of Early Rheumatoid Arthritis (RA)
NCT01276106	PHASE2	COMPLETED	Study of AC-201 in Patients With Type 2 Diabetes Mellitus
NCT01298882	PHASE2	COMPLETED	Diacerein on Insulin Secretion in Diabetes
NCT01712204	PHASE2	COMPLETED	A Proof-of-Concept Study of AC-201 to Prevent Gout Flares
NCT02177643	PHASE2	UNKNOWN	Effect of Diacerein in the Metabolic Control of Patients With DM Type 2 and Secondary Failure to Metformin
NCT02287818	PHASE2	COMPLETED	A Study of AC-201 Controlled-Release Tablet (CR Tablet) in Patients With Gout
NCT02470689	PHASE2	UNKNOWN	Diacerin for the Treatment of Epidermolysis Bullosa Simplex
NCT03154333	PHASE2	TERMINATED	Safety and Efficacy of Diacerein 1% Ointment for Subjects With Epidermolysis Bullosa Simplex (EBS)
NCT03208309	PHASE2	COMPLETED	Effect of Diacerein in the Metabolic Control of Patients With DM Type 2 and Secondary Failure to Metformin
NCT03286582	PHASE2	TERMINATED	A Proof-of-Concept Study of Topical AC-203 in Patients With Bullous Pemphigoid
NCT03389308	PHASE2	COMPLETED	Long Term Open-label Study Evaluating Safety of Diacerein 1% Ointment Topical Formulation in Subjects With Epidermolysis Bullosa Simplex
NCT03468322	PHASE2	COMPLETED	A Double-blind, Intra-individual Comparison, POC Trial of AC-203 in EB Patients
NCT03754634	PHASE2	COMPLETED	A Prospective, Open, Multicenter Clinical Trial of Eltrombopag Combined With Diacerein in Eltrombopag-inefficient or Relapsed ITP
NCT05226754	PHASE2	UNKNOWN	Study Design of the Diacerein in Patients With Covid-19
NCT06972888	PHASE2	COMPLETED	A Phase II Clinical Study of AC-201 Tablets in Subjects With Plaque Psoriasis
NCT03472287	PHASE1	COMPLETED	To Evaluate the Pharmacokinetic of Diacerein and Rhein After Maximum Use in Patients With Epidermolysis Bullosa (EB)
NCT03472534	PHASE1	COMPLETED	A 21 Day Irritation Study in Healthy Volunteers With Diacerein 1% Ointment
NCT03472547	PHASE1	COMPLETED	A Study of Sensitizing Potential of Diacerein 1% Ointment in Healthy Subjects
NCT03473184	PHASE1	COMPLETED	A 4-Day Study to Evaluate the Photoxicity of Diacerein 1% Topical Ointment in Healthy Volunteers
NCT03473197	PHASE1	COMPLETED	A 6-Week Study to Evaluate the Photoallergic Potential of Diacerein 1% Ointment in Healthy Volunteers
NCT04351100	Not specified	COMPLETED	Efficacy of Diacerein on Ocular Surface Disease in Degenerative Arthritis Patients

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).