| Drug ID: | Drug121 |
|---|---|
| Drug Name: | Apremilast |
| CID: | 11561674 |
| DrugBank ID: | DB05676 |
| Modality: | Small Molecule |
| Groups: | NULL |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT02289417 |
| Molecular Formula: | C22H24N2O7S |
| Molecular Weight: | 460.5 g/mol |
| Isomeric SMILES: | CCOC1=C(C=CC(=C1)[C@@H](CS(=O)(=O)C)N2C(=O)C3=C(C2=O)C(=CC=C3)NC(=O)C)OC |
| Synonyms: | Apremilast; 608141-41-9; OTEZLA; CHEBI:78540; apremilastum; UNII-UP7QBP99PN; UP7QBP99PN; HSDB 8221; N-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide; Acetamide, N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)- |
| Phase 0: | 1 |
| Phase 1: | 30 |
| Phase 2: | 55 |
| Phase 3: | 48 |
| Phase 4: | 30 |
| Description: | NULL |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt1002 | 11561674 | Apremilast | 5142 | PDE4B | Homo sapiens (human) | Inhibitor | |
| dt1003 | 11561674 | Apremilast | 5141 | PDE4A | Homo sapiens (human) | Inhibitor | |
| dt1004 | 11561674 | Apremilast | 5144 | PDE4D | Homo sapiens (human) | Inhibitor | |
| dt1005 | 11561674 | Apremilast | 5142 | PDE4B | Homo sapiens (human) | None | |
| dt1006 | 11561674 | Apremilast | 5144 | PDE4D | Homo sapiens (human) | 24882690 | Inhibition |
| dt1007 | 11561674 | Apremilast | 5141 | PDE4A | Homo sapiens (human) | 24882690 | Inhibition |
| dt1008 | 11561674 | Apremilast | 5142 | PDE4B | Homo sapiens (human) | 24882690 | Inhibition |
| dt1009 | 11561674 | Apremilast | 5143 | PDE4C | Homo sapiens (human) | 24882690 | Inhibition |
| dt1010 | 11561674 | Apremilast | 1019 | CDK4 | Homo sapiens (human) | 37713619 | Inhibitor |
| dt1011 | 11561674 | Apremilast | 1021 | CDK6 | Homo sapiens (human) | 37713619 | 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 ID | Title | Phase | Status | Sponsor | Indications | Interventions | |
|---|---|---|---|---|---|---|---|
| NCT02289417 | Efficacy and Safety Study of Apremilast to Treat Active Ulcerative Colitis | PHASE2 | COMPLETED | Amgen | Ulcerative Colitis | DRUG: Apremilast|DRUG: Placebo | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| 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 |
Early Discontinuation of Apremilast in Patients with Psoriasis and Gastrointest…
PMID: 37517029
Year: 2023
Relationship Type:
Treatment
Score: 6.5
INTRODUCTION: Apremilast, the first oral targeted treatment for moderate to severe psoriasis, is associated with diarrhea, nausea, and vomiting, whic…
The Influence of Apremilast-Induced Macrophage Polarization on Intestinal Wound…
PMID: 37240465
Year: 2023
Relationship Type:
Mechanism
Score: 6.5
There is compelling evidence suggesting a pivotal role played by macrophages in orchestrating intestinal wound healing. Since macrophages display sig…
Multifunctional nanoparticles based on marine polysaccharides for apremilast de…
PMID: 36179875
Year: 2022
Relationship Type:
Mechanism
Score: 6.5
Hydrophobic drug encapsulation inside targeted nanoparticles can enhance accumulation in inflamed sites, limit toxicity to healthy tissue, and improv…