Biomarker & Intervention Discovery

Chronic Urticaria (CSU)

This page lists 10 druggable gene targets, 53 approved or trial-tested drug candidates and 10 recent clinical trials for Chronic Urticaria (CSU), with each agent ranked by the strength of its evidence (clinical, mechanistic or correlative). Candidates include existing drugs that could be repurposed. Sources are linked so you can check every claim.

Spontaneous remissionSpontaneous remission at 1 year: ~50%; at 5 years: ~65-70%; but 10-15% remain chronic beyond 5 years; remission…
Best-intervention remissionOmalizumab (anti-IgE): complete symptom resolution in 36-44% at 12 weeks (GLACIAL, ASTERIA trials); high-dose…
Gap sizeModerate — omalizumab is transformative but not accessible as first-line; many patients on inadequate antihistamine…
Primary barrieraccess/practice
Full remission profile →
Research Tracker Chronic Disease Interventions Chronic Urticaria (CSU)

Remission & chronicity

Spontaneous remission
Spontaneous remission at 1 year: ~50%; at 5 years: ~65-70%; but 10-15% remain chronic beyond 5 years; remission followed by relapse common
Best-intervention remission
Omalizumab (anti-IgE): complete symptom resolution in 36-44% at 12 weeks (GLACIAL, ASTERIA trials); high-dose antihistamines (4x standard dose): 50-60% symptom control; cyclosporine for antihistamine-refractory: 50-60% response; dupilumab for CSU: 73% UAS7 ≤6 at 24 weeks (Phase 3 LIBERTY-CSU CUPID 2023)
Gap size
Moderate — omalizumab is transformative but not accessible as first-line; many patients on inadequate antihistamine doses or antihistamine monotherapy long-term
Primary barrier
access/practice
Omalizumab (Xolair) was FDA-approved for CSU in 2014 but remains unavailable as first-line (prior authorisation requiring antihistamine failure first); many patients spend years on sedating antihistamines or systemic OCS; dupilumab (2023 Phase 3 data) adds a second biologic option

Biomarker Targets & Therapeutic Agents

Gene targets queried against DGIdb, Open Targets, ChEMBL, PubMed, and Europe PMC. Agents ranked: Clinical > Mechanistic > Correlative.

BTK 254CYSLTR1 201FCER1A 7HRH1 374HRH2 231HRH4 144IL4R 9KIT 278MRGPRX2 71MS4A2 3

BTK

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
PRN694 ↓ inhibits Mechanistic DGIdb
RN486 ↓ inhibits Mechanistic DGIdb
PD166285 ? unclear Mechanistic DGIdb
PTD10 ↓ inhibits Mechanistic DGIdb
BRANEBRUTINIB ↓ inhibits Mechanistic DGIdb
ACALABRUTINIB ↓ inhibits Mechanistic DGIdb
COMPOUND 71 [WO2018191577A1] ↓ inhibits Mechanistic DGIdb
COMPOUND 25 [PMID: 31260299] ↓ inhibits Mechanistic DGIdb
COMPOUND 38 [PMID: 24915291] ↓ inhibits Mechanistic DGIdb
IBRUTINIB ↓ inhibits Mechanistic 0.5 nM (IC50) DGIdb
ZM447439 ? unclear Mechanistic DGIdb
BTK INHIBITOR TL-895 ? unclear Mechanistic DGIdb
ZYBT1 ↓ inhibits Mechanistic DGIdb
EVOBRUTINIB ↓ inhibits Mechanistic DGIdb
FENEBRUTINIB ↓ inhibits Mechanistic DGIdb
TOLEBRUTINIB ↓ inhibits Mechanistic DGIdb
RILZABRUTINIB ? unclear Mechanistic DGIdb
CGI1746 ↓ inhibits Mechanistic DGIdb
TAMATINIB ? unclear Mechanistic DGIdb
ZANUBRUTINIB ↓ inhibits Mechanistic DGIdb
ENTRECTINIB ? unclear Mechanistic 158.49 nM (Ki) DGIdb
LUXEPTINIB ↓ inhibits Mechanistic DGIdb
BTK INHIBITOR 16 [PMID: 30122225] ↓ inhibits Mechanistic DGIdb
ZELEBRUDOMIDE ? unclear Mechanistic DGIdb
BIIB068 ↓ inhibits Mechanistic DGIdb
PROTAC 23 [PMID: 38321747] ↓ inhibits Mechanistic DGIdb
NVP-TAE684 ? unclear Mechanistic DGIdb
COMPOUND 36 [PMID: 21958547] ↓ inhibits Mechanistic DGIdb
CINSEBRUTINIB ↓ inhibits Mechanistic DGIdb
COMPOUND 9 [PMID: 26006010] ↓ inhibits Mechanistic DGIdb
DASATINIB ANHYDROUS ? unclear Mechanistic DGIdb
NEMTABRUTINIB ? unclear Mechanistic DGIdb
JNJ-64264681 ↓ inhibits Mechanistic DGIdb
SPEBRUTINIB ↓ inhibits Mechanistic DGIdb
CHEMBL:CHEMBL1997335 ? unclear Mechanistic DGIdb
RITLECITINIB ↓ inhibits Mechanistic DGIdb
BIRELENTINIB ↓ inhibits Mechanistic DGIdb
PF-562271 ? unclear Mechanistic DGIdb
ORELABRUTINIB ↓ inhibits Mechanistic DGIdb
MIDOBRUTINIB ↓ inhibits Mechanistic DGIdb

Showing top 40 of 254 agents ranked by evidence tier.

CYSLTR1

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
CR-3465 ↓ inhibits Mechanistic DGIdb
SR2640 ↓ inhibits Mechanistic DGIdb
ZAFIRLUKAST ↓ inhibits Mechanistic 1.731 nM (IC50) DGIdb
PRANLUKAST ↓ inhibits Mechanistic 0.8 nM (IC50) DGIdb
LTE4 ↑ activates Mechanistic DGIdb
MONTELUKAST SODIUM ↓ inhibits Mechanistic DGIdb
IRALUKAST ↓ inhibits Mechanistic DGIdb
BAYCYSLT2 ↓ inhibits Mechanistic DGIdb
SULUKAST ↓ inhibits Mechanistic DGIdb
NEDOCROMIL ? unclear Mechanistic DGIdb
CINALUKAST ? unclear Mechanistic DGIdb
VERLUKAST ↓ inhibits Mechanistic 8.0 nM (IC50) DGIdb
MASILUKAST ? unclear Mechanistic DGIdb
MK-571 ↓ inhibits Mechanistic DGIdb
COMPOUND 15B [PMID: 31811124] ↓ inhibits Mechanistic DGIdb
LY-2300559 ? unclear Mechanistic DGIdb
RECOMBINANT TRANSFORMING GROWTH FACTOR-BETA 1 ? unclear Mechanistic DGIdb
TRIPLE MODULATOR 10 [PMID: 29878767] ↓ inhibits Mechanistic DGIdb
BAYU9773 ↓ inhibits Mechanistic DGIdb
N-METHYL LTC4 ↑ activates Mechanistic DGIdb
POBILUKAST ↓ inhibits Mechanistic 10.0 nM (Ki) DGIdb
ICI198615 ↓ inhibits Mechanistic DGIdb
COMPOUND 13E [PMID: 31811124] ↓ inhibits Mechanistic DGIdb
LTD4 ↑ activates Mechanistic DGIdb
LTC4 ↑ activates Mechanistic DGIdb
MONTELUKAST ? unclear Mechanistic 0.5 nM (IC50) Open Targets
SR-2640 ↓ inhibits Mechanistic 23.0 nM (IC50) ChEMBL
CHEMBL89340 ↓ inhibits Mechanistic 3.1 nM (IC50) ChEMBL
ABLUKAST ↓ inhibits Mechanistic 4000.0 nM (IC50) ChEMBL
FPL-55712 ↓ inhibits Mechanistic 4000.0 nM (IC50) ChEMBL
CHEMBL89768 ↓ inhibits Mechanistic 3.1 nM (IC50) ChEMBL
CHEMBL97356 ↓ inhibits Mechanistic 11.0 nM (Ki) ChEMBL
CHEMBL313177 ↓ inhibits Mechanistic 6.42 nM (IC50) ChEMBL
CHEMBL316170 ↓ inhibits Mechanistic 1.06 nM (IC50) ChEMBL
CHEMBL82790 ↓ inhibits Mechanistic 4.7 nM (IC50) ChEMBL
CHEMBL84707 ↓ inhibits Mechanistic 1.91 nM (IC50) ChEMBL
CHEMBL86264 ↓ inhibits Mechanistic 8.49 nM (IC50) ChEMBL
CHEMBL87528 ↓ inhibits Mechanistic 3.36 nM (IC50) ChEMBL
CHEMBL314340 ↓ inhibits Mechanistic 1.16 nM (IC50) ChEMBL
CHEMBL314237 ↓ inhibits Mechanistic 0.76 nM (IC50) ChEMBL

Showing top 40 of 201 agents ranked by evidence tier.

FCER1A

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
BENZYLPENICILLOYL POLYLYSINE ? unclear Mechanistic DGIdb
R112 ? unclear Mechanistic DGIdb
IGE HEAVY CHAIN ↑ activates Mechanistic DGIdb
OMALIZUMAB ? unclear Mechanistic DGIdb
CHEMBL275575 ↓ inhibits Mechanistic 71000.0 nM (IC50) ChEMBL
CHEMBL412391 ↓ inhibits Mechanistic 25000.0 nM (IC50) ChEMBL
CHEMBL267118 ↓ inhibits Mechanistic 82000.0 nM (IC50) ChEMBL

HRH1

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
HISTAMINE ↑ activates Mechanistic 13.0 nM (EC50) DGIdb
RISPERIDONE ↓ inhibits Mechanistic 2.6 nM (Ki) DGIdb
EPINASTINE ↓ inhibits Mechanistic DGIdb
PYRILAMINE ↓ inhibits Mechanistic 12.59 nM (IC50) DGIdb
ORPHENADRINE ? unclear Mechanistic DGIdb
MIZOLASTINE ↓ inhibits Mechanistic DGIdb
BETAHISTINE ↑ activates Mechanistic DGIdb
METHAPYRILENE FUMARATE ↓ inhibits Mechanistic DGIdb
MIANSERIN ? unclear Mechanistic 3.388 nM (IC50) DGIdb
MEQUITAZINE ↓ inhibits Mechanistic DGIdb
SERTINDOLE ↓ inhibits Mechanistic 570.0 nM (Ki) DGIdb
BROMPHENIRAMINE ? unclear Mechanistic DGIdb
LORATADINE ↓ inhibits Mechanistic DGIdb
TRIMEPRAZINE ? unclear Mechanistic DGIdb
BU-E 47 ↓ inhibits Mechanistic DGIdb
DEXCHLORPHENIRAMINE MALEATE ? unclear Mechanistic DGIdb
AZELASTINE ↓ inhibits Mechanistic DGIdb
ASENAPINE ↓ inhibits Mechanistic DGIdb
BROMODIPHENHYDRAMINE ? unclear Mechanistic DGIdb
OLOPATADINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
BEPOTASTINE BESILATE ? unclear Mechanistic DGIdb
FEXOFENADINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
PROPIOMAZINE ? unclear Mechanistic DGIdb
CETIRIZINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
DIPHENHYDRAMINE ↓ inhibits Mechanistic DGIdb
ARPROMIDINE ↓ inhibits Mechanistic DGIdb
PHENIRAMINE ? unclear Mechanistic DGIdb
QUETIAPINE FUMARATE ↓ inhibits Mechanistic DGIdb
AZATADINE ? unclear Mechanistic DGIdb
DOXEPIN HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
TRIPROLIDINE ↓ inhibits Mechanistic DGIdb
PROMETHAZINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
HYDROXYZINE ↓ inhibits Mechanistic DGIdb
ILOPERIDONE ? unclear Mechanistic DGIdb
PEMIROLAST ? unclear Mechanistic DGIdb
CHLORPHENIRAMINE POLISTIREX ↓ inhibits Mechanistic DGIdb
DIMETHINDENE ↓ inhibits Mechanistic 0.6918 nM (Ki) DGIdb
VAPITADINE ? unclear Mechanistic DGIdb
ARIPIPRAZOLE LAUROXIL ↓ inhibits Mechanistic DGIdb
BRILAROXAZINE ? unclear Mechanistic DGIdb

Showing top 40 of 374 agents ranked by evidence tier.

HRH2

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
NIZATIDINE ? unclear Mechanistic DGIdb
FAMOTIDINE ↓ inhibits Mechanistic DGIdb
TIOTIDINE ↓ inhibits Mechanistic DGIdb
BETAZOLE ? unclear Mechanistic DGIdb
EPINASTINE ? unclear Mechanistic DGIdb
RANITIDINE BISMUTH CITRATE ↓ inhibits Mechanistic DGIdb
HISTAMINE ? unclear Mechanistic 463.0 nM (EC50) DGIdb
ST-1006 ↑ activates Mechanistic DGIdb
INCB-38579 ↓ inhibits Mechanistic DGIdb
CIMETIDINE ↓ inhibits Mechanistic DGIdb
CIPROXIFAN ↓ inhibits Mechanistic DGIdb
ABT-239 ↓ inhibits Mechanistic DGIdb
CIMETIDINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
AMTHAMINE ↑ activates Mechanistic DGIdb
EBROTIDINE ↓ inhibits Mechanistic DGIdb
METHANTHELINE BROMIDE ↓ inhibits Mechanistic DGIdb
UR-PG146 ↑ activates Mechanistic DGIdb
ASENAPINE ? unclear Mechanistic DGIdb
DOXEPIN HYDROCHLORIDE ? unclear Mechanistic DGIdb
PITOLISANT ↓ inhibits Mechanistic DGIdb
BETAZOLE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
MK-0249 ↓ inhibits Mechanistic DGIdb
OXO-ARPROMIDINE ↑ activates Mechanistic DGIdb
RANITIDINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
LAFUTIDINE ↓ inhibits Mechanistic DGIdb
TOLAZOLINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
JNJ-39758979 ↓ inhibits Mechanistic DGIdb
BURIMAMIDE ↑ activates Mechanistic 3981.07 nM (Ki) DGIdb
IMPROMIDINE ↑ activates Mechanistic DGIdb
CONESSINE ↓ inhibits Mechanistic DGIdb
CLOBENPROPIT ↓ inhibits Mechanistic DGIdb
ARPROMIDINE ↑ activates Mechanistic DGIdb
TOLAZOLINE ? unclear Mechanistic Open Targets
METHANTHELINE ? unclear Mechanistic Open Targets
VUF-5297 ↑ activates Mechanistic 696.0 nM (EC50) ChEMBL
CHEMBL72424 ↓ inhibits Mechanistic 10000.0 nM (Ki) ChEMBL
CHEMBL70603 ↓ inhibits Mechanistic 10000.0 nM (Ki) ChEMBL
CHEMBL44220 ↓ inhibits Mechanistic 19952.62 nM (Ki) ChEMBL
CHEMBL72571 ↓ inhibits Mechanistic 3981.07 nM (Ki) ChEMBL
CHEMBL310087 ↓ inhibits Mechanistic 12589.25 nM (Ki) ChEMBL

Showing top 40 of 231 agents ranked by evidence tier.

HRH4

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
JNJ 7777120 ↓ inhibits Mechanistic DGIdb
(R)-Α-METHYLHISTAMINE ↑ activates Mechanistic DGIdb
IODOPHENPROPIT ↓ inhibits Mechanistic DGIdb
THIOPERAMIDE ↓ inhibits Mechanistic 27.0 nM (Ki) DGIdb
2-METHYLHISTAMINE ↑ activates Mechanistic DGIdb
JNJ-10191584 ↓ inhibits Mechanistic DGIdb
BURIMAMIDE ↓ inhibits Mechanistic 180.0 nM (Ki) DGIdb
CCL16 ↑ activates Mechanistic DGIdb
4-METHYLHISTAMINE ↑ activates Mechanistic DGIdb
ADRIFORANT ↓ inhibits Mechanistic DGIdb
2-(3-BROMOPHENYL)HISTAMINE ↑ activates Mechanistic DGIdb
CLOZAPINE ↓ inhibits Mechanistic DGIdb
HISTAMINE ↑ activates Mechanistic 75.0 nM (EC50) DGIdb
VOTUCALIS ? unclear Mechanistic DGIdb
N-[3H]METHYLHISTAMINE ↑ activates Mechanistic DGIdb
SELIFORANT ↓ inhibits Mechanistic DGIdb
IMETIT ↑ activates Mechanistic 51.0 nM (EC50) DGIdb
CONESSINE ↓ inhibits Mechanistic DGIdb
N-ETHYLHISTAMINE ↑ activates Mechanistic DGIdb
CIPROXIFAN ↓ inhibits Mechanistic DGIdb
(S)-Α-METHYLHISTAMINE ↑ activates Mechanistic DGIdb
INCB-38579 ↓ inhibits Mechanistic DGIdb
UR-63325 ↓ inhibits Mechanistic DGIdb
IMMEPIP ↑ activates Mechanistic 56.23 nM (EC50) DGIdb
N,N-DIMETHYLHISTAMINE ↑ activates Mechanistic DGIdb
MK-0249 ↓ inhibits Mechanistic DGIdb
[3H]PYRILAMINE ↓ inhibits Mechanistic DGIdb
VUF 8430 ↑ activates Mechanistic DGIdb
IMPROMIDINE ↑ activates Mechanistic 12.3 nM (Ki) DGIdb
[125I]CCL16 (HUMAN) ↑ activates Mechanistic DGIdb
H4 ANTAGONIST 48 ↓ inhibits Mechanistic DGIdb
JNJ-39758979 ↓ inhibits Mechanistic DGIdb
CHEMBL:CHEMBL452847 ? unclear Mechanistic DGIdb
METHIMEPIP ↑ activates Mechanistic 1995.26 nM (Ki) DGIdb
HTMT ↑ activates Mechanistic DGIdb
ST-1006 ↑ activates Mechanistic DGIdb
CHEMBL:CHEMBL454890 ? unclear Mechanistic DGIdb
TOREFORANT ↓ inhibits Mechanistic DGIdb
PITOLISANT ↓ inhibits Mechanistic DGIdb
N-Α-METHYLHISTAMINE ↑ activates Mechanistic DGIdb

Showing top 40 of 144 agents ranked by evidence tier.

IL4R

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
BIZAXOFUSP ? unclear Mechanistic DGIdb
DUPILUMAB ↓ inhibits Mechanistic DGIdb
ROMILKIMAB ? unclear Mechanistic DGIdb
MANFIDOKIMAB ? unclear Mechanistic DGIdb
PITRAKINRA ? unclear Mechanistic DGIdb
SUNITINIB ? unclear Mechanistic DGIdb
CINTREDEKIN BESUDOTOX ? unclear Mechanistic DGIdb
LIGUFALIMAB ? unclear Mechanistic DGIdb
STAPOKIBART ? unclear Mechanistic DGIdb

KIT

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
OSI-930 ? unclear Mechanistic DGIdb
CHMFL-KIT-8140 ↓ inhibits Mechanistic DGIdb
IMATINIB ↓ inhibits Mechanistic 260.0 nM (IC50) DGIdb
PEXIDARTINIB ↓ inhibits Mechanistic DGIdb
REGORAFENIB ↓ inhibits Mechanistic DGIdb
SORAFENIB ↓ inhibits Mechanistic 740.0 nM (Kd) DGIdb
TANDUTINIB ↓ inhibits Mechanistic 170.0 nM (IC50) DGIdb
RIPRETINIB ↓ inhibits Mechanistic DGIdb
XL820 ↓ inhibits Mechanistic DGIdb
VATALANIB ↓ inhibits Mechanistic 730.0 nM (IC50) DGIdb
PAZOPANIB HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
ENMD-2076 ↓ inhibits Mechanistic DGIdb
TRAMETINIB DIMETHYL SULFOXIDE ? unclear Mechanistic DGIdb
PEMBROLIZUMAB ? unclear Mechanistic DGIdb
VELZATINIB ↓ inhibits Mechanistic DGIdb
PONATINIB ? unclear Mechanistic DGIdb
CABOZANTINIB S-MALATE ↓ inhibits Mechanistic DGIdb
CRIZOTINIB ? unclear Mechanistic DGIdb
LABUXTINIB ↓ inhibits Mechanistic DGIdb
BAY 61-3606 ? unclear Mechanistic DGIdb
CATEQUENTINIB ↓ inhibits Mechanistic DGIdb
PLX5622 ↓ inhibits Mechanistic DGIdb
RISVODETINIB ↓ inhibits Mechanistic DGIdb
VENETOCLAX ? unclear Mechanistic DGIdb
XL999 ? unclear Mechanistic DGIdb
EDICOTINIB ↓ inhibits Mechanistic DGIdb
AMUVATINIB ↓ inhibits Mechanistic DGIdb
ILORASERTIB ↓ inhibits Mechanistic DGIdb
AC710 ↓ inhibits Mechanistic DGIdb
LENVATINIB ? unclear Mechanistic DGIdb
AVAPRITINIB ↓ inhibits Mechanistic DGIdb
MOTESANIB ↓ inhibits Mechanistic DGIdb
SU-11652 ↓ inhibits Mechanistic DGIdb
JNJ-28312141 ↓ inhibits Mechanistic DGIdb
RG-1530 ↓ inhibits Mechanistic DGIdb
MASITINIB ↓ inhibits Mechanistic DGIdb
SERALUTINIB ↓ inhibits Mechanistic DGIdb
FAMITINIB ↓ inhibits Mechanistic DGIdb
MIDOSTAURIN ↓ inhibits Mechanistic DGIdb
SORAFENIB TOSYLATE ↓ inhibits Mechanistic DGIdb

Showing top 40 of 278 agents ranked by evidence tier.

MRGPRX2

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
GPR15L ↑ activates Mechanistic DGIdb
PAMP-12 (HUMAN) ↑ activates Mechanistic DGIdb
COMPOUND 2 [PMID: 19230660] ↑ activates Mechanistic DGIdb
SRIF-28 ↑ activates Mechanistic DGIdb
COMPOUND 48/80 ↑ activates Mechanistic DGIdb
ERAS-5024 ↑ activates Mechanistic DGIdb
CORTISTATIN-14 ↑ activates Mechanistic 501.19 nM (EC50) DGIdb
QWF ↓ inhibits Mechanistic DGIdb
PAMP-20 ↑ activates Mechanistic DGIdb
TAN-67 ↑ activates Mechanistic DGIdb
(R)-ZINC-3573 ↑ activates Mechanistic 740.0 nM (EC50) DGIdb
SUBSTANCE P ↑ activates Mechanistic 1071.52 nM (EC50) DGIdb
CHEMBL505263 ↑ activates Mechanistic 1995.26 nM (EC50) ChEMBL
CHEMBL503202 ↑ activates Mechanistic 1258.93 nM (EC50) ChEMBL
CHEMBL502132 ↑ activates Mechanistic 630.96 nM (EC50) ChEMBL
CHEMBL502480 ↑ activates Mechanistic 398.11 nM (EC50) ChEMBL
CHEMBL463274 ↑ activates Mechanistic 316.23 nM (EC50) ChEMBL
CHEMBL503688 ↑ activates Mechanistic 158.49 nM (EC50) ChEMBL
HTL-0022562 ↑ activates Mechanistic 900.0 nM (EC50) ChEMBL
CHEMBL5184300 ↓ inhibits Mechanistic 2.512 nM (IC50) ChEMBL
CHEMBL5184932 ↑ activates Mechanistic 290.0 nM (EC50) ChEMBL
CHEMBL2028997 ↑ activates Mechanistic 2450.0 nM (EC50) ChEMBL
DEXTRORPHAN ↑ activates Mechanistic 6000.0 nM (EC50) ChEMBL
ANALOG OF DYNORPHIN A ↑ activates Mechanistic 1100.0 nM (EC50) ChEMBL
CODEINE ↑ activates Mechanistic 10000.0 nM (EC50) ChEMBL
CHEMBL323503 ↑ activates Mechanistic 15135.61 nM (EC50) ChEMBL
MORPHINE ↑ activates Mechanistic 6606.93 nM (EC50) ChEMBL
LEVOPROPOXYPHENE ↑ activates Mechanistic 31622.78 nM (EC50) ChEMBL
CHEMBL5665367 ↑ activates Mechanistic 13489.63 nM (EC50) ChEMBL
CHEMBL5665410 ↑ activates Mechanistic 13803.84 nM (EC50) ChEMBL
CHEMBL3307199 ↑ activates Mechanistic 9332.54 nM (EC50) ChEMBL
CHEMBL5665374 ↑ activates Mechanistic 5011.87 nM (EC50) ChEMBL
CHEMBL327745 ↑ activates Mechanistic 288.4 nM (EC50) ChEMBL
CHEMBL5665368 ↑ activates Mechanistic 25118.86 nM (EC50) ChEMBL
CHEMBL5665375 ↑ activates Mechanistic 20892.96 nM (EC50) ChEMBL
CHEMBL5665408 ↑ activates Mechanistic 4265.8 nM (EC50) ChEMBL
CHEMBL3343989 ↑ activates Mechanistic 8912.51 nM (EC50) ChEMBL
CHEMBL5192321 ↑ activates Mechanistic 416.87 nM (EC50) ChEMBL
DEXTROMETHORPHAN ↑ activates Mechanistic 5888.44 nM (EC50) ChEMBL
HYDROCODONE ↑ activates Mechanistic 10964.78 nM (EC50) ChEMBL

Showing top 40 of 71 agents ranked by evidence tier.

MS4A2

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
GEMCITABINE ? unclear Mechanistic DGIdb
OMALIZUMAB ? unclear Mechanistic DGIdb
R112 ? unclear Mechanistic DGIdb

Clinical Trials

Drug, biologic and supplement trials (treatment or prevention) from ClinicalTrials.gov whose main condition is Chronic Urticaria (CSU): recruiting, active or completed, most recently updated first. Data retrieved 2026-10-28.

A Study to Evaluate Efficacy of Remibrutinib Compared to Dupilumab at Early Timepoints in Adults With Chronic Spontaneous Urticaria Inadequately Controlled by Second Generation H1-antihistamines Active Not Recruiting
NCT06868212 Phase: 3 Started: 2025-07-11

This is a US, multi-center, randomized, double-blind, double-dummy, Phase 3b study to evaluate efficacy of remibrutinib (25 mg twice daily \[b.i.d.\] by mouth \[p.o.\]) compared to dupilumab (600 mg loading dose administered subcutaneously (s.c.) followed by 300 mg every 2 weeks s.c.) at early timep...

Study of the Efficacy and Safety of ICP-332 in Participants With Chronic Spontaneous Urticaria Recruiting
NCT07378527 Phase: 2/3 Started: 2026-02-13

The purpose of this study is to compare the efficacy and safety of ICP-332 in moderate to severe chronic spontaneous urticaria subjects inadequately controlled by second generation H1-antihistamines

Study of CM512 Injection in Subjects With Chronic Spontaneous Urticaria(CSU) Recruiting
NCT07166211 Phase: 2 Started: 2025-11-27

This study is a multicenter, randomized, double-blind, placebo-controlled phase II clinical study to evaluate the efficacy, safety, pharmacokinetics, pharmacodynamics, and immunogenicity of CM512 in subjects with CSU.

Efficacy of Bilastine Up-dosing (40 mg ) Versus Combination of Bilastine (20 mg )With Levocitirizine (5 mg) in the Treatment of Chronic Spontaneous Urticaria Completed
NCT07365683 Phase: N/A Started: 2025-08-18

This study aims to compare the effectiveness and safety of two commonly used antihistamines, bilastine 20 mg and levocetirizine 5 mg, in patients diagnosed with chronic urticaria. Chronic urticaria is a skin condition characterized by recurrent itchy wheals that significantly affect quality of life....

Modified Xiao-Feng Powder for Chronic Urticaria Completed
NCT04967092 Phase: 2 Started: 2021-08-15

Urticaria is a common skin disorder and 15-25% of people experience at least one attack of urticaria during their lifetime. Urticaria can be divided into acute urticaria (AU) and chronic urticaria (CU). CU is more common in adults, and affects women more frequently than men. According to Chinese med...

A Study to Assess the Efficacy and Safety of AK002 in Subjects With Antihistamine-Resistant Chronic Urticaria Completed
NCT03436797 Phase: 2 Started: 2018-01-23

This is a Phase 2a, open-label study to assess the effects of AK002

Effect of Omalizumab (Xolair) on Basophils in Patients With Chronic Idiopathic Urticaria Completed
NCT01701583 Phase: 4 Started: 2013-04

This study looks at changes in cell proteins in people with chronic hives treated with omalizumab.

Efficacy and Safety Study of Omalizumab (Xolair®) to Treat Chronic Urticaria Completed
NCT01713725 Phase: 2 Started: 2012-03

Chronic urticaria can be defined as the occurrence of widespread daily or almost daily wheals for at least 6 weeks, which may be accompanied by angioedema. While the wheals are transient, the resolution of angioedema is slower than wheals and could take up to 72 hours. The natural course of chronic ...

Methotrexate in the Treatment of Chronic Idiopathic Urticaria Completed
NCT01960283 Phase: 3 Started: 2011-11

Chronic urticaria is defined by urticarial lesions persisting at 6 weeks. The cause is not found in about 75% of cases (chronic idiopathic urticaria). The gold standard treatment consists of anti-H1 molecules. In severe cases, refractory to anti-H1, few therapeutic alternatives exist. Methotrexate, ...

Bilastine Updosing in Chronic Spontaneous Urticaria Completed
NCT02213367 Phase: 3 Started: 2014-07

Chronic spontaneous urticaria (CSU), formerly also known as chronic idiopathic urticaria and chronic urticaria (CU), is one of the most frequent skin diseases. At any time, 0.5-1% of the population suffers from the disease. Although all age groups can be affected, the peak incidence is seen between ...

Agents Found By Disease-Level Search

Searched directly from “Chronic Urticaria (CSU)” via ClinicalTrials.gov interventions and Open Targets' disease→drug data — independent of the 10-gene target panel above. This surfaces agents whose mechanism doesn't route through a curated gene (combination therapies, standard-of-care drugs, targets outside the panel).

53 agents shown (approved or with trial evidence) — 45 not found by the gene-target search above.

Omalizumab

Phase 3 · 13 trials · source: ClinicalTrials.gov, Open Targets
NCT01292473 NCT02477332 NCT06509334

desloratadine

Phase 3 · 8 trials · source: ClinicalTrials.gov, Open Targets
NCT00598611 NCT00598611 NCT00757562

ozureprubart (JYB1904)NOT in gene-target list

· 3 trials · source: ClinicalTrials.gov
NCT07402213 NCT06509334 NCT06509334

LigelizumabNOT in gene-target list

Phase 3 · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT03437278 NCT02649218 NCT03580369

Remibrutinib

Phase 3 · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT07816328 NCT05976243 NCT06868212

Dupilumab SAR231893NOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT04180488 NCT04681729

non sedating H1-antihistamineNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT04180488 NCT04681729

Levocetirizine

Phase 3 · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT00619801 NCT00264303

LOU064NOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT04109313 NCT05795153

rilonacept 160 mgNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT00288704 NCT00288704

Dupilumab

Phase 3 · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT06868212 NCT03749135

LOU064 25 mg (b.i.d)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05030311

LOU064 25 mg (b.i.d) as a tablet.NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05030311

bezuclastinib

· 1 trial · source: ClinicalTrials.gov
NCT04996875

High Dose Vitamin D3NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01371877

Low Dose Vitamin D3NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01371877

ZYIL1 capsuleNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05186051

omalizumab 300 mg every four weeksNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05916937

omalizumab 300 mg every six weeksNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05916937

Stress interventionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01111136

cyclosporine vs azathioprineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03250143

AK006 IVNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06577116

ligelizumab (QGE031)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02477332

rilzabrutinib

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT05107115

HRS-3095 TabletNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07230418

ShotBlocker®NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04210323

IlarisNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06838143

LOU064 (blinded)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05677451

Methotrexate (Novatrex ®) + anti-H1NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01960283

EDP-978NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07540910

Intravenous immunoglobulinsNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01360658

GSK2646264 0.5% topical creamNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02424799

GSK2646264 1% topical creamNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02424799

LP-003 200mgNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06604949

canakinumab (company code: ACZ885D)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01105507

levocetirizine dihydrochloride

· 1 trial · source: ClinicalTrials.gov
NCT00525382

lirentelimab (AK002)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03436797

NatureU Histra DissloveNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07611032

BLU-808NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06931405

DFV890NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04868968

canakinumabNOT in gene-target list

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00991146

drug effectNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07833696

Levocetirizine (as levocetirizine dihydrochloride), 5mg ( then 20 mg) per day . Oral administration.NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02372604

Levocetirizine, (as levocetirizine dihydrochloride) 20 mg ( then 5 mg) per day. Oral administration.NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02372604

QuilizumabNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01987947

5-mg DesloratadineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00536380

10-mg DesloratadineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00536380

20-mg DesloratadineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00536380

barzolvolimab (CDX-0159)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04538794

TEV-45779NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04976192

XOLAIR® InjectionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04976192

Omalizumab 75-375 mgNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00481676

Placebo to omalizumabNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00481676

Generated by the Open Source Medicine Foundation Biomarker Pipeline — 2026-10-08. Data sources: DGIdb, Open Targets, ChEMBL, PubMed, ClinicalTrials.gov. Not medical advice.