Mesalamine

Summary

Mesalamine (CHEMBL704) is an approved small-molecule non-steroidal anti-inflammatory drug (ATC A07EC02) targeting PPARG; indicated across 19 conditions including proctitis and ulcerative colitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A07EC02
• Targets: 1 (PPARG)
• Indications: 19 conditions
• Clinical trials: 123
• Chemistry: 153.14 Da · C7H7NO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL704
Name	Mesalamine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4075
ChEBI	CHEBI:6775
ATC	A07EC02
Molecular formula	C7H7NO3
Molecular weight	153.14
InChIKey	KBOPZPXVLCULAV-UHFFFAOYSA-N

SMILES: C1=CC(=C(C=C1N)C(=O)O)O

IUPAC name: 5-amino-2-hydroxybenzoic acid

ChEBI definition: A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position.

Pharmacological roles (ChEBI): non-steroidal anti-inflammatory drug.

Also known as: Apriso, Asacol, Asacol hd, Canasa, Coltec ec, Delzicol, Fisalamine, Iialda, Ipocol, Lialda, MAX-002, Mesalamine

Patent coverage: 14,592 distinct patent families (52,574 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 50,764 (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

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
PPARG	Peroxisome proliferator-activated receptor-γ	Full agonist	1.82	2.6%	P37231

Broader ChEMBL bioactivity targets: 25 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Lysine-specific demethylase 4E, Fructose-bisphosphate aldolase, ATP-dependent DNA helicase Q1, 4’-phosphopantetheinyl transferase ffp, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Tumor necrosis factor, Thyroid hormone receptor beta, Menin/Histone-lysine N-methyltransferase MLL, Prostaglandin G/H synthase 2.

Bioactivity

ChEMBL activities: 22 potent at pChembl ≥ 5 of 45 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
TST	6.55	IC50	280	nM	CHEMBL_ACT_19209179
TDP1	6	Potency	1000	nM	CHEMBL_ACT_3927579
TDP1	5.6	Potency	2512	nM	CHEMBL_ACT_3928548
A8B2U2	5.45	Potency	3540	nM	CHEMBL_ACT_4611188
RECQL	5.4	Potency	3981	nM	CHEMBL_ACT_3675296
KDM4E	5.4	Potency	3981	nM	CHEMBL_ACT_3725919
CYP2C19	5.3	Potency	5012	nM	CHEMBL_ACT_4016450
CYP2C19	5.3	AC50	5012	nM	CHEMBL_ACT_6064727
CASP1	5.2	Potency	6310	nM	CHEMBL_ACT_4875606
RECQL	5.15	Potency	7080	nM	CHEMBL_ACT_3692135
PTGS2	5.12	IC50	7530	nM	CHEMBL_ACT_19274302
Q9WU19	5.11	IC50	7800	nM	CHEMBL_ACT_18669909
P05979	5.11	IC50	7730	nM	CHEMBL_ACT_19274294
CASP7	5.1	Potency	7943	nM	CHEMBL_ACT_3801875
CYP3A4	5.1	Potency	7943	nM	CHEMBL_ACT_4949416
CYP3A4	5.1	Potency	7943	nM	CHEMBL_ACT_5018295
CYP3A4	5.1	AC50	7943	nM	CHEMBL_ACT_6061625
ALDH1A1	5.05	Potency	8912	nM	CHEMBL_ACT_4158642
HSD17B10	5	Potency	10000	nM	CHEMBL_ACT_3688664
HIF1A	5	Potency	10000	nM	CHEMBL_ACT_4132731
HIF1A	5	Potency	10000	nM	CHEMBL_ACT_4519500
HSD17B10	5	Potency	10000	nM	CHEMBL_ACT_4881168

Target pathways

Aggregated over 1 target gene(s): PPARG.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
PPARA activates gene expression	1	PPARG
Transcriptional regulation of white adipocyte differentiation	1	PPARG
Nuclear Receptor transcription pathway	1	PPARG
SUMOylation of intracellular receptors	1	PPARG
Regulation of PTEN gene transcription	1	PPARG
MECP2 regulates transcription factors	1	PPARG
MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis	1	PPARG
Transcriptional regulation of brown and beige adipocyte differentiation by EBF2	1	PPARG

Dominant GO biological processes

GO term	Targets
negative regulation of transcription by RNA polymerase II	1
placenta development	1
regulation of transcription by RNA polymerase II	1
fatty acid metabolic process	1
response to nutrient	1
regulation of blood pressure	1
hormone-mediated signaling pathway	1
positive regulation of gene expression	1
negative regulation of gene expression	1
negative regulation of macrophage derived foam cell differentiation	1
positive regulation of cholesterol efflux	1
negative regulation of cholesterol storage	1
negative regulation of lipid storage	1
long-chain fatty acid transport	1
negative regulation of angiogenesis	1

Indications & clinical

Indications

19 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
proctitis	4	MONDO:0005538	EFO:0005628
ulcerative colitis	4	MONDO:0005101	EFO:0000729
Crohn disease	3	MONDO:0005011	EFO:0000384
irritable bowel syndrome	3	MONDO:0005052	EFO:0000555
collagenous colitis	3	MONDO:0000703	EFO:1001293
lymphocytic colitis	3	MONDO:0000704	EFO:1001294
diverticulitis	3	MONDO:0004235	MONDO:0004235
colitis	2	MONDO:0005292	EFO:0003872
colorectal adenoma	2	MONDO:0005484	EFO:0005406
eosinophilic esophagitis	2	MONDO:0005361	EFO:0004232
inflammatory bowel disease	2	MONDO:0005265	EFO:0003767
colorectal neoplasm	2	MONDO:0005335	MONDO:0005575
chronic beryllium disease	1	MONDO:0015274	EFO:0007168
HIV infectious disease	1	MONDO:0005109	EFO:0000764

5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 123.

Phase distribution

Phase	Trials
PHASE3	46
PHASE2	24
Not specified	16
PHASE4	14
PHASE1	12
PHASE2/PHASE3	6
PHASE1/PHASE2	4
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00194818	PHASE4	COMPLETED	Asacol Dosing Study for Active Ulcerative Colitis
NCT00652145	PHASE4	COMPLETED	Dose Escalation and Remission (DEAR)
NCT01090102	PHASE4	COMPLETED	Mesalamine to Reduce T Cell Activation in HIV Infection
NCT01124149	PHASE4	COMPLETED	Ability to Maintain or Achieve Clinical and Endoscopic Remission With MMX Mesalamine Once Daily in Adults With Ulcerative Colitis
NCT01201122	PHASE4	COMPLETED	Once Versus Twice Daily Mesalamine to Induce Remission in Pediatric Ulcerative Colitis
NCT01316718	PHASE4	COMPLETED	Mesalazine for the Treatment of Diarrhoea-predominant Irritable Bowel Syndrome (IBS-D)
NCT01534754	PHASE4	COMPLETED	Mesalazine and/or Lactobacillus Casei in the Diverticular Disease of the Colon
NCT01536535	PHASE4	COMPLETED	Predicting Response to Standardized Pediatric Colitis Therapy
NCT01696942	PHASE4	TERMINATED	Cimzia Versus Mesalamine for Crohn’s Recurrence
NCT01789294	PHASE4	UNKNOWN	Clinical Management of Childhood Intestinal Lymphoid Nodular Hyperplasia
NCT02331823	PHASE4	UNKNOWN	Research on New Regimens for Retreatment Pulmonary Tuberculosis
NCT03110198	PHASE4	UNKNOWN	Mesalazine With Hydrocortisone Sodium Succinate Enema for 4-Week Treatment in Patients With Ulcerative Colitis
NCT04133194	PHASE4	UNKNOWN	Adherence of a 1.600 mg Single Tablet 5-ASA Treatment of Ulcerative Colitis
NCT05205603	PHASE4	COMPLETED	Efficacy of Mesalazine Combined With Biologics in the Treatment of Moderate to Severe Ulcerative Colitis
NCT05986136	PHASE2/PHASE3	RECRUITING	Activation of Autophagy and Suppression of Apoptosis by Dapagliflozin Attenuates Inflammatory Bowel Disease
NCT00151892	PHASE3	COMPLETED	Efficacy and Safety of SPD476 in Maintaining Remission in Patients With Ulcerative Colitis
NCT00209300	PHASE3	COMPLETED	Pentasa Once Daily in Ulcerative Colitis for Maintenance of Remission
NCT00245505	PHASE3	TERMINATED	The Effect on Mucosal Healing With Pentasa Sachet in Mild to Moderate Active Drug: Crohn’s Disease
NCT00300118	PHASE3	COMPLETED	Oral Budesonide vs. Oral Mesalazine in Active Crohn’s Disease (CD)
NCT00343850	PHASE3	COMPLETED	Once Daily Versus Conventional Dosing of Asacol in the Maintenance of Quiescent Ulcerative Colitis
NCT00350415	PHASE3	COMPLETED	A Double Blind Study for the Treatment of Acute Ulcerative Colitis
NCT00449722	PHASE3	COMPLETED	OD vs. TID Dosing With Mesalazine Granules in Active Ulcerative Colitis
NCT00450086	PHASE3	COMPLETED	Budesonide Capsules vs. Mesalazine Granules vs. Placebo in Collagenous Colitis
NCT00505778	PHASE3	COMPLETED	A Comparison of Once a Day Dose Compared to 2 Doses/Day
NCT00548574	PHASE3	COMPLETED	Efficacy and Safety of Two Doses of SPD476 (Mesalazine) 2.4g and 4.8g Once Daily, With Reference to Asacol 0.8g Three Times Daily in Subjects With Acute, Mild to Moderate Ulcerative Colitis
NCT00577473	PHASE3	COMPLETED	Safety and Efficacy of Asacol 4.8 g/Day Versus Asacol 2.4 g/Day (ASCEND I)
NCT00626288	PHASE3	COMPLETED	Mesalazine Therapy in Patients With Irritable Bowel Syndrome
NCT00695643	PHASE3	TERMINATED	Mesalazine Granules vs. Placebo for the Prevention of Recurrence of Diverticulitis
NCT00708656	PHASE3	COMPLETED	The Colitis Once Daily Asacol Study
NCT00713310	PHASE3	COMPLETED	Assessing the Safety/Efficacy of Asacol® Given Every 12 Hours to Children and Adolescents With Active Ulcerative Colitis
NCT00744016	PHASE3	COMPLETED	Mesalamine Pellet Formulation to Maintain Remission of Mild to Moderate Ulcerative Colitis
NCT00746447	PHASE3	COMPLETED	Once Daily (OD) Versus Three Times Daily (TID) Dosing With Mesalazine Granules for Prevention of Recurrence of Ulcerative Colitis (UC)
NCT00747110	PHASE3	COMPLETED	Budesonide Capsules Versus Mesalazine Granules in Active Ulcerative Colitis (UC)
NCT00767728	PHASE3	COMPLETED	Mesalamine Pellet to Maintain Remission of Mild to Moderate Ulcerative Colitis
NCT00774007	PHASE2/PHASE3	COMPLETED	A Randomized Controlled Pilot Trial of Mesalazine in Patients With Irritable Bowel Syndrome
NCT00862121	PHASE3	TERMINATED	A Study With Pentasa in Patients With Active Crohn’s Disease
NCT00946946	PHASE3	COMPLETED	Preventing Postoperative Relapse in Crohn’s Disease Patients at Risk: Azathioprine Versus Mesalazine
NCT00952952	PHASE2/PHASE3	COMPLETED	Trial of Mesalamine for the Treatment of Active Microscopic Colitis
NCT00984568	PHASE3	TERMINATED	Conventional Step-Up Versus Infliximab Monotherapy in Patients With Ulcerative Colitis (P05553)
NCT01004185	PHASE3	TERMINATED	Assessing the Safety/Efficacy of Asacol® Given Every 12 Hours to Children and Adolescents for the Maintenance of Remission of Ulcerative Colitis

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 chlorpropamide, dabrafenib, gliclazid	CPIC	G6PD

PharmGKB also curates 0 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

84 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
FULVESTRANT	ChEMBL + PubChem	Phase 4 (approved)	PPARG
BENZBROMARONE	ChEMBL	Phase 4 (approved)	PPARG
BEXAROTENE	ChEMBL	Phase 4 (approved)	PPARG
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	PPARG
CANNABIDIOL	ChEMBL	Phase 4 (approved)	PPARG
CARVEDILOL	ChEMBL	Phase 4 (approved)	PPARG
CEFAMANDOLE	ChEMBL	Phase 4 (approved)	PPARG
CEFOTAXIME	ChEMBL	Phase 4 (approved)	PPARG
CEFOXITIN	ChEMBL	Phase 4 (approved)	PPARG
CEFTAZIDIME	ChEMBL	Phase 4 (approved)	PPARG
CEFTRIAXONE	ChEMBL	Phase 4 (approved)	PPARG
CLOBETASOL PROPIONATE	ChEMBL	Phase 4 (approved)	PPARG
EFAVIRENZ	ChEMBL	Phase 4 (approved)	PPARG
ELAFIBRANOR	ChEMBL	Phase 4 (approved)	PPARG
FENOFIBRATE	ChEMBL	Phase 4 (approved)	PPARG
FENOFIBRIC ACID	ChEMBL	Phase 4 (approved)	PPARG
GEMFIBROZIL	ChEMBL	Phase 4 (approved)	PPARG
GLYBURIDE	ChEMBL	Phase 4 (approved)	PPARG
INDOMETHACIN	ChEMBL	Phase 4 (approved)	PPARG
LASOFOXIFENE	ChEMBL	Phase 4 (approved)	PPARG
LEVOTHYROXINE	ChEMBL	Phase 4 (approved)	PPARG
LIOTHYRONINE	ChEMBL	Phase 4 (approved)	PPARG
LUMIRACOXIB	ChEMBL	Phase 4 (approved)	PPARG
MASOPROCOL	ChEMBL	Phase 4 (approved)	PPARG
METHYLENE BLUE	ChEMBL	Phase 4 (approved)	PPARG
MONTELUKAST	ChEMBL	Phase 4 (approved)	PPARG
NINTEDANIB	ChEMBL	Phase 4 (approved)	PPARG
PEMAFIBRATE	ChEMBL	Phase 4 (approved)	PPARG
PIOGLITAZONE	ChEMBL	Phase 4 (approved)	PPARG
RIMONABANT	ChEMBL	Phase 4 (approved)	PPARG
ROSIGLITAZONE	ChEMBL	Phase 4 (approved)	PPARG
SULINDAC	ChEMBL	Phase 4 (approved)	PPARG
TELMISARTAN	ChEMBL	Phase 4 (approved)	PPARG
TERIFLUNOMIDE	ChEMBL	Phase 4 (approved)	PPARG
TIPRANAVIR	ChEMBL	Phase 4 (approved)	PPARG
TROGLITAZONE	ChEMBL	Phase 4 (approved)	PPARG
ZAFIRLUKAST	ChEMBL	Phase 4 (approved)	PPARG
ALEGLITAZAR	ChEMBL	Phase 3	PPARG
BALAGLITAZONE	ChEMBL	Phase 3	PPARG
BEZAFIBRATE	ChEMBL	Phase 3	PPARG
CANDESARTAN	ChEMBL	Phase 3	PPARG
DOCONEXENT	ChEMBL	Phase 3	PPARG
GAMOLENIC ACID	ChEMBL	Phase 3	PPARG
ICOSAPENT	ChEMBL	Phase 3	PPARG
IMIGLITAZAR	ChEMBL	Phase 3	PPARG
LANIFIBRANOR	ChEMBL	Phase 3	PPARG
LERIGLITAZONE	ChEMBL	Phase 3	PPARG
LOBEGLITAZONE	ChEMBL	Phase 3	PPARG
MURAGLITAZAR	ChEMBL	Phase 3	PPARG
NAMODENOSON	ChEMBL	Phase 3	PPARG
QUERCETIN	ChEMBL	Phase 3	PPARG
RESVERATROL	ChEMBL	Phase 3	PPARG
RIVOGLITAZONE	ChEMBL	Phase 3	PPARG
TESAGLITAZAR	ChEMBL	Phase 3	PPARG
TIRATRICOL	ChEMBL	Phase 3	PPARG
ARHALOFENATE	ChEMBL	Phase 2	PPARG
ATX08-001	ChEMBL	Phase 2	PPARG
CANNABIGEROL	ChEMBL	Phase 2	PPARG
CIGLITAZONE	ChEMBL	Phase 2	PPARG
CXA-10	ChEMBL	Phase 2	PPARG