Ranitidine

Summary

Ranitidine (CHEMBL1790041) is an approved small molecule (ATC A02BA02) targeting HRH2; indicated across 20 conditions including gastroesophageal reflux disease and peptic ulcer disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A02BA02
• Targets: 1 (HRH2)
• Indications: 20 conditions
• Clinical trials: 49
• Chemistry: 314.41 Da · C13H22N4O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1790041
Name	Ranitidine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5039
ATC	A02BA02
Molecular formula	C13H22N4O3S
Molecular weight	314.41
InChIKey	VMXUWOKSQNHOCA-UHFFFAOYSA-N

SMILES: CNC(=C[N+](=O)[O-])NCCSCC1=CC=C(O1)CN(C)C

IUPAC name: 1-N’-[2-[[5-[(dimethylamino)methyl]furan-2-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine

Also known as: NSC-757851, Ranitidina, Ranitidine, ranitidine, SID11111714, SID11111715, SID11113371, SID90341455, SID104171226, SID124881292, RANITIDINE, SID144203801

Parent form; salt/anhydrous children: CHEMBL2110372, CHEMBL2111286

Patent coverage: 9,096 distinct patent families (30,599 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
HRH2	H2 receptor	Antagonist	7.1		P25021

Broader ChEMBL bioactivity targets: 26 (assay-derived). Sample: Prelamin-A/C, Multidrug and toxin extrusion protein 1, Alpha-2C adrenergic receptor, Histamine H2 receptor, Thyrotropin receptor, Menin/Histone-lysine N-methyltransferase MLL, Potassium-transporting ATPase, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Acetylcholinesterase.

Bioactivity

ChEMBL activities: 29 potent at pChembl ≥ 5 of 42 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ATP4A	7.4	IC50	40	nM	CHEMBL_ACT_992044
P47747	7.27	Ki	53.7	nM	CHEMBL_ACT_76180
HRH2	7.2	Kd	63	nM	CHEMBL_ACT_12456306
P47747	7.19	Kd	64.57	nM	CHEMBL_ACT_1090407
LMNA	7.1	Potency	79.4	nM	CHEMBL_ACT_3621702
HRH2	7.05	Ki	89	nM	CHEMBL_ACT_25011063
P47747	6.77	Kd	169.8	nM	CHEMBL_ACT_85447
HRH2	6.64	AC50	227.5	nM	CHEMBL_ACT_25114345
P47747	6.3	Ki	501.2	nM	CHEMBL_ACT_676987
ACHE	6.19	IC50	650	nM	CHEMBL_ACT_95376
NFKB1	6.15	Potency	707.9	nM	CHEMBL_ACT_3672699
NFKB1	6.15	Potency	707.9	nM	CHEMBL_ACT_4585980
ACHE	6.02	AC50	950	nM	CHEMBL_ACT_25142332
ACHE	5.64	IC50	2300	nM	CHEMBL_ACT_1293353
CHRM2	5.59	AC50	2550	nM	CHEMBL_ACT_25195520
HSD17B10	5.5	Potency	3162	nM	CHEMBL_ACT_4873513
P47747	5.47	IC50	3400	nM	CHEMBL_ACT_225669
HIF1A	5.4	Potency	3981	nM	CHEMBL_ACT_4126948
HIF1A	5.4	Potency	3981	nM	CHEMBL_ACT_4520359
HRH3	5.32	AC50	4800	nM	CHEMBL_ACT_25200249
CHRM1	5.3	AC50	5000	nM	CHEMBL_ACT_25234834
CHRM2	5.25	AC50	5563	nM	CHEMBL_ACT_25195161
Q63921	5.11	AC50	7783	nM	CHEMBL_ACT_25173977
TSHR	5.1	Potency	7943	nM	CHEMBL_ACT_3924770
TSHR	5.1	Potency	7943	nM	CHEMBL_ACT_4619557
SLC47A1	5.08	IC50	8300	nM	CHEMBL_ACT_12637843
CHRM1	5.07	AC50	8600	nM	CHEMBL_ACT_25135021
CHRM3	5.07	AC50	8600	nM	CHEMBL_ACT_25136284
SLC6A4	5.03	AC50	9260	nM	CHEMBL_ACT_25151111

Target pathways

Aggregated over 1 target gene(s): HRH2.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Histamine receptors	1	HRH2
G alpha (s) signalling events	1	HRH2

Dominant GO biological processes

GO term	Targets
gastric acid secretion	1
immune response	1
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
chemical synaptic transmission	1
positive regulation of vasoconstriction	1
signal transduction	1
G protein-coupled receptor signaling pathway	1

Indications & clinical

Indications

20 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
gastroesophageal reflux disease	4	MONDO:0007186	EFO:0003948
peptic ulcer disease	4	MONDO:0004247	HP:0004398
Barrett esophagus	3	MONDO:0013662	EFO:0000280
gastric ulcer	3	MONDO:0001126	EFO:0009454
multiple sclerosis	3	MONDO:0005301	MONDO:0005301
renal cell carcinoma	2	MONDO:0005086	EFO:0000681
T-cell leukemia	2	MONDO:0005525	EFO:0005592
Helicobacter pylori infectious disease	2	MONDO:0006781	EFO:1000961
breast neoplasm	2	MONDO:0021100	MONDO:0007254
breast carcinoma in situ	2	MONDO:0004658	MONDO:0004658
breast carcinoma	2	MONDO:0004989	EFO:0000305
orthostatic hypotension	1	MONDO:0005469	EFO:0005252
peptic esophagitis	1	MONDO:0006896	EFO:1001095
immune system disorder	1	MONDO:0005046	EFO:0000540
neoplasm	1	MONDO:0005070	MONDO:0004992

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

Clinical trials

Total trials: 49.

Phase distribution

Phase	Trials
PHASE1	16
PHASE4	11
PHASE3	9
PHASE2	6
Not specified	6
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00247130	PHASE4	WITHDRAWN	Comparison of Intravenous Omeprazole to Ranitidine on Recurrent Bleeding After Endoscopic Treatment of Bleeding Ulcer
NCT00590928	PHASE4	COMPLETED	Gastric pH in Critically Ill Patients
NCT00702871	PHASE4	COMPLETED	A Clinico-Bacteriological Study and Effect of Stress Ulcer Prophylaxis on Occurrence of Ventilator Associated Pneumonia
NCT01737840	PHASE4	COMPLETED	Comparison of Pantoprazole and Ranitidine in Dyspepsia
NCT01896557	PHASE4	COMPLETED	Ranitidin Versus Omeprazole in Patients Taking Clopidogrel
NCT02123498	PHASE4	WITHDRAWN	The Study of Eustachian Tube Dysfunction and Laryngopharyngeal Reflux
NCT02197143	PHASE4	COMPLETED	A Comparison of Efficacy of Intravenous Esomeprazole and Ranitidine Treatment of Dyspeptic Pain
NCT02205489	PHASE4	COMPLETED	Management Of The Infusion-Associated Reactions In RRMS Patients Treated With LEMTRADA
NCT02441894	PHASE4	COMPLETED	Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer
NCT03145012	PHASE4	COMPLETED	Histamine Receptor 2 Antagonists as Enhancers of Anti-Tumour Immunity
NCT03583567	PHASE4	COMPLETED	Effect of Anti-histamine in Prevention Systolic Hypotension After Protamine
NCT00131248	PHASE3	COMPLETED	Medical Treatment for Gastroesophageal Reflux Disease (GERD) in Preterm Infants
NCT00161200	PHASE3	TERMINATED	Esophageal Metaplasia Using a Novel Antibody: Reversibility by Proton Pump Inhibitor
NCT00401752	PHASE3	COMPLETED	Efficacy and Safety Study of Esomeprazole 20mg qd vs Ranitidine 150mg Bid in Patients With an NSAID-induced Gastric Ulcer
NCT00633412	PHASE3	COMPLETED	A Comparative Efficacy and Safety Study of Nexium Delayed-Release Capsules (40mg qd and 20mg qd) Versus Ranitidine 150mg Bid for the Healing of NSAID-Associated Gastric Ulcers When Daily NSAID Use is Continued in Subjects in the US Only
NCT00633672	PHASE3	COMPLETED	A Comparative Efficacy and Safety Study of Nexium Delayed-Release Capsules (40mg qd and 20mg qd) Versus Ranitidine 150mg Bid for the Healing of NSAID-Associated Gastric Ulcers When Daily NSAID Use is Continued
NCT00668317	PHASE3	TERMINATED	Bronchial Hyper-responsiveness in Reflux Cough
NCT00838526	PHASE3	COMPLETED	Rabeprazole Extended-Release 50 mg vs. Ranitidine 150 mg for Maintenance of Healed Erosive Gastroesophageal Reflux Disease (GERD)
NCT00839306	PHASE3	COMPLETED	Rabeprazole Extended Release 50 mg Versus Ranitidine 150 mg for Maintenance of Healed Erosive Gastroesophageal Reflux Disease (GERD)
NCT03368664	PHASE3	TERMINATED	A Study to Evaluate Efficacy, Safety, and Tolerability of Alemtuzumab in Pediatric Patients With RRMS With Disease Activity on Prior DMT
NCT04862585	PHASE2/PHASE3	COMPLETED	Safely Stopping Pre-medications in Patients With Breast Cancer Who Are Receiving Paclitaxel
NCT00030992	PHASE2	COMPLETED	BMS 247550 to Treat Kidney Cancer
NCT00527878	PHASE2	TERMINATED	Effect of Ranitidine on Hyper-IgE Recurrent Infection (Job’s) Syndrome
NCT01332630	PHASE2	COMPLETED	TPI 287 in Breast Cancer Metastatic to the Brain
NCT02441673	PHASE2	UNKNOWN	Nefopam vs Tramadol in the Prevention of Post Anaesthetic Shivering
NCT02999633	PHASE2	TERMINATED	Safety and Efficacy of Isatuximab in Lymphoblastic Leukemia
NCT03140033	PHASE2	UNKNOWN	Sublingual Misoprostol to Reduce Blood Loss During Elective Cesarean Delivery
NCT02966665	PHASE1	RECRUITING	: Vascular Function in Health and Disease
NCT01131702	PHASE1	COMPLETED	Bioequivalency Study of Ranitidine Tablets 300 mg of Dr. Reddy’s Under Fasting Conditions
NCT01287520	PHASE1	COMPLETED	A Study of LY2090314 in Patients With Advanced or Metastatic Cancer
NCT01392755	PHASE1	COMPLETED	A Study to Evaluate The Effects of Two Different Meal Types, Omeprazole And Ranitidine On Danoprevir Pharmacokinetics When Coadministered With Ritonavir in Healthy Volunteers
NCT01538797	PHASE1	COMPLETED	Effect of Single Doses of YF476 on Stomach Acidity Compared With Ranitidine and Placebo in Fasted and Fed States
NCT01539655	PHASE1	COMPLETED	Study in Healthy Volunteers to Assess Effect of Omeprazole and Ranitidine on the Pharmacokinetics of Vandetanib
NCT01682408	PHASE1	COMPLETED	Assess Pharmacokinetics of Fostamatinib in Fed and Fasted State in Combination With Ranitidine to Assess Bioavailability
NCT01908257	PHASE1	COMPLETED	Lesinurad Interaction Study With Ranitidine
NCT02170792	PHASE1	COMPLETED	Bioavailability of BIBR 953 ZW After Dose of BIBR 1048 MS
NCT02172417	PHASE1	COMPLETED	Tiotropium in Combination With Concomitant Cimetidine or Ranitidine in Healthy Male and Female Subjects
NCT02195804	PHASE1	COMPLETED	Bioavailability Study of Ranitidine Hydrochloride (Maximum Strength ZANTAC 150®) Compared to Two Different 150 mg Ranitidine Hydrochloride Oral Disintegrating Tablet (ODT) in Fasting, Healthy Male Volunteers
NCT03011463	PHASE1	COMPLETED	Pharmacokinetic Interaction Between Trospium With an Inhibitor of OCT1 and of P-gp in Subjects Genotyped for OCT1
NCT03468777	PHASE1	TERMINATED	A Crossover Study to Assess the Drug-drug Interaction of Acid Reducing Agent(s) on the Pharmacokinetics of a Single Oral Dose of Lumicitabine (JNJ-64041575) in Healthy Adult Participants

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

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.

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

Molecule	Source	Status	Shared targets
Cinacalcet	ChEMBL + PubChem	Phase 4 (approved)	HRH2
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	HRH2
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	HRH2
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	HRH2
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	HRH2
LINAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	HRH2
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	HRH2
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	HRH2
PRAMIPEXOLE	ChEMBL + PubChem	Phase 4 (approved)	HRH2
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	HRH2
AMIODARONE	ChEMBL	Phase 4 (approved)	HRH2
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	HRH2
AMLODIPINE	ChEMBL	Phase 4 (approved)	HRH2
AMOXAPINE	ChEMBL	Phase 4 (approved)	HRH2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	HRH2
ASENAPINE	ChEMBL	Phase 4 (approved)	HRH2
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	HRH2
BENZTROPINE	ChEMBL	Phase 4 (approved)	HRH2
BETAZOLE	ChEMBL	Phase 4 (approved)	HRH2
BOSUTINIB	ChEMBL	Phase 4 (approved)	HRH2
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	HRH2
CABERGOLINE	ChEMBL	Phase 4 (approved)	HRH2
CARVEDILOL	ChEMBL	Phase 4 (approved)	HRH2
CETIRIZINE	ChEMBL	Phase 4 (approved)	HRH2
CHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	HRH2
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	HRH2
CIMETIDINE	ChEMBL	Phase 4 (approved)	HRH2
CITALOPRAM	ChEMBL	Phase 4 (approved)	HRH2
CLEMASTINE	ChEMBL	Phase 4 (approved)	HRH2
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	HRH2
CLONIDINE	ChEMBL	Phase 4 (approved)	HRH2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	HRH2
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	HRH2
DARIFENACIN	ChEMBL	Phase 4 (approved)	HRH2
DEXCHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	HRH2
DICYCLOMINE	ChEMBL	Phase 4 (approved)	HRH2
DILTIAZEM	ChEMBL	Phase 4 (approved)	HRH2
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	HRH2
DOXAZOSIN	ChEMBL	Phase 4 (approved)	HRH2
DOXEPIN	ChEMBL	Phase 4 (approved)	HRH2
DYCLONINE	ChEMBL	Phase 4 (approved)	HRH2
EBASTINE	ChEMBL	Phase 4 (approved)	HRH2
ECONAZOLE	ChEMBL	Phase 4 (approved)	HRH2
ENCAINIDE	ChEMBL	Phase 4 (approved)	HRH2
FAMOTIDINE	ChEMBL	Phase 4 (approved)	HRH2
FLUOXETINE	ChEMBL	Phase 4 (approved)	HRH2
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	HRH2
GENTIAN VIOLET	ChEMBL	Phase 4 (approved)	HRH2
HALOPERIDOL	ChEMBL	Phase 4 (approved)	HRH2
HISTAMINE	ChEMBL	Phase 4 (approved)	HRH2
HYDROXYZINE	ChEMBL	Phase 4 (approved)	HRH2
IMATINIB	ChEMBL	Phase 4 (approved)	HRH2
IMIPRAMINE	ChEMBL	Phase 4 (approved)	HRH2
IMIQUIMOD	ChEMBL	Phase 4 (approved)	HRH2
INDOCYANINE GREEN ACID FORM	ChEMBL	Phase 4 (approved)	HRH2
IPRINDOLE	ChEMBL	Phase 4 (approved)	HRH2
KETOCONAZOLE	ChEMBL	Phase 4 (approved)	HRH2
KETOTIFEN	ChEMBL	Phase 4 (approved)	HRH2
LANSOPRAZOLE	ChEMBL	Phase 4 (approved)	HRH2
LOPERAMIDE	ChEMBL	Phase 4 (approved)	HRH2