Apremilast
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Also known as Apremilast accordCC-10004CC10004OtezlaAPREMILAST (CC-10004)
Summary
Apremilast (CHEMBL514800) is an approved small-molecule phosphodiesterase IV inhibitor (ATC L04AA32) targeting PDE4A, PDE4B, and PDE4C; indicated across 30 conditions including behcet disease and psoriasis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L04AA32
- Targets: 4 (PDE4A, PDE4B, PDE4C…)
- Indications: 30 conditions
- Clinical trials: 137
- Chemistry: 460.5 Da · C22H24N2O7S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL514800 |
| Name | Apremilast |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 11561674 |
| ChEBI | CHEBI:78540 |
| ATC | L04AA32 |
| Molecular formula | C22H24N2O7S |
| Molecular weight | 460.5 |
| InChIKey | IMOZEMNVLZVGJZ-QGZVFWFLSA-N |
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
IUPAC name: N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-1,3-dioxoisoindol-4-yl]acetamide
ChEBI definition: A member of the class of isoindoles that is isoindole-1,3-dione substituted at position 4 by an acetamido group and at position 1 by a 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl group. Used for treatment of psoriatic arthritis.
Pharmacological roles (ChEBI): phosphodiesterase IV inhibitor, non-steroidal anti-inflammatory drug.
Also known as: Apremilast, Apremilast accord, CC-10004, CC10004, Otezla, APREMILAST, APREMILAST (CC-10004), Apremilast (CC-10004), apremilast
Patent coverage: 1,790 distinct patent families (4,576 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 3,967 (87%) 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 |
|---|---|---|---|---|---|
| PDE4A | phosphodiesterase 4A | Inhibition | 7.85 | 0.4% | P27815 |
| PDE4B | phosphodiesterase 4B | Inhibition | 7.57 | 0.2% | Q07343 |
| PDE4C | phosphodiesterase 4C | Inhibition | 6.93 | 0.2% | Q08493 |
| PDE4D | phosphodiesterase 4D | Inhibition | 7.48 | 0.7% | Q08499 |
Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Phosphodiesterase 4, 3’,5’-cyclic-AMP phosphodiesterase 4B, 3’,5’-cyclic-AMP phosphodiesterase 4D.
Bioactivity
ChEMBL activities: 21 potent at pChembl ≥ 5 of 21 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PDE4D | 8.57 | AC50 | 2.7 | nM | CHEMBL_ACT_25185835 |
| PDE4D | 8 | IC50 | 10 | nM | CHEMBL_ACT_26023300 |
| PDE4B | 7.78 | IC50 | 16.5 | nM | CHEMBL_ACT_27970964 |
| PDE4B | 7.62 | IC50 | 24 | nM | CHEMBL_ACT_19231008 |
| PDE4B | 7.57 | IC50 | 27 | nM | CHEMBL_ACT_19221559 |
| PDE4B | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_18172478 |
| PDE4D | 7.49 | IC50 | 32.44 | nM | CHEMBL_ACT_26196246 |
| PDE4D | 7.48 | IC50 | 33 | nM | CHEMBL_ACT_19221560 |
| PDE4D | 7.46 | IC50 | 35 | nM | CHEMBL_ACT_19231174 |
| PDE4D | 7.32 | IC50 | 47.6 | nM | CHEMBL_ACT_20636038 |
| PDE4D | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_19233917 |
| PDE4B | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_22838527 |
| PDE4A | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_22875410 |
| PDE4A | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_2608001 |
| PDE4A | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_26122704 |
| PDE4D | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_29201686 |
| PDE4D | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_29243148 |
| PDE4A | 6.96 | IC50 | 110 | nM | CHEMBL_ACT_19233921 |
| PDE4D | 6.3 | IC50 | 500 | nM | CHEMBL_ACT_25527385 |
| PDE4D | 6.27 | IC50 | 540 | nM | CHEMBL_ACT_19263185 |
| HTR2B | 5.35 | AC50 | 4500 | nM | CHEMBL_ACT_25227997 |
Target pathways
Aggregated over 4 target gene(s): PDE4A, PDE4B, PDE4C, PDE4D.
Top Reactome pathways
3 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| DARPP-32 events | 4 | PDE4A, PDE4B, PDE4C, PDE4D |
| G alpha (s) signalling events | 3 | PDE4A, PDE4C, PDE4D |
| Turbulent (oscillatory, disturbed) flow shear stress activates signaling by PIEZO1 and integrins in endothelial cells | 1 | PDE4D |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cAMP catabolic process | 4 |
| signal transduction | 4 |
| negative regulation of cAMP/PKA signal transduction | 4 |
| cellular response to xenobiotic stimulus | 2 |
| positive regulation of type II interferon production | 2 |
| positive regulation of interleukin-2 production | 2 |
| T cell receptor signaling pathway | 2 |
| cellular response to epinephrine stimulus | 2 |
| regulation of cardiac muscle cell contraction | 2 |
| negative regulation of relaxation of cardiac muscle | 2 |
| regulation of calcium ion transmembrane transport via high voltage-gated calcium channel | 2 |
| G protein-coupled receptor signaling pathway | 1 |
| sensory perception of smell | 1 |
| regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway | 1 |
| regulation of cAMP/PKA signal transduction | 1 |
Indications & clinical
Indications
4 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| Behcet disease | 4 | MONDO:0007191 | EFO:0003780 |
| psoriasis | 4 | MONDO:0005083 | EFO:0000676 |
| psoriatic arthritis | 4 | MONDO:0011849 | EFO:0003778 |
| immune system disorder | 4 | MONDO:0005046 | EFO:0000540 |
22 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| ankylosing spondylitis | 3 | MONDO:0005306 | EFO:0003898 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| pneumonia | 3 | MONDO:0005249 | EFO:0003106 |
| influenza | 3 | MONDO:0005812 | EFO:0007328 |
| atopic eczema | 2 | MONDO:0004980 | EFO:0000274 |
| rheumatoid arthritis | 2 | MONDO:0008383 | EFO:0000685 |
| acne | 2 | MONDO:0011438 | EFO:0003894 |
| ulcerative colitis | 2 | MONDO:0005101 | EFO:0000729 |
| gout | 2 | MONDO:0005393 | EFO:0004274 |
| prostatitis | 2 | MONDO:0005280 | EFO:0003830 |
| rosacea | 2 | MONDO:0006604 | EFO:1000760 |
| hidradenitis suppurativa | 2 | MONDO:0006559 | EFO:1000710 |
| lichen planus | 2 | MONDO:0006572 | EFO:1000726 |
| vitiligo | 2 | MONDO:0008661 | EFO:0004208 |
| allergic contact dermatitis | 2 | MONDO:0006525 | EFO:1000668 |
| dermatomyositis | 2 | MONDO:0016367 | EFO:0000398 |
| lichen planus, oral | 2 | MONDO:0043923 | EFO:0008517 |
| dermatitis | 2 | MONDO:0002406 | MONDO:0002406 |
| alcohol abuse | 2 | MONDO:0002046 | MONDO:0007079 |
| erythema multiforme | 2 | MONDO:0006545 | EFO:1000694 |
| uveitis | 1 | MONDO:0020283 | EFO:1001231 |
| discoid lupus erythematosus | 1 | MONDO:0019558 | MONDO:0019558 |
4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 137.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 45 |
| PHASE3 | 35 |
| PHASE4 | 28 |
| Not specified | 16 |
| PHASE1 | 8 |
| PHASE1/PHASE2 | 3 |
| PHASE2/PHASE3 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT07352566 | PHASE4 | NOT_YET_RECRUITING | Utilization of a Microdevice for Psoriasis and Atopic Dermatitis |
| NCT07432386 | PHASE4 | NOT_YET_RECRUITING | Methotrexate Versus Apremilast for Pruritus in Psoriasis |
| NCT02144857 | PHASE4 | UNKNOWN | Effects of Treatment With Biological Agents on Vascular and Cardiac Function in Psoriasis |
| NCT02400749 | PHASE4 | COMPLETED | Apremilast in Palmo-Plantar Psoriasis |
| NCT02412644 | PHASE4 | COMPLETED | Apremilast 30mg Bid With Narrowband UVB in the Treatment of Plaque Psoriasis |
| NCT02425826 | PHASE4 | COMPLETED | A Phase 4 Study of Efficacy and Safety of Apremilast in Subjects With Moderate Plaque Psoriasis. |
| NCT02558361 | PHASE4 | WITHDRAWN | Treatment With Apremilast in Patients With Psoriatic Arthritis |
| NCT03000309 | PHASE4 | COMPLETED | Use of Apremilast in Patients Who Are Dissatisfied With Stable Maintenance Topical Therapy |
| NCT03022617 | PHASE4 | COMPLETED | A Study Evaluating the Efficacy and Tolerability of Oral Apremilast for the Treatment of Nail Psoriasis |
| NCT03082729 | PHASE4 | COMPLETED | Vascular Inflammation in Psoriasis - Apremilast |
| NCT03422640 | PHASE4 | UNKNOWN | Trial Evaluating the Efficacy of Apremilast for the Treatment of Frontal Fibrosing Alopecia |
| NCT03441789 | PHASE4 | COMPLETED | Efficacy and Safety of Enstilar Foam in Combination With Apremilast (Otezla) in Patients With Moderate Plaque Psoriasis |
| NCT03453190 | PHASE4 | UNKNOWN | Apremilast in Combination With Clobetasol Spray for the Treatment of Plaque Psoriasis |
| NCT03521687 | PHASE4 | COMPLETED | Apremilast in the Treatment of Central Centrifugal Cicatricial Alopecia (CCCA) |
| NCT03553433 | PHASE4 | UNKNOWN | Apremilast Treatment for Pruritus and Quality of Life in Scalp Psoriasis |
| NCT03587194 | PHASE4 | COMPLETED | Evaluation of Add on Enstilar in Patients Using Otezla for Psoriasis |
| NCT03690544 | PHASE4 | COMPLETED | Apremilast for RAS |
| NCT03741933 | PHASE4 | WITHDRAWN | Apremilast and Moderate to Severe Chronic Hand Dermatitis |
| NCT03747939 | PHASE4 | COMPLETED | Efficacy, Safety, and Tolerability Study of Apremilast to Treat Early Oligoarticular Psoriatic Arthritis. |
| NCT03774875 | PHASE4 | COMPLETED | A Study of the Impact of Apremilast (CC-10004) on Quality of Life, Efficacy, and Safety in Adults With Manifestations of Plaque Psoriasis and Impaired Quality of Life |
| NCT03783026 | PHASE4 | COMPLETED | A Study to Evaluate the Impact of Apremilast on Magnetic Resonance Imaging (MRI) Outcomes in Adults With Psoriatic Arthritis |
| NCT04102449 | PHASE4 | WITHDRAWN | Validation of the PsASon ULtrasound Scores in Patients With Psoriatic Arthritis Undergoing TReatment With Apremilast |
| NCT04515732 | PHASE4 | UNKNOWN | Danish Population-based Assessment of Psoriasis and Psoriatic Arthritis (DANPAPP) |
| NCT04555707 | PHASE4 | UNKNOWN | The Maintenance Effect of Enstilar Foam in Combination With Otezla |
| NCT04908475 | PHASE4 | COMPLETED | Study of Subcutaneous Risankizumab Injection Compared to Oral Apremilast Tablets to Assess Change in Disease Activity And Adverse Events in Adult Participants With Moderate Plaque Psoriasis Who Are Candidates for Systemic Therapy |
| NCT05926882 | PHASE4 | COMPLETED | Efficacy of Oral Apremilast in the Treatment of Alopecia Areata at the Tertiary Care Hospital, Karachi. |
| NCT06032858 | PHASE4 | COMPLETED | Efficacy and Safety of Apremilast in Psoriasis |
| NCT06260904 | PHASE4 | COMPLETED | Efficacy and Safety of add-on Apremilast Versus add-on Methotrexate in Patients With Oral Lichen Planus |
| NCT02735707 | PHASE3 | RECRUITING | Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia |
| NCT04227314 | PHASE3 | RECRUITING | Randomized Double Blind Controlled Trial Comparing the Safety and Efficacy of Apremilast Versus Placebo in Severe Forms of Recurrent Aphthous Stomatitis |
| NCT04528082 | PHASE3 | RECRUITING | Apremilast Pediatric Study in Children With Active Oral Ulcers Associated With Behçet’s Disease |
| NCT04804553 | PHASE3 | RECRUITING | Apremilast Pediatric Study in Children With Active Juvenile Psoriatic Arthritis |
| NCT04908189 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Determine the Efficacy and Safety of Deucravacitinib Compared With Placebo in Participants With Active Psoriatic Arthritis (PsA) Who Are Naïve to Biologic Disease Modifying Anti-rheumatic Drugs or Had Previously Received TNFα Inhibitor Treatment |
| NCT05565560 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Assess the Efficacy and Safety of Apremilast in Japanese Pediatric Participants With Moderate to Severe Plaque Psoriasis |
| NCT05767047 | PHASE3 | RECRUITING | A Study of Apremilast in Children With Oral Ulcers Associated With Behçet’s Disease or Juvenile Psoriatic Arthritis |
| NCT06088199 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Apremilast in Pediatric Participants in Children With Mild to Moderate Plaque Psoriasis |
| NCT06863493 | PHASE2/PHASE3 | NOT_YET_RECRUITING | Comparison of Otezla to SFA-002 to Placebo in Plaque Psoriasis Patients |
| NCT01172938 | PHASE3 | COMPLETED | Efficacy and Safety Study of Apremilast to Treat Active Psoriatic Arthritis |
| NCT01194219 | PHASE3 | COMPLETED | Study to Evaluate Safety and Effectiveness of Oral Apremilast (CC-10004) in Patients With Moderate to Severe Plaque Psoriasis |
| NCT01212757 | PHASE3 | COMPLETED | PALACE 2: Efficacy and Safety Study of Apremilast to Treat Active Psoriatic Arthritis |
| NCT01212770 | PHASE3 | COMPLETED | PALACE 3: Efficacy and Safety Study of Apremilast to Treat Active Psoriatic Arthritis |
| NCT01232283 | PHASE3 | COMPLETED | Study to Evaluate Safety and Effectiveness of Oral Apremilast (CC-10004) in Patients With Moderate to Severe Plaque Psoriasis. |
| NCT01307423 | PHASE3 | COMPLETED | Efficacy and Safety Study of Apremilast to Treat Active Psoriatic Arthritis (PsA) |
| NCT01690299 | PHASE3 | COMPLETED | Phase 3b Safety and Efficacy Study of Apremilast to Treat Moderate to Severe Plaque-plaque Psoriasis |
| NCT01925768 | PHASE3 | COMPLETED | Safety and Efficacy Study of Apremilast to Treat Psoriatic Arthritis |
| NCT02307513 | PHASE3 | COMPLETED | A Phase 3 Randomized, Double-blind Study to Evaluate the Efficacy and Safety of Apremilast (CC-10004) in Subjects With Active Behçet’s Disease |
| NCT03123471 | PHASE3 | COMPLETED | A Study of the Efficacy and Safety of Apremilast (CC-10004) in Subjects With Moderate to Severe Plaque Psoriasis of the Scalp |
| NCT03168256 | PHASE3 | COMPLETED | CF101 Therapy in Patients With Moderate-to-severe Plaque Psoriasis |
| NCT03191539 | PHASE3 | UNKNOWN | Assessment of the Clinical and Ultrasound Response to Apremilast by Clinical Evaluation and by a Joint-periarticular-nail Ultrasound Index in Patients With Active Psoriatic Arthritis |
| NCT03611751 | PHASE3 | COMPLETED | An Investigational Study to Evaluate Experimental Medication BMS-986165 Compared to Placebo and a Currently Available Treatment in Participants With Moderate-to-Severe Plaque Psoriasis |
| NCT03624127 | PHASE3 | COMPLETED | Effectiveness and Safety of BMS-986165 Compared to Placebo and Active Comparator in Participants With Psoriasis |
| NCT03701763 | PHASE3 | COMPLETED | Efficacy and Safety Study of Apremilast (CC-10004) in Pediatric Subjects From 6 Through 17 Years of Age With Moderate to Severe Plaque Psoriasis |
| NCT03721172 | PHASE3 | COMPLETED | Apremilast as a Direct Treatment for Mild-to-moderate Plaque Psoriasis Versus Placebo: an Analysis of Clinical Safety and Efficacy |
| NCT03777436 | PHASE3 | COMPLETED | An Efficacy and Safety Study of Apremilast (CC-10004) in Subjects With Moderate to Severe Genital Psoriasis |
| NCT03930186 | PHASE3 | COMPLETED | A Phase 3B, Open-label, Single-arm Study of the Efficacy and Safety of Apremilast, in Subjects With Plaque Psoriasis That is Not Adequately Controlled by Topical Therapy |
| NCT04175613 | PHASE3 | COMPLETED | A Long-term Extension Study of Apremilast (CC-10004) in Pediatric Subjects From 6 Through 17 Years of Age With Moderate to Severe Plaque Psoriasis |
| NCT04590586 | PHASE3 | COMPLETED | Study of Multiple Candidate Agents for the Treatment of COVID-19 in Hospitalized Patients |
| NCT04610476 | PHASE3 | UNKNOWN | Impact of Tapering Immunosuppressants on Maintaining Minimal Disease Activity in Adult Subjects With Psoriatic Arthritis |
| NCT05174065 | PHASE3 | COMPLETED | Phase 3, Randomized Study of Apremilast in Japanese Participants With Palmoplantar Pustulosis (PPP) |
| NCT06088043 | PHASE3 | COMPLETED | A Study About How Well TAK-279 Works and Its Safety in Participants With Moderate-to-severe Plaque Psoriasis During 52 Weeks of Treatment |
| NCT06108544 | PHASE3 | COMPLETED | A Study About How Well TAK-279 Works and Its Safety in Participants With Moderate-to-severe Plaque Psoriasis During 60 Weeks of Treatment With a Withdrawal and Retreatment Period |
| NCT06122649 | PHASE3 | COMPLETED | A Study to Investigate Efficacy and Safety of Apremilast 30 mg Twice Daily (BID) in Chinese Participants With Moderate to Severe Plaque-type Psoriasis (PsO) |
| NCT06586112 | PHASE3 | COMPLETED | A Study to Evaluate the Efficacy and Safety of ESK-001 in Patients With Moderate to Severe Plaque Psoriasis |
| NCT06588738 | PHASE3 | COMPLETED | A Study in Patients With Moderate to Severe Plaque Psoriasis to Evaluate the Efficacy and Safety of ESK-001 |
| NCT04488081 | PHASE2 | ACTIVE_NOT_RECRUITING | I-SPY COVID-19 TRIAL: An Adaptive Platform Trial for Critically Ill Patients |
| NCT06509984 | PHASE2 | RECRUITING | A 20-Week Study Assessing the Efficacy of Apremilast in Patients with EB Simplex Generalized |
| NCT07029529 | PHASE2 | RECRUITING | Phase 2 Study of Apremilast in Women and Men With Alcohol Use Disorder |
| NCT07325266 | PHASE2 | RECRUITING | Human Laboratory Study of Apremilast for Alcohol Use Disorder |
| NCT00456092 | PHASE2 | COMPLETED | Phase II Study of Apremilast (CC-10004) in Adults With in Psoriatic Arthritis |
| NCT00521339 | PHASE2 | COMPLETED | Apremilast Safety and PK Study in Recalcitrant Plaque Psoriasis |
| NCT00604682 | PHASE2 | COMPLETED | Open-Label,Single-Arm Pilot Study to Evaluate the Pharmacodynamics, Pharmacokinetics, Safety, and Preliminary Efficacy of CC1004 in Subjects With Severe Plaque Type Psoriasis |
| NCT00606450 | PHASE2 | COMPLETED | Double-Blind, Randomized, Placebo-controlled Comparison of CC-10004 in Subjects With Moderate to Severe Plaque Type Psoriasis |
| NCT00701311 | PHASE2 | COMPLETED | An Open-Label Study of CC-10004 for Chronic Prostatitis/Chronic Pelvic Pain Syndrome |
| NCT00708916 | PHASE1/PHASE2 | COMPLETED | Safety Study of Clinical and Immune Effects of Phosphodiesterase 4 (PDE-4) Inhibitor in Cutaneous Lupus Patients |
| NCT00773734 | PHASE2 | COMPLETED | Efficacy and Safety Study of Apremilast (CC-10004) in Subjects With Moderate-to-Severe Plaque-Type Psoriasis (Core Study) |
| NCT00814632 | PHASE2 | COMPLETED | CC-10004 For The Treatment Of Vulvodynia |
| NCT00866359 | PHASE2 | COMPLETED | A Study to Evaluate the Efficacy and Safety of Apremilast (CC-10004) in the Treatment of Behçet Disease |
| NCT00869089 | PHASE2 | COMPLETED | Safety and Efficacy of CC-10004 for Prurigo Nodularis |
| NCT00889421 | PHASE1/PHASE2 | TERMINATED | Apremilast in the Treatment of Uveitis |
| NCT00931242 | PHASE2 | COMPLETED | Study of Apremilast in Atopic or Contact Dermatitis |
| NCT00944658 | PHASE2 | COMPLETED | Spondylitis Trial of Apremilast for Better Rheumatic Therapy |
| NCT00997581 | PHASE2 | WITHDRAWN | Apremilast Therapy for Acute Gouty Arthritis |
| NCT01041625 | PHASE2 | UNKNOWN | Pilot Study of Apremilast (CC-10004) in the Treatment of Moderate to Severe Lichen Planus |
| NCT01045551 | PHASE2 | COMPLETED | Open Label Pilot Study of Apremilast in Treatment of Rosacea |
| NCT01074502 | PHASE2 | TERMINATED | Apremilast in the Treatment of Moderate to Severe Acne |
| NCT01200264 | PHASE2 | WITHDRAWN | Apremilast for Chronic Plaque Psoriasis (CPP) Patients Who Have Failed One Course of Biologic Therapy |
| NCT01200472 | PHASE2 | COMPLETED | Efficacy Study of Apremilast (CC-10004) in Subjects With Erosive Hand Osteoarthritis |
| NCT01204138 | PHASE2 | WITHDRAWN | Concomitant Use of Apremilast for the Treatment of Active RA Despite TNF-Inhibition and Methotrexate- CATARA |
| NCT01250548 | PHASE2 | COMPLETED | The Controlled Trial of Apremilast for Rheumatoid Arthritis Treatment (CARAT) |
| NCT01285310 | PHASE2 | TERMINATED | Study of Apremilast to Evaluate the Safety and Effectiveness for Patients With Rheumatoid Arthritis |
| NCT01393158 | PHASE2 | COMPLETED | Apremilast for Atopic Dermatitis - A Pilot Study in Adults |
| NCT01988103 | PHASE2 | COMPLETED | Efficacy and Safety Study of Two Doses of Apremilast (CC-10004) In Japanese Patients With Moderate-To-Severe Plaque-Type Psoriasis |
| NCT02087943 | PHASE2 | COMPLETED | Efficacy and Safety Study of Apremilast in Subjects With Moderate to Severe Atopic Dermatitis |
| NCT02289417 | PHASE2 | COMPLETED | Efficacy and Safety Study of Apremilast to Treat Active Ulcerative Colitis |
| NCT02576678 | PHASE2 | COMPLETED | A Study of Safety, Tolerability and Pharmacokinetics of Apremilast (CC-10004) in Pediatric Subjects With Moderate to Severe Plaque Psoriasis |
| NCT02695212 | PHASE2 | COMPLETED | Single Center Study of Apremilast for the Treatment of Hidradenitis Suppurativa |
| NCT03036995 | PHASE2 | COMPLETED | Repigmentation Using Apremilast and Phototherapy In Diffuse VITILIGO |
| NCT03049267 | PHASE2 | COMPLETED | Short-term Safety, Efficacy and Mode of Action of Apremilast in Moderate Suppurative Hidradenitis |
| NCT03123016 | PHASE2 | COMPLETED | Combined Therapy With Narrow-Band Ultraviolet B Phototherapy and Apremilast for the Treatment of Vitiligo |
| NCT03160248 | PHASE2 | COMPLETED | An Investigator-initiated Study of Apremilast to Demonstrate Efficacy Nummular Eczema |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 10 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.
362 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| TADALAFIL | ChEMBL + PubChem | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| CRISABOROLE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| DIPYRIDAMOLE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| ENOXIMONE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| ENSIFENTRINE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| IBUDILAST | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| INAMRINONE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| LOSARTAN | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| MILRINONE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| PENTOXIFYLLINE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| ROFLUMILAST | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| SILDENAFIL | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| THEOPHYLLINE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| VARDENAFIL | ChEMBL | Phase 4 (approved) | PDE4A, PDE4B, PDE4C, PDE4D |
| CILOMILAST | ChEMBL | Phase 3 | PDE4A, PDE4B, PDE4C, PDE4D |
| MUFEMILAST | ChEMBL | Phase 3 | PDE4A, PDE4B, PDE4C, PDE4D |
| PAPAVERINE | ChEMBL | Phase 3 | PDE4A, PDE4B, PDE4C, PDE4D |
| TETOMILAST | ChEMBL | Phase 3 | PDE4A, PDE4B, PDE4C, PDE4D |
| ADIBENDAN | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| AZD-6482 | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| BMS-911543 | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| CDC-801 | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| CIPAMFYLLINE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| DENBUFYLLINE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| ENPROFYLLINE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| IMAZODAN | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| INDOLIDAN | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| LIXAZINONE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| LOTAMILAST | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| MK-0873 | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| NITRAQUAZONE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| PELRINONE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| PICLAMILAST | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| PUMAFENTRINE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| REVAMILAST | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| ROLIPRAM | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| STREPTONIGRIN | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| TOCLADESINE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| TRANIMILAST | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| TREQUINSIN | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| ZAPRINAST | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| ZARDAVERINE | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4C, PDE4D |
| ORISMILAST | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4D |
| TOFIMILAST | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4D |
| UK-500001 | ChEMBL | Phase 2 | PDE4A, PDE4B, PDE4D |
| BELINOSTAT | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| ETHINYL ESTRADIOL | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| GLAFENINE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| ISTRADEFYLLINE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| LAROPIPRANT | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| OXYBENZONE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| PALBOCICLIB | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| PHENAZOPYRIDINE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| PRIMAQUINE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| TELMISARTAN | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| TRIAMTERENE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| TROGLITAZONE | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| VERAPAMIL | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| VISMODEGIB | ChEMBL | Phase 4 (approved) | PDE4A, PDE4D |
| IGURATIMOD | ChEMBL | Phase 3 | PDE4A, PDE4D |
| ZATOLMILAST | ChEMBL | Phase 3 | PDE4B, PDE4D |
| BENZETHONIUM | ChEMBL | Phase 2 | PDE4A, PDE4D |
| BUCLADESINE | ChEMBL | Phase 2 | PDE4A, PDE4D |
| DAXALIPRAM | ChEMBL | Phase 2 | PDE4B, PDE4D |
| FILAMINAST | ChEMBL | Phase 2 | PDE4B, PDE4D |
| TOFISOPAM | ChEMBL | Phase 2 | PDE4A, PDE4D |
| Pyrazinamide | PubChem | Approved | PDE4A, PDE4D |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | PDE4D |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | PDE4A |
| TAFAMIDIS | ChEMBL + PubChem | Phase 4 (approved) | PDE4D |
| 2-MERCAPTOETHANESULFONIC ACID | ChEMBL | Phase 4 (approved) | PDE4A |
| ABACAVIR | ChEMBL | Phase 4 (approved) | PDE4D |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | PDE4D |
| ACARBOSE | ChEMBL | Phase 4 (approved) | PDE4A |
| ADENOSINE | ChEMBL | Phase 4 (approved) | PDE4D |
| ALECTINIB | ChEMBL | Phase 4 (approved) | PDE4A |
| ALPIDEM | ChEMBL | Phase 4 (approved) | PDE4D |
| AMINOGLUTETHIMIDE | ChEMBL | Phase 4 (approved) | PDE4D |
| AMLEXANOX | ChEMBL | Phase 4 (approved) | PDE4D |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | PDE4D |
| AMSACRINE | ChEMBL | Phase 4 (approved) | PDE4D |
| ANASTROZOLE | ChEMBL | Phase 4 (approved) | PDE4D |
| ANTAZOLINE | ChEMBL | Phase 4 (approved) | PDE4D |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | PDE4D |
| AUROTHIOGLUCOSE | ChEMBL | Phase 4 (approved) | PDE4A |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | PDE4D |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | PDE4D |
| BENZIODARONE | ChEMBL | Phase 4 (approved) | PDE4A |
| BISACODYL | ChEMBL | Phase 4 (approved) | PDE4A |
| BROMHEXINE | ChEMBL | Phase 4 (approved) | PDE4A |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | PDE4D |
| BUCLIZINE | ChEMBL | Phase 4 (approved) | PDE4D |
| BUFEXAMAC | ChEMBL | Phase 4 (approved) | PDE4A |
| BUTAMBEN | ChEMBL | Phase 4 (approved) | PDE4D |
| BUTOCONAZOLE | ChEMBL | Phase 4 (approved) | PDE4D |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | PDE4D |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | PDE4D |
| CARBENOXOLONE | ChEMBL | Phase 4 (approved) | PDE4D |
| CARPROFEN | ChEMBL | Phase 4 (approved) | PDE4D |
| CEFPODOXIME PROXETIL | ChEMBL | Phase 4 (approved) | PDE4D |
Related Atlas pages
- Genes: PDE4A, PDE4B, PDE4C, PDE4D
- Indicated for: Behcet disease, psoriasis, psoriatic arthritis, immune system disorder
- In clinical trials for: ankylosing spondylitis, severe acute respiratory syndrome, pneumonia, influenza, atopic eczema, rheumatoid arthritis, acne, ulcerative colitis, gout, prostatitis, rosacea, hidradenitis suppurativa, lichen planus, vitiligo, allergic contact dermatitis, dermatomyositis, lichen planus, oral, dermatitis, alcohol abuse, erythema multiforme
- Drugs: Tadalafil, Crisaborole, Dipyridamole, Enoximone, Ensifentrine, Ibudilast, Inamrinone, Losartan, Milrinone, Pentoxifylline, Roflumilast, Sildenafil, Theophylline, Vardenafil, Cilomilast, Mufemilast, Papaverine, Tetomilast, Belinostat, Ethinyl Estradiol, Glafenine, Istradefylline, Laropiprant, Oxybenzone, Palbociclib, Phenazopyridine, Primaquine, Telmisartan, Triamterene, Troglitazone, Verapamil, Vismodegib, Iguratimod, Zatolmilast, Pyrazinamide, Dihydroergotamine, Tafamidis, 2-MERCAPTOETHANESULFONIC ACID, Abacavir, Abemaciclib, Acarbose, Adenosine, Alectinib, Alpidem, Aminoglutethimide, Amlexanox, Amoxapine, Amsacrine, Anastrozole, Antazoline, Apomorphine, Aurothioglucose, Benfluorex, Benzbromarone, Benziodarone, Bisacodyl, Bromhexine, Bromocriptine, Buclizine, Bufexamac, Butamben, Butoconazole, Cabozantinib, Candesartan Cilexetil, Carbenoxolone, Carprofen, Cefpodoxime Proxetil