Drug ID:Drug12
Drug Name:Caffeine
CID:2519
DrugBank ID:DB00201
Modality:Small Molecule
Groups:approved
US Approved:YES
Other Approved:YES
Identifier: NCT03358706, , NCT02760615
Molecular Formula:C8H10N4O2
Molecular Weight:194.19 g/mol
Isomeric SMILES:CN1C=NC2=C1C(=O)N(C(=O)N2C)C
Synonyms:caffeine; 58-08-2; Guaranine; 1,3,7-Trimethylxanthine; Methyltheobromine; Theine; Thein; Cafeina; Koffein; Mateina
Phase 0: 18
Phase 1: 110
Phase 2: 38
Phase 3: 45
Phase 4: 39
Description:A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes smooth muscle, stimulates cardiac muscle, stimulates diuresis, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide phosphodiesterases, antagonism of adenosine receptors, and modulation of intracellular calcium handling. [PubChem]

Molecular Structure

2D Molecular Structure

Knowledge Graph

dtIDCIDCompound NameGene IDGene NameSpeciesPubMed IDsAction
dt100 2519 Caffeine 5142 PDE4B Homo sapiens (human) None
dt101 2519 Caffeine 747 DAGLA Homo sapiens (human) Activator
dt102 2519 Caffeine 134 ADORA1 Homo sapiens (human) Antagonist
dt103 2519 Caffeine 4907 NT5E Homo sapiens (human) 37713619 Inhibitor
dt104 2519 Caffeine 135 ADORA2A Homo sapiens (human) Antagonist
dt105 2519 Caffeine 136 ADORA2B Homo sapiens (human) 20164566 Antagonist
dt106 2519 Caffeine 140 ADORA3 Homo sapiens (human) 20164566 Antagonist
dt107 2519 Caffeine 5144 PDE4D Homo sapiens (human) Inhibitor
dt108 2519 Caffeine 5140 PDE3B Homo sapiens (human) Inhibitor
dt109 2519 Caffeine 8654 PDE5A Homo sapiens (human) Inhibitor

  • No data available

Phase Distribution
Phase Description
  • Phase 0: Exploratory trials to assess drug behavior in humans
  • Phase 1: Safety trials to determine safe dosage range
  • Phase 2: Efficacy trials to evaluate therapeutic effects
  • Phase 3: Large-scale trials to confirm efficacy and safety
  • Phase 4: Post-marketing surveillance for long-term safety and efficacy

Trial IDTitlePhaseStatusSponsorIndicationsInterventions
NCT03358706 A Study to Evaluate the Effect of Ustekinumab on Cytochrome P450 Enzyme Activities Following Induction and Maintenance Dosing in Participants With Active Crohn's Disease or Ulcerative Colitis PHASE1 TERMINATED Janssen Research & Development, LLC Crohn Disease|Ulcerative Colitis DRUG: Ustekinumab IV Infusion|DRUG: Ustekinumab S… Details
NCT02760615 Phase 4, Vedolizumab-4002 Post-marketing, Disease-Drug-Drug Interaction Study PHASE4 WITHDRAWN Takeda Colitis, Ulcerative|Crohn Disease DRUG: Caffeine|DRUG: Losartan|DRUG: Omeprazole|DR… Details
IRCT20150304021342N2 The effects of dietary modification programme (low-fat, low-carb and high-protein diet) on mood status, fatigue and quality of life in patients with ulcerative colitis Not Available Not Recruiting Esfahan University of Medical Sciences Ulcerative colitis. Ulcerative colitis Intervention 1: Intervention group: Patients who … Details
NCT04624230 Evaluation of Oral Tofacitinib in Children Aged 2 to 17 Years Old Suffering From Moderate to Severe Ulcerative Colitis PHASE3 RECRUITING Pfizer Ulcerative Colitis DRUG: tofacitinib Details
NCT06651281 Extension Study of Long-term Safety and Efficacy of Tulisokibart in Participants With Crohn's Disease or Ulcerative Colitis (MK-7240-011) PHASE3 RECRUITING Merck Sharp & Dohme LLC Crohn Disease|Colitis, Ulcerative DRUG: Tulisokibart|DRUG: Placebo to tulisokibart Details
NCT04857112 Study Evaluating Efficacy and Safety of Amiselimod (MT-1303) in Mild to Moderate Ulcerative Colitis PHASE2 ACTIVE_NOT_RECRUITING Bausch Health Americas, Inc. Ulcerative Colitis DRUG: Low Dose MT-1303|DRUG: High Dose MT-1303|DR… Details
NCT05986136 Activation of Autophagy and Suppression of Apoptosis by Dapagliflozin Attenuates Inflammatory Bowel Disease PHASE2|PHASE3 RECRUITING Mostafa Bahaa Inflammatory Bowel Diseases DRUG: Mesalamine|DRUG: Dapagliflozin 10mg Tab Details
NCT06353828 Phase 2a Study to Evaluate IcBD-01 Enema in Active Ulcerative Colitis Patients PHASE2 ACTIVE_NOT_RECRUITING CannaMore Biotechs Ulcerative Colitis DRUG: CBD, synthetic form|DRUG: Placebo Details
NCT04478825 Efficacy and Safety of Rectally Administered BBT-401-1S in Subjects With Ulcerative Colitis PHASE1 TERMINATED Bridge Biotherapeutics, Inc. Ulcerative Colitis DRUG: BBT-401-1S Details
NCT06570772 Study to Investigate Comparative Efficacy, Safety and Immunogenicity Between AVT16 and Entyvio PHASE3 RECRUITING Alvotech Swiss AG Ulcerative Colitis BIOLOGICAL: AVT16|BIOLOGICAL: Vedolizumab Details
NCT01290042 Study to Evaluate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AMG 181. PHASE1 COMPLETED Amgen Ulcerative Colitis|Crohn's Disease DRUG: AMG 181|OTHER: Placebo for AMG 181 Details
NCT05507203 ABTECT-1 - ABX464 Treatment Evaluation for Ulcerative Colitis Therapy -1 PHASE3 RECRUITING Abivax S.A. Ulcerative Colitis DRUG: ABX464|DRUG: Placebo Details
NCT00207688 A Long Term Safety Study of Infliximab (Remicade) in in Ulcerative Colitis Patients None COMPLETED Janssen Research & Development, LLC Ulcerative Colitis DRUG: Infliximab 5 mg/kg|DRUG: Infliximab 10 mg/k… Details
NCT04677179 A Study of LY3471851 in Adult Participants With Moderately to Severely Active Ulcerative Colitis (UC) PHASE2 TERMINATED Nektar Therapeutics Colitis, Ulcerative DRUG: LY3471851|DRUG: Placebo Details
NCT02611830 Efficacy and Safety of Vedolizumab Subcutaneously (SC) as Maintenance Therapy in Ulcerative Colitis PHASE3 COMPLETED Takeda Colitis, Ulcerative DRUG: Vedolizumab 300 mg IV|DRUG: Placebo IV|DRUG… Details
NCT02958865 Study to Compare Oral PF-06651600, PF-06700841 and Placebo in Subjects With Moderate to Severe Ulcerative Colitis PHASE2 COMPLETED Pfizer Ulcerative Colitis DRUG: PF-06651600 or Placebo|DRUG: PF-06700841 or… Details
NCT06420492 Study of Novel Therapeutics for Acute Remedy of Colitis PHASE2 NOT_YET_RECRUITING Brigham and Women's Hospital Ulcerative Colitis|Ulcerative Colitis Chronic Mod… DRUG: BRS201 Details
NCT03943550 Double-Blinded, Placebo-Controlled Phase 1b Study for Safety, PK, Efficacy, PD of RO7049665 in Participants With Ulcerative Colitis (UC) PHASE1 TERMINATED Hoffmann-La Roche Ulcerative Colitis DRUG: RO7049665|DRUG: Placebo Details
NCT04133194 Adherence of a 1.600 mg Single Tablet 5-ASA Treatment of Ulcerative Colitis PHASE4 RECRUITING Flemming Bendtsen Ulcerative Colitis DRUG: Mesalazine|DRUG: Mesalazine Details
NCT02392221 Impact of Therapeutic Strategies in the Pediatric Inflammatory Bowel Disease: a Population Based Study (1988-2011). None COMPLETED Centre Hospitalier Universitaire, Amiens Pediatric Inflammatory Bowel Disease None Details

Disease IDDisease NameDefinitionCategoryRelated DrugsMechanism
No data available

Strategy IDTherapeutic StrategySynonymsRelated DrugsMechanism
S04 T-cell homing and retention T-cell trafficking vedolizumab; anti-MAdCAM1 antibodies ; etrolizumab Inhibition of the interaction between α4β7 integrins on T c… Details
S06 Anti-fibrosis fibrosis; tissue remodelling GS-5745; STNM01 Tissue remodelling and destruction in patients with IBD is … Details
S07 Blockade of cytokine Cytokine signalling apremilast; roflumilast; filgotinib; tofacitinib; ABT494; ABT-874; ustekinumab; isankizumab; LY-2525623; AMG139; MEDI2079; guselkumab Various T-cell subsets, their differentiation pathways and … Details

Does caffeine have a double-edged sword role in inflammation and carcinogenesis…

PMID: 37072923
Year: 2023
Relationship Type: Association Score: 7.5

Caffeine (1,3,7-trimethylxanthine, also abbreviated to CAF) is a natural chemical with stimulant effects and is commonly included in many drinks and …

Association Between Caffeine Intake and Bowel Habits and Inflammatory Bowel Dis…

PMID: 40600201
Year: 2025
Relationship Type: Association Score: 6.5

BACKGROUND: The effect of caffeine in coffee, a popular beverage, on gastrointestinal symptoms has been the subject of ongoing debate worldwide. The …

Unraveling the link between plasma caffeine concentrations and inflammatory bow…

PMID: 38211690
Year: 2024
Relationship Type: Association Score: 6.5

BACKGROUND: Caffeine is believed to possess anti-inflammatory properties, yet direct population-based evidence regarding its impact on inflammatory b…

Coffee and caffeine intake reduces risk of ulcerative colitis: a case-control s…

PMID: 38073066
Year: 2024
Relationship Type: Association Score: 6.5

BACKGROUND AND AIM: Although diet is one of the potential environmental factors affecting ulcerative colitis (UC), evidence is not sufficient to draw…